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verapamil

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Description

Verapamil is a calcium channel blocker that is used to treat high blood pressure, angina (chest pain), and irregular heartbeat. It works by relaxing blood vessels and slowing down the heart rate. Verapamil is synthesized in a multi-step process that involves several chemical reactions. It is an important drug because it can help to prevent heart attacks, strokes, and other serious health problems. Verapamil is studied because it is effective in treating a wide range of cardiovascular conditions. Research is ongoing to develop new and improved versions of verapamil.'

Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2520
CHEMBL ID6966
CHEBI ID77733
CHEBI ID9948
SCHEMBL ID16742
SCHEMBL ID13287282
MeSH IDM0022608

Synonyms (208)

Synonym
AC-16016
AB00053495-20
BRD-A09533288-001-02-7
BRD-A09533288-003-05-6
nsc-272306na
CHEMBL6966
cp-16,533-1
chebi:77733 ,
cp-165331
verapamil slow release
gtpl2406
ansyr
cp-165331 / cp-16533-1
benzeneacetonitrile, .alpha.-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-.alpha.-(1-methylethyl)-
DIVK1C_000399
KBIO1_000399
NCI60_020143
tarka
BSPBIO_000242
BIO2_000233
BIO1_000914
BIO1_000425
BIO1_001403
BIO2_000713
SPECTRUM5_001786
BSPBIO_002358
PRESTWICK3_000141
BSPBIO_001513
IDI1_033983
LOPAC0_001237
IDI1_000399
2-(3,4-dimethoxyphenyl)-5-((2-(3,4-dimethoxyphenyl)ethyl)(methyl)amino)-2-isopropylpentanenitrile, (+/-)-
5-[(3,4-dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methyl-amino]-2-isopropyl-pentanenitrile
isotopin
calcan
AB00053495
vasolan
ccris 6749
verapamil [usan:inn:ban]
verapamilo [inn-spanish]
cp-16533-1
c27h38n2o4
5-((3,4-dimethoxyphenethyl)methylamino)-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
benzeneacetonitrile, alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino) propyl)-3,4-dimethoxy-alpha-(1-methylethyl)-
benzeneacetonitrile, alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-3,4-dimethoxy-alpha-(1-methylethyl)-
alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)-methylamino)propyl)-3,4-dimethoxy-alpha-(1-methylethyl)benzeneacetonitrile
valeronitrile, 5-((3,4-dimethoxyphenethyl)methylamino)-2-(3,4-dimethoxyphenyl)-2-isopropyl-
isoptimo
dilacoran
verapamilum [inn-latin]
d-365
einecs 200-145-1
alpha-isopropyl-alpha-((n-methyl-n-homoveratryl)-gamma-aminopropyl)-3,4-dimethoxyphenylacetonitrile
alpha-((n-methyl-n-homoveratryl)-gamma-aminopropyl)-3,4-dimethoxyphenylacetonitrile
52-53-9
verapamil
C07188
iproveratril
DB00661
verapamil (usan/inn)
D02356
NCGC00024710-07
NCGC00024710-08
anpec
verelan
covera-hs
verelan pm
izoptin
veratensin
verpamil
isoptine
lekoptin
finoptin
isoptin sr
securon
falicard
isoptin
verapamil al
calan
hsdb 3928
calan sr
KBIO2_000233
KBIOGR_000233
KBIOSS_002346
KBIO2_002801
KBIO2_007479
KBIO3_000466
KBIOSS_000233
KBIO3_002823
KBIOGR_002343
KBIOGR_001372
KBIO3_000465
KBIO2_005369
KBIO2_004911
KBIO2_002343
SPBIO_001820
SPECTRUM4_000906
PRESTWICK0_000141
PRESTWICK1_000141
SPECTRUM2_001740
NINDS_000399
SPBIO_002181
PRESTWICK2_000141
2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methyl-amino]-2-(1-methylethyl) pentanenitrile
CMAP_000023
BPBIO1_000268
NCGC00024710-05
NCGC00024710-04
NCGC00024710-09
NCGC00024710-06
2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile
HMS2089H17
HMS1989L15
NCGC00016083-14
L001330
(+/-)-verapamil
HMS1791L15
2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]-2-propan-2-ylpentanenitrile
NCGC00016083-09
bdbm81939
nsc_62969
cas_52-53-9
AKOS005468962
5-((3,4-dimethoxyphenethyl)(methyl)amino)-2-(3,4-dimethoxyphenyl)-2-isopropylpentanenitrile
STK538085
A829133
dtxcid7021152
dtxsid9041152 ,
tox21_110300
cas-52-53-9
CCG-205311
NCGC00016083-11
NCGC00016083-08
NCGC00016083-06
NCGC00016083-16
NCGC00016083-10
NCGC00016083-04
NCGC00016083-17
NCGC00016083-18
NCGC00016083-15
NCGC00016083-07
NCGC00016083-13
NCGC00016083-05
FT-0675801
unii-cj0o37ku29
r,s-verapamil
dl-verapamil
nsc 272306na
cp 16533-1
verapamilum
verapamilo
cj0o37ku29 ,
d 365
einecs 260-462-6
FT-0603225
NCGC00016083-20
BP-21223
(+/-)-5-((3,4-dimethoxyphenethyl)methylamino)-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
verapamil [mi]
verapamil [vandf]
verapamil [inn]
verapamil [who-dd]
verapamil [usan]
SCHEMBL16742
NCGC00344584-01
tox21_110300_1
F2173-0851
smr001550201
MLS006011414
verapamil, dexverapamil, verapamyl hydrochloride, verapamil hydrochloride
SCHEMBL13287282
cordilox (salt/mix)
.alpha.-((n-methyl-n-homoveratryl)-.gamma.-aminopropyl)-3,4-dimethoxyphenylacetonitrile
2-(3,4-dimethoxyphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino]-2-isopropylpentanenitrile #
isoptin (salt/mix)
akilen (salt/mix)
calan (salt/mix)
covera-hs (salt/mix)
HMS3402L15
(a+/-)-verapamil hydrochloride
AB00053495_21
delta-365
cp 16533-1 (verapamil)
SBI-0051204.P003
()-verapamil hydrochlorid
Q410291
E75969
HY-14275
(+/-)-verapamil hydrochlorid
SDCCGSBI-0051204.P005
NCGC00016083-34
CS-0002967
(+/-)-verapamil;cp-16533-1
()-verapamil;cp-16533-1
NCGC00016083-25
mfcd00056240
EN300-708774
?verapamil
alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-3,4-dimethoxy-alpha-(1-methylethyl)benzeneacetonitrile
verapamilum (inn-latin)
verapamilum (latin)
chebi:9948
rac-2-(3,4-dimethoxyphenyl)-5-((2-(3,4-dimethoxyphenyl)ethyl)(methyl)amino)-2-(propan-2-yl)pentanenitrile
alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino) propyl)-3,4-dimethoxy-alpha-(1-methylethyl)-benzeneacetonitrile
c08da01
alpha-isopropyl-alpha-
verapamilo (inn-spanish)

Research Excerpts

Overview

Verapamil is a non-dihydropyridine calcium channel blocker (CCB) widely used in the treatment of hypertension, chronic stable angina, secondary prevention of reinfarction, paroxysmal supra-ventricular tachycardia and for rate control in atrial fibrillation/flutter. It also holds promise for the therapy of chronic rhinosinusitis with and without nasal polyps.

ExcerptReferenceRelevance
"Verapamil is a non-dihydropyridine calcium channel blocker (CCB) widely used in the treatment of hypertension, chronic stable angina, secondary prevention of reinfarction, paroxysmal supra-ventricular tachycardia and for rate control in atrial fibrillation/flutter."( Verapamil: prevention and treatment of cardio-renal syndromes in diabetic hypertensive patients?
Bei, A; Calò, L; Cice, G; Di Lullo, L; Lido, P; Noce, A; Palazzetti, D; Perrone, MA; Romanello, D; Tesauro, M, 2022
)
2.89
"Verapamil is a calcium channel blocker that holds promise for the therapy of chronic rhinosinusitis (CRS) with and without nasal polyps. "( Topical Administration of Verapamil in Poly(ethylene glycol)-Modified Liposomes for Enhanced Sinonasal Tissue Residence in Chronic Rhinosinusitis:
Amiji, MM; Bleier, BS; D'Souza, A; Kutlehria, S; Taha, MS, 2023
)
2.65
"Verapamil (VER) is a calcium channel blocker that is widely used to treat various cardiovascular diseases and is also effective in migraine prophylaxis. "( Analytical techniques for the determination of verapamil in biological samples and dosage forms: an overview.
Jouyban, A; Pourkarim, F; Rahimpour, E, 2019
)
2.21
"Verapamil is a calcium channel blocker with an inhibitory effect on hyphae development, adhesion, and colonization of C."( Antifungal and anti-biofilm effect of the calcium channel blocker verapamil on non-albicans Candida species.
Amorim, JBO; Fugisaki, LRO; Menezes, RT; Oliveira, LD; Oliveira, PS; Pereira, TC; Ribeiro, FC; Santos, ELS; Scorzoni, L, 2020
)
1.52
"Verapamil acts as an open-channel blocker of hKv1.5 channel, presumably due to direct binding to specific amino acids within pore region of hKv1.5 channel, such as Thr479, Thr480, Val505, Ile508, Val512 and Val516. "( Identification of Verapamil Binding Sites Within Human Kv1.5 Channel Using Mutagenesis and Docking Simulation.
Ding, WG; Kojima, A; Matsuura, H; Mi, X; Seto, T; Tano, A, 2019
)
2.29
"Verapamil appears to be an effective prophylactic drug in the treatment of CH and despite the scarcity of controlled trials, it is still the drug of choice. "( Verapamil and Cluster Headache: Still a Mystery. A Narrative Review of Efficacy, Mechanisms and Perspectives.
Barloese, MCJ; Jensen, RH; Petersen, AS; Snoer, A; Soerensen, AMS, 2019
)
3.4
"Verapamil is a pharmaceutical that belongs to a group of calcium channel blockers and is mainly used as a treatment of angina pectoris and arterial hypertension. "( Toxic effects, bioconcentration and depuration of verapamil in the early life stages of common carp (Cyprinus carpio L.).
Fedorova, G; Grabic, R; Grabicova, K; Kroupova, HK; Machova, J; Prokes, M; Steinbach, C; Valentova, O, 2013
)
2.09
"As verapamil is a substrate for CYP3A4, which is induced by rifampin, we evaluated the pharmacokinetic/pharmacodynamic relationships of verapamil and rifampin coadministration in mice."( Acceleration of tuberculosis treatment by adjunctive therapy with verapamil as an efflux inhibitor.
Almeida, DV; Ammerman, NC; Bishai, WR; Gupta, S; Maiga, MC; Tyagi, S, 2013
)
1.14
"Verapamil intoxication is a life-threatening condition that often presents with severe hemodynamic instability and requires vasopressor support. "( Acute respiratory distress syndrome after verapamil intoxication: case report and literature review.
Altintas, ND; Izdes, S; Soykut, C, 2014
)
2.11
"Verapamil is an L-type calcium channel blocker (CCB) that has been shown to have immunomodulatory properties in a variety of tissues. "( Verapamil modulates interleukin-5 and interleukin-6 secretion in organotypic human sinonasal polyp explants.
Bleier, BS; Han, X; Kocharyan, A; Singleton, A, 2015
)
3.3
"Verapamil is a calcium channel blocker commonly used in treatments of hypertension. "( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
2.08
"Verapamil is a L-type voltage gated calcium channels inhibitor (VGCCI), which is a highly prescribed drug used in the treatment of hypertension, angina pectoris, cardiac arrhythmia and cluster headaches. "( Verapamil - L type voltage gated calcium channel inhibitor diminishes aggressive behavior in male Siamese fighting fish.
Dębski, B; Kania, BF; Wrońska, D; Zawadzka, E, 2015
)
3.3
"Verapamil is a Ca"( Acetyl L-carnitine targets adenosine triphosphate synthase in protecting zebrafish embryos from toxicities induced by verapamil and ketamine: An in vivo assessment.
Ali, SF; Dumas, M; Gu, Q; Guo, X; Kanungo, J; Paule, MG; Robinson, BL, 2017
)
2.11
"Verapamil is a calcium channel antagonist that has been shown to inhibit the synthesis/secretion of extracellular matrix molecules and increase collagenase."( Keloidectomy with core fillet flap and intralesional verapamil injection for recurrent earlobe keloids.
Alghobary, MF; El-Kamel, MF; Selim, MK,
)
1.1
"Verapamil is a calcium channel blocker that also inhibits the P-glycoprotein (Pgp) membrane transporter. "( Verapamil in treatment resistant depression: a role for the P-glycoprotein transporter?
Clarke, G; Cryan, JF; Dinan, TG; O'Mahony, SM, 2009
)
3.24
"Verapamil is known to be a P-glycoprotein (P-gp) substrate and norverapamil is formed via hepatic cytochrome P450 (CYP 3A) in the rat. "( Effects of oral epigallocatechin gallate on the oral pharmacokinetics of verapamil in rats.
Choi, DH; Choi, JS; Chung, JH, 2009
)
2.03
"Verapamil is a substrate of both P-gp and CYP3A4."( Pharmacokinetic interaction between oral lovastatin and verapamil in healthy subjects: role of P-glycoprotein inhibition by lovastatin.
Choi, DH; Choi, JS; Chung, JH, 2010
)
1.33
"Verapamil is an inhibitor of P-gp mediated uptake; elevation of cyclosporine uptake in the presence of 5 muM verapamil was compromised by the presence of 25 mM HEPES."( Effect of HEPES buffer on the uptake and transport of P-glycoprotein substrates and large neutral amino acids.
Kwatra, D; Luo, S; Mitra, AK; Pal, D; Paturi, KD; Shah, SJ, 2010
)
1.08
"Verapamil (VRP) is a calcium channel blocker that is a highly prescribed compound and commonly present in aquatic environment, but the ecotoxicological effects of this pharmaceutical in fish have not been fully documented. "( Ecotoxocological effects of short-term exposure to a human pharmaceutical Verapamil in juvenile rainbow trout (Oncorhynchus mykiss).
Li, P; Li, ZH; Randak, T, 2010
)
2.03
"Verapamil is a prototypical phenylalkylamine (PAA), and it was the first calcium channel blocker to be used clinically. "( Verapamil block of T-type calcium channels.
Bergson, P; Duban, ME; Hanck, DA; Lee, SP; Lipkind, G, 2011
)
3.25
"Verapamil is a calcium channel blocker that binds to the alpha-subunit of L-type calcium channels and inhibits the mucin gene via the calmodulin and CaM kinase pathway."( Effect of verapamil on bronchial goblet cells of asthma: an experimental study on sensitized animals.
Ghafarzadegan, K; Hadi, R; Khakzad, MR; Meshkat, M; Mirsadraee, M; Mohammadpour, A; Saghari, M, 2012
)
1.5
"Verapamil is a useful drug with therapeutic targeting on GCH and a potential way to limit mucous production and improve bronchial inflammation."( Effect of verapamil on bronchial goblet cells of asthma: an experimental study on sensitized animals.
Ghafarzadegan, K; Hadi, R; Khakzad, MR; Meshkat, M; Mirsadraee, M; Mohammadpour, A; Saghari, M, 2012
)
2.22
"Verapamil (Ver) is a well known, worldwide used drug to correct cardiac arrhythmias. "( Verapamil-induced autophagy-like process in colon adenocarcinoma COLO 205 cells; the ultrastructural studies.
Gajkowska, B; Kania, E; Orzechowski, A; Pająk, B, 2012
)
3.26
"Verapamil is a common calcium antagonist described with antianginal, antihypertensive and antiarrythmic properties. "( Verapamil drug metabolism studies by automated in-tube solid phase microextraction.
Borlak, J; Levsen, K; Mullett, WM; Pawliszyn, J; Walles, M; Wünsch, G, 2002
)
3.2
"Verapamil is a commonly prescribed cardiovascular drug, but surprisingly its metabolism in the target tissue of pharmacotherapy is basically unknown. "( Verapamil: new insight into the molecular mechanism of drug oxidation in the human heart.
Borlak, J; Levsen, K; Thum, T; Walles, M, 2002
)
3.2
"1. Verapamil is a well-known and world-wide prescribed calcium antagonist, but it suffers from extensive first-pass metabolism. "( Verapamil: identification of novel metabolites in cultures of primary human hepatocytes and human urine by LC-MS(n) and LC-NMR.
Borlak, J; Elend, M; Levsen, K; Preiss, A; Thum, T; Walles, M, 2003
)
2.38
"Verapamil is a widely prescribed calcium antagonist, but suffers from extensive first pass metabolism. "( Metabolism of verapamil: 24 new phase I and phase II metabolites identified in cell cultures of rat hepatocytes by liquid chromatography-tandem mass spectrometry.
Borlak, J; Levsen, K; Thum, T; Walles, M, 2003
)
2.12
"Verapamil is a widely used calcium channel antagonist, and it has been shown that calcium channel blockers inhibit the synthesis/secretion of extracellular matrix molecules, including collagen, glycosaminoglycans, and fibronectin, and increase collagenase."( Combination of surgery and intralesional verapamil injection in the treatment of the keloid.
Copcu, E; Oztan, Y; Sivrioglu, N,
)
1.12
"Verapamil is a widely used Ca(2+) channel antagonist in the treatment of cardiovascular disorders including atrial arrhythmias. "( Inhibition of ultra-rapid delayed rectifier K+ current by verapamil in human atrial myocytes.
Chiu, SW; Gao, Z; Lau, CP; Li, GR, 2004
)
2.01
"Verapamil is an effective prophylactic treatment for cluster headaches and, therefore, is widely used. "( Verapamil induced gingival enlargement in cluster headache.
Ferrari, MD; Goadsby, PJ; Matharu, MS; van Vliet, JA, 2005
)
3.21
"A verapamil SR strategy is a viable alternative to beta-blocker therapy for hypertensive patients with coronary artery disease, especially those at risk of depression."( A Study of Antihypertensive Drugs and Depressive Symptoms (SADD-Sx) in patients treated with a calcium antagonist versus an atenolol hypertension Treatment Strategy in the International Verapamil SR-Trandolapril Study (INVEST).
Handberg, E; Kupfer, S; Pepine, CJ; Ried, LD; Tueth, MJ,
)
1.04
"Verapamil, which is a L-type Ca2+ channel antagonist, produced a bradycardiac effect at the onset of AW, but no effect was observed in early remission."( Responses to cardiovascular drugs during alcohol withdrawal.
Kähkönen, S,
)
0.85
"Verapamil is a lipid-soluble calcium channel blocker with significant mortality in overdose. "( Intralipid prolongs survival in a rat model of verapamil toxicity.
Cave, G; Harvey, M; Nicholson, T; Tebbutt, S, 2006
)
2.03
"A verapamil SR strategy is an alternative to an atenolol strategy for the treatment of Hispanic patients with hypertension and CAD and can reduce the risk of new-onset diabetes."( Blood pressure control and cardiovascular outcomes in high-risk Hispanic patients--findings from the International Verapamil SR/Trandolapril Study (INVEST).
Aranda, JM; Cangiano, JL; Conti, CR; Cooper-DeHoff, RM; Garcia-Barreto, D; Gaxiola, E; Hewkin, A; Pepine, CJ, 2006
)
1.1
"Verapamil is a potent phenylalkylamine antihypertensive believed to exert its therapeutic effect primarily by blocking high-voltage-activated L-type calcium channels. "( State-dependent verapamil block of the cloned human Ca(v)3.1 T-type Ca(2+) channel.
Freeze, BS; Hanck, DA; McNulty, MM, 2006
)
2.12
"Verapamil (V) is a specific inhibitor of the P-glycoprotein (mdr1) in the hepatocyte canalicular membrane. "( Influence of Verapamil and Cyclosporin A on bile acid metabolism and transport in rat liver slices.
Barth, A; Braun, J; Müller, D, 2006
)
2.15
"Verapamil appears to be a safe and effective treatment alternative to propranolol for relieving anginal symptoms, improving exercise tolerance, and reducing elevated systemic blood pressure in patients with both angina pectoris and mild to moderate systemic hypertension."( Comparison of oral propranolol and verapamil for combined systemic hypertension and angina pectoris. A placebo-controlled double-blind randomized crossover trial.
Frishman, WH; Klein, NA; Klein, P; LeJemtel, TH; Pollack, S; Roth, S; Sonnenblick, EH; Strair, R; Strom, JA; Tawil, R; Wong, B, 1982
)
1.26
"Verapamil is an organic calcium antagonist which is believed to prevent the passage of calcium (Ca2+) across the cell membrane into the cell. "( Verapamil: influence upon basal and stimulated rat growth hormone and prolactin release in vitro.
Stachura, ME, 1983
)
3.15
"Verapamil is proving to be an important addition to existing drug regimens available for the treatment of stable angina pectoris."( Verapamil in treatment of chronic stable angina.
Charlap, S; Frishman, WH, 1983
)
2.43
"Verapamil was found to be an effective inhibitor of isometric tension in in vitro, experimental anaphylaxis in guinea pig trachealis smooth muscle. "( Effect of calcium antagonists in experimental asthma.
Barbero, L; Markowicz, J; Weiss, EB, 1982
)
1.71
"Verapamil is a calcium channel blocking agent used primarily for treatment of arrhythmias and coronary artery disease. "( Effect of verapamil on left ventricular function at rest and during exercise in normal men.
D'Agostino, HJ; Jones, RH; Pritchett, EL; Shand, DG,
)
1.98
"Verapamil is an important and safe modality of treatment, with or without digoxin, in the long-term control of heart rate in chronic atrial fibrillation."( Superiority of oral verapamil therapy to digoxin in treatment of chronic atrial fibrillation.
David, D; Di Segni, E; Guerrero, J; Kaplinsky, E; Klein, HO; Lang, R; Levy, A; Sareli, P; Weiss, E, 1983
)
1.31
"Verapamil is a slow-channel calcium-blocking agent that has been released recently by the Food and Drug Administration for treatment of cardiac dysrhythmias in all age groups. "( Verapamil: an effective calcium blocking agent for pediatric patients.
Garson, A; Gillette, PC; Porter, CJ, 1983
)
3.15
"Verapamil is a useful drug for treating supraventricular tachycardia; however, severe side effects occasionally have been reported in infants. "( The use of calcium gluconate prior to verapamil in infants with paroxysmal supraventricular tachycardia.
Berant, M; Blazer, S; Roguin, N; Shapir, Y; Zeltzer, M, 1984
)
1.98
"Verapamil was found to be a more effective antianginal drug than nifedipine."( [Comparative effectiveness of finoptin, corinfar and their combination in patients with angina pectoris].
Mazur, NA; Romakov, AIu; Sagirov, AM; Sumarokov, AB, 1984
)
0.99
"Verapamil hydrochloride is a calcium entry blocking drug that is being prescribed with increasing frequency for cardiovascular disorders in the perioperative setting. "( Verapamil decreases MAC for halothane in dogs.
Kates, RE; Mason, DM; Maze, M, 1983
)
3.15
"Verapamil hydrochloride is an organic calcium antagonist that is known to decrease the contraction of smooth muscle. "( The effect of verapamil on the lower esophageal sphincter pressure in normal subjects and in achalasia.
Becker, BS; Burakoff, R, 1983
)
2.07
"Verapamil appears to be a safe and effective drug for treating angina of effort."( Treatment of stable angina of effort with verapamil: a double-blind, placebo-controlled randomized crossover study.
Brodsky, SJ; Cutler, SS; Klein, MD; McCabe, CH; Ryan, TJ; Weiner, DA, 1982
)
1.25
"Verapamil is an effective primary therapy and a satisfactory alternative to propranolol in patients with stable effort angina."( A double-blind randomized trial of propranolol and verapamil in the treatment of effort angina.
Fletcher, PJ; Kelly, DT; Morris, J; Sadick, NN; Tan, AT, 1982
)
1.24
"Verapamil is a calcium antagonist that is pharmacologically different from other currently marketed antiarrhythmics. "( Verapamil (Isoptin, Knoll; Calan, Searle).
McMahon, MT; Sheaffer, SL, 1982
)
3.15
"Verapamil is an effective antianginal drug that appears most efficacious at a dose of 360 mg/day, but side effects are common at a dose of 480 mg/day."( Verapamil versus placebo in relieving stable angina pectoris.
Bailly, DJ; Butman, S; Citron, PD; Landa, DW; Pine, MB; Plasencia, GO; Wong, RK, 1982
)
2.43
"Verapamil 99 is a commonly prescribed medicine for treatment of hypertension, angina, and migraine headache. "( Massive overdose of sustained-release verapamil: a case report and review of literature.
Ashraf, M; Chaudhary, K; Nelson, J; Thompson, W, 1995
)
2
"Dexverapamil is a competitive inhibitor of the P-glycoprotein (Pgp) efflux pump, a potent mechanism of multidrug resistance (mdr-1) in vitro. "( Phase I and pharmacokinetic study of the multidrug resistance modulator dexverapamil with EPOCH chemotherapy.
Balis, FM; Bates, SE; Bryant, G; Chabner, BA; Jamis-Dow, C; Klecker, RW; Kohler, DR; Steinberg, SM; Wilson, WH; Wittes, RE, 1995
)
1.14
"Verapamil (CAS 52-53-9) is a calcium channel blocker with a vasodilatatory effect. "( Pharmacokinetic parameters of verapamil and its active metabolite norverapamil in patients with hepatopathy.
Brátová, M; Fendrich, Z; Hůlek, P; Macek, K; Vlcek, J, 1995
)
2.02
"Both Verapamil and aTP are an equally safe and effective treatment of PST, but transient and minor side effects are frequent after ATP administration."( [Adenosine triphosphate in the treatment of supraventricular paroxysmal tachycardia: a comparison with verapamil].
Alises Moraleda, JM; Cortés Bermejo, S; García de Pedro, J; Gil Madre, J; Laín Teres, N; Lázaro Rodríguez, S; Sentenac Merchán, G; Sepúlveda Berrocal, MA, 1995
)
1.02
"Verapamil is a calcium channel blocker widely used as an antihypertensive agent, and its pharmacological effects may partly be due to some degree of beta blockade. "( Is verapamil also a non-selective beta blocker?
Drici, MD; Iacono, P; Jacomet, Y; Lapalus, P, 1993
)
2.35
"Verapamil (VRP) is an effective modulator of P170-associated multidrug resistance (MDR), but its clinical application is limited by cardiovascular side-effects. "( D-verapamil downmodulates P170-associated resistance to doxorubicin, daunorubicin and idarubicin.
Baccarani, M; Cerno, M; Damiani, D; Melli, C; Michelutti, A; Michieli, M, 1993
)
2.45
"Verapamil is an antagonist of L-type Ca2+ channels, and part of its binding site is located in the sixth transmembrane segment (S6) in the fourth repeat of the protein. "( Verapamil blocks a rapidly activating delayed rectifier K+ channel cloned from human heart.
Brown, AM; Dage, RC; Fedida, D; Rampe, D; Wible, B, 1993
)
3.17
"Verapamil is a racemic calcium channel-blocking drug that undergoes extensive hepatic first-pass metabolism to an active metabolite, norverapamil. "( Pharmacokinetics of verapamil and norverapamil enantiomers after administration of immediate and controlled-release formulations to humans:evidence suggesting input-rate determined stereoselectivity.
Bhatti, MM; Foster, RT; Lewanczuk, RZ; Pasutto, FM, 1995
)
2.06
"Verapamil is an effective protective medicine for light-induced retinopathy."( [Protective effect of verapamil on light-induced rat retinopathy].
Liang, Y; Zhang, H, 1996
)
2.05
"Verapamil is a calcium antagonist that has been shown to modulate wound healing through multiple mechanisms. "( The effects of subconjunctival verapamil on filtering blebs in rabbits.
Agarwala, A; Edward, DP; Gupta, B; Moy, JJ, 1996
)
2.02
"Verapamil, which is an inhibitor of mouse mdr2 phosphatidylcholine flippase, did not inhibit the present flippase activity."( The phospholipid flippase activity of gastric vesicles.
Kamakura, M; Morii, M; Suzuki, H; Takeguchi, N, 1997
)
1.02
"Verapamil is a chiral calcium channel blocking drug which is useful clinically as the racemate in treating hypertension and arrhythmia. "( Pharmacokinetics of the enantiomers of verapamil after intravenous and oral administration of racemic verapamil in a rat model.
Bhatti, MM; Foster, RT, 1997
)
2.01
"Norverapamil, which is an active metabolite of verapamil, can be detected in the aqueous and vitreous of the rabbit eye after topical administration, suggesting enzymatic degradation of verapamil within the eye."( Distribution of verapamil and norverapamil in the eye and systemic circulation after topical administration of verapamil in rabbits.
Erickson, KA; Giovanoni, RL; Netland, PA; Siegner, SW, 1998
)
1.16
"R/S-Verapamil is a high permeability drug in the proximal rat small intestine throughout the luminal concentration range studied and complete intestinal absorption was expected."( The absence of stereoselective P-glycoprotein-mediated transport of R/S-verapamil across the rat jejunum.
Karlsson, A; Lennernäs, H; Sandström, R, 1998
)
1.01
"Verapamil is an effective drug to slow ventricular rate in atrial fibrillation (AF). "( Verapamil prolongs atrial fibrillation by evoking an intense sympathetic neurohumoral effect.
Dai, CP; Friedman, HS; Hussain, A; Mallipeddi, D; Rodney, E; Sharafkhaneh, A; Sinha, A; Sinha, B; Wattanasuwan, N; Win, M, 1999
)
3.19
"Verapamil is a non-competitive inhibitor of DQHS formation in human liver microsomes with a Ki = 15 microM."( Metabolism of artelinic acid to dihydroqinqhaosu by human liver cytochrome P4503A.
Aguilar, AJ; Grace, JM; Skanchy, DJ, 1999
)
1.02
"Verapamil is a papaverine-derived calcium channel blocker widely used for the treatment of hypertension and supraventricular tachyarrhythmias. "( Use of partial liquid ventilation to manage pulmonary complications of acute verapamil-sustained release poisoning.
Szekely, LA; Thompson, BT; Woolf, A, 1999
)
1.97
"Norverapamil is a chiral drug with the same ability as verapamil in reversing MDR (multi-drug resistance) against some cytostatics."( Achiral and chiral HPLC analysis of norverapamil and its metabolites in microsomal samples.
Brandsteterová, E; Tracy, T; Wainer, IW, 1999
)
1.09
"Verapamil is a calcium channel blocker primarily used for treatment of cardiovascular disorders."( A mixed-drug intoxication involving venlafaxine and verapamil.
Farley, NJ; Garavaglia, JC; Kunsman, CM; Kunsman, GW; Presses, CL, 2000
)
1.28
"Verapamil is an effective vasodilator. "( Effects of verapamil on coronary vascular resistance in rabbits: measurement with pulsed Doppler velocimetry.
Hsu, CP; Huang, CH; Kan, CB; Lai, ST; Tsao, NW, 2001
)
2.14
"Verapamil is a novel antiarrhythmic agent which appears to act as a calcium-ion antagonist, blocking calcium transport across the myocardial cell membrane. "( [Verapamil in the study and treatment of supraventricular tachycardias, with special reference to pre-excitation].
Krikler, DM, 1975
)
2.61
"Verapamil is a novel antiarrhythmic and antianginal agent which, although introduced in 1962, has only recently gained prominence not only as a significant agent in cardiovascular therapeutics but also as a powerful tool to examine the nature of some of the biophysical phenomena at the membrane of cardiac and other excitable tissues. "( Verapamil: a review of its pharmacological properties and therapeutic use.
Ellrodt, G; Peter, CT; Singh, BN, 1978
)
3.14
"Verapamil is a good alternative to beta-blockers in the prophylactic treatment of angina."( Double-blind comparison of verapamil and practolol in the treatment of angina pectoris.
Fagher, B; Persson, S; Svensson, SE, 1977
)
1.28
"Verapamil is a new anti-anginal and anti-arrhythmic drug whose pharmacological actions can be related to its specific blocking effect on the transmembrane transport of calcium ions. "( Verapamil and the heart: Pharmacological and Therapeutic Considerations.
DPhil, BN, 1975
)
3.14
"Verapamil was found to be a useful drug to suppress PSVT, to decrease the ventricular response in flutter or atrial fibrillation and to convert some ventricular tachycardias to sinus rhythm."( [Antiarrhythmic effects of verapamil].
Férez, S; Malo, R; Martínez-Ríos, MA; Salazar, E; Shapiro, M,
)
1.15
"Verapamil is a potent calcium antagonist known to inhibit excitation-contraction coupling in both myocardium and myometrium. "( Calcium antagonists and islet function. I. Inhibition of insulin release by verapamil.
Devis, G; Malaisse, WJ; Somers, G; Van Obberghen, E, 1975
)
1.93
"Verapamil is an effective antiarrhythmic agent which is, in general, free from significant side effects."( Clinical experience with verapamil.
Hunt, D; Sloman, G; Vohra, J, 1975
)
1.28
"Verapamil appears to be an effective hypotensive and does not produce profound psychomotor impairment at clinically used doses during the first weeks of treatment."( Behavioral performance effects of verapamil in normotensive and renovascular hypertensive baboons.
Hienz, RD; Turkkan, JS,
)
1.13
"With verapamil there is a small tendency for a reduction in reinfarction, with nifedipine a clear worsening, and with diltiazem a reduction almost reaching statistical significance."( Protective effects of calcium antagonists against ischaemia and reperfusion damage.
Ferrari, R; Visioli, O, 1991
)
0.74
"Verapamil is a calcium-channel blocking agent with antianginal and antiarrhythmic properties that have been widely studied. "( The effects of verapamil on training in patients with ischemic heart disease.
Horgan, JH; MacGowan, GA; O'Callaghan, D; Webb, H, 1992
)
2.08
"Verapamil is a calcium channel blocker ideally suited for the treatment of A-V nodal reciprocating supraventricular tachycardia. "( [Idiopathic recurrent ventricular tachycardia: role of verapamil in its treatment].
Arriagada, C; Fajuri, A; González, R; Marchesse, M; Serrat, H, 1989
)
1.97
"Verapamil is a papaverine derivative calcium channel blocking drug that has been effectively utilized in the prophylaxis of migraine. "( Verapamil in migraine prophylaxis--a five-year review.
Solomon, GD, 1989
)
3.16
"Verapamil is a phenylalkylamine derivative which antagonises calcium influx through the slow channels of vascular smooth muscle and cardiac cell membranes."( Verapamil. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension.
McTavish, D; Sorkin, EM, 1989
)
2.44
"Verapamil is a highly lipophilic base with a pKa of 8.7."( Effects of verapamil on gastric acid secretion in vitro and in vivo.
Herling, AW; Ljungström, M, 1988
)
1.39
"Verapamil was found to be a competitive inhibitor of both imipramine binding and serotonin uptake in brain and platelets."( Tricyclic antidepressants and calcium channel blockers: interactions at the (-)-desmethoxyverapamil binding site and the serotonin transporter.
Carmi, R; Rehavi, M; Weizman, A, 1988
)
1.22
"Verapamil is a calcium-channel blocking agent, commonly used for chronic treatment of heart conditions. "( Verapamil as a co-mutagen in the Salmonella/mammalian microsome mutagenicity test.
Baguley, BC; Ferguson, LR,
)
3.02
"Verapamil is a calcium channel blocking agent with possible antimanic properties. "( Verapamil: a new antimanic drug with potential interactions with lithium.
Allen, S; Dubovsky, SL; Franks, RD, 1987
)
3.16
"Verapamil is a calcium channel blocker at the membrane level and may affect cytosol calcium-calmodulin as well."( Verapamil inhibition of lymphocyte proliferation and function in vitro.
Jaffe, BM; Lewis, T; McMillen, MA; Wait, RB, 1985
)
2.43
"Verapamil is an effective and relatively-safe antihypertensive drug. "( Verapamil withdrawal as a possible cause of myocardial infarction in a hypertensive woman with a normal coronary angiogram.
Beilin, LJ; Dimmitt, SB; Hockings, BE, 1988
)
3.16
"Verapamil is a widely used calcium channel blocker. "( Cerebral infarction associated with oral verapamil overdose.
Samniah, N; Schlaeffer, F, 1988
)
1.98
"Verapamil is a calcium channel blocker that inhibits mast cell degranulation, platelet aggregation, and neutrophil function and is a potent vasodilator. "( Efficacy of verapamil in the salvage of failing random skin flaps.
Nichter, LS; Sobieski, MW, 1988
)
2.1
"Verapamil is a racemic mixture of two optical isomers, the (-)-form being the more active component. "( Pharmacokinetics of conventional and slow-release verapamil.
Bühler, F; Follath, F; Ha, HR; Schütz, E, 1986
)
1.97
"Verapamil is an agent which inhibits the transmembrane flux of calcium ions and is used clinically in the management of cardiac arrhythmias. "( The calcium channel blocker verapamil and cancer chemotherapy.
Simpson, WG, 1985
)
2.01

Effects

Verapamil overdose is has a comparatively high mortality rate and there is no effective antidote. It has a lowering effect on the blood pressure even in the presence of advanced renal failure.

Verapamil has profound electrophysiologic effects on the slow inward current. It has antioxidant activity, which enhances the production of nitric oxide (NO) It has shown a great potential in the management of keloid and hypertrophic scars.

ExcerptReferenceRelevance
"Verapamil overdose is has a comparatively high mortality rate and there is no effective antidote. "( Comparison of Effects of Separate and Combined Sugammadex and Lipid Emulsion Administration on Hemodynamic Parameters and Survival in a Rat Model of Verapamil Toxicity.
Ates, NG; Demir Piroglu, I; Demir, A; Gergerli, R; Guven, S; Karakilic, E; Kose, HC; Piroglu, MD; Tulgar, S, 2016
)
2.08
"Verapamil alone has a more significant prophylactic than therapeutic antifibrotic effect against induced liver fibrosis; it was more significant than silymarin. "( Improved antifibrotic effect of a combination of verapamil and silymarin in rat-induced liver fibrosis.
Gouda, NA; Khodeir, MM; Mahmoud, ME; Shafik, AN, 2011
)
2.07
"Verapamil has a narrow range of dose-dependence and cytotoxicity in high concentrations."( [Conservative treatment of Peyronie's disease in the light of new pathogenetic data].
Ivanchenko, LP; Kalashnikova, EA; Mazo, EB; Mufaged, ML; Terekhov, SM,
)
0.85
"Verapamil has a negative inotropic action in isolated cardiac muscle. "( Effect of verapamil on left ventricular function: a randomized, placebo-controlled study.
Farias, MA; Frye, RL; Ritman, EL; Smith, HC; Vlietstra, RE, 1983
)
2.11
"Verapamil has a well-documented history as an effective antianginal agent when directly compared with a beta-blocker, and is more effective in reducing myocardial ischemia compared with amlodipine monotherapy."( Verapamil revisited: a transition in novel drug delivery systems and outcomes.
Prisant, LM,
)
2.3
"Verapamil has a lowering effect on the blood pressure even in the presence of advanced renal failure."( [The treatment of renal hypertension with verapamil in childhood (author's transl].
Alatas, H; Bein, G; Schärer, K, 1977
)
1.24
"Verapamil has been used in perfusion solution to improve kidney performance, but evidence was anecdotal, and no research has been reported on recipient outcomes. "( Performance of Renal Allografts Perfused With Verapamil-Treated Perfusion Solution.
Boyer, AJ; Hostetler, CA; Ketcham, RE; Orlowski, JP; Squires, RA, 2021
)
2.32
"Verapamil has been shown to be able to reverse development of multidrug resistance mediated by P-glycoprotein."( Metabolomics analysis of multidrug resistance in colorectal cancer cell and multidrug resistance reversal effect of verapamil.
Gao, M; Wang, K; Wang, X; Wang, Z; Xu, X; Zhang, H, 2021
)
1.55
"Verapamil has antioxidant activity, which enhances the production of nitric oxide (NO)."( Nitric Oxide Produced by the Antioxidant Activity of Verapamil Improves the Acute Wound Healing Process.
Choi, JY; Han, YN; Kim, KJ; Lee, SJ; Lee, YJ; Moon, SH; Rhie, JW, 2021
)
1.59
"Verapamil has been shown to inhibit TNF-α and IL-1β in vitro and in vivo."( Successful control of hidradenitis suppurativa with verapamil: a case report.
Geniaux, H; Laroche, ML; Teste, M; Vanoost, J, 2019
)
1.49
"Verapamil has been hypothesized to mitigate ischemia reperfusion injury (IRI) to the allograft."( Does intra-operative verapamil administration in kidney transplantation improve graft function.
Bidnur, S; Caldas, M; Ghosh, S; Gupta, N; Moore, RB; Sharma, N; Todd, GT, 2019
)
1.55
"Verapamil has been used in the prevention of CH for almost 3 decades, however, the mode of action and therapeutic target is still unknown."( Verapamil and Cluster Headache: Still a Mystery. A Narrative Review of Efficacy, Mechanisms and Perspectives.
Barloese, MCJ; Jensen, RH; Petersen, AS; Snoer, A; Soerensen, AMS, 2019
)
3.4
"Verapamil has been detected in aquatic environments in concentrations ranging from ng L(-1) to μg L(-1)."( Toxic effects, bioconcentration and depuration of verapamil in the early life stages of common carp (Cyprinus carpio L.).
Fedorova, G; Grabic, R; Grabicova, K; Kroupova, HK; Machova, J; Prokes, M; Steinbach, C; Valentova, O, 2013
)
1.36
"Verapamil has shown a great potential in the management of keloid and hypertrophic scars."( Role of verapamil in preventing and treating hypertrophic scars and keloids.
Cen, Y; Chen, J; Li, Z; Mao, Y; Wang, R; Zhang, Z, 2016
)
1.59
"Verapamil overdose is has a comparatively high mortality rate and there is no effective antidote. "( Comparison of Effects of Separate and Combined Sugammadex and Lipid Emulsion Administration on Hemodynamic Parameters and Survival in a Rat Model of Verapamil Toxicity.
Ates, NG; Demir Piroglu, I; Demir, A; Gergerli, R; Guven, S; Karakilic, E; Kose, HC; Piroglu, MD; Tulgar, S, 2016
)
2.08
"Verapamil has shown antimanic activity in some but not all studies."( Verapamil augmentation of lithium treatment improves outcome in mania unresponsive to lithium alone: preliminary findings and a discussion of therapeutic mechanisms.
Buttenfield, J; Frank, E; Haskett, R; Kupfer, DJ; Luckenbaugh, DA; Mallinger, AG; Manji, HK; Thase, ME, 2008
)
2.51
"Verapamil has been shown to be neuroprotective in several acute neurotoxicity models due to blockade of calcium entry into neurons. "( Verapamil protects dopaminergic neuron damage through a novel anti-inflammatory mechanism by inhibition of microglial activation.
Ali, S; Chen, HL; Chen, SH; Crews, FT; Hong, JS; Liu, Y; Lo, YC; Lu, RB; Qian, L; Wei, K; Wilson, B; Wu, HM,
)
3.02
"Verapamil has been shown to inhibit glucose transport in several cell types. "( Metabolic flux analysis gives an insight on verapamil induced changes in central metabolism of HL-1 cells.
Heinzle, E; Niklas, J; Noor, F; Pironti, A; Strigun, A; Yang, TH, 2011
)
2.07
"Verapamil alone has a more significant prophylactic than therapeutic antifibrotic effect against induced liver fibrosis; it was more significant than silymarin. "( Improved antifibrotic effect of a combination of verapamil and silymarin in rat-induced liver fibrosis.
Gouda, NA; Khodeir, MM; Mahmoud, ME; Shafik, AN, 2011
)
2.07
"Verapamil has significant effect on volume and acidity of carbachol induced gastric secretion."( Comparison of verapamil and cimetidine for their effects on volume and acidity of Carbachol induced gastric secretion in fasting rabbits.
Ahmad, S; Haroon, M; Jan, M; Javid, M; Orakzai, SA; Qamar, M; Tariq, S,
)
1.93
"Verapamil has the capability to inhibit and induce cytochrome P450 (CYP) 3A and P-glycoprotein (P-gp), but the relative extent and time course of these events in vivo are unclear. "( The effect of short- and long-term administration of verapamil on the disposition of cytochrome P450 3A and P-glycoprotein substrates.
Gorski, JC; Hall, SD; Hamman, MA; Lemma, GL; Wang, Z; Zaheer, NA, 2006
)
2.03
"Verapamil has a narrow range of dose-dependence and cytotoxicity in high concentrations."( [Conservative treatment of Peyronie's disease in the light of new pathogenetic data].
Ivanchenko, LP; Kalashnikova, EA; Mazo, EB; Mufaged, ML; Terekhov, SM,
)
0.85
"Verapamil (Vp) has been found to augment the creatine kinase (CK) and lactate dehydrogenase (LDH) leakage from isolated mouse heart incubated in vitro at 25 degrees C. "( Competitive effects of verapamil and calcium ion as regulators of myocardial enzyme leakage.
Cohen, L; Gilula, Z; Herbstman, D; Lazaron, B; Meier, P,
)
1.88
"Verapamil, which has profound electrophysiologic effects on the slow inward current, is emerging as a valuable antiarrhythmic agent."( Calcium channel blocking agents in the treatment of cardiovascular disorders. Part I: Basic and clinical electrophysiologic effects.
Antman, EM; Braunwald, E; Muller, JE; Stone, PH, 1980
)
0.98
"Verapamil has a negative inotropic action in isolated cardiac muscle. "( Effect of verapamil on left ventricular function: a randomized, placebo-controlled study.
Farias, MA; Frye, RL; Ritman, EL; Smith, HC; Vlietstra, RE, 1983
)
2.11
"Verapamil and diltiazem have been evaluated with mixed results for atrial flutter and fibrillation."( Update on calcium-channel blocking agents.
Bussey, HI; Talbert, RL,
)
0.85
"Verapamil has previously been found to inhibit insulin release from pancreatic beta-cells in laboratory animals. "( Influence of verapamil on glucose tolerance.
Andersson, DE; Röjdmark, S, 1984
)
2.08
"(-)-verapamil has been demonstrated to possess 8 to 10 times more potent negative dromotropic effect on AV conduction than (+)-verapamil."( Stereoselective first-pass metabolism of highly cleared drugs: studies of the bioavailability of L- and D-verapamil examined with a stable isotope technique.
Echizen, H; Eichelbaum, M; Schmidt, E; Vogelgesang, B, 1984
)
0.96
"Verapamil has been demonstrated to inhibit the elimination of digoxin and to increase its steady state plasma level by 60-80%. "( Influence of verapamil on the inotropism and pharmacokinetics of digoxin.
Christiansen, BD; Klitgaard, NA; Nielsen-Kudsk, F; Pedersen, KE; Thayssen, P, 1983
)
2.08
"Oral verapamil has previously been shown to reduce heart rate at rest and during mild exercise in chronic atrial fibrillation. "( Verapamil improves exercise capacity in chronic atrial fibrillation: double-blind crossover study.
David, D; Di Segni, E; Gefen, J; Guerrero, J; Kaplinsky, E; Klein, HO; Lang, R; Libhaber, C; Sareli, P; Weiss, E, 1983
)
2.22
"Verapamil kinetics have been determined in liver disease (mainly in cirrhotic patients), in intensive-care patients, and in healthy control subjects. "( Verapamil disposition in liver disease and intensive-care patients: kinetics, clearance, and apparent blood flow relationships.
Rietbrock, I; Rietbrock, N; Vöhringer, HF; Woodcock, BG, 1981
)
3.15
"Verapamil has been studied extensively in adult animals. "( The comparative electrophysiologic and hemodynamic effects of verapamil in puppies and adult dogs.
Driscoll, D; Entman, ML; Gibson, R; Gillette, P; Hartley, C, 1981
)
1.95
"Verapamil has complex influences on ventricular function owing to its direct myocardial effects, vasodilation, and reflex activation of the sympathetic nervous system. "( Effect on verapamil on ventricular function: studies in denervated human heart.
Edwards, T; Herman, BA; Schulman, DS; Uretsky, BF; Ziady, G, 1993
)
2.13
"Verapamil has been shown to ameliorate silent myocardial perfusion defects documented by thallium-201 in patients with HC."( Effect of verapamil on absolute myocardial blood flow in hypertrophic cardiomyopathy.
Camici, PG; Cecchi, F; Choudhury, L; Gistri, R; Montereggi, A; Salvadori, PA; Sorace, O, 1994
)
1.41
"Verapamil has been shown to partially restore drug sensitivity in tumour cells rendered resistant in vitro."( A randomised clinical study of verapamil in addition to combination chemotherapy in small cell lung cancer. West of Scotland Lung Cancer Research Group, and the Aberdeen Oncology Group.
Milroy, R, 1993
)
1.29
"Verapamil has also been suggested to potentiate the cardiotoxicity of doxorubicin."( Effect of verapamil on doxorubicin cardiotoxicity: altered muscle gene expression in cultured neonatal rat cardiomyocytes.
Akimoto, H; Billingham, ME; Bruno, NA; Slate, DL; Torti, FM; Torti, SV, 1993
)
1.41
"Verapamil has been the most commonly used agent for the treatment of PSVT with a narrow QRS complex."( [Paroxysmal supraventricular tachycardia in pregnancy. Value of adenosine and other anti-arrhythmia agents].
Hösl, P; Johannigmann, J; Rust, M; Schmidt, G, 1996
)
1.02
"Verapamil has well proven efficacy in the treatment of patients with hypertension, and early studies indicated its efficacy in the treatment of coronary artery disease. "( Verapamil: a review of its pharmacological properties and therapeutic use in coronary artery disease.
Benfield, P; Brogden, RN, 1996
)
3.18
"Verapamil has been associated with hyperprolactinaemia, but there have been no population-based studies. "( Hyperprolactinaemia and verapamil: prevalence and potential association with hypogonadism in men.
Aron, DC; Dombrowski, R; Fuehrer, S; Kwak, YS; Romeo, JH, 1996
)
2.04
"Verapamil has been found to be protective against crystal deposition."( Limitation of shockwave-induced enhanced crystal deposition in traumatized tissue by verapamil in rabbit model.
Akbay, C; Bakir, K; Korkmaz, C; Sarica, K; Sayin, N; Topçu, O; Yağci, F, 1999
)
1.25
"Verapamil and digoxin have been shown to modulate tachycardia-induced atrial electrical remodeling. "( Profibrillatory effects of verapamil but not of digoxin in the goat model of atrial fibrillation.
Allessie, MA; Duytschaever, MF; Garratt, CJ, 2000
)
2.05
"Verapamil has been shown to be a competitive inhibitor of Pgp, and was one of the first multidrug-resistant reversing agents identified."( Verapamil decreases accumulation of 99Tcm-MIBI and 99Tcm-tetrofosmin in human breast cancer and soft tissue sarcoma cell lines.
Kalinowska, W; Rodrigues, M; Sinzinger, H; Zielinski, C, 2001
)
2.47
"Verapamil has been shown to attenuate the extent of myocardial injury in murine models of chronic Trypanosoma cruzi infection. "( Cardioprotective effects of verapamil on myocardial structure and function in a murine model of chronic Trypanosoma cruzi infection (Brazil Strain): an echocardiographic study.
Chandra, M; Dominguez-Rosales, JA; Factor, SM; Jelicks, LA; Morris, SA; Petkova, SB; Rojkind, M; Shirani, J; Shtutin, V; Tanowitz, HB; Weiss, LM; Wittner, M, 2002
)
2.05
"Verapamil has a well-documented history as an effective antianginal agent when directly compared with a beta-blocker, and is more effective in reducing myocardial ischemia compared with amlodipine monotherapy."( Verapamil revisited: a transition in novel drug delivery systems and outcomes.
Prisant, LM,
)
2.3
"Verapamil has a lowering effect on the blood pressure even in the presence of advanced renal failure."( [The treatment of renal hypertension with verapamil in childhood (author's transl].
Alatas, H; Bein, G; Schärer, K, 1977
)
1.24
"(-)Verapamil has no comparable effects on the excitability of the atrial myocardium."( Relationship of antiarrhythmic to inotropic activity and antiarrhythmic qualities of the optical isomers of verapamil.
Raschack, M, 1976
)
0.98
"Verapamil has been associated with improved quality of life compared with propranolol (a beta-blocker) and nifedipine."( Quality of life in the treatment of hypertension. The effect of calcium antagonists.
Bulpitt, C; Fletcher, A, 1992
)
1
"Verapamil has been shown to overcome acquired drug resistance to vincristine in P388 leukemia both in vitro and in vivo. "( Verapamil preferentially potentiates in-vitro cytotoxicity of vincristine on malignant lymphoid cells.
Costea, NV; Malik, IA,
)
3.02
"Verapamil has been the most commonly used agent in the general population but it has several shortcomings, such as its potential to cause or exacerbate systemic hypotension, congestive heart failure, bradyarrhythmias, and ventricular fibrillation."( Adenosine in the treatment of maternal paroxysmal supraventricular tachycardia.
Koos, BJ; Mason, BA; Ricci-Goodman, J, 1992
)
1
"Verapamil has beneficial effects on ischemic myocardium, including reduction in electrophysiological derangements, prevention of intracellular K+ loss, and preservation of high-energy phosphates, but the mechanisms underlying these actions are not clear. "( Verapamil diminishes action potential changes during metabolic inhibition by blocking ATP-regulated potassium currents.
Bassett, AL; Kimura, S; Myerburg, RJ; Xi, H, 1992
)
3.17
"Verapamil has been proposed to be effective in early stages of atherogenic lesion formation to decrease aortic lesion area in cholesterol fed rabbits (Sievers R., et al., 1987)."( Calcium antagonists increase the amount of mRNA for the low-density lipoprotein receptor in skin fibroblasts.
Eckardt, H; Filipovic, I, 1991
)
1
"Verapamil has been proposed to modulate the multidrug resistance phenotype by competitive inhibition of an energy dependent efflux of cytotoxic drug. "( Transport of the multidrug resistance modulators verapamil and azidopine in wild type and daunorubicin resistant Ehrlich ascites tumour cells.
Bindslev, N; Demant, EJ; Friche, E; Jensen, PB; Sehested, M; Skovsgaard, T, 1990
)
1.98
"Even verapamil, however, has been shown to lead to hemodynamic improvement in some patients, at least after acute administration."( [Treatment of heart failure with calcium antagonists].
Dirschinger, J; Hall, D; Kraus, F; Rudolph, W, 1990
)
0.73
"(R)-verapamil, which has less calcium antagonistic activity and less in vivo toxicity than racemic verapamil, and D792, which has higher reversing potency and less in vivo toxicity than racemic verapamil, should be suitable for clinical applications to overcome drug resistance in cancer patients."( Reversal of multi-drug resistance in human KB cell lines by structural analogs of verapamil.
Keilhauer, G; Lechner, C; Ludwig, H; Pirker, R; Raschack, M, 1990
)
0.99
"Verapamil has in insurmountable inhibitory effect on 5-HT-induced aggregation at relatively low concentrations."( How can we inhibit 5-HT-induced platelet aggregation and why should we bother?
Bevan, J; Heptinstall, S, 1988
)
1
"Verapamil treatment has no significant effect, neither on the enzyme activation nor on the glycogen utilization."( [Enzyme activity of cardiac glycogen metabolism: study of an in situ hypoxia protocol in the rat].
Grably, S; Rossi, A; Verdys, M, 1989
)
1
"Verapamil has been shown to enhance immunotoxin activity but only at concentrations that are too high for in vivo use. "( Enhancement of the activity of immunotoxins by analogues of verapamil.
FitzGerald, DJ; Frank, Z; Pastan, I; Pirker, R; Raschack, M; Willingham, MC, 1989
)
1.96
"Verapamil has the same anti-anginal effect during exercise as beta-adrenoceptor blockers but has the advantage of increasing rather than decreasing the cardiac output and so fatigue both at rest and exercise commonly seen with beta-adrenoceptor blockers is not found with verapamil."( Verapamil in angina pectoris.
Kelly, DT, 1986
)
2.44
"Verapamil has been established as the drug of choice in the treatment of supraventricular dysrhythmias and is recognized as useful in the treatment of ischemic heart disease and hypertension. "( Terminating SVT-mediated recurrent ventricular fibrillation with verapamil.
Applebaum, D,
)
1.81
"Verapamil has been shown to be effective in reducing the frequency of episodes of ischemic pain in patients with unstable angina pectoris, and to be more effective than beta-adrenoceptor antagonists in such patients. "( Verapamil in unstable angina pectoris: failure to demonstrate a relationship between efficacy and plasma levels.
Elliott, SL; Horowitz, JD; Powell, AC, 1988
)
3.16
"Verapamil has been shown to be effective in the management of supraventricular tachycardia (SVT). "( Verapamil preceded by calcium in supraventricular tachycardia.
Branconi, JM; Hicks, P; Royal, SH; Sloan, R; Stringer, KA,
)
3.02
"Verapamil has been shown to reverse acquired drug resistance to Adriamycin (ADR) and vinblastine in the P388 leukemia and Ehrlich ascites carcinoma model systems. "( Effect of verapamil on in vitro cytotoxicity of adriamycin and vinblastine in human tumor cells.
Cox, TC; Crowley, J; Goodman, GE; Yen, YP, 1987
)
2.12
"Verapamil has been shown to potentiate cyclosporine's effect in inhibiting lectin-stimulated proliferation of murine and human lymphocytes, and in prolonging graft survival in experimental heterotopic cardiac transplantation in rats. "( The effect of verapamil on cellular uptake, organ distribution, and pharmacology of cyclosporine.
Baumgarten, WK; Fuortes, M; Holman, MJ; McMillen, MA; Mitchnick, E; Schaefer, HC; Tesi, RJ, 1987
)
2.08
"Verapamil and diltiazem have been shown in animals (opossum, baboon) to produce decreased contractions in esophageal smooth muscle, resulting in a decreased amplitude of peristalsis and decreased lower esophageal sphincter pressures."( Calcium-channel blocking agents for gastrointestinal disorders.
Castell, DO, 1985
)
0.99
"Verapamil has proven effective in preventing acute renal failure in animal models if given prior to the insult and hence possibly has a role in the preservation of cadaveric renal tissue for transplantation. "( Verapamil prevents post-transplant oliguric renal failure.
Charlesworth, JA; Duggan, KA; Macdonald, GJ; Pussell, BA, 1985
)
3.15
"Verapamil has been reported to reverse the abnormality of sodium transport seen in leucocytes from patients with essential hypertension and the present study demonstrates that sodium pump activity in leucocytes from control subjects is also stimulated by exposure to verapamil in vitro."( Effect of the calcium antagonist verapamil on human leucocyte sodium transport in vitro.
Gray, HH; Hilton, PJ; Johnson, VE; Poston, L, 1985
)
1.27
"Verapamil has been shown to depress the contractility of ischemic myocardium. "( Effect of verapamil on pH of ischemic canine myocardium.
Epstein, SE; Markle, DR; McGuire, DA; Patterson, RE; Vitale, D; Watson, RM, 1985
)
2.11
"Verapamil has become a popular antiarrhythmic drug for the acute management of supraventricular tachycardia in infants and children. "( Successful management of atrial flutter in a newborn with verapamil.
Casta, A; Richardson, CJ; Sapire, DW; Wolf, WJ, 1985
)
1.96

Actions

Verapamil caused a 45% increase in CsA area under the curve, maximum concentration, steady-state concentration, and trough level. Exercise capacity increased in 34 of 43 patients (79%) manifesting an increase in peak filling rate. Only one of 12 patients (8%) with unchanged or decreased peak fill rate (p less than .001)

ExcerptReferenceRelevance
"Verapamil injection can enhance autophagy, reduce the weight of fatty liver mice, improve liver function and liver regeneration."( Verapamil induces autophagy to improve liver regeneration in non-alcoholic fatty liver mice.
Bai, YN; Lai, JL; Lian, YE; Wang, YD; Wu, JY, 2021
)
2.79
"Verapamil promotes functional β-cell mass and improves glucose homeostasis in diabetic mice and humans with type 1 diabetes (T1D). "( Verapamil Prevents Decline of IGF-I in Subjects With Type 1 Diabetes and Promotes β-Cell IGF-I Signaling.
Chen, J; Lu, B; Qian, WJ; Sethupathy, P; Shalev, A; Xu, G, 2023
)
3.8
"Verapamil promotes β-cell IGF-I signaling by increasing phosphorylation of IGF-I receptor and its downstream effector AKT."( Verapamil Prevents Decline of IGF-I in Subjects With Type 1 Diabetes and Promotes β-Cell IGF-I Signaling.
Chen, J; Lu, B; Qian, WJ; Sethupathy, P; Shalev, A; Xu, G, 2023
)
3.07
"Verapamil did not increase systemic exposure to VI following administration of the UMEC/VI combination."( Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study.
Crater, G; Hughes, S; Kelleher, D; Mehta, R; Preece, A, 2013
)
1.51
"Verapamil can enhance the cytotoxic effects of chemotherapeutic drugs and multidrug resistance by targeting the transport function of the P-glycoprotein (P-gp)."( Verapamil inhibits tumor progression of chemotherapy-resistant pancreatic cancer side population cells.
Bao, Q; Bruns, CJ; Camaj, P; Ellwart, JW; Guba, M; Hartig, R; Jauch, KW; Mysliwietz, J; Nelson, PJ; Schwarz, B; Zhao, L; Zhao, Y, 2016
)
2.6
"Verapamil can inhibit fertilization in vitro through regulating Myb expression of sperm, while GABA, dbcAMP and Verapamil may affect the process of fertilization through the way other than Myb expression."( [Study of effect and mechanism of c-myb on the fertilization in mouse].
Wu, LF; Zhang, J; Zheng, YH, 2005
)
1.05
"Verapamil could enhance the absorption of isoquercitrin, hyperoside, myricetin and quercetin-3'-O-glucoside by inhibiting P-glycoprotein (P-gp) drug efflux pump."( [Absorption of flavonoids from Abelmoschus manihot extract by in situ intestinal perfusion].
Duan, JA; Guo, JM; Qian, DW; Shu, Y; Xue, CF, 2011
)
1.09
"Verapamil and ibutilide blunt the atrial fibrillation-induced shortening of atrial refractoriness that may predispose to an immediate recurrence of atrial fibrillation after cardioversion. "( Comparison of verapamil and ibutilide for the suppression of immediate recurrences of atrial fibrillation after transthoracic cardioversion.
Knight, BP; Morady, F; Oral, H; Ozaydin, M; Pelosi, F; Sticherling, C; Strickberger, SA; Tada, H, 2002
)
2.12
"Verapamil does not inhibit (99m)TcN-NOET uptake in situ in normal and ischemic canine myocardium. "( Verapamil does not inhibit 99mTcN-NOET uptake in situ in normal or ischemic canine myocardium.
Bontron, R; Broisat, A; Fagret, D; Ghezzi, C; Mathieu, JP; Pasqualini, R; Riou, LM; Vanzetto, G, 2003
)
3.2
"Verapamil is known to suppress shortening of the atrial effective refractory period (AERP) during relatively short-term atrial pacing, although the effect of a long-term stimulation model is unclear. "( Verapamil suppresses the inhomogeneity of electrical remodeling in a canine long-term rapid atrial stimulation model.
Inuo, K; Izumi, T; Kojima, J; Moriguchi, M; Niwano, S; Yoshizawa, N, 2003
)
3.2
"Verapamil did not cause a significant change either in the SN or in the PVD cycle length."( Response to pharmacological challenge of dissociated pulmonary vein rhythm.
Abdul-Karim, A; Bhargava, M; Burkhardt, D; Erciyes, D; Khaykin, Y; Marrouche, N; Martin, DO; Natale, A; Rossillo, A; Saliba, W; Schweikert, R; Verma, A; Wazni, OM, 2005
)
1.05
"Verapamil can inhibit proliferation of HCT cells via inducing cell apoptosis."( In vitro growth inhibition of human colonic tumor cells by Verapamil.
Cao, QZ; Niu, G; Tan, HR, 2005
)
2.01
"Verapamil did not increase the intestinal absorption of fexofenadine, even though the jejunal permeability of fexofenadine, verapamil, and antipyrine showed a tendency to increase in G2."( First-pass effects of verapamil on the intestinal absorption and liver disposition of fexofenadine in the porcine model.
Bergman, E; Bondesson, U; Forsell, P; Hedeland, M; Knutson, L; Lennernäs, H; Petri, N, 2006
)
1.37
"Verapamil was found to inhibit the responses significantly."( Positive inotropic effect of Murraya koenigii (Linn.) Spreng extract on an isolated perfused frog heart.
Juvekar, AR; Shah, KJ, 2006
)
1.06
"Verapamil can cause significantly effect on transport of Danshensu: P(app,A-B) increased and P(app,B-A) decreased ."( [Transport mechanism of danshensu across Caco-2 monolayer model].
Cheng, YY; Zhao, XP; Zhu, DF, 2006
)
1.06
"Verapamil was found to enhance PYM-induced cytotoxicity and apoptosis in KB cells. "( Synergistic effects of verapamil on pingyangmycin-induced cytotoxicity and apoptosis in KB cells.
Chang, YC; Ho, YC; Tai, KW, 2007
)
2.09
"Verapamil prevented the increase in fibrillatory frequency in PAF patients in relatively long-term observation. "( Effect of oral L-type calcium channel blocker on repetitive paroxysmal atrial fibrillation: spectral analysis of fibrillation waves in the Holter monitoring.
Fujiki, A; Fukaya, H; Hatakeyama, Y; Izumi, T; Niwano, S; Sasaki, T, 2007
)
1.78
"For verapamil to inhibit superoxide generation, cytochalasin B was necessary."( Cytochalasin B facilitates the inhibition of human polymorphonuclear leukocyte generation of superoxide by verapamil.
Busse, WW; Pratt, A; Steiner, RD, 1984
)
0.96
"Verapamil was found to produce considerable tracheal smooth muscle relaxation from a threshold concentration of 2 X 10(-7) M and with maximum effect at 10(-3) M."( The potential bronchodilator action of verapamil.
Cade, JF; Clegg, EA; Moulds, RF; Pain, MC; Rubinfeld, AR; Santamaria, JD, 1984
)
1.26
"Verapamil was found to lower the basal blood glucose concentration in the 36 h fasted subjects."( Blood glucose lowering effect of verapamil in fasted man.
Andersson, DE; Röjdmark, S, 1984
)
1.27
"Verapamil may produce an unrecognized source of weakness in the anesthetized patient either alone or through interaction with anesthetic agents or adjuncts."( Neuromuscular and electrocardiographic responses to verapamil in dogs.
Gintautas, J; Kraynack, BJ; Lawson, NW, 1983
)
1.24
"Verapamil was found to blunt the glucose response to glucagon in the patients with NIDDM, whereas it augmented the glucose response to glucagon in the controls."( Calcium-antagonistic effects on glucose response to glucagon in patients with non insulin-dependent diabetes mellitus and in normoglycemic subjects.
Andersson, DE; Hed, R; Röjdmark, S; Sundblad, L, 1981
)
0.98
"verapamil, inhibit binding (IC50 = 250 nM)."( Specific calcium antagonist binding sites in brain.
Marangos, PJ; Martino, AM; Miller, C; Patel, J, 1982
)
0.99
"Verapamil failed to produce a consistent shift in the membrane responsiveness curve (Vmax versus take-off membrane potentials), although the development of early, slow action potentials was blocked."( Effects of verapamil on action potentials of Purkinje fibers.
Dersham, GH; Han, J, 1980
)
1.37
"Verapamil significantly increase the level of these metabolites."( Protective effect of verapamil on regional myocardial ischaemic injury in dog.
Kobusiewicz, W; Ledwozyw, A; Michalak, J; Ogonowska-Kobusiewicz, M; Zywicki, W, 1995
)
1.33
"Verapamil did not enhance drug accumulation but inhibited drug efflux in K562r cells."( [Intracellular accumulation, retention, and distribution of anthracyclines in a multidrug-resistant variant K562r].
Chen, WY; Hu, X, 1994
)
1.01
"Verapamil produced an increase in the formation and release of malonyldialdehyde."( Calcium channel antagonist verapamil modulates human spermatozoal functions.
Anand, RJ; Kanwar, U; Sanyal, SN, 1994
)
1.31
"Verapamil can produce depression of left ventricular function, delayed atrioventricular conduction, and hypotension, which can be potentiated by hyperkalemia. "( Effect of hyperkalemia on myocardial depression by verapamil in isolated hearts.
Boyd, SG; Jolly, SR; Mehta, P; Movahed, A; Reeves, WC; Wilson, VP, 1993
)
1.98
"Verapamil blunted the increase in plasma potassium in diabetic and nondiabetic rats compared with the respective controls."( Effect of verapamil on disposition of intravenous potassium in diabetic anephric uremic rats.
Blum, M; Cabili, S; Davidovics, Y; Iaina, A; Peer, G; Serban, I; Wollman, Y, 1993
)
1.41
"Verapamil caused a lower ventricular rate, but only six (19%) of the patients (n = 31) converted to sinus rhythm within 4 h (p < 0.01) and 16 (52%) within 24 h (NS)."( The effect of magnesium versus verapamil on supraventricular arrhythmias.
Birkeland, K; Gullestad, L; Høyer, MM; Kjekshus, J; Mølstad, P; Vanberg, P, 1993
)
1.29
"Verapamil can cause reduction in the extent of ischemic injury after reperfusion of hypertrophied myocardium."( Verapamil reduces the size of reperfused ischemically injured myocardium in hypertrophied rat hearts as assessed by magnetic resonance imaging.
Derugin, N; Higgins, CB; Lauerma, K; Saeed, M; Wendland, MF; Yu, KK, 1996
)
2.46
"Verapamil Vp was used because it was described that calcium channel blockers protect cells from nephrotoxicants and from ischaemia."( Evidence for renal ischaemia as a cause of mercuric chloride nephrotoxicity.
Elías, MM; Girardi, G, 1995
)
1.01
"Verapamil as a cause for his increased prolactin concentration was not considered initially."( Verapamil-induced hyperprolactinemia complicated by a pituitary incidentaloma.
Aron, DC; Dombrowski, RC; Romeo, JH, 1995
)
2.46
"Verapamil overdose, because of its frequency and severity, represents a significant problem for the emergency physician. "( Cardiac dysrhythmias in severe verapamil overdose: characterization with a canine model.
Koury, SI; Stone, CK; Thomas, SH, 1996
)
2.02
"Verapamil did not increase DNR toxicity in four of these eight cases, but was more efficient in one other MDR1(+) case."( Effect of the multidrug inhibitor GG918 on drug sensitivity of human leukemic cells.
Faussat, AM; Marie, JP; Simonin, G; Zhou, DC; Zittoun, R, 1997
)
1.02
"Dexverapamil did not increase epirubicin toxicity."( Phase II trial of dexverapamil and epirubicin in patients with non-responsive metastatic breast cancer.
Kroeger, N; Kupper, H; Lehnert, M; Mross, K; Schueller, J; Thuerlimann, B, 1998
)
1.13
"Verapamil can increase the plasma concentration of digoxin up to 60-90%."( P-glycoprotein system as a determinant of drug interactions: the case of digoxin-verapamil.
Beijnen, JH; Koks, CH; Schellens, JH; Verschraagen, M, 1999
)
1.25
"Verapamil showed to increase all parameters of phagocytosis in comparison with control."( [Pentoxifylline and verapamil influence on the phagocytosis of peritoneal macrophages from women with endometriosis].
Czygier, M; Laudański, P; Szamatowicz, J, 2000
)
1.35
"Verapamil promotes AF in normal dogs by promoting multiple circuit reentry, an effect dependent on intact autonomic tone and not shared by diltiazem."( Effects of verapamil on atrial fibrillation and its electrophysiological determinants in dogs.
Bénardeau, A; Fareh, S; Nattel, S, 2001
)
2.14
"Verapamil blunted the increase of the coronary vascular resistance index to the CPT in comparison with its change at CPT after propranolol."( Comparison of the effect of verapamil and propranolol on response of coronary vasomotion to cold pressor test in symptomatic patients with hypertrophic cardiomyopathy.
Dimitrow, PP; Dubiel, JS; Krzanowski, M; Nizankowski, R; Szczeklik, A, 2000
)
1.32
"Verapamil can inhibit HSFB proliferation, collagen synthesis and gene expression by a dose-depended manner, especially treated with 100 mumol/L Verapamil."( [The biological effect of verapamil on hypertrophic scar fibroblast].
Guo, S; Lu, K; Wang, Z, 2001
)
2.05
"Verapamil produced an increase in the A-H interval in 4 of the 5 cases studied with His bundle recordings."( [Antiarrhythmic effects of verapamil].
Férez, S; Malo, R; Martínez-Ríos, MA; Salazar, E; Shapiro, M,
)
1.15
"For verapamil SR, the mean increase in HR was 5 beats/min (to 80 beats/min) and the mean decrease in HR was 13 beats/min (to 62 beats/min)."( Comparative efficacy, safety and pharmacokinetics of verapamil SR vs verapamil IR in hypertensive patients.
Cubeddu, LX; Faggin, BM; Fuenmayor, NT, 1992
)
1.01
"Verapamil failed to inhibit the secretion of pepsinogen induced by the drugs in ordinary culture medium containing Ca2+."( Role of intracellular Ca2+ and the calmodulin messenger system in pepsinogen secretion from isolated rabbit gastric mucosa.
Itoh, M; Miyamoto, T; Noguchi, Y; Yokochi, K, 1992
)
1
"Verapamil did not lower ambulatory blood pressure at this dose (which is lower than is now commonly used), but reductions in ambulatory blood pressure were similar for atenolol, metoprolol, and chlorthalidone."( Effectiveness of antihypertensive medications in office and ambulatory settings: a placebo-controlled comparison of atenolol, metoprolol, chlorthalidone, verapamil, and an atenolol-chlorthalidone combination.
Durel, LA; Hayashi, PJ; Schneiderman, N; Weidler, DJ, 1992
)
1.2
"Verapamil was found to increase the G2 blocking effect of bleomycin A5 prominently in mouse S-180 and human HEP-2 cell lines."( [Mechanism of enhancement of bleomycin A5 antitumor activity by verapamil].
He, NG; Liu, ZM; Song, PG; Xue, SB; Zhang, HQ, 1991
)
1.24
"Verapamil did not cause variations in GH secretion following GHRH and insulin-induced hypoglycemia, whereas nifedipine significantly reduced the elevation in GH induced by GHRH; however the GHRH-mediated GH rise still remained within the normal range in all subjects."( Calcium ion and pituitary hormones: effect of calcium channel blockers on stimulated secretion of pituitary hormones.
Delitala, G; Palermo, M; Tomasi, PA,
)
0.85
"Verapamil tended to increase the renal and systemic effects of stevioside."( Effect of calcium and verapamil on renal function of rats during treatment with stevioside.
Melis, MS; Sainati, AR, 1991
)
1.32
"Verapamil induced a 44% increase in steady-state plasma concentrations of digoxin, from 0.80 +/- 0.24 to 1.15 +/- 0.40 nmol/L (p less than 0.01)."( Digoxin-verapamil interaction: reduction of biliary but not renal digoxin clearance in humans.
Angelin, B; Arvidsson, A; Beck, O; Dahlqvist, R; Hedman, A; Nilsson, B; Olsson, M; Schenck-Gustafsson, K, 1991
)
1.44
"Verapamil induced an increase in the cellular cholesterol content in preloaded cells."( Verapamil enhances high-density lipoprotein processing in Hep G2 cells preloaded with cholesterol.
Auclair, M; Chappey-Gillet, B; Mazière, C; Mazière, JC; Salmon, S, 1990
)
2.44
"Verapamil failed to inhibit insulin-stimulated choleresis at a taurocholate infusion rate of 80 nmole/g liver/min."( Effect of verapamil on insulin-stimulated choleresis.
Hanks, JB; Jones, RS; Krusch, DA; Sack, J, 1990
)
1.4
"Verapamil was found to enhance the cytotoxic effect of vincristine against ovarian cancer cells."( [In vitro drug-resistance decrease of ovarian cancer cells].
Lu, SM, 1990
)
1
"Verapamil caused a 45% increase in CsA area under the curve, maximum concentration, steady-state concentration, and trough level."( The effects of calcium channel blockers on cyclosporine and its metabolites in renal transplant recipients.
Awni, WM; Heim-Duthoy, KL; Kasiske, BL; Rao, KV; Tortorice, KL, 1990
)
1
"Verapamil was found to inhibit the secretion of amylase but to have no effect on lipase, trypsin, or total protein."( The effect of verapamil on pancreatic exocrine secretion.
Bank, S; Burns, GP; Gersten, M; Stein, TA; Zimmerman, HM, 1986
)
1.35
"Verapamil may cause detrimental results when given to patients with the Wolff-Parkinson-White syndrome and atrial fibrillation."( Deleterious effects of intravenous verapamil in Wolff-Parkinson-White patients and atrial fibrillation.
Agmon, J; Katz, A; Ovsyscher, IA; Rechavia, E; Sagie, A; Sclarovsky, S; Strasberg, B, 1989
)
1.28
"Verapamil was shown to increase growth inhibition and decrease viability of PY815 mastocytoma cells treated with the anti-cancer drug mAMSA 4'-(9-acridinylamino)methanesulphon-m-anisidide (mAMSA) or its normally inactive congener, 4'-(9-acridinylamino)methanesulphon-o-anisidide (oAMSA). "( Potentiation of 4'-(9-acridinylamino)methanesulphon-m-anisidine) action by verapamil.
Darkin, S; Ralph, RK, 1986
)
1.94
"The verapamil-induced increase in Qrbc is probably mainly mediated by a relaxation of the afferent arteriole of the juxtamedullary nephrons."( The calcium entry blocker verapamil increases red cell flux in the vasa recta of the exposed renal papilla.
Hansell, P; Sjöquist, M; Ulfendahl, HR, 1988
)
1.06
"Verapamil did not inhibit ANG II-stimulated Ca2+ efflux or the change in cell shape."( Effect of angiotensin II on Ca2+ kinetics and contraction in cultured rat glomerular mesangial cells.
Kim, JK; Meyer-Lehnert, H; Schrier, RW; Takeda, K, 1988
)
1
"Verapamil reversed the increase in force at high frequencies produced by theophylline."( Interaction of theophylline, verapamil, and diltiazem on hamster diaphragm muscle force in vitro.
Esau, SA, 1988
)
1.29
"Verapamil induced an increase in heart rate at rest due to sympathetic counterregulation secondary to a reduction of systolic and diastolic blood pressure."( Verapamil abolishes exercise-induced regional contractile dysfunction in dogs.
Ehrendorfer, S; Krumpl, G; Mayer, N; Raberger, G; Schneider, W, 1988
)
2.44
"Verapamil did not inhibit AVP-stimulated Ca2+ efflux and cell contraction."( AVP-induced Ca fluxes and contraction of rat glomerular mesangial cells.
Kim, JK; Meyer-Lehnert, H; Schrier, RW; Takeda, K, 1988
)
1
"verapamil) inhibit ( +/- )-[3H]nitrendipine binding with micromolar inhibition constants, but the benzothiazepine D-cis-diltiazem, a potent Ca2+-channel blocker, is without effect."( A novel 1,4-dihydropyridine-binding site on mitochondrial membranes from guinea-pig heart, liver and kidney.
Glossmann, H; Zernig, G, 1988
)
1
"Verapamil was chosen because of its aqueous solubility and hence suitability for aerosol administration in higher doses than previously given."( Effects of the calcium channel blocker, verapamil, on asthmatic airway responses to muscarinic, histaminergic, and allergenic stimuli.
Fish, JE; Norman, PS, 1986
)
1.26
"Verapamil and diltiazem cause a significant increase in plasma digoxin concentrations."( Clinical pharmacokinetics of verapamil, nifedipine and diltiazem.
Echizen, H; Eichelbaum, M,
)
1.14
"The verapamil-induced increase in calcium plasma-to-lumen translocation was abolished by bile duct ligation."( Direct effects of calcium channel blockers on duodenal calcium transport in vivo.
Fox, J; Green, DT, 1986
)
0.75
"Verapamil appeared to increase pulmonary venous admixture."( Verapamil in multifocal atrial tachycardia. Hemodynamic and respiratory changes.
Burnett, CR; Hazard, PB, 1987
)
2.44
"Verapamil was found to enhance the activity of both ADR and AD-32 against a HBTCL (T24), found to be resistant to both agents."( Effects of N-trifluoroacetyladriamycin-14-valerate (AD-32) on human bladder tumor cell lines.
Herrod, HG; Hunter, RF; Israel, M; Niell, HB, 1987
)
0.99
"Verapamil may enhance the cytotoxicity of EGF-PE by blocking lysosomal degradation of EGF-PE."( [The effect of calcium antagonists on intracellular transport of epidermal growth factor and the conjugate of epidermal growth factor with pseudomonas exotoxin].
Akiyama, S, 1985
)
0.99
"Verapamil-mediated increase in net VP-16 transport was rapid (1 to 2 min), and allowed for the same elevation of steady-state VP-16 concentration, whether verapamil was added simultaneously with VP-16 or was added after a steady-state level of VP-16 was achieved."( Verapamil-induced augmentation of etoposide accumulation in L1210 cells in vitro.
Ross, WE; Yalowich, JC, 1985
)
2.43
"The verapamil-induced increase of drug accumulation in resistant cells is accounted for at least in part by the blockage or slowing of Rho-123 efflux from these cells."( Reversal of resistance to rhodamine 123 in adriamycin-resistant Friend leukemia cells.
Krishan, A; Lampidis, TJ; Munck, JN; Tapiero, H, 1985
)
0.75
"The verapamil-induced increase in peak left ventricular filling rate at rest (from 3.1 +/- 1.3 to 3.7 +/- 1.3 end-diastolic volumes/sec; p less than .001) was associated with an increase in exercise tolerance (from 5.9 +/- 3.6 to 8.7 +/- 4.7 min; p less than .001); exercise capacity increased in 34 of 43 patients (79%) manifesting an increase in peak filling rate but only one of 12 patients (8%) with unchanged or decreased peak filling rate (p less than .001)."( Verapamil-induced improvement in left ventricular diastolic filling and increased exercise tolerance in patients with hypertrophic cardiomyopathy: short- and long-term effects.
Bacharach, SL; Bonow, RO; Dilsizian, V; Green, MV; Maron, BJ; Rosing, DR, 1985
)
2.19

Treatment

Verapamil pretreatment significantly increased oxidation of all substrates by the subsequently isolated Polytron mitochondria, but only succinate-supported respiration returned to control levels. Treatment with verapamIL, an inhibitor of P-gp, significantly improved the absorption of enrofloxacin in both healthy and sick dogs.

ExcerptReferenceRelevance
"Verapamil treatment (24, 48 mg/kg/day) significantly affected nano mechanical properties of the femurs, and tended to improve bone microstructures and macro mechanical properties of the femurs, which provided guidance for the selection of verapamil dose in the treatment of type 2 diabetic patients."( Effect of verapamil on bone mass, microstructure and mechanical properties in type 2 diabetes mellitus rats.
Cen, H; Gong, H; Hu, X; Li, C; Shi, P; Wu, X, 2022
)
2.57
"Verapamil treatment had no significant effect on blood glucose, but blood glucose tended to decline with the increase of verapamil-treated time and dose. "( Improved fatigue properties, bone microstructure and blood glucose in type 2 diabetic rats with verapamil treatment.
Gong, H; Hu, X; Jia, S; Li, J; Wu, X, 2022
)
2.38
"Verapamil treatment was successful in reducing defibrillator discharge frequency of the KCNQ1/TRPM4 dual mutation patient."( In Vitro Drug Screening Using iPSC-Derived Cardiomyocytes of a Long QT-Syndrome Patient Carrying KCNQ1 & TRPM4 Dual Mutation: An Experimental Personalized Treatment.
Guo, Y; Han, Y; Li, Y; Liang, X; Lu, Y; Sang, W; Tang, B; Wang, F; Wang, L; Xiaokereti, J; Xing, Q; Zhang, J; Zhang, L; Zhou, X; Zukela, T, 2022
)
1.44
"Verapamil treatment reduced expression of TXNIP and NOD-like receptor pyrin domain-containing-3 inflammasome activation in the perihematomal area."( Verapamil inhibits TXNIP-NLRP3 inflammasome activation and preserves functional recovery after intracerebral hemorrhage in mice.
Ishrat, T; Ismael, S; Parveen, A; Patrick, D; Salman, M; Stanfill, AG, 2022
)
2.89
"Verapamil treatment reduced sperm concentration."( Verapamil-induced ion channel and miRNA expression changes in rat testis and/or spermatozoa may be associated with male infertility.
Etem Önalan, E; Güngör, İH; Kaya Tektemur, N; Kuloğlu, T; Tektemur, A; Türk, G, 2020
)
2.72
"Verapamil treatment commenced 48 h post-streptozotocin insult and continued for 16 weeks."( Inhibition of thioredoxin-interacting protein and inflammasome assembly using verapamil mitigates diabetic retinopathy and pancreatic injury.
Eissa, LD; El-Azab, MF; Ghobashy, WA, 2021
)
1.57
"When verapamil treatment was stopped, the patient experienced AF recurrence."( Treatment with verapamil for restoration of sinus rhythm in atrial fibrillation with rapid ventricular response: A case report.
Chen, L; Liang, D; Lin, J; Lin, Y; Qi, G; Tian, W; Wang, X, 2019
)
1.32
"Verapamil treatment was significantly more effective in decreasing the incidence of no-reflow (risk ratio [RR]: 0.33; 95% confidence interval [CI]: 0.23 to 0.50) as well as reducing the corrected thrombolysis in myocardial infarction (TIMI) frame count (CTFC) (weighted mean difference: -11.62; 95% CI: -16.04 to -7.21) and improving the TIMI myocardial perfusion grade (TMPG) (RR: 0.43; 95% CI: 0.29 to 0.64)."( Short-term effect of verapamil on coronary no-reflow associated with percutaneous coronary intervention in patients with acute coronary syndrome: a systematic review and meta-analysis of randomized controlled trials.
Li, L; Liu, Y; Su, Q, 2013
)
1.43
"Verapamil treatment effected particularly E15 cells and immunoexpression of HPCs significantly decreased."( Hepatic progenitor cell inhibition during embryonic period with high dose verapamil; liable joint to the cancer therapy.
Bilir, A; Oktem, G; Soner, BC; Uslu, S; Uysal, A, 2013
)
1.34
"Verapamil treatment prevented increased permeability in HT29 cells and led to an increase in IgA transport."( Salutary effect of calcium channel blockade following hypoxic and septic insult.
Ali, AA; Diebel, LN; Liberati, DM; Mutchnick, S, 2014
)
1.12
"Verapamil treatment reduced the severity and number of lytic lesions in cardiomyocytes, induced considerable glycogen accumulation in the sarcoplasm and its sequestration, promoted normalization, and prevented pronounced decrease of the relative RyR2 mRNA and SERCA2a mRNA in rat myocardium."( Expression of ryanodine receptor mRNA and sarcoplasmic Ca²⁺-ATPase mRNA in the myocardium and intracellular reorganization of cardiomyocytes in dyslipidemia and during verapamil treatment.
Klinnikova, MG; Lushnikova, EL; Nepomnyashchikh, LM; Pichigin, VI; Yuzhik, EI, 2015
)
1.33
"Verapamil treatment may preserve the oxidant capacity of the kidneys and subsequently limit the crystal deposition induced by hyperoxaluria."( Hyperoxaluria-induced tubular ischemia: the effects of verapamil on the antioxidant capacity of the affected kidneys.
Eryildirim, B; Hamarat, B; Kafkasli, A; Narter, F; Ozturk, O; Sahin, C; Sarica, K; Yazici, O, 2016
)
1.4
"The verapamil-treated group showed a faster wound closure rate in comparison with control and gel-base groups (P = .007 and P = .011). "( Verapamil, a Calcium-Channel Blocker, Improves the Wound Healing Process in Rats with Excisional Full-Thickness Skin Wounds Based on Stereological Parameters.
Ashkani-Esfahani, S; Fatheazam, R; Hosseinabadi, OK; Kardeh, S; Khoshneviszadeh, M; Mehrvarz, S; Moafpourian, Y; Moezzi, P; Nadimi, E; Noorafshan, A; Rafiee, S, 2016
)
2.44
"Verapamil treatment during EPS totally abrogated the EPS-induced NMDA receptor mRNA expression."( Electric pulse stimulation induces NMDA glutamate receptor mRNA in NIH3T3 mouse fibroblasts.
Hatakeyama, H; Kanazaki, M; Kanzaki, M; Nagatomi, R; Okutsu, S; Tsubokawa, H, 2008
)
1.07
"The verapamil treatment induced a decrease in parameters reflecting cardiac function; resting heart rate [from mean 97 to 80 beats per min (17.5%), p<0.001] and mean arterial pressure (8.5%, p=0.001)."( N-terminal-pro-B-type natriuretic peptide during pharmacological heart rate reduction in hyperthyroidism.
Andersen, HU; Corell, P; Faber, J; Jarlov, A; Kistorp, C; Schultz, M, 2009
)
0.83
"Verapamil pre-treatment significantly elevated imipramine concentrations in all brain regions studied. "( Verapamil in treatment resistant depression: a role for the P-glycoprotein transporter?
Clarke, G; Cryan, JF; Dinan, TG; O'Mahony, SM, 2009
)
3.24
"Verapamil pretreatment completely restored the adrenocortical responses to normal level."( [Calcium-dependent mechanisms of stress disorders and noradrenergic responses of the hypothalamo-pituitary-adrenal system in neonatally androgenized female rats].
Nosenko, ND; Reznikov, OH; Sinitsyn, PV, 2008
)
1.07
"Verapamil treatment augmented prolongation of MAPD( 90) caused by dofetilide or domperidone (P < .01)."( Gender-related differences in drug-induced prolongation of cardiac repolarization in prepubertal guinea pigs.
Hreiche, R; Morissette, P; Turgeon, J; Zakrzewski-Jakubiak, H, 2009
)
1.07
"Verapamil pretreatment of the cells also inhibited matrix vesicle alkaline phosphatase activity and reduced the ability of these matrix vesicles to subsequently calcify on a type I collagen extracellular matrix scaffold."( Verapamil inhibits calcification and matrix vesicle activity of bovine vascular smooth muscle cells.
Chen, NX; Chen, X; Kircelli, F; Moe, SM; O'Neill, KD, 2010
)
2.52
"Verapamil, after a pre-treatment of 0.5-10 s, accelerated the decay of whole-cell or macroscopic outside-out currents within milliseconds of ACh application even at clinically attainable doses."( Mechanism of verapamil action on wild-type and slow-channel mutant human muscle acetylcholine receptor.
Di Castro, MA; Eusebi, F; Fucile, S; Grassi, F; Moriconi, C, 2010
)
1.45
"Verapamil poisoned rats treated with 2.25 g/kg of SBE-CD showed increased toxicity."( Effect of cyclodextrin infusion in a rat model of verapamil toxicity.
Aks, SE; Bryant, SM; Mottram, AR, 2011
)
1.34
"Verapamil add-on treatment has been suggested as a novel therapeutic concept for overcoming transporter-mediated pharmacoresistance. "( Add-on treatment with verapamil in pharmacoresistant canine epilepsy.
Jambroszyk, M; Potschka, H; Tipold, A, 2011
)
2.13
"Verapamil add-on treatment (6.2-7.3 mg/kg) did not affect phenobarbital concentrations in plasma or cerebrospinal fluid. "( Add-on treatment with verapamil in pharmacoresistant canine epilepsy.
Jambroszyk, M; Potschka, H; Tipold, A, 2011
)
2.13
"Verapamil treatment reduced both cardiac (P < 0.02) and hepatic (P < 0.003) iron levels significantly by 34% and 28%, respectively."( Interdependence of cardiac iron and calcium in a murine model of iron overload.
Brewer, C; Otto-Duessel, M; Wood, JC, 2011
)
1.09
"In verapamil-treated mice, no contrast enhancement was observed."( In vivo imaging of human breast cancer mouse model with high level expression of calcium sensing receptor at 3T.
Baio, G; Carbotti, G; Cilli, M; Emionite, L; Fabbi, M; Ghedin, P; Neumaier, CE; Prato, S; Salvi, S; Tagliafico, A; Truini, M, 2012
)
0.89
"Verapamil treated fibrotic rat's liver revealed significant regression in liver fibrosis scores with positive α-SMA immunostaining."( Improved antifibrotic effect of a combination of verapamil and silymarin in rat-induced liver fibrosis.
Gouda, NA; Khodeir, MM; Mahmoud, ME; Shafik, AN, 2011
)
1.34
"Verapamil treatment reversed MEK-induced viability of kidney SP cells."( ABCG2 protects kidney side population cells from hypoxia/reoxygenation injury through activation of the MEK/ERK pathway.
Gao, DK; Ge, GQ; Liu, HB; Liu, SB; Liu, WH; Sun, SR; Wang, HM; Zhang, P, 2013
)
1.11
"Verapamil/CDDP co-treatment inhibited tumor xenograft growth via the downregulation of MRP1 expression."( Mechanisms of verapamil-enhanced chemosensitivity of gallbladder cancer cells to platinum drugs: glutathione reduction and MRP1 downregulation.
Chen, T; Li, H; Li, X; Liu, Q; Wang, H; Wang, J; Wang, W; Yi, J, 2013
)
1.47
"Verapamil treatment reversed the progesterone enhanced Cd cytolethality."( Involvement of calcium channels in the sexual dimorphism of cadmium-induced hepatotoxicity.
Baker, TK; Carfagna, MA; Smith, WC; VanVooren, HB, 2003
)
1.04
"Verapamil treatment seems to ameliorate the renal effects of exercise on GFR in these patients, and this may in part be mediated via a stimulatory effect on ANP."( Effect of light exercise on renal hemodynamics in patients with hypertension and chronic renal disease.
Iversen, BM; Myking, O; Ofstad, J; Svarstad, E, 2002
)
1.04
"By verapamil treatment, a clinically relevant plasma concentration of the calcium channel inhibitor was attained (mean +/- SEM, 290 +/- 152 ng/mL). "( Verapamil does not inhibit 99mTcN-NOET uptake in situ in normal or ischemic canine myocardium.
Bontron, R; Broisat, A; Fagret, D; Ghezzi, C; Mathieu, JP; Pasqualini, R; Riou, LM; Vanzetto, G, 2003
)
2.38
"In verapamil treated patients atrial fibrillation occurred 1.5-2 times more often than in amlodipine treated patients or in patients receiving no calcium antagonists."( [Effect of calcium antagonists verapamil and amlodipine on the risk of development of atrial fibrillation after coronary artery bypass grafting].
Afanas'ev, SA; Akhmedov, ShD; Antonchenko, IV; Dzhavadova, GK; Evtushenko, AV; Kandinskiĭ, ML; Kozlov, BN; Popov, SV; Shipulin, VM; Vecherskiĭ, IuIu, 2003
)
1.12
"The verapamil treatment resulted in rapid increase in ABCA1 protein and its mRNA, but not the ABCG1 mRNA, another target gene product of the nuclear receptor liver X receptor (LXR)."( Verapamil increases the apolipoprotein-mediated release of cellular cholesterol by induction of ABCA1 expression via Liver X receptor-independent mechanism.
Abe-Dohmae, S; Arakawa, R; Inoue, K; Nishimaki-Mogami, T; Suzuki, S; Tamehiro, N; Tanaka, AR; Ueda, K; Yokoyama, S, 2004
)
2.25
"Verapamil treatment eliminated evidence of vasospasm and ameliorated histological and functional evidence of cardiomyopathic progression."( Secondary coronary artery vasospasm promotes cardiomyopathy progression.
Collins, KA; Earley, JU; Hack, AA; Korcarz, CE; Lang, RM; Lapidos, KA; Lyons, MR; McNally, EM; Wheeler, MT; Zarnegar, S, 2004
)
1.04
"Verapamil treatment only restored GSH levels in heart, having no effect on other alterations induced by DOCA-salt chronic administration in the antioxidant defences analysed."( Effects of chronic quercetin treatment on antioxidant defence system and oxidative status of deoxycorticosterone acetate-salt-hypertensive rats.
Duarte, J; Galisteo, M; García-Saura, MF; Jiménez, R; Vargas, F; Villar, IC; Zarzuelo, A, 2004
)
1.04
"Verapamil treatment did not reverse the intrinsic drug resistance of parental cells, but partially modulated the sensitivity of CABA-PTX cells to PTX and induced total sensitivity to vinblastine."( Induction of a multifactorial resistance phenotype by high paclitaxel selective pressure in a human ovarian carcinoma cell line.
Canevari, S; D'Ascenzo, S; Dolo, V; Millimaggi, D; Miotti, S; Pavan, A; Violini, S, 2004
)
1.04
"The verapamil-treated group showed lower values of MDA (P < 0.05) and higher values of GSH (P < 0.05) than group II."( Effects of carbon dioxide pneumoretroperitoneum on free radical formation in remote organs and use of verapamil as an antioxidant.
Aksoy, Y; Demirbas, M; Dincel, C; Ellidokuz, E; Guler, C; Kilinç, A; Samli, M, 2004
)
1.02
"The verapamil- pretreated group (group IV) showed statistical significantly lower values of MDA and protein carbonyl content when compared with group II and III (p < 0.05), whereas tissue GSH concentrations were unchanged in all groups."( The effect of verapamil on the prevention of ischemia/reperfusion injury in the experimental retroperitoneoscopic donor nephrectomy model.
Demirbas, M; Dincel, C; Guler, C; Köken, T; Polat, C; Samli, M, 2004
)
1.17
"Verapamil treatment significantly increased the peak plasma concentration by 2.9-fold (95% confidence interval [CI], 2.4- to 4.0-fold) and the area under the plasma concentration-time curve from time 0 to infinity [AUC(0-infinity)] of fexofenadine by 2.5-fold (95% CI, 2.0- to 3.3-fold). "( Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.
Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
2.02
"Verapamil pretreatment at a dose of 25 mg/kg significantly reduced stress-induced ulcers."( The effects of verapamil on stress- and histamine-induced gastric lesions in rats.
Batu, O; Erol, K; Kilic, FS; Sirmagul, B, 2004
)
1.4
"Verapamil treatments did not affect the biodisposition of DM in plasma."( Enhancing the uptake of dextromethorphan in the CNS of rats by concomitant administration of the P-gp inhibitor verapamil.
Beaudry, F; Deschênes, JL; Flarakos, T; Gritsas, A; Hage, A; Marier, JF; Seliniotakis, E; Vachon, P, 2005
)
1.26
"Verapamil treatment resulted in a significant decrease in the longest pacing CL at which DA was induced (207+/-19 vs 178+/-17 ms, p<0.0001)."( Discordant repolarization alternans-induced atrial fibrillation is suppressed by verapamil.
Furukawa, Y; Hiromoto, K; Kanemori, T; Masuyama, T; Mine, T; Ohyanagi, M; Shimizu, H, 2005
)
1.28
"In verapamil-pretreated group, insulin administration could only partially reverse the inhibition (65%)."( An inherent acceleratory effect of insulin on small intestinal transit and its pharmacological characterization in normal mice.
Dkhar, SA; Naveen, AT; Peddyreddy, MK; Ramaswamy, S; Shewade, DG, 2006
)
0.85
"Verapamil pretreatment prevented Iso-induced apoptosis in PLN(-/-) mice, indicating the involvement of a Ca(2+)-dependent pathway."( Calmodulin kinase II inhibition protects against myocardial cell apoptosis in vivo.
Anderson, ME; Eren, M; Gleaves, L; Hou, Y; Joiner, ML; Ni, G; Oddis, CV; Price, EE; Vaughan, DE; Xiao, RP; Yang, J; Yang, Y; Zhang, R; Zhu, WZ, 2006
)
1.06
"Verapamil treatment reversed this increased histamine sensitivity while propranolol aggravated it."( Comparative influence of propranolol and verapamil on glycemic control and histamine sensitivity associated with L-thyroxine-induced hyperthyroidism - an experimental study.
Bhatt, PA; Makwana, D, 2008
)
1.33
"Verapamil treatment did not influence this response, while metoprolol caused significant reductions."( Orthostatic response before and after nitroglycerin in metoprolol- and verapamil-treated angina pectoris.
Hyldstrup, L; Mogensen, NB; Nielsen, PE, 1983
)
1.22
"In verapamil-treated dogs inosine and hypoxanthine levels increased to only 1.2 +/- 0.3 (epicardium) and 1.9 +/- 0.6 nmol X mg protein-1 (endocardium) (both NS compared with preocclusion values)."( Preservation of high-energy phosphates by verapamil in reperfused myocardium.
Alker, KJ; Braunwald, E; Hale, SL; Ingwall, J; Kloner, RA; Lange, R, 1984
)
1.05
"The verapamil treatment could be withdrawn after ten days, while the digoxin treatment was continued."( Treatment of intrauterine supraventricular tachycardia with digoxin and verapamil.
Karlsson, K; Lilja, H; Lindecrantz, K; Sabel, KG, 1984
)
0.98
"Verapamil pretreatment significantly counteracted the intrarenal vasoconstriction produced by norepinephrine, sustaining renal blood flow during the norepinephrine infusion."( Effects of verapamil in models of ischemic acute renal failure in the rat.
Bonventre, JV; Cheung, JY; Leaf, A; Malis, CD, 1983
)
1.38
"Verapamil pretreatment completely blocked the decrease of mitochondrial Ca2+ uptake rate induced by 30 or 60 min of ischemia."( Verapamil pretreatment preserves mitochondrial function and tissue magnesium in the ischemic kidney.
Mela-Riker, LM; Widener, LL, 1984
)
2.43
"3. Verapamil pretreatment decreased the ultrastructural damage caused by ischaemia and reperfusion."( The cardioprotective effect of verapamil.
Nayler, WG; Slade, AM, 1982
)
1.06
"Oral verapamil is effective treatment for effort angina and may prevent the decrease in left ventricular ejection fraction due to exercise-induced ischemia."( Verapamil in stable effort angina: effects on left ventricular function evaluated with exercise radionuclide ventriculography.
Bautovich, G; Freedman, SB; Harris, PJ; Kelly, DT; Sadick, N; Tan, AT, 1982
)
2.16
"No verapamil treatment period was shortened due to unacceptable paroxysmal supraventricular tachycardia, but five of 22 placebo treatment periods were shortened (p equal to 0.02)."( Oral verapamil for paroxysmal supraventricular tachycardia: a long-term, double-blind randomized trial.
Cary, JR; Hillis, LD; Mauritson, DR; Rude, RE; Walker, WS; Winniford, MD, 1982
)
1.29
"Verapamil pretreatment resulted in values of the ATP/ADP ratio which were lower than, but not significantly different from, those observed in the control group."( Protective effect of verapamil on regional myocardial ischaemic injury in dog.
Kobusiewicz, W; Ledwozyw, A; Michalak, J; Ogonowska-Kobusiewicz, M; Zywicki, W, 1995
)
1.33
"Verapamil treatment was less effective, but still exhibited positive effects on TA levels at several time points (20 min, 10 h, and 24 h) throughout the entire 24-h period."( The importance of calcium-related effects on energetics at hypothermia: effects of membrane-channel antagonists on energy metabolism of rat liver.
Churchill, TA; Fuller, BJ; Green, CJ, 1995
)
1.01
"Dexverapamil treatment was begun 18 hours before day 1 of vinblastine administration and was given orally every 6 hours for 12 doses."( Phase I/II trial of dexverapamil plus vinblastine for patients with advanced renal cell carcinoma.
Cordon-Cardo, C; Fischer, P; Lianes, P; Lyn, P; Motzer, RJ; Ngo, RL; O'Brien, JP, 1995
)
1.12
"Verapamil pretreatment (as continuous intrarenal infusion at the rate of 1.25 micrograms/kg/min) attenuated the fall in GFR (from 0.16 +/- 0.01 and 0.19 +/- 0.03 ml/min/100 g before CsA to 0.20 +/- 0.05 ml/min/100 g BW, 60 min after CsA administration) (NS) and in RBF (from 2.42 +/- 0.2 and 2.6 +/- 0.22 ml/min/100 g before CsA to 1.79 +/- 0.17 ml/min/100 g BW, 60 min after CsA administration (P < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)"( Prevention of acute cyclosporin nephrotoxicity by verapamil and atrial natriuretic factor in the rat.
Bagnis, C; Bitker, MO; Deray, G; Dubois, M; Jacobs, C; Jacquiaud, C, 1994
)
1.26
"Verapamil failures were treated with ATP and vice versa."( [Adenosine triphosphate in the treatment of supraventricular paroxysmal tachycardia: a comparison with verapamil].
Alises Moraleda, JM; Cortés Bermejo, S; García de Pedro, J; Gil Madre, J; Laín Teres, N; Lázaro Rodríguez, S; Sentenac Merchán, G; Sepúlveda Berrocal, MA, 1995
)
1.23
"verapamil treatment, HR decreased (-16%, p < 0.0005) and the atrial contribution to LV filling decreased (-27%, p < 0.05); other parameters differed significantly from baseline values."( Acute intravenous versus chronic oral drug effects of verapamil on left ventricular diastolic function in patients with hypertrophic cardiomyopathy.
Blanksma, PK; Lie, KI; Posma, JL; Van der Wall, E, 1994
)
1.26
"With verapamil pretreatment, CsA-induced reduction in glomerular size was reduced (-0.6% and -3.6%, respectively, for 10(-6) M and 10(-7) M verapamil)."( Protective effect of verapamil in cyclosporin-incubated human and murine isolated glomeruli.
Cambar, J; L'Azou, B; Lakhdar, B; Potaux, L, 1994
)
1.06
"Verapamil treatment was associated with increased intracellular accumulation of drug, as shown by fluorescence of cells exposed to ethidium or DAPI, a fluorescent surrogate for berenil."( Effect of verapamil on antitrypanosomal activity of drugs in mice.
Agbe, SA; Yielding, KL, 1993
)
1.41
"In verapamil-treated cells without verapamil pretreatment, increased internalization and degradation were not significant, and binding was not increased."( [Enhancement on expression of LDL receptors in cultured rhesus renal epithelial cells by verapamil].
Liu, NF, 1994
)
1.02
"Verapamil treatment (1 mg/kg) did not alter the SAR response to histamine, whereas the responses of SARs to histamine at different dosages were significantly diminished by treatment with nifedipine (1 mg/kg)."( Effects of calcium channel and H1-receptor blockers on the responses of slowly adapting pulmonary stretch receptors to histamine in vagotomized rabbits.
Kanno, T; Matsumoto, S; Nagayama, T; Shimizu, T; Yamasaki, M, 1993
)
1.01
"Verapamil pretreatment attenuated these lesions and further intensified the ATP increase in a dose-related manner."( Role of gastric glandular mucosal energy metabolism in cold-restraint gastric lesion formation.
Cho, CH; Koo, MW; Ogle, CW,
)
0.85
"Verapamil treatment enhanced (p < 0.02) the platelet-mediated relaxation in rings with intact endothelium and abolished platelet-mediated constriction (p < 0.01) in the de-endothelialized rings."( Verapamil and aspirin modulate platelet-mediated vasomotion in arterial segments with intact or disrupted endothelium.
Behrens, P; Lawson, D; Mehta, JL; Nicolini, F; Raymenants, E; Yang, B, 1993
)
2.45
"Verapamil pretreatment also decreased Ca2+ accumulation and DNA damage while attenuating liver injury."( Ca2+ antagonists inhibit DNA fragmentation and toxic cell death induced by acetaminophen.
Corcoran, GB; Gurule, MW; Kamendulis, LM; Ray, SD; Yorkin, RD, 1993
)
1.01
"Thus verapamil post-treatment can prevent reperfusion-induced myocardial injury but functional recovery may be delayed due to the drug's inherent direct myocardial depressant effect."( Effect of verapamil post-treatment in myocardial reperfusion injury.
Gupta, YK; Manchanda, SC; Maulik, MG; Maulik, SK; Reddy, KS; Seth, SD, 1993
)
1.14
"Verapamil treatment alone did not alter insulin-stimulated 2-DG uptake in muscle, but simultaneous administration of verapamil and trandolapril resulted in the most pronounced effect on insulin-stimulated 2-DG uptake (+106%)."( Effects of trandolapril and verapamil on glucose transport in insulin-resistant rat skeletal muscle.
Dietze, GJ; Fogt, DL; Henriksen, EJ; Jacob, S, 1996
)
1.31
"Verapamil pretreatment unmasked the intracellular action of the anesthetics. "( Effect of volatile anesthetics with and without verapamil on intracellular activity in vascular smooth muscle.
Namba, H; Tsuchida, H, 1996
)
1.99
"Verapamil treatment attenuated the OP response by approximately 50% for both compounds."( Catecholamine concentrations and contractile responses of isolated vessels from hens treated with cyclic phenyl saligenin phosphate or paraoxon in the presence or absence of verapamil.
Correll, L; Ehrich, M; Flaherty, DM; Jortner, B; McCain, WC, 1996
)
1.21
"Verapamil treatment statistically significantly reduced (p < 0.05) mean 24 hour systolic blood pressure from 148.88 +/- 7.56 mmHg to 132.24 +/- 6.13 mmHg and diastolic respectively from 96.68 +/- 6.05 to 83.04 +/- 5.40 mmHg. "( [Evaluation of the antihypertensive efficacy and safety of using sustained release verapamil in elderly subjects using ambulatory blood pressure monitoring].
Bednarz, S; Janicki, K; Jasiński, T; Klima, M; Pieniazek, W, 1996
)
1.96
"Verapamil treatment of infected animals restored RV beta AR receptor density, alpha s and alpha i1-3 to control levels but had no influence on any aspect of pertussis-toxin-dependent [32P]ADP-ribosylation."( Cardioprotective actions of verapamil on the beta-adrenergic receptor complex in acute canine Chagas' disease.
Barr, S; Bilezikian, JP; Brewer, A; Chen, G; Morris, SA; Rohde, S; Tanowitz, HB; Walsh, D; Wittner, M, 1996
)
1.31
"Verapamil treatment also prevented the loss of the asymmetrical distribution of phosphatidylethanolamine and sarcolemmal disruption, the latter occurring during 120 min of ischaemia in untreated cells."( Sarcolemmal phosphatidylethanolamine reorganization during simulated ischaemia and reperfusion: reversibility and ATP dependency.
Hoebe, KH; Musters, RJ; Op den Kamp, JA; Post, JA; Pröbstl-Biegelmann, E; van Veen, TA; Verkleij, AJ,
)
0.85
"Verapamil treatment was associated with a 10% decrease of TPA-ag levels and metoprolol treatment with a 2% increase (P < .001 for treatment difference)."( Fibrinolytic variables and cardiovascular prognosis in patients with stable angina pectoris treated with verapamil or metoprolol. Results from the Angina Prognosis study in Stockholm.
Björkander, I; Eriksson, SV; Forslund, L; Held, C; Hjemdahl, P; Rehnqvist, N; Wallén, NH; Wiman, B, 1997
)
1.23
"Verapamil treatment was also associated with a decrease in CsA dose requirement (7.6+/-0.58 mg/kg/day at baseline vs."( A randomized controlled trial of verapamil on cyclosporine nephrotoxicity in heart and lung transplant recipients.
Cardella, C; Cattran, D; Chan, C; Maurer, J; Pei, Y, 1997
)
1.3
"Verapamil pretreatment levelled the calcium gradient in normoxic liver by reducing the periportal calcium content."( The effect of verapamil on mitochondrial calcium content in normoxic, hypoxic and reoxygenated rat liver.
Angermüller, S; Beier, K; Juchem, R; Konrad, T; Kusterer, K; Usadel, KH, 1997
)
1.38
"Verapamil-treated segments distal to the matrices also showed significantly lower neointimal smooth muscle cell density and increased lumen size."( Controlled periadventitial administration of verapamil inhibits neointimal smooth muscle cell proliferation and ameliorates vasomotor abnormalities in experimental vein bypass grafts.
Bhuta, S; Brauner, R; Chaudhuri, G; Drake, T; Drinkwater, DC; Fishbein, I; Golomb, G; Laks, H; Mishaly, D; Shvarts, O, 1997
)
1.28
"Verapamil pretreatment attenuated the BP and HR responses in rats."( Effect of verapamil on cadmium induced hypertension in rats.
Puri, VN, 1996
)
1.42
"Verapamil treatment caused an increase in intracellular contents of putrescine, cadaverine, and N8-acetylspermidine, in unstressed proliferating cells, or of N1-acetylspermidine, in cells subjected to heat shock to induce acetylation of spermidine at N1."( Characterization of a diamine exporter in Chinese hamster ovary cells and identification of specific polyamine substrates.
Gerner, EW; Gillies, RJ; Xie, X, 1997
)
1.02
"Verapamil pretreatment before cardiac arrest may contribute to preserve cadaver hearts with dilating the coronary vessels and probably preventing the calcium influx into cardiomyocytes during ischemia and reperfusion."( [Verapamil pretreatment extended the viability of non-beating donor hearts in situ].
Iijima, K, 1997
)
1.93
"Verapamil treatment did not modulate either colchicine or vinblastine efflux kinetics, suggesting that the intracellular drugs are not available to the transmembrane P-gp binding sites."( P-glycoprotein is more efficient at limiting uptake than inducing efflux of colchicine and vinblastine in HL-60 cells.
Boval, B; Chappey, O; Declèves, X; Niel, E; Scherrmann, JM, 1998
)
1.02
"In verapamil-treated embryos, the hearts were smaller and showed delayed development."( A quantitative study of the ventricular myoarchitecture in the stage 21-29 chick embryo following decreased loading.
Clark, EB; Hu, N; Pexieder, T; Sedmera, D, 1998
)
0.81
"Verapamil pretreatment prevented glomerular cross-sectional area (GCSA) diminution and glomerular calcium content rise (GCSA [micron2] Vp + Hg, 28,281 +/- 4654, Ca2+ [nmol/mg protein] Vp + Hg, 18 +/- 5)."( Verapamil protection against mercuric chloride-induced renal glomerular injury in rats.
Elías, MM; Girardi, G, 1998
)
2.46
"Verapamil treatment reduced the expression of cardiac NOS2 protein and the mRNAs for NOS2, TNF-alpha, and IL-1beta."( Expression of cardiac cytokines and inducible form of nitric oxide synthase (NOS2) in Trypanosoma cruzi-infected mice.
Bacchi, CJ; Braunstein, VL; Chan, J; Chandra, M; Factor, SM; Huang, H; Jelicks, LA; Morris, SA; Shirani, J; Tanowitz, HB; Weiss, LM; Wittner, M; Yarlett, N, 1999
)
1.02
"Verapamil treatment did not restore the forward pattern of systolic blood flow but decreased diastolic blood flow velocity to a level comparable with that in healthy subjects."( Effect of verapamil on systolic and diastolic coronary blood flow velocity in asymptomatic and mildly symptomatic patients with hypertrophic cardiomyopathy.
Dubiel, JS; Krzanowski, M; Nizankowski, R; Petkow Dimitrow, P; Szczeklik, A, 2000
)
1.43
"Verapamil treatment significantly reduced the increase in the lenticular content of calcium, magnesium and iron, indicating a probable protective effect of verapamil in radiation-induced cataract formation."( Effect of verapamil on lenticular calcium, magnesium and iron in radiation exposed rats.
Bardak, Y; Cekiç, O; Cengiz, M; Totan, Y, 1998
)
1.42
"Verapamil pretreatment increased the protein synthesis activity at both levels of granular endoplasmic reticulum and free polysomes in cytoplasm and decreased ATPase activity."( Evaluation of calcium channel blockers as potential hepatoprotective agents in oxidative stress injury of perfused hepatocytes.
Farghali, H; Kmonícková, E; Lotková, H; Martínek, J, 2000
)
1.03
"The verapamil-treated PRP or control PRP were sheared at 37 degrees C for 120 sec."( In vitro-inhibition of shear-induced platelet aggregation by verapamil.
Liao, F; You, Y, 2001
)
1.03
"Verapamil treatment significantly improved CHF score at 3 months (3.5 +/- 0.5, p<0.05) compared with baseline (5.6 +/- 0.5) or placebo (5.5 +/- 0.5)."( Effect of verapamil in elderly patients with left ventricular diastolic dysfunction as a cause of congestive heart failure.
Cherng, WJ; Hung, MJ; Kuo, LT; Wang, CH,
)
1.26
"Verapamil treatment was able to restore adequate vasodilator response to pacing stress."( Verapamil improves the pacing-induced vasodilatation in symptomatic patients with hypertrophic cardiomyopathy.
Dimitrow, PP; Dubiel, JS; Grodecki, J; Kawecka-Jaszcz, K; Krzanowski, M; Lelakowski, J; Małecka, B; Szczeklik, A, 2002
)
2.48
"In verapamil-pretreated CsA-intoxicated glomeruli, size decrease was reduced (-1.5 percent at T10, -3.1 percent at T20 and -4.8 percent at T30), when compared with CsA alone (-4.7 percent at T10, -10.1 percent at T20 and -12 percent at T30)."( [Protective effect of verapamil and dopamine against cyclosporine-induced vasoconstriction in isolated glomeruli in rats].
Cambar, J; L'Azou, B; Lagroye, I; Lakhdar, B; Plande, J, 1992
)
1.11
"Verapamil treatment increased sodium channel mRNA level up to 3-fold, whereas in vitro A23187 treatment decreased the mRNA level 5-fold."( Class I and IV antiarrhythmic drugs and cytosolic calcium regulate mRNA encoding the sodium channel alpha subunit in rat cardiac muscle.
Catterall, WA; Duff, HJ; Offord, J; West, J, 1992
)
1
"Verapamil pretreatment of cytoplasts from resistant cells revealed the subcellular DNP-sensitive uptake present in parental cytoplasts."( Energy-dependent accumulation of daunorubicin into subcellular compartments of human leukemia cells and cytoplasts.
Daniel, JC; Lecerf, JM; Levy, SB; Slapak, CA, 1992
)
1
"Verapamil cotreatment resulted in increased muscle loss over that caused by doxorubicin alone in both rabbits and the monkey."( Verapamil substantially increases the chemomyectomy effect of doxorubicin injected into rabbit or monkey eyelid.
Ekern, M; McLoon, LK; Wirtschafter, J, 1992
)
2.45
"In verapamil-treated rats (5 mg/kg/day), no histological or biochemical evidence of renal injury was detected."( Verapamil increases the nephrotoxic potential of gentamicin in rats.
Fadali, GA; Farag, MM; Kandil, M, 1992
)
2.24
"Verapamil untreated rats showed hyperalgesia, autotomies and hypersynchronic discharges in contralateral hemisphere, increased range of evoked potentials and disorders in microcirculatory system which evidence developing pain syndrome."( [Effects of verapamil on the development of pain syndrome in rats after section of the sciatic nerve].
Gorizontova, MP; Kryzhanovskiĭ, GN; Kukushkin, ML; Reshetniak, VK; Smirnova, VS, 1992
)
1.38
"In verapamil-treated subjects, volume expansion produced an additional increase in ANF and inhibited the PRA-AII-ALD axis, suggesting that in young healthy individuals, verapamil does not interfere with the reflex compensatory hormonal mechanisms activated under circumstances of acute volume-salt overload, with rapid expansion of the central vascular compartment."( Comparative effects of verapamil and volume overload on atrial natriuretic factors and the renin-angiotensin aldosterone-vasopressin system.
Buckley, JW; Cubeddu, LX; Hedner, T; Masotto, C; Negro-Villar, A; Posvar, E, 1992
)
1.11
"Verapamil treatment decreased significantly tissue activity of trypsin (p less than 0.001) and chemotrypsin (p less than 0.0001) and increased serum lipase (p less than 0.05), and calcium."( [The effects of verapamil in experimental acute pancreatitis in the rat].
Díez Miralles, M; González Santos, J; Graells Ferrer, ML; Medrano Heredia, J; Pardo Correcher, JM; Regalado Pareja, RI; Ruiz Macía, JA, 1992
)
1.35
"Verapamil treatment, which increased survival time and survival rate, significantly attenuated the changes in serum Mg2+ which normally followed hemorrhage."( Serum magnesium increases following severe hemorrhage in dogs blocked by verapamil treatment.
Allison, EJ; Carroll, RG; Iams, SG; Pryor, WH, 1990
)
1.23
"In verapamil-treated kidneys, PTH failed to stimulate renin release."( Parathyroid hormone and calcium: interactions in the control of renin secretion in the isolated, nonfiltering rat kidney.
Helwig, JJ; Judes, C; Musso, MJ; Nickols, GA, 1991
)
0.8
"Verapamil pretreatment produced a similarly selective dilatation of larger coronary arterioles and protected against the ischaemia-induced fall in capillary red cell content."( Calcium antagonists and myocardial microperfusion.
Köbler, W; Möller, P; Neumann, FJ; Parekh, N; Steinhausen, M; Tillmanns, H; Waas, W; Zimmermann, R, 1991
)
1
"In verapamil-treated rats, there was an apparent reduction in infarct size as compared with untreated rats; 20% reduction in infarct size 5 h after coronary occlusion and 12% reduction after 24 h."( Problems related to infarct size measurements in the rat heart.
Greve, G; Saetersdal, T, 1991
)
0.8
"Verapamil pretreatment resulted in a positive inotropic state."( The effect of verapamil on cardiac sympathetic function.
Avenant, JC; Meyer, EC; Sommers, DK, 1991
)
1.36
"Verapamil treatment of PD rats (PD-V) normalized [Ca2+]i in their synaptosomes (361 +/- 8.5 nM)."( Phosphate depletion increases cytosolic calcium of brain synaptosomes.
Fadda, GZ; Hajjar, SM; Koureta, P; Massry, SG; Smogorzewski, M, 1991
)
1
"Verapamil treatment decreased ventricular pressure in experimental (P less than 0.05) compared with saline control and normal embryos; at stage 27, 1.59 +/- 0.21 vs."( Effect of chronic verapamil treatment on ventricular function and growth in chick embryos.
Clark, EB; Hansen, J; Hu, N; Litter, JE; Turner, DR, 1991
)
1.34
"Verapamil treatment could not completely reverse ADR resistance."( Mechanisms involved in the development of adriamycin resistance in human leukemic cells.
Ideguchi, H; Kato, S; Muta, K; Nawata, H; Nishimura, J, 1990
)
1
"Verapamil treatment of these cells also resulted in significant depletion of cellular GSH."( Glutathione depletion in human and in rat multi-drug resistant breast cancer cell lines.
Batist, G; Greene, D; Lehnert, S; Schecter, R; Woo, A, 1991
)
1
"Verapamil pretreatment followed by atropine administration resulted in a significantly greater tachycardia."( Atropine and verapamil interactions in healthy volunteers.
Avenant, JC; Meyer, EC; Sommers, DK, 1991
)
1.37
"Verapamil treatment of the aortic constricted hearts prevented the rise in intracellular calcium, and attenuated phosphomonoester sugar accumulation."( Calcium inhibition of glycolysis contributes to ischaemic injury.
Auffermann, W; Buser, P; Parmley, WW; Wagner, S; Wikman-Coffelt, J; Wu, S, 1990
)
1
"Verapamil treatment of normal rats for 21 days did not affect synaptosomal content of calcium or phospholipids."( Effect of verapamil on CRF-induced abnormalities in phospholipid contents of brain synaptosomes.
Islam, A; Massry, SG; Smogorzewski, M, 1990
)
1.4
"Verapamil treatment of normal rats for 21 days did not affect synaptosomal NE content, release, or uptake, Na(+)-K(+)-ATPase activity, or calcium content."( Verapamil corrects abnormalities in norepinephrine metabolism of brain synaptosomes in CRF.
Islam, A; Massry, SG; Minasian, R; Smogorzewski, M; Soliman, AR, 1990
)
2.44
"Verapamil pretreatment increased the concentration of cephaloridine in the renal cortex at 0.5 hr, but did not alter the peak concentration (2 hr after the dose) or cortical concentrations at 1 or 3 hr."( Effect of verapamil on cephaloridine nephrotoxicity in the rabbit.
Browning, MC, 1990
)
1.4
"Verapamil treatment significantly reduces intimal hyperplasia in experimental vein grafts and inhibits smooth muscle cell proliferation in culture."( Reduction of intimal hyperplasia and enhanced reactivity of experimental vein bypass grafts with verapamil treatment.
Cross, KS; el-Sanadiki, MN; Hagen, PO; McCann, RL; Mikat, E; Murray, JJ; Schuman, RW, 1990
)
1.22
"Verapamil treatment has no significant effect, neither on the enzyme activation nor on the glycogen utilization."( [Enzyme activity of cardiac glycogen metabolism: study of an in situ hypoxia protocol in the rat].
Grably, S; Rossi, A; Verdys, M, 1989
)
1
"Verapamil treatment had no effect on the accumulation of vincristine in leukemic cells."( Effect of verapamil in vitro and in vivo on the accumulation of vincristine in leukemic cells from patients with low malignant lymphoma.
Gruber, A; Peterson, C; Reizenstein, P,
)
1.26
"Verapamil treatment immediately after the hemorrhage (group 3, N = 4) increased the survival rate to 75% (three of four animals)."( Verapamil treatment of canine hemorrhagic shock.
Allison, EJ; Carroll, RG; Farmer, PL; Iams, SG; Pryor, WH, 1989
)
2.44
"4. Verapamil pretreatment during the Langendorff perfusion significantly increased Ca2+-uptake in sarcolemma vesicles both before the onset of ischaemia and after 30 min of reperfusion, whereas no beneficial effect was found on the impaired uptake activity during the ischaemic period."( Effects of verapamil on ischaemia-induced impairment of ATP-dependent calcium extrusion in rat heart sarcolemma.
Goddijn, MM; Haas, M; Punt, NC; van Amsterdam, FT; Zaagsma, J, 1989
)
1.18
"Verapamil-treated animals formed considerably fewer adhesions than did controls after adhesiolysis (postscore 0.5 versus 3.5; P less than .001)."( Calcium channel blockade prevents postsurgical reformation of adnexal adhesions in rabbits.
Kazensky, C; Lambert, H; Steinleitner, A, 1989
)
1
"Verapamil-treated hamsters received intraperitoneal injections of verapamil at a dose of 5 mg/kg per day for 70 days from age 20 days."( Effects of verapamil on experimental cardiomyopathy in the Bio 14.6 Syrian hamster.
Hayashi, H; Kaneko, M; Kobayashi, A; Nishiyama, T; Yamashita, T; Yamazaki, N, 1987
)
1.38
"Verapamil-treated dogs showed higher pH of ischemic subendocardium after 15 min ischemia (6.75 +/- 0.07) than did the nifedipine (6.48 +/- 0.04) or placebo (6.43 +/- 0.05) groups, even if the animals were paced (6.71 +/- 0.11) to prevent the negative chronotropic effect of verapamil (P less than 0.01)."( Contrasting effects of verapamil and nifedipine on pH of ischemic myocardium in the dog.
Aamodt, R; Epstein, SE; Goldstein, SR; Greene, R; Markle, DR; Patterson, RE; Ro, YM; Speir, E; Steadman, K, 1989
)
1.31
"Verapamil treatment increased the E/A-ratio to 1.3 +/- 0.4 (p less than 0.001) and filling fraction to 45% +/- 4% (p = 0.055) because of increased early filling."( Effects of verapamil on left ventricular relaxation and filling dynamics in coronary artery disease: a study by pulsed Doppler echocardiography.
Myhre, E; Myreng, Y, 1989
)
1.39
"Verapamil pretreatment markedly improved GFR and urine and renal perfusate flow but not tubular function."( Treatment with verapamil and adenosine triphosphate-MgCl2 reduces cyclosporine nephrotoxicity.
Baue, AE; Chaudry, IH; Sumpio, B, 1987
)
1.35
"Verapamil treatment significantly decreased blood pressure, heart rate and the ratio of ventricular weight to body weight in treated SHR."( Effects of long-term verapamil treatment on blood pressure, cardiac hypertrophy and collagen metabolism in spontaneously hypertensive rats.
Ruskoaho, HJ; Savolainen, ER, 1985
)
1.31
"Verapamil treatment reduced Ca++ concentrations by 40% to 314 +/- 23 mM/g tissue."( Carbon monoxide effects on calcium levels in vascular smooth muscle.
Lin, H; McGrath, JJ, 1988
)
1
"Both verapamil and diltiazem treatment decreased antipyrine clearance (verapamil, 42.5 to 30.1 ml/min, P less than .01; diltiazem, 41.7 to 29.9 ml/min, P less than .01), resulting in prolonged antipyrine half-life with no change in distribution volume."( Substrate-selective inhibition by verapamil and diltiazem: differential disposition of antipyrine and theophylline in humans.
Abernethy, DR; Carrum, G; Dickinson, TH; Egan, JM, 1988
)
1.01
"Verapamil treatment resulted in a significant decrease in systolic and diastolic blood pressure and a reduction in maximum left ventricular pressure."( Effect of calcium blocking agent verapamil on blood pressure, ventricular contractility, parathyroid hormone, calcium and phosphorus in plasma, catecholamines, corticosterone and plasma renin activity in spontaneously hypertensive rats.
Ancov, V; Grigorova, R; Ilieva, T; Lolov, R; Nicolov, N; Petkova, M; Sheitanova, S; Todorova, M; Tzoncheva, A; Velkov, Z, 1988
)
1.28
"Verapamil pretreatment partially prevented cardiac depression during alcohol perfusion."( Reversibility of acute alcohol cardiac depression: 31P NMR in hamsters.
Auffermann, W; Higgins, CB; Parmley, WW; Sievers, R; Wikman-Coffelt, J; Wu, S, 1988
)
1
"Verapamil treatment reduced mean total theophylline clearance by 14%, due to decreased clearances via 1- and 3-demethylation and 8-hydroxylation."( Selective inhibitory effects of nifedipine and verapamil on oxidative metabolism: effects on theophylline.
Birkett, DJ; Miners, JO; Robson, RA, 1988
)
1.25
"Verapamil treatment of animals subjected to ischemia was not associated with sustained elevations of left atrial pressure to values above those measured in animals receiving the vehicle."( Effects of intracoronary verapamil administration in a sheep model of acute myocardial ischemia and reperfusion.
Korn, RL; Pollock, JV; Spath, JA, 1988
)
1.3
"With verapamil treatment, CO modestly increased (7%), O2 extraction decreased and VO2 did not change."( Effect of propranolol and verapamil on oxygen utilization, acidosis and fatigue during exercise in stable angina pectoris.
Anderson, SD; Devenish-Meares, S; Harris, PJ; Kelly, DT; Roubin, GS; Sadick, NA, 1987
)
1.03
"In verapamil-treated dishes, there was flattening and a cobblestone appearance of the cells."( Long-term effects of verapamil on aortic smooth muscle cells cultured in the presence of hypercholesterolemic serum.
Halperin, G; Stein, O; Stein, Y,
)
0.96
"Verapamil pretreatment (2, 4, 8 or 16 mg/kg), injected intraperitoneally 30 min before experimentation, significantly prevented stress-induced mucus depletion and gastric ulceration; however, it did not itself influence stomach wall mucus levels in nonstressed animals."( Effects of verapamil, carbenoxolone and N-acetylcysteine on gastric wall mucus and ulceration in stressed rats.
Cho, CH; Koo, MW; Ogle, CW, 1986
)
1.38
"Verapamil pretreatment restored KCl contractile responses to normal in reperfused coronary rings and partially restored endothelium-dependent relaxation."( Reperfusion after acute coronary occlusion in dogs impairs endothelium-dependent relaxation to acetylcholine and augments contractile reactivity in vitro.
Horwitz, LD; McMurtry, IF; VanBenthuysen, KM, 1987
)
0.99
"Verapamil-treated myopathic hamsters had evidence of markedly improved mitochondrial function when compared with untreated animals."( Evaluation of the hereditary Syrian hamster cardiomyopathy by 31P nuclear magnetic resonance spectroscopy: improvement after acute verapamil therapy.
Higgins, CB; James, TL; Jasmin, G; Markiewicz, W; Parmley, WW; Sievers, R; Wikman-Coffelt, J; Wu, SS, 1986
)
1.2
"Verapamil treatment in hypertrophic cardiomyopathy is a valuable approach by which symptomatic improvement and a favourable effect on some left ventricular functions can be achieved."( Use of verapamil in the treatment of hypertrophic cardiomyopathy.
Cervenka, V; Dvorák, J; Gregor, P; Sládková, T; Vísek, V; Widimský, P, 1986
)
1.45
"Verapamil treatment was associated with a significant reduction in diastolic blood pressure (P = 0.02 vs."( Influence of oral verapamil on glucoregulatory hormones in man.
Baylor, P; Charlap, S; Frishman, WH; Kambosos, D; Plawes, S; Shamoon, H, 1985
)
1.32
"Verapamil treatment, however, significantly reduced the percentage of ovulated ova that were mature (68.8%) in comparison to ovulated ova from human chorionic gonadotropin-treated control ovaries (95.0%)."( Examination of the role of calcium in ovulation in the in vitro perfused rabbit ovary with use of ethyleneglycol-bis(beta-aminoethyl ether)-n,n'-tetraacetic acid and verapamil.
Kitai, H; Santulli, R; Wallach, EE; Wright, KH, 1985
)
1.19
"Verapamil treatment resulted in a maximum 80% inhibition of metastases, the degree of inhibition varying among the different metastatic systems."( Inhibition of spontaneous and experimental tumor metastasis by the calcium antagonist verapamil.
Iida, H; Kawabata, H; Makishima, F; Sakurai, Y; Tsukagoshi, S; Tsuruo, T; Yamori, T, 1985
)
1.21
"Verapamil-treated animals had decreased frequency and severity of gastric stress ulceration as assessed by ulcer index, ulcer grade, and number of ulcers/animal."( Verapamil attenuates stress-induced gastric ulceration.
Leahy, AL; Nee, JM; Pollock, TW; Wait, RB, 1985
)
2.43
"Verapamil pretreatment significantly increased oxidation of all substrates by the subsequently isolated Polytron mitochondria, but only succinate-supported respiration returned to control levels."( Protection of canine cardiac mitochondrial function by verapamil-cardioplegia during ischemic arrest.
Entman, ML; Lewis, RM; McMillin-Wood, JB; Michael, LH; Yoon, SB, 1985
)
1.24
"Verapamil pretreatment does not alter the increase in serum potassium induced by succinylcholine in normal dogs."( Verapamil does not alter succinylcholine-induced increases in serum potassium during halothane anesthesia in normal dogs.
Gronert, GA; Nugent, M; Roth, JL, 1985
)
2.43
"Oral treatment with verapamil or vehicle was started, 24 h post-intracerebroventricular (ICV) streptozotocin/(STZ), in 12-month-old animals and continued for 3 months."( Verapamil Prevents Development of Cognitive Impairment in an Aged Mouse Model of Sporadic Alzheimer's Disease.
Ahmed, HA; Ishrat, T; Ismael, S; Mirzahosseini, G, 2021
)
2.38
"The treatment with verapamil enhanced Trx-R activity, significantly inhibited TLR4 mediated NLRP3-inflammasome assembly with subsequent diminishing of inflammatory markers (TNF-α and IL-1β) release into the vitreous, suppression of pathological angiogenesis, and preservation of RGC count and pancreatic islets diameter."( Inhibition of thioredoxin-interacting protein and inflammasome assembly using verapamil mitigates diabetic retinopathy and pancreatic injury.
Eissa, LD; El-Azab, MF; Ghobashy, WA, 2021
)
1.17
"Treatment of verapamil inhibits TGF-β1 induced collagen production via inhibiting CaMK II."( Verapamil inhibits ureteral scar formation by regulating CaMK II-mediated Smad pathway.
Gao, ZY; Guo, X; Li, YW; Lu, Q; Wang, JS; Xiao, W; Yang, K; Yuan, WX; Zeng, MQ, 2021
)
2.42
"Treatment with verapamil, an inhibitor of P-gp, significantly improved the absorption of enrofloxacin in both healthy and infected broilers."( E. coli infection modulates the pharmacokinetics of oral enrofloxacin by targeting P-glycoprotein in small intestine and CYP450 3A in liver and kidney of broilers.
Bughio, S; Dai, X; Guo, M; Ren, W; Sun, Y; Wang, L; Zhang, Y, 2014
)
0.74
"Treatment with verapamil reduced the OXC mean residence time (4.91 vs 4.20 h) and apparent volume of distribution (4.72 vs 3.15 L/kg)."( Influence of verapamil on the pharmacokinetics of oxcarbazepine and of the enantiomers of its 10-hydroxy metabolite in healthy volunteers.
Alexandre Junior, V; Antunes, Nde J; Coelho, EB; Della Pasqua, O; Lanchote, VL; Marques, MP; Takayanagui, OM; Tozatto, E; Wichert-Ana, L, 2016
)
1.14
"Treatment of verapamil attenuated inflammation as well as joint destruction in arthritis models."( Chronic Calcium Channel Inhibitor Verapamil Antagonizes TNF-α-Mediated Inflammatory Reaction and Protects Against Inflammatory Arthritis in Mice.
Li, W; Li, Z; Liu, Y; Meng, Q; Pan, J; Wang, W; Wang, X; Yan, P; Zhai, Y; Zhang, H; Zhang, P; Zhang, Z; Zhao, Y, 2016
)
1.07
"Pretreatment with verapamil completely abolished both calcium channel agonist-induced influx of calcium and apoptosis in these cells."( Verapamil inhibits L-type calcium channel mediated apoptosis in human colon cancer cells.
Jeppsson, B; Liu, Q; Melander, A; Thorlacius, H; Wang, Y; Zawadzki, A, 2008
)
2.11
"Treatment with verapamil, which presumably leads to a conformational change in the channel, completely abolished K+-induced contraction, while residual contraction still occurred when Ca2+ entry was blocked with Cd2+. "( High K+-induced contraction requires depolarization-induced Ca2+ release from internal stores in rat gut smooth muscle.
Bajorat, R; Kirschstein, T; Köhling, R; Porath, K; Rehberg, M; Tokay, T, 2009
)
0.71
"Treatment with verapamil and siRNA against MDR1 significantly increased the sensitivity to amrubicinol in PC-6/AMR-OH cells with increased cellular accumulation of amrubicinol."( Over-expression of MDR1 in amrubicinol-resistant lung cancer cells.
Kasai, D; Maeno, K; Miyazaki, M; Oguri, T; Ozasa, H; Sato, S; Takakuwa, O; Uemura, T, 2011
)
0.71
"Treatment with verapamil blocked these effects."( Thioredoxin interacting protein is a novel mediator of retinal inflammation and neurotoxicity.
Abdelsaid, MA; Al-Gayyar, MM; El-Remessy, AB; Matragoon, S; Pillai, BA, 2011
)
0.71
"Treatment with verapamil (30 microM) markedly inhibited endotoxin (1 microg/ml)-induced TNFalpha production in these cells."( Preventive effects of a verapamil against tumor necrosis factor-alpha-induced shock symptoms: approached from lipoprotein metabolic disorders.
Furusawa, S; Iizuka, Y; Sakaguchi, S; Satoh, S; Takayanagi, M, 2002
)
0.96
"Treatment with verapamil induced a dose-dependent potentiation in the biochemical parameters of nephrotoxicity that was significant only at the highest dose used (7 mg/kg)."( The effect of calcium load and the calcium channel blocker verapamil on gentamicin nephrotoxicity in rats.
Al-Qarawi, AA; Ali, BH; Mousa, HM, 2002
)
0.9
"Pretreatment with verapamil (10(-6) mol/L) or nickel (Ni(2+)) (2 mmol/L) inhibited the contractions to a magnitude of 63.81% +/- 7.69% and 88.36% +/- 12.17% (mean +/- standard error of the mean), respectively."( Application of electric field stimulation for investigations of human placental blood vessels.
Falkay, G; Gáspár, R; Resch, BE, 2003
)
0.64
"Treatment with verapamil suppressed load-induced bone formation rate by 77% and 59% (P < 0.01)."( Parathyroid hormone enhances mechanically induced bone formation, possibly involving L-type voltage-sensitive calcium channels.
Burr, DB; Duncan, RL; Gattone, VH; Li, J; Turner, CH, 2003
)
0.66
"Pretreatment with verapamil alone does not improve maintenance of sinus rhythm after DC cardioversion in patients with AF. "( Sinus rhythm maintenance following DC cardioversion of atrial fibrillation is not improved by temporary precardioversion treatment with oral verapamil.
Edvardsson, N; Firsovaite, V; Fredholm, O; Kronvall, T; Lindholm, CJ; Meurling, CJ; Möller, SJ; Olsson, SB; Pettersson, T; Platonov, PG; Roijer, A, 2004
)
0.86
"Treatment with verapamil potentiated morphine analgesia in a dose-dependent manner."( Involvement of peripheral mechanism in the verapamil-induced potentiation of morphine analgesia in mice.
Dake, Y; Fukazawa, Y; Kishioka, S; Maeda, T; Ozaki, M; Shimizu, N; Yamamoto, C; Yamamoto, H, 2004
)
0.93
"Treatment with verapamil as a PGP inhibitor did not affect the transport of ketobemidone in Caco-2 cells, indicating that PGP is not involved."( Ketobemidone is a substrate for cytochrome P4502C9 and 3A4, but not for P-glycoprotein.
Al-Shurbaji, A; Annas, A; Artursson, P; Lazorova, L; Svensson, JO; Yasar, U, 2005
)
0.67
"Treatment with verapamil (1.0, 2.5, 5.0 and 10.0 mg/kg/12 h i.p.) started 24 h after NBM lesions and lasted 8 days."( Verapamil prevents, in a dose-dependent way, the loss of ChAT-immunoreactive neurons in the cerebral cortex following lesions of the rat nucleus basalis magnocellularis.
Caballero-Bleda, M; Popović, M; Popović, N; Puelles, L; van Groen, T; Witter, MP, 2006
)
2.12
"Pretreatment with verapamil before LPS challenge reduced acute liver injury, down-regulated production of LPS-induced pro-inflammatory cytokines (TNF-alpha and IL-6), up-regulated production of anti-inflammatory cytokines (IL-10) and inhibited NF-kappa B activation in the liver in a dose-dependent manner."( Verapamil modulates LPS-induced cytokine production via inhibition of NF-kappa B activation in the liver.
Chen, C; Li, G; Li, JS; Liu, FK; Qi, XP; Sun, Z; Wu, XY; Xu, Z; Yang, XD, 2006
)
2.1
"Pretreatment with verapamil (an antagonist of the L-type calcium channel, 10 micromol/L) partially eliminated the above effects of UII (300 nmol/L) on the CSB."( Urotensin II inhibits carotid sinus baroreflex in anesthetized male rats.
He, RR; Wu, YM; Xiao, L; Xue, HM, 2007
)
0.66
"Treatment with verapamil (5 mg/kg, i.p.) significantly reduced fasting serum glucose and insulin levels, AUC glucose, and significantly increased K(ITT) values."( Comparative influence of propranolol and verapamil on glycemic control and histamine sensitivity associated with L-thyroxine-induced hyperthyroidism - an experimental study.
Bhatt, PA; Makwana, D, 2008
)
0.95
"Treatment with verapamil or CaCl2 following PEP treatment also effectively enhanced the cytotoxic effect of PEP, suggesting an interaction with PEP-induced damage."( Modulation of the cytotoxicity of the antitumor antibiotic peplomycin by membrane-interacting drugs and by increased levels of calcium ions.
Ishida, A; Mizuno, S; Nanjo, T; Uehara, Y, 1983
)
0.61
"In treated dogs, verapamil was given, 0.15 mg/kg intravenous bolus, immediately after first ligation and was followed by an infusion of 7.5 micrograms/kg/min."( Effect of verapamil on conduction delay produced by myocardial ischemia and reperfusion.
Fujimoto, T; Hamamoto, H; Mandel, WJ; Peter, T, 1981
)
0.99
"Treatment with verapamil had to be discontinued because of constipation in one patient; treatment with nifedipine was discontinued because of headache in 11 and ankle edema in one."( Factors influencing the hypotensive effects of calcium antagonists.
Bertel, O; Bolli, P; Buhler, F; Erne, P; Hulthen, UL; Kiowski, W; Muller, FB,
)
0.47
"Pretreatment with verapamil reduced the size of these subendocardial infarcts from 34 +/- 8 to 8 +/- 3% of the ischemic circumflex vascular bed at risk (identified by postmortem perfusion of the previously occluded and unoccluded arteries with different dyes)."( Verapamil in two reperfusion models of myocardial infarction. Temporary protection of severely ischemic myocardium without limitation of ultimate infarct size.
Jennings, RB; Reimer, KA, 1984
)
2.03
"Pretreatment with verapamil (0.1 mg/L) prior to ischemia offered moderate additional protection, but its use during reperfusion failed to enhance overall recovery."( Cardioplegia and slow calcium-channel blockers. Studies with verapamil.
Braimbridge, MV; Hearse, DJ; Manning, AS; Yamamoto, F, 1983
)
0.83
"Pretreatment with verapamil (25-35 microM), nifedipine (35-45 microM), diltiazem (25 microM), or EGTA (1.5-5 mM) markedly attenuated the BB-induced (1.6 mM) LDH leakage rate during 2 h of incubations."( Protective effects of calcium channel blockers on acute bromobenzene toxicity to isolated rat hepatocytes. Inhibition of phenylephrine-induced calcium oscillations.
Danielsson, A; Karlsson, K; Lindström, P; Sehlin, J; Wu, J, 1995
)
0.61
"Pretreatment with verapamil (10 mg i.v."( Interaction of propranolol, verapamil, and nifedipine on the myocardial depressant effect of cocaine.
Brewster, PS; Fraker, TD; Temesy-Armos, PN; Wilkerson, RD, 1995
)
0.91
"Pretreatment with verapamil (10 or 20 mg/kg i.p.) or nimodipine (5 mg/kg i.p.) antagonized the HPA activation induced by morphine, blocking both the decrease in hypothalamic NA levels and the elevation in plasma corticosterone induced by the opioid."( L-type Ca2+ channel ligands modulate morphine effects on the hypothalamus-pituitary-adrenocortical axis in rats.
Martinez-Piñero, MG; Milanés, MV; Vargas, ML, 1993
)
0.61
"Pretreatment with verapamil (0.32 mg/kg), was ineffective against aconitine-induced ventricular arrhythmias and mortality."( R 56 865, a Na+/Ca(2+)-overload inhibitor, protects against aconitine-induced cardiac arrhythmias in vivo.
De Clerck, F; Lu, HR, 1993
)
0.61
"Pretreatment with verapamil (1 or 10 microM), nifedipine (0.1 microM) or incubation with Ca(2+)-free, EGTA (0.1 mM)-containing physiological salt solution (PSS) suppressed the contraction produced by caffeine or theophylline in PDA (5 microM)-treated tissues."( The effects of phorbol 12,13-diacetate on responses of guinea-pig isolated trachea to methylxanthines, isoprenaline and ryanodine.
Cortijo, J; Morcillo, EJ; Sanz, CM; Small, RC; Villagrasa, V, 1994
)
0.61
"Treatment with verapamil or nifedipine was associated with electron microscopic changes consistent with increased differentiation and resulted in increased carcinoembryonic antigen expression, suggesting that the increase in mdr-1 expression was associated with the process of differentiation."( Increased mdr-1/P-glycoprotein expression after treatment of human colon carcinoma cells with P-glycoprotein antagonists.
Bates, SE; Fojo, AT; Herzog, CE; Tsokos, M, 1993
)
0.63
"Treatment with verapamil, tamoxifen, nicergoline or cyclosporin A only partially restores the activity of FCE 24517 against LoVo/24517 cells."( Characterisation of a LoVo subline resistant to a benzoyl mustard derivative of distamycin A (FCE 24517).
Broggini, M; Capolongo, L; Grandi, M; Melegaro, G; Mongelli, N, 1993
)
0.63
"Treatment with verapamil but not with ryanodine during ischemia attenuated the increase in m-calpain activity."( Calpain activity alters in rat myocardial subfractions after ischemia or reperfusion.
Kawashima, S; Yamasaki, Y; Yoshida, K, 1993
)
0.63
"Pretreatment with verapamil (2 mg/kg; n = 5) significantly reduced the increase in permeability caused by 10(-8) mol/L PAF (1909.1 +/- 620.2 nl/60 min/gm; p < 0.05)."( L-type calcium channel blockers modulate the microvascular hyperpermeability induced by platelet-activating factor in vivo.
Durán, WN; Hobson, RW; Kim, D; Kobayashi, I; Oshiro, H; Takenaka, H, 1995
)
0.61
"Pretreatment with verapamil reduced the increase of ALT in plasma and the morphological signs of necrosis induced by AA administration."( Effect of verapamil on allyl alcohol hepatotoxicity.
Atzori, L; Congiu, L, 1996
)
1.02
"Treatment with verapamil (VRP) reduced the resistance to tallimustine, but not to MEN 10710, in MCF7/DX cells."( Cytotoxic and antitumor activity of MEN 10710, a novel alkylating derivative of distamycin.
Animati, F; Bigioni, M; Lombardi, P; Manzini, S; Palma, C; Pratesi, G; Salvatore, C; Supino, R; Zunino, F, 1997
)
0.64
"Treatment with verapamil, an L-type Ca++ channel blocker, before 10 nM U46619 challenge, or during the plateau [Ca++]i elevation and contraction, decreased these parameters by approximately 50%."( Role of extracellular Ca++ influx via L-type and non-L-type Ca++ channels in thromboxane A2 receptor-mediated contraction in rat aorta.
Paul, RJ; Rapoport, RM; Tosun, M, 1998
)
0.64
"The treatment with verapamil led to a normal rhythm and function of the heart."( [Verapamil sensitive ventricular tachycardia with myocardial failure in a 2-year-old child].
Gossen, N; Liersch, R; Ulbricht, LJ; Winter, K, 1999
)
1.53
"Pretreatment with verapamil (2 mg."( Mechanisms of big endothelin-1-induced diuresis and natriuresis : role of ET(B) receptors.
Abassi, ZA; Brodsky, S; Hoffman, A; Ramadan, R; Winaver, J, 2000
)
0.63
"Pre-treatment with verapamil may have reduced the dysfunction (probably because of a reduction in mechanical remodeling during atrial fibrillation)."( Left atrial and appendage mechanical function after pharmacological or electrical cardioversion in patients with chronic atrial fibrillation: a multicenter, randomized study.
Cattarini, G; Mazzone, C; Miccio, M; Morgera, T; Pandullo, C; Salvi, R; Scardi, S, 2000
)
0.63
"Pretreatment with verapamil reversed the MDR phenotype."( Increased resistance to anticancer therapy of mouse cells lacking the poly(ADP-ribose) polymerase attributable to up-regulation of the multidrug resistance gene product P-glycoprotein.
Herceg, Z; Wesierska-Gadek, J; Wurzer, G, 2000
)
0.63
"Pre-treatment with verapamil (10 and 20 mg/kg, i.m.) significantly suppressed amphetamine-induced hypervigilance, stereotypy, oral hyperkinesia and tachypnoea but was unable to reverse other amphetamine-induced behavioural effects."( Behavioural and anti-psychotic effects of Ca2+ channel blockers in rhesus monkey.
Dubey, MP; Kalsotra, A; Kumar, R; Nath, C; Palit, G, 2001
)
0.63
"Treatment with verapamil had similar effects; however, there are no statistically significant dose dependent decreases in growth with increasing verapamil doses."( Calcium channel antagonists inhibit growth of subcutaneous xenograft meningiomas in nude mice.
Jensen, RL; Wurster, RD, 2001
)
0.65
"Pretreatment with verapamil (10 micromol/l) prevented angiotensin II-induced apoptosis."( Angiotensin II-induced apoptosis in rat cardiomyocyte culture: a possible role of AT1 and AT2 receptors.
Goldenberg, I; Grossman, E; Jacobson, KA; Shainberg, A; Shneyvays, V, 2001
)
0.63
"Treatment with Verapamil or aspirin reduced both chronic hypoxic pulmonary hypertension and the hypertrophy of the right ventricle."( Effects of verapamil and aspirin on experimental chronic hypoxic pulmonary hypertension and right ventricular hypertrophy in rats.
Kentera, D; Susić, D; Zdravković, M, 1979
)
0.99
"Pretreatment with verapamil 25 mg/Kg s.c."( Effect of verapamil on the transmural energy metabolism in the isoproterenol-induced myocardial lesion.
Higuchi, M; Takenaka, F, 1978
)
0.98
"Pretreatment with verapamil (10(-5) M), nifedipine (10(-6) M) or diltiazem (10(-5) M) had no effect on the increase in [Ca2+]i following addition of H2O2."( Cytosolic calcium increase in coronary endothelial cells after H2O2 exposure and the inhibitory effect of U78517F.
Hayashi, S; Kimura, M; Maeda, K, 1992
)
0.61
"Treatment with verapamil or low Ca2+ also induced fluctuations in cell volume."( Calcium-dependent control of volume regulation in renal proximal tubule cells: II. Roles of dihydropyridine-sensitive and -insensitive Ca2+ entry pathways.
McCarty, NA; O'Neil, RG, 1991
)
0.62
"Pretreatment with verapamil extends the ischaemic time after which reperfusion results in myocardial salvage in this model of ischaemia and reperfusion. "( Myocardial protection with verapamil during ischaemia and reperfusion: dissociation between myocardial salvage and the degree of ATP depletion during ischaemia.
Donnelly, TJ; Parmley, WW; Sievers, R; Wolfe, CL, 1991
)
0.91
"Treatment with verapamil caused significant increase of EDF from 61.2 to 78.2 cm/sek and increase EDF/LDF ratio from 1.02 to 1.30."( [Effects of verapamil and propranolol on the left-ventricular diastolic function in patients with primary arterial hypertension].
Markiewicz, M; Rymar, B; Trojnar, R; Wysokiński, A, 1991
)
1
"When treated by verapamil, coronary patients responded differently. "( [Effects of verapamil on the functional state of the liver in ischemic heart disease].
Makarovskiĭ, VV; Makeeva, LG; Shafranskiĭ, IuA; Svetova, SD; Vertkina, NV; Zharov, EI, 1991
)
1.01
"Pretreatment with verapamil (10 micrograms/kg/min delivered intravenously) prevented the fall in GFR (320 +/- 70 microliters/min 100 g), as did pretreatment with nitrendipine, 1 micrograms/kg/min (460 +/- 90 microliters/min/100 g)."( Evidence that calcium channel blockade prevents cyclosporine-induced exacerbation of renal ischemic injury.
Bia, MJ; Tyler, K, 1991
)
0.6
"Treatment with verapamil (10(-6) M) or washing in Ca(2+)-free Krebs Ringer solution after incubation with SCN(-)-Krebs Ringer selectively inhibited the slow phases of the aortic contractions."( Unusual effects of SCN and lyotropic anions on contractility of vascular smooth muscle from female rats.
Altura, BM; Altura, BT; Zhang, AM, 1991
)
0.62
"Pretreatment with verapamil to reperfusion hearts decreased MPO activity to 4.7 +/- 0.7 IU."( [Neutrophil infiltration in ischemic porcine myocardium and protective effect of verapamil].
Guo, ZG; Luo, WS; Tang, XL, 1990
)
0.83
"Treatment of verapamil alone appeared to be equivalent to that with only antivenom."( Verapamil potentiation of Chironex (box-jellyfish) antivenom.
Burnett, JW; Callanan, VI; Endean, R; Fenner, PJ; Othman, IB; Williamson, JA, 1990
)
2.07
"Pretreatment of verapamil with intravenous calcium did not alter the disposition of intravenous verapamil."( Evaluation of the pharmacokinetics and electrocardiographic effects of intravenous verapamil with intravenous calcium chloride pretreatment in normal subjects.
Bauman, JL; Beckman, KJ; Hariman, RJ; Hoon, TJ; Parker, RB; Schoen, MD, 1991
)
0.84
"Treatment with verapamil dramatically reversed this effect."( Periovulatory calcium channel blockade enhances reproductive performance in an animal model for endometriosis-associated subfertility.
Cantor, B; Lambert, H; Robin, B; Serpa, N; Steinleitner, A; Suarez, M, 1991
)
0.62
"Pretreatment with verapamil (2.5 or 5 mg/kg, i.p.) dose dependently lessened glandular wall calcium levels and worsened ethanol-induced mucosal damage."( Calcium and ethanol-induced gastric mucosal damage in rats.
Cho, CH; Ogle, CW; Wong, SH, 1991
)
0.6
"Pretreatment with verapamil reversed the effects of calcium infusion."( Influence of calcium infusion on plasma atrial natriuretic peptide in conscious dogs: intervention with calcium antagonist, verapamil.
Lembke, JM; Saelens, DA; Zawada, ET, 1990
)
0.81
"Treatment with verapamil (0.505 mg/kg over 2 days) lowered basal arterial pressures but did not change the effects of CSA on pressor sensitivity."( Altered pressor responses to NE and ANG II during cyclosporin A administration to conscious rats.
Smith-Powell, L; Telles, T; Textor, SC, 1990
)
0.62
"Pretreatment with verapamil induced significantly faster recovery from ethanol-induced changes in overall activity."( Verapamil effects on physiological and behavioral responses to ethanol in the rat.
De Lacy, PA; Janowsky, DS; Mack, CM; Rezvani, AH, 1990
)
2.05
"Pre-treatment with verapamil or washing the cells in calcium-free medium attenuated the stimulatory effect of AII on [Ca++]i."( Angiotensin II increases cytosolic calcium and stimulates catecholamine release in cultured bovine adrenomedullary cells.
Goldstein, DS; Keiser, HR; Stull, R; Zimlichman, R; Zimlichman, S, 1987
)
0.59
"Pretreatment with verapamil, a voltage-dependent Ca2+ channel inhibitor, also blocks both the sustained [Ca2+]i elevation and arachidonate liberation without altering peak intracellular Ca2+ release."( Receptor-stimulated phospholipase A2 activation is coupled to influx of external calcium and not to mobilization of intracellular calcium in C62B glioma cells.
Brooks, RC; Lapetina, EG; McCarthy, KD; Morell, P, 1989
)
0.6
"Pretreatment with verapamil markedly improved survival of skin flaps after 6 hours of venous cross-clamping compared with animals receiving placebo only (99% vs 53.3%; p less than 0.01)."( Verapamil improves survival of rat hyperemic island skin flaps.
Fayman, MS; Hinder, RA; Oosthuizen, MM; Stein, HJ, 1989
)
2.04
"The treatment of verapamil toxicity was examined in lightly sedated dogs. "( Treatment of verapamil toxicity in intact dogs.
Algeo, S; Gay, R; Goldman, S; Lee, R; Morkin, E; Olajos, M, 1986
)
0.98
"Pretreatment with verapamil essentially ablated the phenomenon of postischemic stunning: segment shortening was restored to 115 +/- 8% of normal after 3 h of reflow (p less than 0.01 versus control), endocardial ATP stores were partially preserved (30.6 +/- 1.2 nmol/mg protein; p less than 0.05 versus control) and creatine phosphate overshoot was blunted (endocardial creatine phosphate content decreased by -5.6 +/- 2.9 nmol/mg protein; p less than 0.05 versus control)."( Effect of verapamil on postischemic "stunned" myocardium: importance of the timing of treatment.
Kloner, RA; Przyklenk, K, 1988
)
1
"Pretreatment with verapamil in a dose of 2.0 x 10(-5)mol/kg given intraperitoneally (i.p.) diminished hypotensive effect of PGI2 i.c.v."( Influence of verapamil on central and peripheral effects of prostacyclin on circulatory system in rats.
Brus, R; Juraszczyk, Z; Kapustecki, J; Kozik, W; Kryj, M; Krzemiński, T; Kurcok, A, 1987
)
0.97
"4. Treatment with verapamil increased the Cmax (mean +/- s.d.: 227 +/- 117 vs 116 +/- 62 ng ml-1, P less than 0.05) and AUC (1389 +/- 617 vs 837 +/- 316 ng ml-1 h, P = 0.0625) of propranolol in all subjects."( The effect of combined therapy on the pharmacokinetics and pharmacodynamics of verapamil and propranolol in patients with angina pectoris.
Lennard, MS; McCourty, JC; Silas, JH; Tucker, GT, 1988
)
0.83
"Treatment with verapamil elicited biphasic dose-response effects on rat locomotor activity: doses equimolar to CRF treatment slightly increased CRF-stimulated locomotion, while doses of verapamil ten times greater slightly depressed CRF-stimulated locomotion."( The effects of verapamil on the locomotor-activating properties of corticotropin releasing factor (CRF) in the rat.
Aldenhoff, JB; Koob, GF; Swerdlow, NR, 1986
)
0.96
"Treatment with verapamil during long-term ethanol consumption prevented the development of these metabolic and functional abnormalities."( The preventive effect of verapamil on ethanol-induced cardiac depression: phosphorus-31 nuclear magnetic resonance and high-pressure liquid chromatographic studies of hamsters.
Garrett, J; Higgins, CB; James, T; Parmley, WW; Sievers, R; Wendland, M; White, R; Wikman-Coffelt, J; Wu, S, 1987
)
0.92
"Treatment with verapamil, 120 mg/day, reduced his symptoms in spite of an insignificant decrease in the arrhythmia observed with Holter dynamic electrocardiography."( Swallowing-induced paroxysmal supraventricular tachycardia.
Haraoka, S; Takemoto, M; Terasaka, R, 1987
)
0.61
"Pretreatment with Verapamil did not prevent calcium accumulation."( Time-course of changes in water, sodium, potassium and calcium contents of various brain regions in rats after systemic kainic acid administration.
Joó, F; Szerdahelyi, P; Sztriha, L, 1986
)
0.59
"Pretreatment with verapamil inhibited thromboxane synthesis, the rise in pulmonary artery pressure and the hypoxia without affecting the transient leukopenia."( Effects of verapamil on thromboxane synthesis and pulmonary hypertension in sheep.
Davies, BJ; McDonald, JW; Noulty, EJ; Pisters, LL; Smallbone, BW; Taylor, NE, 1986
)
0.98
"Treatment with verapamil (intravenous bolus dose of 0.2 mg/kg body weight followed by infusion of 0.56 +/- 0.14 mg/kg per h) was begun 1 hour after occlusion and infusion was continued for the remainder of the experiment."( Effect of verapamil on infarct size in dogs subjected to coronary artery occlusion with transient reperfusion.
Alker, KJ; Braunwald, E; Campbell, CA; Kloner, RA, 1986
)
1.01
"Pretreatment with verapamil (0.08 mg/kg iv) did not reduce this upward shift: LVEDP rose from 6 +/- 1 to 16 +/- 1 mmHg (P less than 0.01, n = 7) and there were similar small increases in end-diastolic segment length.(ABSTRACT TRUNCATED AT 250 WORDS)"( Effects of verapamil on regional myocardial diastolic function in pacing-induced ischemia in dogs.
Bourdillon, PD; Grossman, W; Paulus, WJ; Serizawa, T, 1986
)
0.98
"Pretreatment with verapamil, 80 mg and 120 mg (every 8 hours for 3 days), reduced the oral clearance of quinidine from 17.0 L/hr to 11.6 and 11.3 L/hr, respectively (P less than 0.01)."( The effect of coadministration of verapamil on the pharmacokinetics and metabolism of quinidine.
Beckman, H; Blevins, R; Edwards, DJ; Lavoie, R; Rubenfire, M, 1987
)
0.88
"Pretreatment with verapamil reduced the size of these subendocardial infarcts from 34 +/- 8 to 8 +/- 3% of the ischemic circumflex vascular bed (anatomic area at risk)."( Effects of calcium-channel blockers on myocardial preservation during experimental acute myocardial infarction.
Jennings, RB; Reimer, KA, 1985
)
0.59
"Pretreatment with verapamil significantly decreased gastric ulcerative response to cold-restraint stress in the rat."( Verapamil attenuates stress-induced gastric ulceration.
Leahy, AL; Nee, JM; Pollock, TW; Wait, RB, 1985
)
2.04

Toxicity

Only 3 patients complained of adverse effects from verapamil during the double-blind phase of the study. Carvedilol and verap amil (10 micromol/L) reduced the LD50 (dose which results in the death of half the number of cells) of the Hs578T-Dox subline. Phosphorylation at serine 473 of the Akt protein (P-Akt), a protein representing a common pathway for insulin receptors (IR), insulinlike growth factor receptors (IGFR), and hybrid receptors formed by IR and IGFR subunits.

ExcerptReferenceRelevance
" This seems to be a rare side effect as there have only been three other reported cases of secondary extrapyramidal syndromes in the literature."( [Parkinson syndrome, a possible adverse effect of calcium inhibitors].
Lauribe, P; Lévy, S; Malaterre, HR; Paganelli, F; Ramond, B, 1992
)
0.28
" These studies have shown this drug combination to be associated with severe toxic effects."( Effects of verapamil on the acute toxicity of doxorubicin in vivo.
Anderson, J; Baker, PB; Desai, P; Dwivedi, C; Engineer, FN; Sharma, HM; Sridhar, R, 1992
)
0.67
" AB and hypoxia/reoxygenation caused additive, not synergistic, LDH release whereas CS-AB had no adverse effect."( Direct amphotericin B-mediated tubular toxicity: assessments of selected cytoprotective agents.
Bredl, CR; Schimpf, BA; Zager, RA, 1992
)
0.28
" In addition, detailed histopathological examination shows that treatment of mice with chemotherapeutic drugs and R-verapamil does not change the organ-related toxicity pattern but only moderately accentuates inherent toxic side effects of the chemotherapeutic agents."( Chemotherapy and chemosensitization of transgenic mice which express the human multidrug resistance gene in bone marrow: efficacy, potency, and toxicity.
Gottesman, MM; Licht, T; Merlino, GT; Mickisch, GH; Pastan, I, 1991
)
0.49
" A direct toxic effect of CsA on renal tubule epithelia was demonstrated using nigrosine uptake and LDH release as indicators of cell death."( Mechanisms of cyclosporine A toxicity in defined cultures of renal tubule epithelia: a role for cysteine proteases.
Hartz, PA; Wilson, PD, 1991
)
0.28
"Four hypertensive patients with chronic renal insufficiency or end-stage renal disease who were treated with sustained-release verapamil hydrochloride subsequently developed acute toxic effects."( Acute toxic effects of sustained-release verapamil in chronic renal failure.
Bierman, MH; Hammeke, MD; Pritza, DR, 1991
)
0.75
" At severely toxic levels when arterial blood pressure fell by 50%, all three drugs decreased cardiac output."( Effects of calcium channel blocker overdose-induced toxicity in the conscious dog.
Gambone, LM; Schoffstall, JM; Shaw, RP; Sit, SP; Spivey, WH, 1991
)
0.28
" However, at a more severe level, their toxic effects are similar and manifested predominantly by their actions on the slow calcium channel."( Effects of calcium channel blocker overdose-induced toxicity in the conscious dog.
Gambone, LM; Schoffstall, JM; Shaw, RP; Sit, SP; Spivey, WH, 1991
)
0.28
" Iatrogenic toxicity resulting from this accumulation of potentially toxic drugs such as CQ within normal cells could complicate the reversal of mdr in vivo."( Reversal of drug-resistant falciparum malaria by calcium antagonists: potential for host cell toxicity.
Grogl, M; Long, GW; Martin, SK; Watt, G,
)
0.13
" All systemic toxic effects observed were easily treated or disappeared with either temporary or permanent discontinuation of the verapamil infusion or by a decrease in the dose of verapamil."( Systemic toxic effects associated with high-dose verapamil infusion and chemotherapy administration.
Appleton, CP; Dalton, WS; Miller, TP; Mosley, K; Pennock, GD; Plezia, P; Roeske, WR; Salmon, SE, 1991
)
0.74
" Another side effect is constipation, which is frequent after verapamil."( Calcium antagonists--assessment of side effects.
Thulin, T, 1990
)
0.52
" There was no apparent relationship between drug reversal of vcr resistance and the cytotoxic actions of the drug per se since the calcium channel blocker diltiazem (dil) significantly potentiated the actions of vcr on MDR L100 cells without being more toxic to these cells (compared to vcr-sensitive L0 cells)."( Pharmacological modification of multi-drug resistance (MDR) in vitro detected by a novel fluorometric microculture cytotoxicity assay. Reversal of resistance and selective cytotoxic actions of cyclosporin A and verapamil on MDR leukemia T-cells.
Larsson, R; Nygren, P, 1990
)
0.47
" Verapamil might, however, modify the adverse cardiac effects of 5-FU by preventing supraventricular tachyarrhythmia."( Failure of preventing 5-fluorouracil cardiotoxicity by prophylactic treatment with verapamil.
Albertsson, M; Eskilsson, J, 1990
)
1.41
"Nephrotoxicity is the most troublesome side effect of cyclosporin A (CSA) therapy."( Lack of effect of verapamil and MDL 646, a cytoprotective PGE1 analogue on cyclosporin A nephrotoxicity in vitro.
Hall, TJ; Heckel, C, 1990
)
0.61
" Calcium channel blockers have ameliorated tissue injury due to toxic and ischemic insults."( Effect of verapamil on cephaloridine nephrotoxicity in the rabbit.
Browning, MC, 1990
)
0.68
"03%) was the predominant adverse reaction, followed by dizziness (3."( Efficacy and safety of verapamil SR 240 mg in essential hypertension: results of a multicentric phase IV study.
Pfennigsdorf, G; Schumacher, A; Sosna, J; Speders, S, 1989
)
0.59
" The pharmacokinetic characteristics of SR verapamil account for its more favorable side-effect profile observed with this formulation."( Comparative efficacy, safety, and kinetics of immediate- and slow-release verapamil in hispanic patients with essential hypertension.
Cubeddu, LX; Faggin, BM; Fuenmayor, NT, 1989
)
0.77
"1 mM verapamil was toxic to the cells grown over five days (44 +/- 5 micrograms protein/flask)."( In vitro cyclosporine toxicity. The effect of verapamil.
Chan, P; Moorhead, JF; Scoble, JE; Senior, JC; Sweny, P; Varghese, Z, 1989
)
1.05
" Additional nutritional factors may play a crucial role in achieving the amelioration of this model of toxic nephropathy."( The effect of oral calcium load or verapamil on gentamicin-induced nephrotoxicity.
Aladjem, M; Bogin, E; Tamir, A, 1989
)
0.55
" G1-phase CHO cells showed a 2-fold increase in the susceptibility to the toxic effects of sodium arsenite as compared to asynchronous CHO cells."( Differential cytotoxicity of sodium arsenite in human fibroblasts and Chinese hamster ovary cells.
Jan, KY; Ko, JL; Lee, TC, 1989
)
0.28
"There is a narrow margin between therapeutic and toxic doses and serum levels of digitalis glycosides."( Digitalis toxicity.
Antman, EM; Smith, TW, 1985
)
0.27
" Diltiazem with a beta-blocker is usually well-tolerated, with a low incidence of adverse effects, similar to the experience with diltiazem monotherapy."( Combined use of calcium-channel and beta-adrenergic blockers for the treatment of chronic stable angina. Rationale, efficacy, and adverse effects.
Parisi, AF; Strauss, WE, 1988
)
0.27
"Nephrotoxicity is a serious side effect that limits the use of cyclosporine (CyA) as an immunosuppressive agent."( Treatment with verapamil and adenosine triphosphate-MgCl2 reduces cyclosporine nephrotoxicity.
Baue, AE; Chaudry, IH; Sumpio, B, 1987
)
0.63
"In the in vitro perfusion of the isolated heart, toxic doses of cardiac glycosides produce an inotropic response which is followed by a decline in contractile force and an increase in the resting tension."( Digitalis-induced mechanical toxicity: protection by slow Ca++ channel blockers.
Agbanyo, M; Bains, R; Hoeschen, RJ; Khatter, JC; Navaratnam, S, 1986
)
0.27
" These data suggest that the calcium channel blocker verapamil is a metabolically safe drug to use as monotherapy in essential hypertension."( No metabolic side effects of long-term treatment with verapamil in hypertension.
Hals, O; Lauve, O; Midtbø, K, 1988
)
0.77
" Immediate pretreatment with verapamil increased the mortality of mice given the LD50 dose of lidocaine to 74%, and in mice given the LD50 doses of bupivacaine, to 82%."( Verapamil increases the toxicity of local anesthetics.
Rosenblatt, RM; Tallman, RD; Wang, YL; Weaver, JM, 1988
)
2.01
"High circulating concentrations of calcium are toxic to the heart and may cause cardiac arrhythmias and arrest."( Verapamil reverses calcium cardiotoxicity.
Chernow, B; Holaday, J; Malcolm, D; Zaloga, GP, 1987
)
1.72
" Cepharanthine, which had no toxic action on survival, increased intracellular ADR uptake by about 20% for 1 h incubation at 37 degrees C, and increased cellular ADR retention after incubation in an ADR-free medium for 4 h from 15% to 75%."( Modification of cellular efflux and cytotoxicity of adriamycin by biscoclaulin alkaloid in vitro.
Karino, Y; Kawasaki, S; Nagaoka, S; Nakanishi, T; Sasaki, K, 1987
)
0.27
"Calcium-channel blockers are useful for the treatment of hypertrophic cardiomyopathy (HCM), but, their adverse effects, especially, those of diltiazem, have not been of much concern."( Adverse effects of atrial fibrillation and syncope induced by calcium-channel blockers in hypertrophic cardiomyopathy.
Doiuchi, J; Hamada, M; Ito, T; Kokubu, T; Ochi, T, 1985
)
0.27
" Verapamil also potentiates the effect of a toxic conjugate formed between Pseudomonas exotoxin and a monoclonal antibody to the human transferrin receptor (anti-TFR-PE) and enhances the effect of Pseudomonas exotoxin (PE) alone."( Verapamil enhances the toxicity of conjugates of epidermal growth factor with Pseudomonas exotoxin and antitransferrin receptor with Pseudomonas exotoxin.
Akiyama, S; Fitzgerald, DJ; Gottesman, MM; Hanover, JA; Pastan, I; Willingham, MC, 1984
)
2.62
" This indicates that the effect of the ionophore was not due to nonspecific release of toxic products from the effector cells."( A role for calcium-activated calmodulin in murine nonspecific cell-mediated cytotoxicity.
Cain, CA; Fan, S; Tompkins, WA; Weltzin, R, 1983
)
0.27
" Adverse effects during Phase 2 were mild, consisting of constipation (6 patients) and prolongation of the P-R interval (5 patients); however, no patient required alteration of the 480 mg/day dosage."( Efficacy and safety of verapamil in patients with angina pectoris after 1 year of continuous, high-dose therapy.
Creager, MA; Cutler, SS; Klein, MD; McCabe, CH; Ryan, TJ; Weiner, DA, 1983
)
0.58
" Only 3 patients complained of adverse effects from verapamil during the double-blind phase of the study."( Effectiveness and safety of oral verapamil to control exercise-induced tachycardia in patients with atrial fibrillation receiving digitalis.
Baessler, C; Morganroth, J; Panidis, IP, 1983
)
0.8
" Adverse effects were few and consisted primarily of mild constipation in six patients taking verapamil, and pedal edema and transient flushing in 2 patients each using diltiazem."( The efficacy and safety of high-dose verapamil and diltiazem in the long-term treatment of stable exertional angina.
Cutler, SS; Klein, MD; McCabe, CH; Ryan, TJ; Weiner, DA, 1984
)
0.76
"The ophthalmic examination of patients with hypertrophic cardiomyopathy treated with high doses of verapamil over a considerable period of time showed no evidence of a side effect of the drug, thus proving its ocular safety."( Evaluation of the ocular safety of verapamil. Scheimpflug photography with densitometric image analysis of lens transparency in patients with hypertrophic cardiomyopathy subjected to long-term therapy with high doses of verapamil.
Dragomirescu, V; Hockwin, O; Kozamanoglu, K; Kremer, F; Laser, H; Ohrloff, C, 1984
)
0.76
" Perturbation of cytophilic IgG with particle-bound protein A elicited a chemiluminescent response from peritoneal macrophages; however, experiments with scavengers of reactive oxygen species indicated that toxic oxygen radicals may not be required for cytotoxicity."( Human peritoneal macrophage cytotoxicity mediated by cytophilic IgG.
Freiberg, M; Keane, WF; Miller, W; Peterson, PK; Staub, D; Verbrugh, HA, 1983
)
0.27
" As there were no predisposing factors, direct drug action is implicated and other reports of the adverse effects of verapamil are noted."( Side effects of verapamil in infants.
Radford, D, 1983
)
0.82
" Our results suggest that the following factors may participate in the IPRO-induced embryotoxicity: (1) IPRO, (2) its toxic metabolites, (3) cAMP."( Analysis of the cardiotoxic effect of isoproterenol in chick embryo.
Janatová, T; Krause, EG; Ostádal, B; Pelouch, V; Rychter, Z,
)
0.13
"Nephrotoxicity is the most common and important side-effect of cyclosporin (CsA) therapy."( Prevention of acute cyclosporin nephrotoxicity by verapamil and atrial natriuretic factor in the rat.
Bagnis, C; Bitker, MO; Deray, G; Dubois, M; Jacobs, C; Jacquiaud, C, 1994
)
0.54
" D-Verapamil was only about half as toxic as racemic verapamil and this too is consistent with clinical observations."( Identification of a multidrug resistance modulator with clinical potential by analysis of synergistic activity in vitro, toxicity in vivo and growth delay in a solid human tumour xenograft.
Bicknell, SR; Hamilton, T; Kaye, SB; Morrison, JG; Plumb, JA; Setanoians, A; Wishart, GC, 1994
)
0.91
" On the contrary, verapamil even accentuates the toxic effects of diclofenac."( Failure of calcium antagonistic agents to prevent hepatotoxicity induced by diclofenac.
Estler, CJ; Lepper, H; Schmitz, G, 1995
)
0.63
" However, tamoxifen alone caused significant toxic effects to TSGH-8301 at > or = 40 microM and to HTB9 at > or = 30 microM."( Combined cytotoxic effects of tamoxifen and chemotherapeutic agents on bladder cancer cells: a potential use in intravesical chemotherapy.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC; Tseng, NF, 1996
)
0.29
"Tamoxifen enhanced the cytotoxicity of chemotherapeutic agents largely through its toxic effects on the bladder cancer cells."( Combined cytotoxic effects of tamoxifen and chemotherapeutic agents on bladder cancer cells: a potential use in intravesical chemotherapy.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC; Tseng, NF, 1996
)
0.29
" The rats were observed for toxic signs and survival over a period of 15 days."( Reversal of acute theophylline toxicity by calcium channel blockers in dogs and rats.
Alleva, FR; Balazs, T; Joseph, X; Vick, JA; Whitehurst, VE; Zhang, J, 1996
)
0.29
" As parameters of toxic kidney damage we have used the urine levels of the following enzymes: N-acetyl-beta-D-glucosaminidase (NAG), gama-glutamyltransferase (GMT) and alkaline phosphatase (ALP)."( The effect of calcium channel blockers on cyclosporine A (Cs A) induced nephrotoxicity in rats.
Bártová, V; Hátle, K; Nĕmecek, K; Stípek, S; Zima, T, 1995
)
0.29
"The hepatotoxicity of acetaminophen overdose depends on the metabolic activation to a toxic reactive metabolite by the hepatic mixed function oxidases."( Effect of nifedipine, verapamil, diltiazem and trifluoperazine on acetaminophen toxicity in mice.
Dimova, S; Koleva, M; Rangelova, D; Stoythchev, T, 1995
)
0.61
" In vitro, but not in vivo, verapamil inhibited the activity of alcohol dehydrogenase (ADH), the key enzyme in the conversion of AA into the toxic metabolite acrolein."( Effect of verapamil on allyl alcohol hepatotoxicity.
Atzori, L; Congiu, L, 1996
)
0.99
" The finding that delta-HCH was more toxic than lindane may be correlated to the differences between the isomers with regard to the action on the different Ca2+ pools."( The mechanism for hexachlorocyclohexane-induced cytotoxicity and changes in intracellular Ca2+ homeostasis in cultured cerebellar granule neurons is different for the gamma- and delta-isomers.
Frandsen, A; Pomés, A; Rodríguez-Farré, E; Rosa, R; Sanfeliu, C; Schousboe, A; Suñol, C, 1997
)
0.3
" These differences can be attributed at least in part to the low catecholamine profile of verapamil and the marked rapid adrenergic activation with short-acting nifedipine, which could also explain the adverse effects found when this agent is given to patients with acute coronary syndromes."( Calcium channel blockers for hypertension: dissecting the evidence for adverse effects.
Opie, LH, 1997
)
0.52
" However, at least as important is a consideration of adverse reactions and the safety of the combination compared to monotherapy."( Safety profile of the combination of verapamil and trandolapril.
Holzgreve, H, 1997
)
0.57
"In randomized placebo-controlled studies adverse events were observed in 25."( Safety profile of the combination of verapamil and trandolapril.
Holzgreve, H, 1997
)
0.57
"In summary, the profile of adverse drug reactions of a fixed-dose combination of verapamil and trandolapril consists the typical side effects of the monocompounds."( Safety profile of the combination of verapamil and trandolapril.
Holzgreve, H, 1997
)
0.8
" Our results show that both A beta(1-42) and A beta(25-35) are toxic to HAEC in a time- and dose-dependent manner, and that this toxicity can be partially prevented by the calcium channel blocker, verapamil, and the antioxidant, superoxide dismutase."( Superoxide free radical and intracellular calcium mediate A beta(1-42) induced endothelial toxicity.
Crawford, F; Fang, C; Mullan, M; Suo, Z, 1997
)
0.49
" Both verapamil and nimodipine pretreatment increased the LD50 and 95% confidence intervals for bupivacaine and increased survival."( The effects of verapamil and nimodipine on bupivacaine-induced cardiotoxicity in rats: an in vivo and in vitro study.
Adsan, H; Onaran, O; Tulunay, M, 1998
)
1.13
" The aim of this study was to determine whether these inhibitors can prevent the toxic effects of Cd on the kidney which is the critical organ."( Effect of calmodulin-inhibitors and verapamil on the nephrotoxicity of cadmium in rat.
Bernard, A; Lermioglu, F, 1998
)
0.58
" The concentration-dependent protection from methapyrilene toxicity afforded by metyrapone correlated with an inhibition of microsomal CYP2C11-associated androstenedione 16alpha hydroxylase activity, and hepatocytes prepared from hypophysectomised rats (containing reduced levels of microsomal immunodetectable CYP2C11 and associated androstenedione 16alpha hydroxylase activity) showed resistance to the toxic effects of methapyrilene."( Methapyrilene hepatotoxicity is associated with oxidative stress, mitochondrial disfunction and is prevented by the Ca2+ channel blocker verapamil.
Morgan, WA; Mullervy, J; Powell, CJ; Ratra, GS; Wright, MC, 1998
)
0.5
" Carvedilol and verapamil (10 micromol/L) reduced the LD50 (dose which results in the death of half the number of cells) of the Hs578T-Dox subline from 200 mg/L to approx."( Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity.
Behnam-Motlagh, P; Grankvist, K; Henriksson, R; Jonsson, O; Persson, M, 1999
)
0.65
" In addition, combination therapy enhances tolerability because one drug of fixed combination can antagonize some of the adverse effects of the second drug."( [Fixed-dose combination therapy: reduction of side effects with enhanced tolerance and antihypertensive efficacy].
Gómez Guindal, JA; González Lama, I; González Maqueda, I, 1999
)
0.3
" None of the Pgp blockers was toxic up to 10 microM, but amiodarone markedly increased CK leakage at 25 microM."( Effect of PSC 833, verapamil and amiodarone on adriamycin toxicity in cultured rat cardiomyocytes.
Estevez, MD; Schramm, U; Wolf, A, 2000
)
0.64
" Adverse events and safety were also evaluated."( Efficacy and safety of a new long-acting drug combination, trandolapril/verapamil as compared to monotherapy in primary hypertension. Swedish TARKA trialists.
Andrup, M; Karlberg, BE; Odén, A, 2000
)
0.54
" Regarding safety, both observational studies and RCTs suggest that adverse effects of CCBs may be linked to short-acting agents, specifically short-acting nifedipine."( Current status of safety and efficacy of calcium channel blockers in cardiovascular diseases: a critical analysis based on 100 studies.
Kübler, W; Opie, LH; Yusuf, S,
)
0.13
" Adverse event rates were compared across the treatment groups by the Fisher exact test."( Safety of controlled-onset extended-release verapamil in middle-aged and older patients with hypertension and coronary artery disease.
Anders, RJ; Black, HR; Elliott, WJ; Johnson, MF; White, WB, 2001
)
0.57
"Low dose verapamil is safe when administered intraarterially to patients with cerebral vasospasm."( Intraarterially administered verapamil as adjunct therapy for cerebral vasospasm: safety and 2-year experience.
Aagaard, BD; Berman, MF; Duong, H; Feng, L; Fitzsimmons, BF; Lin, E; Pile-Spellman, J; Young, WL, 2002
)
1.02
"The present study was performed to compare the cardiovascular adverse effects of verapamil, KR30031 and their optical isomers, and also to measure their ability to overcome multidrug resistance (MDR)."( Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.
Choi, SU; Kwon, MJ; Lee, BH; Lee, CO; Yi, KY; Yoo, SE, 2003
)
0.55
" Adenosine caused adverse effects in 18."( [A randomized, multicenter trial to compare the safety and efficacy of adenosine versus verapamil for termination of paroxysmal supraventricular tachycardia].
Cheng, KA, 2003
)
0.54
" Adverse reactions to adenosine are common but are minor and brief."( [A randomized, multicenter trial to compare the safety and efficacy of adenosine versus verapamil for termination of paroxysmal supraventricular tachycardia].
Cheng, KA, 2003
)
0.54
" When compared clinical effects by quinacrine and the combination therapy, improvement of clinical findings was observed at the same level without any adverse effects."( Toxicity of quinacrine can be reduced by co-administration of P-glycoprotein inhibitor in sporadic Creutzfeldt-Jakob disease.
Eguchi, K; Katamine, S; Kataoka, Y; Nishida, N; Niwa, M; Satoh, K; Shirabe, S; Yamauchi, A, 2004
)
0.32
"In this study, the toxic effect of sanguinarine (SANG) on heart was studied with isolated cardiac muscle strip isolated from Wistar rat."( Induction of contracture and extracellular Ca2+ influx in cardiac muscle by sanguinarine: a study on cardiotoxicity of sanguinarine.
Cheng, HW; Cheng, YW; Hu, CM; Kang, JJ; Liao, JW, 2005
)
0.33
" The most toxic compounds, the second one, characterized by the smallest variations of TEER, included verapamil and diltiazem."( Influence of different calcic antagonists on the Caco-2 cell monolayer integrity or "TEER, a measurement of toxicity?".
Galmier, MJ; Lartigue, C; Mathieu, F; Pognat, JF,
)
0.35
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"Cyclosporine nephrotoxicity remains a major side effect in solid organ transplantation, and can be exacerbated by concomitant administration of sirolimus."( Role of P-glycoprotein in cyclosporine cytotoxicity in the cyclosporine-sirolimus interaction.
Anglicheau, D; Beaune, P; Cassinat, B; Legendre, C; Marquet, P; Méria, P; Pallet, N; Rabant, M; Thervet, E, 2006
)
0.33
" The immune system can be a target for many chemicals including environmental contaminants and drugs with potential adverse effects on human health."( In vitro tests to evaluate immunotoxicity: a preliminary study.
Carfi', M; Corsini, E; Gennari, A; Gribaldo, L; Hartung, T; Malerba, I; Pallardy, M; Pieters, R; Van Loveren, H; Vohr, HW, 2007
)
0.34
"Treatment of RA grafts with phenoxybenzamine was associated with a reduction in perioperative myocardial injury and adverse cardiac events in this study population."( Radial artery graft treatment with phenoxybenzamine is clinically safe and may reduce perioperative myocardial injury.
Bourke, ME; Gunning, D; Kulik, A; Mesana, TG; Rubens, FD; Ruel, M, 2007
)
0.34
" In spite of the low dose ingested, the postmortem cardiac blood verapamil level was clearly toxic (6000 ng/mL, or 6 mg/L)."( Verapamil toxicity: an unusual case report and review of the literature.
Batalis, NI; Harley, RA; Schandl, CA, 2007
)
2.02
" We investigated the toxic mechanisms of As(2)O(3) in H9c2 cardiomyocytes."( Arsenic trioxide-induced apoptosis in H9c2 cardiomyocytes: implications in cardiotoxicity.
Chen, H; Feng, T; Lu, Y; Shan, H; Yang, B; Zhang, Y; Zhao, X, 2008
)
0.35
" Phosphorylation at serine 473 of the Akt protein (P-Akt), a protein representing a common pathway for insulin receptors (IR), insulinlike growth factor receptors (IGFR), and hybrid receptors formed by IR and IGFR subunits, was abolished in the presence of toxic doses of the phenylalkylamine CCB verapamil."( Verapamil toxicity dysregulates the phosphatidylinositol 3-kinase pathway.
Bechtel, LK; Haverstick, DM; Holstege, CP, 2008
)
1.96
"Aim of this study was to investigate antiarrhythmic and toxic effects of verapamil in mice and rats with thyrotoxicosis and hypothyroidism."( [Characteristics of pharmacological and toxic effects of verapamil during cardiac arrhythmia in thyrotoxic and hypothyroid rats].
Afanas'eva, EIu; Arzamastsev, EV; Sokhanenkov, MIu; Sokhanenkova, AE, 2008
)
0.82
" No adverse events resulted from rate control medication."( Safety and efficacy of a rate control protocol for cardiac CT.
Roberts, WT; Timmis, AD; Timmis, JB; Wright, AR, 2009
)
0.35
" Similar (protective) effect had also verapamil, calcium channel blocker, when given in non toxic doses and at the same time schedule as db-cAMP Combination of db-cAMP and verapamil had not synergistic effect in protection from D-GalN+LPS hepatotoxicity; the survival of mice was similar to that seen in protection caused by each agent alone."( The effect of cyclic adenosine monophosphate (cAMP) on acute liver toxicity in mice induced by D-galactosamine and lipopolysaccharide.
Cavar, I; Culo, F; Erceg, D; Kelava, T; Pasalić, M, 2010
)
0.63
"In this study, the toxic effects of verapamil (VRP) were studied on juvenile rainbow trout, Oncorhynchus mykiss, by chronic semi-static bioassay."( Chronic toxicity of verapamil on juvenile rainbow trout (Oncorhynchus mykiss): effects on morphological indices, hematological parameters and antioxidant responses.
Grabic, R; Kolarova, J; Li, P; Li, ZH; Machova, J; Randak, T; Velisek, J; Zlabek, V, 2011
)
0.97
" Seven (24%) patients presented bradycardia considered as nonserious adverse event (NSAE) and four (14%) patients presented arrhythmia (heart block) considered as serious adverse event (SAE)."( Cardiac safety in cluster headache patients using the very high dose of verapamil (≥720 mg/day).
Donnet, A; Lanteri-Minet, M; Piano, V; Silhol, F, 2011
)
0.6
" FC combined with Cd(2+) counteracted the toxic effect of Cd(2+) on endogenous growth and significantly decreased Cd(2+) content (not the case for Cd(2+) at the highest concentration) in coleoptile segments."( Fusicoccin counteracts the toxic effect of cadmium on the growth of maize coleoptile segments.
Karcz, W; Kita, A; Kurtyka, R, 2011
)
0.37
" However, the direct cardiotoxicity in vitro and its mechanisms of toxic action remain unclear."( Direct cardiac toxicity of the tentacle-only extract from the jellyfish Cyanea capillata demonstrated in isolated rat heart.
Beilei, W; Jia, L; Liang, X; Liming, Z; Lin, Z; Qian, H; Qianqian, W; Tao, W; Xiaojuan, W; Xuting, Y, 2012
)
0.38
" The CCBs nimodipine (NDP) and verapamil (VPM) both significantly suppressed toxic secretions from human astrocytes and astrocytoma U-373 MG cells that were induced by interferon (IFN)-γ."( Inhibition of human astrocyte and microglia neurotoxicity by calcium channel blockers.
Hashioka, S; Klegeris, A; McGeer, PL, 2012
)
0.66
" Histopathological examinations and electrocardiogram comparison demonstrated that the intelligent DDDS could markedly inhibit the growth of tumor and potentially offer an approach for safe cancer therapy."( cRGD-functionalized polymeric magnetic nanoparticles as a dual-drug delivery system for safe targeted cancer therapy.
Gao, FY; Ma, M; Shen, JM; Yang, YJ; Yin, T; Yue, F; Zhang, HX, 2013
)
0.39
" Incidents of adverse cardiac drug reactions are more common in patients with preexisting heart disease than the general population."( Drug screening using a library of human induced pluripotent stem cell-derived cardiomyocytes reveals disease-specific patterns of cardiotoxicity.
Bers, DM; Diecke, S; Gong, T; Knowles, JW; Lan, F; Lee, AS; Liang, P; Nguyen, PK; Robbins, RC; Sallam, K; Sanchez-Freire, V; Wang, PJ; Wang, Y; Wu, JC, 2013
)
0.39
" Our data indicate that healthy and diseased individuals exhibit different susceptibilities to cardiotoxic drugs and that use of disease-specific hiPSC-CMs may predict adverse drug responses more accurately than the standard human ether-a-go-go-related gene test or healthy control hiPSC-CM/hESC-CM screening assays."( Drug screening using a library of human induced pluripotent stem cell-derived cardiomyocytes reveals disease-specific patterns of cardiotoxicity.
Bers, DM; Diecke, S; Gong, T; Knowles, JW; Lan, F; Lee, AS; Liang, P; Nguyen, PK; Robbins, RC; Sallam, K; Sanchez-Freire, V; Wang, PJ; Wang, Y; Wu, JC, 2013
)
0.39
"Repeat doses of UMEC and UMEC/VI in combination with and without verapamil were safe and well tolerated."( Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study.
Crater, G; Hughes, S; Kelleher, D; Mehta, R; Preece, A, 2013
)
1.03
" In an embryo-larval toxicity test (sub-chronic exposure), the bioconcentration, depuration, and toxic effects of verapamil were assessed in common carp."( Toxic effects, bioconcentration and depuration of verapamil in the early life stages of common carp (Cyprinus carpio L.).
Fedorova, G; Grabic, R; Grabicova, K; Kroupova, HK; Machova, J; Prokes, M; Steinbach, C; Valentova, O, 2013
)
0.85
"Aconitine (AC) is a highly toxic alkaloid from bioactive plants of the genus Aconitum, some of which have been widely used as medicinal herbs for thousands of years."( P-glycoprotein is responsible for the poor intestinal absorption and low toxicity of oral aconitine: in vitro, in situ, in vivo and in silico studies.
Li, Z; Liu, F; Liu, K; Ruan, J; Xu, L; Yang, C; Zhang, T; Zhang, Z, 2013
)
0.39
" Taken together, potent MDR-modulating activity along with intracellular conversion into the natural flavonoid quercetin warrants development of the quercetin-amino acid conjugates as safe MDR modulators."( Water-soluble and cleavable quercetin-amino acid conjugates as safe modulators for P-glycoprotein-based multidrug resistance.
Chong, Y; Choo, H; Kim, MK, 2014
)
0.4
"To provide a comprehensive evidence-based review of current evidence on mechanism of action, efficacy, and adverse events of calcium antagonists in treatment of hypertrophic scars and keloids."( Mechanism of Action, Efficacy, and Adverse Events of Calcium Antagonists in Hypertrophic Scars and Keloids: A Systematic Review.
Piatkowski de Grzymala, A; van der Hulst, R; Verhiel, S, 2015
)
0.42
" Articles were categorized into two groups: mechanism of action or efficacy and adverse events."( Mechanism of Action, Efficacy, and Adverse Events of Calcium Antagonists in Hypertrophic Scars and Keloids: A Systematic Review.
Piatkowski de Grzymala, A; van der Hulst, R; Verhiel, S, 2015
)
0.42
" We report a serious side effect of ibrutinib potentially attributable to interaction with the moderate CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.88
"This is the first description of a serious side effect of ibrutinib likely due to an interaction with the CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.88
" Secondary end points were the occurrence of hypotension, arrhythmias, and major adverse cardiac events (MACEs) during hospital stay."( Efficacy and Safety of Local Intracoronary Drug Delivery in Treatment of No-Reflow Phenomenon: A Pilot Study.
Abu Arab, T; El Etriby, A; Rafik, R, 2016
)
0.43
"Local intra-coronary delivery of adrenaline ± verapamil is a safe and effective method for the treatment of no-reflow phenomenon complicating PCI."( Efficacy and Safety of Local Intracoronary Drug Delivery in Treatment of No-Reflow Phenomenon: A Pilot Study.
Abu Arab, T; El Etriby, A; Rafik, R, 2016
)
0.69
" The secondary outcomes were the percentage of ST-segment resolution on 12-lead ECG, left ventricular ejection fraction and wall motion score index by two-dimensional echocardiography at 3-5 days after pPCI, as well as major adverse cardiovascular events at 30 days."( Efficacy and safety of intracoronary verapamil versus sodium nitroprusside for the prevention of microvascular obstruction during primary percutaneous coronary intervention for ST-segment elevation myocardial infarction.
Abdelaziz, HK; Elkilany, W; Khalid, S; Saad, M; Sabet, S, 2017
)
0.73
" Both groups had similar 30-day major adverse cardiovascular events (3."( Efficacy and safety of intracoronary verapamil versus sodium nitroprusside for the prevention of microvascular obstruction during primary percutaneous coronary intervention for ST-segment elevation myocardial infarction.
Abdelaziz, HK; Elkilany, W; Khalid, S; Saad, M; Sabet, S, 2017
)
0.73
"Drug-induced nephrotoxicity is one of the most frequent adverse events in pharmacotherapy."( Assessment of hepatic metabolism-dependent nephrotoxicity on an organs-on-a-chip microdevice.
Jiang, L; Li, Z; Qin, J; Shi, Y; Su, W; Tao, T; Xu, C; Zhu, Y, 2018
)
0.48
" There was no association by comparing the amount of insulin administered on adverse effects or glucose administered, suggesting higher doses of insulin are associated with no more adverse effects."( The safety of high-dose insulin euglycaemia therapy in toxin-induced cardiac toxicity.
Isbister, GK; Page, CB; Ryan, NM, 2018
)
0.48
" Verapamil's inhibition of both permeability-glycoprotein (P-gp) and CYP3A4 is suspected to have led to the adverse side effects seen in our patient."( Verapamil as a culprit of palbociclib toxicity.
Gowarty, JL; Herrington, JD, 2019
)
2.87
" However, verapamil has fewer adverse drug reactions than TAC, which allows for a longer treatment period and the possibility that it might be effective for patients who cannot receive TAC."( The Safety and Efficacy of Intralesional Verapamil Versus Intralesional Triamcinolone Acetonide for Keloids and Hypertrophic Scars: A Systematic Review and Meta-analysis.
Fu, ZH; Guo, GH; Jiang, ZY; Liao, XC; Liu, MZ; Min, DH, 2020
)
1.23
"Paclitaxel-induced peripheral neuropathy (PIPN) is a common and dose-limiting adverse event."( P-Glycoprotein Inhibition Exacerbates Paclitaxel Neurotoxicity in Neurons and Patients With Cancer.
Hammer, HS; Khalaf, S; Kroetz, DL; Mortensen, C; Nielsen, F; Poetz, O; Rodriguez-Antona, C; Stage, TB; Steffensen, V; Svenningsen, ÅF; Xiong, C, 2020
)
0.56
" Although triamcinolone acetonide (TAC) is one of the most common and effective treatments for keloids and hypertrophic scars, TAC is not effective in some patients, and some may even experience adverse outcomes."( Efficacy and safety of verapamil vs triamcinolone acetonide for keloids and hypertrophic scars: A systematic review and meta-analysis.
Deng, Z; Liu, L; Liu, R; Yang, B; Zhao, X, 2020
)
0.87
"5 mM did not have any adverse effects on the expression of tyrosine hydroxylase in the noradrenergic neurons of the arch-associated cluster (AAC) located near the heart."( N-acetylcysteine prevents verapamil-induced cardiotoxicity with no effect on the noradrenergic arch-associated neurons in zebrafish.
Gu, Q; Kanungo, J; Robinson, B; Rodgers, J, 2020
)
0.86
" Two serious adverse events occurred, both in the placebo group (inguinal hernia and severe deterioration of cluster headache)."( Safety and efficacy of prednisone versus placebo in short-term prevention of episodic cluster headache: a multicentre, double-blind, randomised controlled trial.
Böger, A; Diener, HC; Freilinger, T; Gaul, C; Holle, D; Jansen, JP; Jürgens, TP; Katsarava, Z; Kaube, H; Kleinschnitz, C; Kraya, T; Nägel, S; Obermann, M; Ose, C; Scherag, A; Sonuc, N; Storch, P; Straube, A, 2021
)
0.62
" RCTs that evaluated treatment effects with the Vancouver Scar Scale or reported adverse effects were included."( Comparing the Efficacy and Safety of Intralesional Verapamil With Intralesional Triamcinolone Acetonide in Treatment of Hypertrophic Scars and Keloids: A Meta-Analysis of Randomized Controlled Trials.
Bi, H; Gu, L; Qin, Z; Wang, P; Wang, Q, 2021
)
0.87
" Although total adverse effects (RR = 0."( Comparing the Efficacy and Safety of Intralesional Verapamil With Intralesional Triamcinolone Acetonide in Treatment of Hypertrophic Scars and Keloids: A Meta-Analysis of Randomized Controlled Trials.
Bi, H; Gu, L; Qin, Z; Wang, P; Wang, Q, 2021
)
0.87
" Although total adverse effects did not change, the incidence of telangiectasia and skin atrophy was lower with verapamil than with TAC."( Comparing the Efficacy and Safety of Intralesional Verapamil With Intralesional Triamcinolone Acetonide in Treatment of Hypertrophic Scars and Keloids: A Meta-Analysis of Randomized Controlled Trials.
Bi, H; Gu, L; Qin, Z; Wang, P; Wang, Q, 2021
)
1.08
" Although total adverse effects did not change, the incidence of telangiectasia and skin atrophy was lower with verapamil than with TAC."( Comparing the Efficacy and Safety of Intralesional Verapamil With Intralesional Triamcinolone Acetonide in Treatment of Hypertrophic Scars and Keloids: A Meta-Analysis of Randomized Controlled Trials.
Bi, H; Gu, L; Qin, Z; Wang, P; Wang, Q, 2021
)
1.08
" This preclinical study supports verapamil as a safe adjuvant that may complement thrombolytic therapy by inhibiting TXNIP's detrimental role in hyperglycemic stroke."( Verapamil as an Adjunct Therapy to Reduce tPA Toxicity in Hyperglycemic Stroke: Implication of TXNIP/NLRP3 Inflammasome.
Ahmed, HA; Ishrat, T; Ismael, S; Mirzahosseini, G; Nasoohi, S; Yoo, A, 2021
)
2.35
" Verapamil had fewer adverse events than TAC and can be used as a safer alternative for the treatment of keloids and hypertrophic scars."( Efficacy and Safety of Verapamil Versus Triamcinolone Acetonide in Treating Keloids and Hypertrophic Scars: A Systematic Review and Meta-Analysis.
Li, X; Zhang, W, 2023
)
2.13

Pharmacokinetics

Diabetes mellitus revealed a tissue-specific effect on CYP3A activity and expression. Low bioavailability (20%), predominant elimination by metabolism (greater than 95%) and a relatively short half-life (t1/2, beta is 3-5 h)

ExcerptReferenceRelevance
" Thereupon, pharmacokinetic parameters were calculated using a two-compartment open model."( Pharmacokinetics of verapamil in man.
Koike, Y; Saito, H; Shimamura, K; Shudo, I, 1979
)
0.58
" Since an isolated, well-known drug effect was studied over a long period of time, it was felt that this was an acceptable method for reaching valid pharmacodynamic conclusions."( The pharmacodynamics of orally taken verapamil and verapamil retard as judged by their negative dromotropic effects.
Schlepper, M; Schwarz, F; Thormann, J, 1975
)
0.53
" Comparable trough verapamil concentrations (Cmin) were observed with verapamil IR (98 micrograms/L) and SR (81 micrograms/L); morning Cmin verapamil concentrations were higher than daytime Cmin values."( Comparative efficacy, safety and pharmacokinetics of verapamil SR vs verapamil IR in hypertensive patients.
Cubeddu, LX; Faggin, BM; Fuenmayor, NT, 1992
)
0.86
" The time to peak concentration was longer (7."( Impact of food on the pharmacokinetics and electrocardiographic effects of sustained release verapamil in normal subjects.
Bauman, JL; Beckman, KJ; Hariman, RJ; Hoon, TJ; McCollam, PL, 1992
)
0.5
" The changes in the volumes of distribution of propranolol and verapamil during exercise may contribute to preventing an increase in the half-life of these drugs in patients performing prolonged physical exercise."( Exercise and the pharmacokinetics of propranolol, verapamil and atenolol.
Mooij, JM; Schiffers, PM; van Baak, MA, 1992
)
0.78
" This concept may also apply to other drugs that have circadian effects in their pharmacokinetic profiles."( Influence of time of administration on verapamil pharmacokinetics.
Henry, JA; Hla, KK; Latham, AN, 1992
)
0.55
"We present an approach to the analysis of pharmacodynamic (PD) data arising from non-steady-state experiments, meant to be used when only PD data, not pharmacokinetic (PK) data, are available."( Semiparametric analysis of non-steady-state pharmacodynamic data.
Sheiner, LB; Verotta, D, 1991
)
0.28
" In both the single dose and steady state phases a linear relationship was observed between increasing dose and pharmacokinetic response over the dose range of 120 mg and 360 mg."( Dose proportionality of pharmacokinetics with a cr-verapamil formulation.
Devane, J; Martin, M; Mulligan, S, 1991
)
0.53
"Stereoselectivity in pharmacokinetics may be characterized by a measurable difference between enantiomers in a pharmacokinetic parameter."( Stereoselectivity in pharmacokinetics: a general theory.
Boddy, AV; Levy, RH, 1991
)
0.28
" These results show that lignocaine displaces verapamil in-vitro and in-vivo from its plasma protein binding sites, but the ensuing pharmacokinetic changes do not lead to significant changes in free verapamil concentrations."( Influence of lignocaine on plasma protein binding and pharmacokinetics of verapamil in dogs.
Belpaire, FM; Bogaert, MG; Bourda, A; De Rick, A; De Smet, F; Rosseel, MT, 1990
)
0.77
" Potential pharmacodynamic and pharmacokinetic interactions between verapamil and propranolol were evaluated in two double-blind, randomised, balanced, crossover studies employing the same six healthy males."( Evaluation of potential pharmacodynamic and pharmacokinetic interactions between verapamil and propranolol in normal subjects.
Brodie, MJ; McInnes, GT; Murdoch, DL; Murray, GD; Thompson, GG; Thomson, GD, 1991
)
0.74
" No differences were observed in the pharmacokinetic properties of the compounds."( The pharmacokinetics and pharmacodynamics of d- and dl-verapamil in rabbits.
Giacomini, JC; Giacomini, KM; Nelson, WL; Rood, D; Theodore, L; Wong, FM,
)
0.38
" Verapamil plasma concentrations were determined and pharmacokinetic parameters derived."( Verapamil pharmacodynamics and disposition in obese hypertensive patients.
Abernethy, DR; Schwartz, JB, 1988
)
2.63
"Ten healthy male volunteers, aged 18-37 years, entered a balanced crossover comparison of the pharmacokinetic profiles of (a) one 240 mg verapamil HCl sustained-release tablet (Isoptin SR 240, Securon SR) (1 X 240 mg) and (b) either: two half 240-mg verapamil HCl sustained-release tablets (2 X half 240-mg tablets, Study 1) or two 120-mg verapamil HCl sustained-release tablets (Isoptin SR 120) (2 X 120 mg, Study 2)."( Sustained-release verapamil: multiple-dose pharmacokinetic comparison of 120-mg and 240-mg tablets and the effect of halving a 240-mg tablet.
Durnin, C; McEwen, J; McMurdo, ME; Moreland, TA, 1989
)
0.81
" During the evening dosage schedule a significantly greater bioavailability (AUC) and a prolonged time to peak concentration was found."( Circadian variation in the pharmacokinetics of verapamil.
Frederiksen, M; Hansen, JF; Jespersen, CM; Klitgaard, NA; Sørum, C, 1989
)
0.53
" Pharmacokinetic studies showed that VRP markedly increased the uptake and retention of VCR in small intestine, liver and kidney of mice."( Modulation by verapamil of vincristine pharmacokinetics and toxicity in mice bearing human tumor xenografts.
Horowitz, ME; Horton, JK; Houghton, JA; Houghton, PJ; Thimmaiah, KN, 1989
)
0.64
"1) increase in peripheral volume of distribution contributed to prolonged elimination half-life (23."( The comparative effects of verapamil and a new dihydropyridine calcium channel blocker on digoxin pharmacokinetics.
Hoch, K; Johnson, BF; Johnson, J; Marwaha, R; Wilson, J, 1987
)
0.57
" The potential for a pharmacokinetic interaction between the two drugs has therefore been investigated in five patients with small cell lung cancer treated with combination chemotherapy comprising adriamycin, VP16, vincristine and cyclophosphamide."( The effect of verapamil on the pharmacokinetics of adriamycin.
Brodie, MJ; Cummings, J; Graham, J; Kaye, SB; Kerr, DJ; Morrison, JG; Thompson, GG, 1986
)
0.63
"A double blind, double dummy, randomized cross-over pharmacokinetic study comparing verapamil 120 mg, conventional tablets administered twice daily and verapamil 240 mg sustained release tablets once daily was performed in 12 patients with essential hypertension."( Pharmacokinetics of verapamil and norverapamil in patients with hypertension: a comparison of oral conventional and sustained release formulations.
Jørgensen, NP; Walstad, RA, 1988
)
0.82
" On day 10, the difference in Cmax between formulations was significant."( Pharmacokinetics and pharmacodynamics of two formulations of verapamil.
Henry, JA; Hla, KK; Latham, AN, 1987
)
0.51
"There is increasing interest in defining the pharmacodynamic and pharmacokinetic characteristics of drugs that are marketed as racemic mixtures."( The pharmacodynamic and pharmacokinetic differences of the D- and L-isomers of verapamil: implications in the treatment of paroxysmal supraventricular tachycardia.
Bauman, JL; Gallestegui, J; Hariman, RJ; Hoon, TJ; Rodvold, KA, 1986
)
0.5
" During recent years their pharmacokinetic properties and metabolism have been studied in more detail."( Clinical pharmacokinetics of verapamil, nifedipine and diltiazem.
Echizen, H; Eichelbaum, M,
)
0.42
" Elimination half-life of verapamil was similar among plasma and tissues evaluated (1."( Physiological pharmacokinetics and pharmacodynamics of (+/-)-verapamil in female rats.
Abernethy, DR; Todd, EL,
)
0.67
" Similarly, elimination half-life determined in 4 volunteers once in presence and once in absence of Q was prolonged by 34."( Effects of quinidine, verapamil and nifedipine on the pharmacokinetics and pharmacodynamics of digitoxin during steady state conditions.
Kuhlmann, J, 1987
)
0.59
" This pharmacokinetic interaction was not the result of a lidocaine-induced decrease in the fraction of verapamil bound to plasma protein because in vitro lidocaine failed to displace verapamil from its protein binding site."( Pharmacodynamic and pharmacokinetic interactions between lidocaine and verapamil.
Abernethy, DR; Chelly, JE; Dlewati, A; Doursout, MF; Hill, DC; Merin, RG, 1987
)
0.72
" Elimination half-life was prolonged in the elderly (7."( Verapamil pharmacodynamics and disposition in young and elderly hypertensive patients. Altered electrocardiographic and hypotensive responses.
Abernethy, DR; Luchi, R; Schwartz, JB; Snow, E; Todd, EL, 1986
)
1.71
"01) by verapamil (80 mg three times daily for 2 days prior to antipyrine administration and 2 days following) while half-life was increased from 13."( The effect of verapamil on antipyrine pharmacokinetics and metabolism in man.
Bach, D; Blevins, R; Edwards, DJ; Kerner, N; Rubenfire, M, 1986
)
1.09
" In practice the important pharmacokinetic properties of verapamil are low bioavailability (20%), predominant elimination by metabolism (greater than 95%) and a relatively short half-life (t1/2, beta is 3-5 h)."( Pharmacokinetics of conventional and slow-release verapamil.
Bühler, F; Follath, F; Ha, HR; Schütz, E, 1986
)
0.77
" The half-life of quinidine was also significantly prolonged by verapamil."( The effect of coadministration of verapamil on the pharmacokinetics and metabolism of quinidine.
Beckman, H; Blevins, R; Edwards, DJ; Lavoie, R; Rubenfire, M, 1987
)
0.79
"Effective use of drugs in therapy depends not only on clinical acumen but also on the availability of relevant pharmacokinetic and pharmacodynamic data."( Pharmacokinetics of calcium-entry blockers.
Blouin, RA; Hamann, SR; McAllister, RG, 1985
)
0.27
" Using well-established pharmacokinetic models, a theoretic basis for these observations is presented."( Verapamil pharmacodynamics after intravenous and oral dosing: theoretic consideration.
Brazzell, RK; Colburn, WA; Holazo, AA, 1986
)
1.71
" injection, the terminal phase half-life and total plasma clearance of verapamil in both groups were similar."( Pharmacokinetics of verapamil in patients with renal failure.
Mooy, J; Muytjens, A; Rahn, KH; Schols, M; v Baak, M; v Hooff, M, 1985
)
0.83
" Therefore, even though there is little variation in the pharmacokinetic parameters between adult dogs and puppies, there is a marked reduction in the sensitivity of the puppies to the ECG effects of verapamil."( Age-related changes in the pharmacodynamics of verapamil.
Arnold, TH; Tackett, RL; Vallner, JJ, 1985
)
0.71
" Absorption from the nasal cavity appeared instantaneous compared to an absorption half-life of 50 +/- 6 min after oral administration."( Pharmacodynamics of acute intranasal administration of verapamil: comparison with i.v. and oral administration.
Arnold, TH; Tackett, RL; Vallner, JJ,
)
0.38
" The study reported here was designed to show whether the pharmacokinetics of verapamil are influenced by concurrent treatment with three different beta-adrenoceptor blockers, and whether there is any pharmacodynamic interaction between these drugs."( Pharmacokinetics and pharmacodynamics of verapamil in combination with atenolol, metoprolol and propranolol.
Fitzsimons, TJ; Holt, D; Johnston, A; Warrington, SJ, 1984
)
0.76
" Pharmacodynamic studies correlate drug dose and plasma concentration with observed effects (whether therapeutic or toxic) and aid in the establishment of appropriate dose ranges for desired drug activity."( Clinical pharmacokinetics of calcium channel antagonists.
McAllister, RG, 1982
)
0.26
" Inhibition of pulmonary vasoconstriction was related to the amount of verapamil in a pool exhibiting mono-exponential efflux of drug with a half-life of 12."( Pulmonary disposition and pharmacodynamics of verapamil.
Blanford, SL; Felder, TB; Gillespie, MN; Kostenbauder, HB; Reinsel, CN,
)
0.62
" Unlike other calcium antagonists, detailed pharmacokinetic data are available for verapamil."( Clinical pharmacokinetics of verapamil.
Blouin, RA; Hamann, SR; McAllister, RG,
)
0.65
" Application of the method is demonstrated by a pharmacokinetic study in a normal volunteer who received 10 mg verapamil hydrochloride by intravenous infusion."( Verapamil and norverapamil determination in human plasma by gas-liquid chromatography using nitrogen-phosphorus detection: application to single-dose pharmacokinetic studies.
Abernethy, DR; Mitchell, JR; Todd, EL, 1984
)
1.92
" Pharmacokinetic parameters obtained after oral administration were not significantly different from those after intravenous dosing."( Pharmacokinetics of calcium blockers in patients with renal insufficiency and in geriatric patients.
Larsen, A; Midtbø, K; Saevareid, L; Storstein, L, 1984
)
0.27
"001) and increased the plasma half-life of the drug from 33."( Influence of verapamil on the inotropism and pharmacokinetics of digoxin.
Christiansen, BD; Klitgaard, NA; Nielsen-Kudsk, F; Pedersen, KE; Thayssen, P, 1983
)
0.64
" Pronounced differences of the various pharmacokinetic parameters were observed between the (-)- and (+)-isomers."( Pharmacokinetics of (+)-, (-)- and (+/-)-verapamil after intravenous administration.
Eichelbaum, M; Mikus, G; Vogelgesang, B, 1984
)
0.53
" From the pharmacokinetic variables determined, we designed an intravenous regimen to maintain a plasma verapamil concentration of 150 ng/ml consisting of (1) a loading bolus (10 mg over 2 minutes), followed by (2) a rapid loading infusion (0."( Pharmacokinetics of verapamil: experience with a sustained intravenous infusion regimen.
Aanonsen, LM; McCarthy, E; Pritchett, EL; Reiter, MJ; Shand, DG; Wagoner, R, 1982
)
0.8
"The pharmacokinetic parameters and oral bioavailability of the antiarrhythmic drug verapamil were determined in six patients with atrial fibrillation."( Clinical pharmacokinetics of verapamil in patients with atrial fibrillation.
Anderson, P; BondessoN, U; Sylvén, C, 1982
)
0.78
"025) and the terminal half-life was prolonged four fold (3."( Pharmacokinetics, bioavailability and ECG response of verapamil in patients with liver cirrhosis.
Albrecht, M; Eichelbaum, M; Kliems, G; Schäfer, K; Somogyi, A, 1981
)
0.51
"To study the effect of the multidrug-resistance reversal agent R-verapamil on the pharmacokinetic behavior of paclitaxel."( Effect of R-verapamil on the pharmacokinetics of paclitaxel in women with breast cancer.
Balis, FM; Berg, SL; Cowan, KH; Denicoff, AM; Noone, M; O'Shaughnessy, JA; Ognibene, FP; Tolcher, A, 1995
)
0.91
" With the immediate-release formulation the total verapamil Cmax was higher than that observed with the sustained-release formulation, and the percentage of the pharmacologically more active S-verapamil in the total was also higher (lower R/S ratio)."( Verapamil stereoisomerism: enantiomeric ratios in plasma dependent on peak concentrations, oral input rate, or both.
Karim, A; Piergies, A, 1995
)
1.99
" When simultaneously administered with vinblastine to P388/ADR-bearing mice, NA-382 maintained significantly higher vinblastine levels in the tumour cells for 24 h and gave a larger area under the time-intracellular vinblastine concentration curve (0 to 24 h) than those receiving vinblastine alone, with long retention of the agent in ascitic fluid."( Antitumour effects and pharmacokinetics of combination of vinblastine with a staurosporine derivative, NA-382, in P388/ADR-bearing mice.
Koga, K; Miyamoto, K; Ohshima, T; Takeda, K; Wakusawa, S, 1995
)
0.29
" A decision was made to examine the pharmacokinetic parameters, independent of compartmental analysis of verapamil and its active metabolite norverapamil, in patients with portal hypertension."( Pharmacokinetic parameters of verapamil and its active metabolite norverapamil in patients with hepatopathy.
Brátová, M; Fendrich, Z; Hůlek, P; Macek, K; Vlcek, J, 1995
)
0.79
"alpha-Blockers and calcium antagonists are commonly used in the treatment of hypertension, but few data are available concerning first dose or steady state (SS) hemodynamic and pharmacokinetic effects of these drugs when they are used in combination therapy."( Combined terazosin and verapamil therapy in essential hypertension. Hemodynamic and pharmacokinetic interactions.
Johnston, W; Laddu, AR; Lenz, ML; Pool, JL; Taylor, AA; Varghese, A, 1995
)
0.6
" P-gp has been detected in vivo and in vitro in numerous tumor cell types but also in normal tissues and particularly in organs involved in the pharmacokinetic behaviour of xenobiotics."( P-glycoprotein and pharmacokinetics.
Jehl, F; Levêque, D,
)
0.13
" Therefore, the purpose of this study was to evaluate the effect of immediate-release (IR) and sustained-release (SR) verapamil on the pharmacokinetic parameters of propranolol in 12 healthy men."( Evaluation of dosage-release formulations on inhibition of drug clearance: effect of sustained- and immediate-release verapamil on propranolol pharmacokinetic parameters.
Bleske, BE; Edwards, DJ; Rodman, DP; Shea, MJ; Touchette, MA; Welage, LS, 1994
)
0.71
"The potential for a pharmacokinetic interaction between epirubicin and the second-generation multidrug resistance modulating agent D-verapamil (DVPM) has been investigated in six patients with advanced colorectal cancer."( Pharmacokinetic interaction between epirubicin and the multidrug resistance reverting agent D-verapamil.
Czejka, M; Scheithauer, W; Schenk, T, 1993
)
0.71
" We studied the pharmacokinetics and metabolism of both epirubicin (EPI) and verapamil (VPL) to explore the possible pharmacokinetic interactions between these two drugs."( Effects of verapamil on the pharmacokinetics and metabolism of epirubicin.
Hamm, K; Hossfeld, DK; Mross, K, 1993
)
0.9
"001) for all pharmacodynamic variables measured."( Aging effects on stereoselective pharmacokinetics and pharmacodynamics of verapamil.
Capili, H; Liu, S; Schwartz, JB; Troconiz, IF; Verotta, D, 1993
)
0.52
" Median tmax values for young and elderly subjects were not significantly different for any enantiomer."( Age and gender related changes in stereoselective pharmacokinetics and pharmacodynamics of verapamil and norverapamil.
Atkinson, L; Gupta, SK; Longstreth, JA; Tu, T, 1995
)
0.51
"A Monte Carlo simulation study was done to investigate the effects of high intrasubject variation in clearance (CL), and volume of distribution (V) on the calculation of the 90% confidence interval (CI) for Cmax for single dose and multiple dose studies."( Evaluation of bioequivalence of highly variable drugs using Monte Carlo simulations. I. Estimation of rate of absorption for single and multiple dose trials using Cmax.
el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1995
)
0.29
"Previous reviews and simulations have shown that the probability of failure for the Cmax for single dose studies was always greater than that for multiple dose studies."( Evaluation of bioequivalence of highly variable drugs using Monte Carlo simulations. I. Estimation of rate of absorption for single and multiple dose trials using Cmax.
el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1995
)
0.29
" Stereospecific assay revealed that: (1) stereoselective R- and S-enantiomer disposition occurred regardless of formulation administered; (2) a trend of R:S concentration ratios of verapamil differed between the two formulations; and (3) fluctuations between Cmax and Cmin values of the two formulations were statistically different over respective dosing intervals (greater fluctuation after CR administration)."( Pharmacokinetics of verapamil and norverapamil enantiomers after administration of immediate and controlled-release formulations to humans:evidence suggesting input-rate determined stereoselectivity.
Bhatti, MM; Foster, RT; Lewanczuk, RZ; Pasutto, FM, 1995
)
0.81
"For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability."( High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.
Gordon, P; Hems, J; Pop, R; Spino, M; Tsang, YC, 1996
)
0.51
" The Cmax varied > 9 fold (30-278 ng/mL) among subjects."( High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.
Gordon, P; Hems, J; Pop, R; Spino, M; Tsang, YC, 1996
)
0.51
"2 mg/kg) pharmacokinetic parameters was studied in rabbits."( The influence of selected general anesthetics on pharmacokinetic parameters of some antiarrhythmic drugs in rabbits. Part V. Verapamil.
Orszulak-Michalak, D,
)
0.34
"The pharmacokinetic actions, bioequivalence, and cardiovascular effects of two verapamil products were studied in a randomized, double-blind, crossover study in eight elderly hypertensive patients (median age, 69."( Postabsorption concentration peaks with brand-name and generic verapamil: a double-blind, crossover study in elderly hypertensive patients.
Barnette, DJ; Bauman, JL; Carter, BL; Porter, JA; Saseen, JJ; Zajac, EJ, 1997
)
0.76
" The published pharmacokinetic data for verapamil enantiomers in the rat model are limited."( Pharmacokinetics of the enantiomers of verapamil after intravenous and oral administration of racemic verapamil in a rat model.
Bhatti, MM; Foster, RT, 1997
)
0.83
"A new method and experimental design are presented to unambiguously estimate the transduction function (phi) and the conduction function (psi) of the generalized pharmacodynamic model: E = phi (psi * r), when measured pharmacokinetic response r is (i) drug plasma concentration and (ii) drug input rate into the systemic circulation."( New mathematical implementation of generalized pharmacodynamic models: method and clinical evaluation.
Gillespie, WR; Liu, Y; Shepherd, AM; Stagni, G, 1997
)
0.3
" Mean half-life for the elimination from the aqueous humor was 33 min."( Ocular pharmacokinetics of verapamil in rabbits.
Daxer, A; Dietrich, H; Eichelbaum, M; Ettl, A; Hofmann, U; Schmid, E, 1998
)
0.6
" The elimination half-life of buspirone was not changed by verapamil and diltiazem."( Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of buspirone.
Kivistö, KT; Lamberg, TS; Neuvonen, PJ, 1998
)
0.93
"Prospective clinical and pharmacokinetic study."( Pharmacokinetic and pharmacodynamic effects of high-dose continuous intravenous verapamil infusion: clinical experience in the intensive care unit.
Boiocchi, M; De Cicco, M; Fabiani, F; Fantin, D; Fracasso, A; Lestuzzi, C; Macor, F; Matovic, M; Nicolosi, G; Robieux, I; Santantonio, C; Toffoli, G; Zanette, G, 1999
)
0.53
"The methodology of predicting the pharmacokinetic parameters (AUC, cmax, tmax) and the assessment of their variability in bioequivalence studies has been developed with the use of artificial neural networks."( Prediction of pharmacokinetic parameters and the assessment of their variability in bioequivalence studies by artificial neural networks.
Cvelbar, P; Opara, J; Primozic, S, 1999
)
0.3
" Models for pharmacokinetic parameter prediction were also used for the assessment of their variability and for detecting the most influential variables for selected pharmacokinetic parameters."( Prediction of pharmacokinetic parameters and the assessment of their variability in bioequivalence studies by artificial neural networks.
Cvelbar, P; Opara, J; Primozic, S, 1999
)
0.3
"The average absolute prediction errors of the neural networks for AUC, cmax, and tmax prediction were: 30."( Prediction of pharmacokinetic parameters and the assessment of their variability in bioequivalence studies by artificial neural networks.
Cvelbar, P; Opara, J; Primozic, S, 1999
)
0.3
" Pharmacokinetic evaluations were performed by means of a two-compartment open model with zero-order absorption and first-order elimination using the WinNonlin pharmacokinetic software package."( Multidrug resistance modulation in vivo: the effect of cyclosporin A alone or with dexverapamil on idarubicin pharmacokinetics in acute leukemia.
Baccarani, M; Baraldo, M; Damiani, D; Ermacora, A; Fanin, R; Furlanut, M; Michieli, M; Pea, F; Russo, D, 1999
)
0.53
" The main pharmacokinetic parameters of IDA, such as CL and volume of distribution at steady state (Vdss), were remarkably affected by the coadministration of CyA or CyA plus D-Ver, but no statistically significant difference was noted because of IDA pharmacokinetic interpatient variation."( Multidrug resistance modulation in vivo: the effect of cyclosporin A alone or with dexverapamil on idarubicin pharmacokinetics in acute leukemia.
Baccarani, M; Baraldo, M; Damiani, D; Ermacora, A; Fanin, R; Furlanut, M; Michieli, M; Pea, F; Russo, D, 1999
)
0.53
"The results show that CyA alone at a dose of 10 mg x kg(-1) daily significantly increased systemic body exposure to both IDA and IDAOL in acute leukemia, and suggest that these pharmacokinetic effects were at least partially decreased when D-Ver was coadministered with CyA."( Multidrug resistance modulation in vivo: the effect of cyclosporin A alone or with dexverapamil on idarubicin pharmacokinetics in acute leukemia.
Baccarani, M; Baraldo, M; Damiani, D; Ermacora, A; Fanin, R; Furlanut, M; Michieli, M; Pea, F; Russo, D, 1999
)
0.53
" When the pharmacokinetic variables were compared between the pregnant and non-pregnant rabbit, it was observed that t(1/2)lambda2 V1 and V(D) were significantly higher in the non-pregnant than in the pregnant rabbit."( Comparison of the pharmacokinetics of verapamil in the pregnant and non-pregnant rabbit: study of maternal and foetal tissue levels.
Aramayona, JJ; Bregante, MA; Fraile, LJ; Garcia, MA; Solans, C, 2000
)
0.58
" The findings suggest that sex-specific differences in drug metabolism may occur in both the gut and the liver and involve multiple metabolic pathways and that pharmacokinetic differences will alter pharmacodynamic responses."( Gender-specific effects on verapamil pharmacokinetics and pharmacodynamics in humans.
Barnas, CR; Jones, MP; Krecic-Shepard, ME; Schwartz, JB; Slimko, J, 2000
)
0.6
" Statistical comparisons of pharmacokinetic parameters and vital sign data were made by ANOVA."( Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2000
)
0.58
"Mean almotriptan peak concentration and area under the plasma concentration-time curve were significantly higher and volume of distribution and oral clearance were significantly lower after coadministration of almotriptan and verapamil compared with administration of almotriptan alone."( Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2000
)
0.77
"In recent years, there has been an increased understanding of P-glycoprotein (P-GP)-mediated pharmacokinetic interactions."( Multidrug resistance (MDR) in cancer. Mechanisms, reversal using modulators of MDR and the role of MDR modulators in influencing the pharmacokinetics of anticancer drugs.
Krishna, R; Mayer, LD, 2000
)
0.31
" Other pharmacokinetic parameters, such as volume of distribution and plasma protein binding did not show any statistical differences."( Pharmacokinetics of verapamil in New Zealand white rabbits during ontogeny.
Aramayona, JJ; Bregante, MA; Fraile, LJ; Garcia, MA; Solans, C, 2000
)
0.63
" In conclusion, it was demonstrated that DEX pretreatment affects not only P-gp-mediated disposition of Rho123 but also pharmacokinetic interactions of P-gp/CYP3A-related compounds with Rho123, probably because concentrations of substrates/inhibitors at target sites such as the intestine and liver are varied."( Pharmacokinetic interaction of cytochrome P450 3A-related compounds with rhodamine 123, a P-glycoprotein substrate, in rats pretreated with dexamethasone.
Murakami, T; Nagai, J; Nasu, R; Sanemasa, M; Takano, M; Yumoto, R, 2001
)
0.31
" Elimination half-life and renal clearance of both S- and R-verapamil were not affected."( Effect of grapefruit juice on pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers.
Ghose, K; Ho, PC; Saville, D; Wanwimolruk, S, 2000
)
0.78
" The pharmacokinetic profile of verapamil in lactating rabbits following endovenous administration is described in the form of a two-compartment model."( Pharmacokinetics of verapamil in lactating rabbits. Prediction of verapamil distribution into rabbit milk.
Aramayona, JJ; Bregante, MA; Fraile, LJ; Garcia, MA; Rueda, S; Solans, C, 2000
)
0.91
"We have estimated the pharmacokinetic and pharmacodynamic interactions of verapamil (VP) enantiomers and also the interaction between VP and its metabolite, norverapamil (NVP)."( Stereoselective pharmacokinetics and pharmacodynamics of verapamil and norverapamil in rabbits.
Hanada, K; Hashiguchi, M; Mori, T; Mori, Y; Ogata, H; Tsukahara, Y, 2001
)
0.79
" A population pharmacokinetic model involving zero-order release of verapamil into the gastrointestinal tract with first-order absorption and elimination was used to describe the steady-state plasma concentration profile for R- and S-verapamil."( Pharmacokinetics of controlled-release verapamil in healthy volunteers and patients with hypertension or angina.
Aarons, L; Gupta, S; Ho Pl, PL; Modi, NB; Sathyan, G, 2002
)
0.82
"The results from this dose-ranging pharmacokinetic investigation in healthy volunteers and patients are consistent with previous reports in healthy subjects."( Pharmacokinetics of controlled-release verapamil in healthy volunteers and patients with hypertension or angina.
Aarons, L; Gupta, S; Ho Pl, PL; Modi, NB; Sathyan, G, 2002
)
0.58
" The pharmacokinetic profiles revealed that verapamil treated group had higher doxorubicin peak plasma and tissue levels and AUCs."( Toxicologic and pharmacokinetic study of low doses of verapamil combined with doxorubicin.
Bartoli, F; Candussio, L; Crivellato, E; Decorti, G; Giraldi, T; Granzotto, M; Rosati, A, 2002
)
0.82
" Using the common calcium antagonist Verapamil, it is shown that these two methods allow rapid identification of phase I and phase II metabolites from biological samples and are suitable for pharmacokinetic and pharmacodynamic studies of pharmaceuticals in biological matrices."( Application of restricted access material (RAM) with precolumn-switching and matrix solid-phase dispersion (MSPD) to the study of the metabolism and pharmacokinetics of Verapamil.
Borlak, J; Levsen, K; Walles, M, 2002
)
0.78
" The aim of the study was to investigate the influence of midazolam on the plasma concentrations and pharmacokinetic parameters of verapamil after intravenous bolus administration in rabbits during 2 h of observation."( Influence of midazolam on pharmacokinetics of verapamil in rabbits.
Orszulak-Michalak, D; Owczarek, J; Wiktorowska-Owczarek, AK,
)
0.59
"The differences in pharmacokinetic behavior and tissue distribution of verapamil and its enantiomers were investigated in rats."( Pharmacokinetic behavior and tissue distribution of verapamil and its enantiomers in rats by HPLC.
He, L; Wang, S, 2003
)
0.8
" The aim of the current work was to evaluate the effect of verapamil, a P-GP substrate, on the pharmacokinetic behaviour of the anthelmintics ivermectin and moxidectin in sheep."( Influence of verapamil on the pharmacokinetics of the antiparasitic drugs ivermectin and moxidectin in sheep.
Lanusse, C; Lifschitz, A; Molento, MB; Prichard, R; Sallovitz, J, 2004
)
0.94
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
"The present study was designed to investigate the pharmacokinetic interaction of morphine with three classes of L-type calcium channel blockers (CCB) and its relationship to morphine-induced mechanical antinociception in mice."( Role of pharmacokinetic effects in the potentiation of morphine analgesia by L-type calcium channel blockers in mice.
Fukazawa, Y; Kishioka, S; Maeda, T; Ozaki, M; Shimizu, N; Yamamoto, C; Yamamoto, H, 2004
)
0.32
"To use a nonparametric approach involving longitudinal splines to model the baseline blood pressure profile and investigate the impact of this modelling on the pharmacodynamic analysis for verapamil in patients with angina or hypertension."( Pharmacodynamics of controlled release verapamil in patients with hypertension: an analysis using spline functions.
Aarons, L; Baxter, C; Gupta, S, 2004
)
0.78
" Pharmacodynamic data were created by subtracting the (systolic) blood pressure following active drug from the placebo response, either by direct subtraction or after modelling the baseline with a longitudinal spline model fitted to the placebo data by nonlinear mixed effects modelling."( Pharmacodynamics of controlled release verapamil in patients with hypertension: an analysis using spline functions.
Aarons, L; Baxter, C; Gupta, S, 2004
)
0.59
" However, the use of a population spline model only allowed a linear pharmacodynamic model to be fitted to the resulting data."( Pharmacodynamics of controlled release verapamil in patients with hypertension: an analysis using spline functions.
Aarons, L; Baxter, C; Gupta, S, 2004
)
0.59
"The chimpanzee (CHP) was evaluated as a pharmacokinetic model for humans (HUMs) using propranolol, verapamil, theophylline, and 12 proprietary compounds."( The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application.
Bai, SA; Christ, DD; Diamond, S; Grace, JE; Grossman, SJ; He, K; Qian, M; Wong, H; Wright, MR; Yeleswaram, K, 2004
)
0.54
" Studies compared the multiple-dose pharmacokinetic interaction profiles of pravastatin, simvastatin, and atorvastatin when coadministered with 4 inhibitors of cytochrome P450-3A4 isoenzymes in healthy subjects."( Comparative pharmacokinetic interaction profiles of pravastatin, simvastatin, and atorvastatin when coadministered with cytochrome P450 inhibitors.
Jacobson, TA, 2004
)
0.32
" Pharmacokinetic parameters of verapamil and norverapamil were determined after the oral administration of verapamil (10 mg kg(-1)) to rabbits in the presence and absence of quercetin (5."( The effect of quercetin on the pharmacokinetics of verapamil and its major metabolite, norverapamil, in rabbits.
Choi, JS; Han, HK, 2004
)
0.86
" No changes in any plasma pharmacokinetic parameters of fexofenadine were found during cimetidine treatment."( Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.
Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.58
"The objective of this study was to evaluate the suitability of the early phase of adjuvant arthritis (pre-AA) as a model of inflammation for pharmacokinetic studies."( Effect of early phase adjuvant arthritis on hepatic P450 enzymes and pharmacokinetics of verapamil: an alternative approach to the use of an animal model of inflammation for pharmacokinetic studies.
Jamali, F; Ling, S, 2005
)
0.55
" A series of compartmental pharmacokinetic models was developed and fit to concentration vs."( Pharmacokinetics of substrate uptake and distribution in murine brain after nasal instillation.
Graff, CL; Pollack, GM; Zhao, R, 2005
)
0.33
" A catenary pharmacokinetic model with slice-specific brain-to-blood efflux rate constants and slice-to-slice diffusivity factors was capable of fitting the data."( Pharmacokinetics of substrate uptake and distribution in murine brain after nasal instillation.
Graff, CL; Pollack, GM; Zhao, R, 2005
)
0.33
" In conclusion, administration of verapamil by inhalation-abrogated extensive first pass metabolism frequently seen after oral application, and this may well be extended to the development of drugs with similar pharmacokinetic defects."( Metabolism of verapamil in cultures of rat alveolar epithelial cells and pharmacokinetics after administration by intravenous and inhalation routes.
Blickwede, M; Borlak, J; Hansen, T; Koch, W; Levsen, K; Walles, M, 2005
)
0.97
"The aim of this study was to investigate the pharmacokinetic changes of verapamil and its major metabolite, norverapamil, after oral administration of verapamil (10 mg/kg) in rabbits with slight, moderate and severe hepatic failure induced by carbon tetrachloride."( Pharmacokinetics of verapamil and its major metabolite, norverapamil from oral administration of verapamil in rabbits with hepatic failure induced by carbon tetrachloride.
Burm, JP; Choi, JS, 2005
)
0.88
"To formulate and evaluate a pharmacodynamic model that characterizes the effects of S-verapamil on the circadian 24-hour ambulatory blood pressure (ABP)."( A pharmacodynamic model of the effects of controlled-onset extended-release verapamil on 24-hour ambulatory blood pressure.
Beasley, BN; Johnson, JA; Lima, JJ; Parker, RB, 2005
)
0.78
" Blood samples were collected after the last dose for determination of the pharmacokinetic of S-verapamil."( A pharmacodynamic model of the effects of controlled-onset extended-release verapamil on 24-hour ambulatory blood pressure.
Beasley, BN; Johnson, JA; Lima, JJ; Parker, RB, 2005
)
0.78
" The AUC from 0 to 24 hours of 9-hydroxyrisperidone, but not other pharmacokinetic parameters, was significantly increased during verapamil treatment."( Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.
Kaneo, S; Nakagami, T; Saito, M; Tateishi, T; Yasui-Furukori, N, 2005
)
0.94
" However, success has been limited by pharmacokinetic interactions because of non-specific blockade of P-glycoprotein (P-gp) in normal tissues or inability to reach relevant concentrations clinically."( Pharmacokinetics of intravenously administered stealth liposomal doxorubicin modulated with verapamil in rats.
Chang, A; Goh, BC; Lee, HS; Liu, XY; Lu, WL; Wang, JC; Zhang, Q, 2006
)
0.55
" Everolimus half-life was only prolonged to a minor extent (32 +/- 6 vs."( Pharmacokinetic interaction between verapamil and everolimus in healthy subjects.
Allison, MJ; Beyer, D; Bizot, MN; Jiang, Q; Kovarik, JM; Schmouder, RL, 2005
)
0.6
" In an accompanying paper, we have presented a unique, generic, physiologically based pharmacokinetic model and described its application to the prediction of rat plasma pharmacokinetics from in vitro data alone."( Application of a generic physiologically based pharmacokinetic model to the estimation of xenobiotic levels in human plasma.
Brightman, FA; Leahy, DE; Searle, GE; Thomas, S, 2006
)
0.33
" The pharmacokinetic parameters (elimination half-life, area under the plasma concentration-time curve, peak plasma levels and the times to attain these plasma levels) of verapamil were evaluated in the rat."( Influence of famotidine on verapamil pharmacokinetics in rats.
Matar, KM,
)
0.62
"A pharmacokinetic interaction between erythromycin and ximelagatran, an oral direct thrombin inhibitor, was demonstrated in this study in healthy volunteers."( Influence of erythromycin on the pharmacokinetics of ximelagatran may involve inhibition of P-glycoprotein-mediated excretion.
Dorani, H; Eriksson, UG; Fritsch, H; Hoffmann, KJ; Karlsson, J; Olsson, L; Sarich, TC; Schützer, KM; Wall, U, 2006
)
0.33
" We studied the interaction between verapamil and erythromycin in the rat to see whether it occurs at the pharmacokinetics or pharmacodynamic level."( Erythromycin potentiates PR interval prolonging effect of verapamil in the rat: a pharmacodynamic drug interaction.
Dakhel, Y; Jamali, F, 2006
)
0.85
"The aims of this study were to assess the potential of CGRP8-37, the C-terminal fragment of calcitonin gene-related peptide (CGRP), to inhibit CGRP-induced vasodilation in the human forearm and to evaluate a pharmacodynamic model to aid the clinical development of novel CGRP-receptor antagonists."( Calcitonin gene-related peptide-induced vasodilation in the human forearm is antagonized by CGRP8-37: evaluation of a human in vivo pharmacodynamic model.
de Hoon, JN; Van der Schueren, BJ; Vanmolkot, FH, 2006
)
0.33
" Venous occlusion plethysmography combined with brachial artery administration of CGRP provides a suitable pharmacodynamic model to aid the clinical development of CGRP-receptor antagonists."( Calcitonin gene-related peptide-induced vasodilation in the human forearm is antagonized by CGRP8-37: evaluation of a human in vivo pharmacodynamic model.
de Hoon, JN; Van der Schueren, BJ; Vanmolkot, FH, 2006
)
0.33
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
"The pharmacokinetic parameters of rabeprazole were not altered by clarithromycin or verapamil irrespective of the CYP2C19 genotypes."( Effects of clarithromycin and verapamil on rabeprazole pharmacokinetics between CYP2C19 genotypes.
Shimizu, M; Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2006
)
0.85
"Besides minimum input parameters for the compound (pKa(s), solubility at one or more pH's, Peff, doses, formulation, diffusivity), physiological and pharmacokinetic properties, transporter data are included in these predictions."( In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.
Bolger, MB; Langguth, P; Spahn-Langguth, H; Tubic, M; Wagner, D, 2006
)
0.33
" Pharmacokinetic parameters (AUC, Cmax) from in silico simulations are within acceptable range comparing with data, observed in vivo."( In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.
Bolger, MB; Langguth, P; Spahn-Langguth, H; Tubic, M; Wagner, D, 2006
)
0.33
" The model developed may be useful in the prediction of absorption of other P-gp substrates including pharmacodynamic consequences."( In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.
Bolger, MB; Langguth, P; Spahn-Langguth, H; Tubic, M; Wagner, D, 2006
)
0.33
" Pharmacokinetic parameters were calculated by non-compartmental analysis for each subject."( The effect of gender on the pharmacokinetics of verapamil and norverapamil in human.
Dadashzadeh, S; Javadian, B; Sadeghian, S, 2006
)
0.59
" In addition, pharmacokinetic and brain distribution studies for 4'-Cl and 4',4''-diCl BZT in Sprague-Dawley rats were conducted."( Transport, metabolism, and in vivo population pharmacokinetics of the chloro benztropine analogs, a class of compounds extensively evaluated in animal models of drug abuse.
Eddington, ND; Newman, AH; Othman, AA; Syed, SA, 2007
)
0.34
" To compare the pharmacokinetic characteristics and bioavailability in six Beagle dogs after oral administration of VH-COERP and verapamil hydrochloride delayed-release pellets (VH-DRP) as reference."( [Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].
Chen, HX; Chen, XJ; Chen, ZP; Li, LR; Xiao, YY; Zhu, JB, 2006
)
0.88
" The concentration of VH in plasma of six dogs and its pharmacokinetic behaviors after oral administration of VH-COERP and VH-DRP at different times were studied by RP-HPLC."( [Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].
Chen, HX; Chen, XJ; Chen, ZP; Li, LR; Xiao, YY; Zhu, JB, 2006
)
0.68
" Compared with the VH-DRP, VH-COERP in vivo has an obviously lag time (4 h) , Tmax was also delayed (8 h) and the relative bioavailability was (94."( [Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].
Chen, HX; Chen, XJ; Chen, ZP; Li, LR; Xiao, YY; Zhu, JB, 2006
)
0.68
" Main pharmacokinetic parameters were calculated and compared by statistic analysis."( [The effect of tetramethylpyrazine on the pharmacokinetics of intragastrically administered cyclosporine A in rats].
He, J; Liu, XL; Peng, WX; Song, J; Tang, J; Xu, P, 2006
)
0.33
"In the group of water pretreated and co-administrated with CsA, no significantly different pharmacokinetic parameters of CsA were found."( [The effect of tetramethylpyrazine on the pharmacokinetics of intragastrically administered cyclosporine A in rats].
He, J; Liu, XL; Peng, WX; Song, J; Tang, J; Xu, P, 2006
)
0.33
"The aim of this study was to develop pharmacokinetic models for pentoxifylline (PTX) and the R(-)-enantiomer of the PTX metabolite 1, lisofylline (LSF), in order to identify some factors influencing the absorption of these compounds from the intestines and to clarify mechanisms involved in their non-linear pharmacokinetics."( Pharmacokinetic modelling of pentoxifylline and lisofylline after oral and intravenous administration in mice.
Obruśnik, A; Pekala, E; Szymura-Oleksiak, J; Wyska, E, 2007
)
0.34
" The pharmacokinetic parameters of verapamil were measured after an oral (9 mg/kg) or intravenous (3 mg/kg) administration of verapamil to rats in the presence and absence of atorvastatin."( Effect of atorvastatin on the intravenous and oral pharmacokinetics of verapamil in rats.
Chang, KS; Choi, DH; Choi, JS; Han, HK; Hong, SP, 2008
)
0.86
" The results showed that when verapamil was administered intravenously, the area under the curve (AUC), elimination half-life (T((1/2)(K10))) and mean residence time (MRT) increased significantly, whereas clearance (Cl) decreased, in rats with liver fibrosis compared with normal rats."( Effects of liver fibrosis on verapamil pharmacokinetics in rats.
Chen, M; Hu, XL; Wang, H; Xu, D, 2008
)
0.93
"The pharmacokinetic parameters of verapamil and one of its metabolites, norverapamil, were compared after oral administration of verapamil (60 mg) in the presence or absence of oral atorvastatin (40 mg) in 12 healthy volunteers."( Drug interaction between oral atorvastatin and verapamil in healthy subjects: effects of atorvastatin on the pharmacokinetics of verapamil and norverapamil.
Choi, DH; Choi, JS; Shin, WG, 2008
)
0.88
" Physiologically based pharmacokinetic (PBPK) simulations of pharmacokinetic profiles provide a simple, reliable and cost-effective way to understand the mechanisms underlying pharmacokinetic processes."( Identification of intestinal loss of a drug through physiologically based pharmacokinetic simulation of plasma concentration-time profiles.
Peters, SA, 2008
)
0.35
" Modulation of intrinsic hepatic clearance and tissue distribution parameters in the generic PBPK model was done to achieve a good fit to the observed intravenous pharmacokinetic profiles of the compounds studied."( Identification of intestinal loss of a drug through physiologically based pharmacokinetic simulation of plasma concentration-time profiles.
Peters, SA, 2008
)
0.35
" It is therefore important to do PBPK simulations of human pharmacokinetic profiles to understand the relevance of intestinal loss of a compound in humans."( Identification of intestinal loss of a drug through physiologically based pharmacokinetic simulation of plasma concentration-time profiles.
Peters, SA, 2008
)
0.35
"This article describes the experimental set-up and pharmacokinetic modeling of P-glycoprotein function in the rat blood-brain barrier using [(11)C]verapamil as the substrate and cyclosporin A as an inhibitor of P-gp."( Pharmacokinetics of P-glycoprotein inhibition in the rat blood-brain barrier.
Bergström, M; Blomquist, G; Hammarlund-Udenaes, M; Hooker, A; Långström, B; Rahman, O; Syvänen, S; Wilking, H, 2008
)
0.55
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"The aim of this work was to compare the suitability of different pharmacodynamic models for PK-PD modeling of verapamil cardiovascular effects in aortic coarctated rats (ACo), a model of renovascular hypertension."( Comparison of different pharmacodynamic models for PK-PD modeling of verapamil in renovascular hypertension.
Bertera, FM; Höcht, C; Mayer, MA; Opezzo, JA; Taira, CA,
)
0.58
" Although all pharmacodynamic models allowed a precise estimation of verapamil PK-PD parameters, linear and E(max) model did not permit an accurate PK-PD parameter estimation for the hypotensive and chronotropic effect, respectively."( Comparison of different pharmacodynamic models for PK-PD modeling of verapamil in renovascular hypertension.
Bertera, FM; Höcht, C; Mayer, MA; Opezzo, JA; Taira, CA,
)
0.6
"Side-by-side comparison of the tested pharmacodynamic models showed that accuracy of PK-PD parameters estimation by using the linear and classical E(max) model depends on the magnitude of concentration-effect curve covered in the study."( Comparison of different pharmacodynamic models for PK-PD modeling of verapamil in renovascular hypertension.
Bertera, FM; Höcht, C; Mayer, MA; Opezzo, JA; Taira, CA,
)
0.37
"The objectives of this study were to develop matrix-type transdermal patches of verapamil hydrochloride (VRP) with pectin as a matrix polymer to investigate the influence of several terpenes on in vitro permeation of VRP through rat skin and to evaluate pharmacodynamic activity of transdermal formulations in rats."( Matrix-type transdermal patches of verapamil hydrochloride: in vitro permeation studies through excised rat skin and pharmacodynamic evaluation in rats.
Alp, FI; Araman, A; Bektaş, A; Güngör, S; Ozdemir, O; Ozsoy, Y; Uydeş-Doğan, BS, 2008
)
0.85
"05) increased the area under the plasma concentration-time curve (AUC) and the peak concentration (C(max)) of verapamil by 49."( Effect of pioglitazone on the pharmacokinetics of verapamil and its major metabolite, norverapamil, in rats.
Burm, JP; Choi, JS, 2008
)
0.81
" In addition, SN-38 showed significant change in oral pharmacokinetic parameters and minor changes in intravenous pharmacokinetic profile."( Effect of P-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of irinotecan in rats.
Bansal, T; Jaggi, M; Khar, RK; Mishra, G; Talegaonkar, S, 2009
)
0.63
" Pharmacokinetic analysis was performed using a monocompartmental model."( Influence of N-hexane inhalation on the enantioselective pharmacokinetics and metabolism of verapamil in rats.
Boralli, VB; Lanchote, VL; Lepera, JS; Marques, MP; Mateus, FH, 2010
)
0.58
" The here obtained pharmacodynamic profiles of the drugs suggest that both milrinone and theophylline may be considered as potent relaxing agents of the lower oesophageal sphincter."( Milrinone and theophylline act as lower oesophageal sphincter relaxing agents: a comparative pharmacodynamic study in the rabbit.
Batzias, GC; Koutsoviti-Papadopoulou, M; Psarra, TA, 2009
)
0.35
" Pharmacokinetic characteristics were compared between the different genotypic groups."( Influence of ABCB1 gene polymorphisms on the pharmacokinetics of verapamil among healthy Chinese Han ethnic subjects.
He, XJ; Li-Ling, J; Qiu, F; Sun, YX; Zhao, LM, 2009
)
0.59
" In the other two routes of administration via the tail vein and hepatic portal vein, diammonium glycyrrhizinate (15 mg kg(-1)) did not affect any of the pharmacokinetic parameters of aconitine (0."( Effects of diammonium glycyrrhizinate on the pharmacokinetics of aconitine in rats and the potential mechanism.
Chen, L; Chen, YX; Davey, AK; Liu, XQ; Wang, JP; Yang, J, 2009
)
0.35
" The pharmacokinetic parameters of verapamil and norverapamil in rats were measured after the oral administration of verapamil (9 mg/kg) in the presence or absence of lovastatin (0."( Effects of lovastatin on the pharmacokinetics of verapamil and its active metabolite, norverapamil in rats: possible role of P-glycoprotein inhibition by lovastatin.
Chang, KS; Choi, DH; Choi, JS; Hong, SP; Koh, YY, 2009
)
0.88
" This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers."( Clinical pharmacokinetics of fexofenadine enantiomers.
Miura, M; Uno, T, 2010
)
0.36
"The pharmacokinetic parameters of verapamil and one of its metabolites, norverapamil, were compared in 14 healthy male Korean volunteers (age range 22-28 years) who had been administered verapamil (60 mg) orally in the presence or absence of oral lovastatin (20 mg)."( Pharmacokinetic interaction between oral lovastatin and verapamil in healthy subjects: role of P-glycoprotein inhibition by lovastatin.
Choi, DH; Choi, JS; Chung, JH, 2010
)
0.89
"The pharmacokinetic parameters of verapamil were significantly altered by the co-administration of lovastatin compared to the control."( Pharmacokinetic interaction between oral lovastatin and verapamil in healthy subjects: role of P-glycoprotein inhibition by lovastatin.
Choi, DH; Choi, JS; Chung, JH, 2010
)
0.89
" The pharmacokinetic parameters of verapamil and norverapamil in rats were determined after the oral administration of verapamil (9 mg/kg) in the presence or absence of simvastatin (0."( Effects of simvastatin on the pharmacokinetics of verapamil and its main metabolite, norverapamil, in rats.
Choi, DH; Choi, JS; Li, C,
)
0.66
" This hypothesis was supported by the outcomes of pharmacokinetic analysis."( Pharmacokinetic interaction between verapamil and methylxanthine derivatives in mice.
Wyska, E, 2010
)
0.64
" Safety and pharmacokinetic analyses were performed during each treatment period."( Effect of verapamil on the pharmacokinetics of aliskiren in healthy participants.
Dahlke, M; Hariry, S; Jarugula, V; Leon, S; Rebello, S, 2011
)
0.77
"The aim was to investigate the effect of Huang-Lian-Jie-Du-Decoction (HLJDD) on the pharmacokinetic behaviour of verapamil in rats."( Effect of Huang-Lian-Jie-Du-Decoction on pharmacokinetics of verapamil in rats.
Hu, N; Jing, XY; Liu, CH; Liu, XD; Wang, GJ; Xie, L; Xie, SS, 2010
)
0.81
" However, HLJDD did not alter the pharmacokinetic behaviour of verapamil after intravenous administration."( Effect of Huang-Lian-Jie-Du-Decoction on pharmacokinetics of verapamil in rats.
Hu, N; Jing, XY; Liu, CH; Liu, XD; Wang, GJ; Xie, L; Xie, SS, 2010
)
0.84
" In conclusion, diabetes mellitus revealed a tissue-specific effect on CYP3A activity and expression (induced in liver and inhibited in intestine), resulting in opposite pharmacokinetic behaviors of verapamil after oral and intravenous administration to diabetic rats."( Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
Chen, G; Hu, N; Liu, H; Liu, L; Liu, X; Pan, X; Wang, G; Wang, X; Xie, L; Xie, S; Zhang, L, 2011
)
0.77
" Plasma concentrations of verapamil in DM rats, rats fed with HFD, and control (CON) rats were measured after intravenous administration of 1 mg/kg verapamil and corresponding pharmacokinetic parameters were estimated."( Pharmacokinetics of verapamil in diabetic rats induced by combination of high-fat diet and streptozotocin injection.
Chen, GM; Hu, N; Li, J; Liu, L; Liu, XD; Wang, GJ; Wang, P; Xie, L; Xie, SS, 2011
)
0.99
"Microdosing studies are effective in enabling the early identification of the pharmacokinetic properties of compounds administered to humans."( Nonlinear pharmacokinetics of oral quinidine and verapamil in healthy subjects: a clinical microdosing study.
Fujita, T; Ikeda, Y; Kumagai, Y; Maeda, K; Nozawa, K; Oyama, Y; Sugiyama, Y; Takano, J, 2011
)
0.62
" In this study, fexofenadine, verapamil, risperidone, ondansetron, and imipramine were used as model compounds to investigate the effectiveness of MIM in pharmacokinetic studies."( Development of a novel high-throughput analytical methodology, multiple injection method, for quantitative analysis in drug metabolism and pharmacokinetic studies using liquid chromatography with tandem mass spectrometry.
Ohkawa, T; Tanaka, Y; Yasui, H, 2011
)
0.66
" The estimated k(inact) and K(I) values for each time-dependent inhibitor were compared with those obtained using human liver microsomes and used to estimate the magnitude of clinical pharmacokinetic drug-drug interaction (DDI)."( Time-dependent inhibition and estimation of CYP3A clinical pharmacokinetic drug-drug interactions using plated human cell systems.
Albaugh, DR; Fisher, MB; Fullenwider, CL; Hutzler, JM, 2012
)
0.38
" Subsequently, a 25mg/kg verapamil administered, electrocardiographs were recorded and pharmacokinetic delineated."( Glucosamine and adjuvant arthritis: a pharmacokinetic and pharmacodynamic study.
Gilzad-Kohan, MH; Jamali, F, 2012
)
0.68
"Conventional mammillary models are frequently used for pharmacokinetic (PK) analysis when only blood or plasma data are available."( Applications of minimal physiologically-based pharmacokinetic models.
Cao, Y; Jusko, WJ, 2012
)
0.38
" Therefore, a physiologically-based pharmacokinetic (PBPK) model for verapamil and its primary metabolite was developed and validated through the recovery of observed clinical plasma concentration data for both moieties and the reported interaction with midazolam, albeit a cytochrome P450 3A4-mediated DDI."( Application of permeability-limited physiologically-based pharmacokinetic models: part II - prediction of P-glycoprotein mediated drug-drug interactions with digoxin.
Barter, Z; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Turner, DB; Yeo, KR, 2013
)
0.62
" The aim of this study was to investigate the potential pharmacokinetic interactions between Rh2 and the HIV protease inhibitor ritonavir."( Pharmacokinetic interactions between 20(S)-ginsenoside Rh2 and the HIV protease inhibitor ritonavir in vitro and in vivo.
Aa, JY; Cao, B; Ge, C; Gu, RR; Li, MJ; Liu, CX; Liu, LS; Ma, T; Mao, Y; Shi, J; Sun, RB; Wang, GJ; Wang, XW; Wu, XL; Xia, WJ; Xiao, WJ; Yu, XY; Zha, WB; Zheng, T; Zhou, J, 2013
)
0.39
" Pharmacokinetic and pharmacodynamic changes depend on the nature and degree of hepatic impairment and on the characteristics of the dosed drug."( [Effect of liver cirrhosis on pharmacokinetics and pharmacodynamics of drugs].
Perlík, F, 2013
)
0.39
" A semi-physiologically based pharmacokinetic model (semi-PBPK) characterizing mechanism-based auto-inhibition was developed to predict the stereoselective pharmacokinetic profiles of verapamil and norverapamil following single or multiple oral doses."( A semi-physiologically-based pharmacokinetic model characterizing mechanism-based auto-inhibition to predict stereoselective pharmacokinetics of verapamil and its metabolite norverapamil in human.
Liu, L; Liu, X; Sai, Y; Wang, D; Wang, J; Xia, S; Xue, W, 2013
)
0.78
" In addition, a physiologically based pharmacokinetic (PBPK) model consisting of 11 compartments (6 tissues +5 sample sites) was applied for mechanistic elucidation and estimation of individual PK parameters."( Effects of verapamil on the pharmacokinetics and hepatobiliary disposition of fexofenadine in pigs.
Bondesson, U; Hedeland, M; Lennernäs, H; Sjögren, E, 2014
)
0.79
" In this study, in vivo-based [I]/Ki values were used to predict the DDI risks of a P-gp substrate dabigatran etexilate (DABE) using physiologically based pharmacokinetic (PBPK) modelling."( Physiologically based pharmacokinetic modelling and in vivo [I]/K(i) accurately predict P-glycoprotein-mediated drug-drug interactions with dabigatran etexilate.
Hu, ZY; Zhao, Y, 2014
)
0.4
"This approach accurately predicted the effects of five P-gp inhibitors on DABE pharmacokinetics (98-133% and 89-104% for the ratios of AUC and Cmax respectively)."( Physiologically based pharmacokinetic modelling and in vivo [I]/K(i) accurately predict P-glycoprotein-mediated drug-drug interactions with dabigatran etexilate.
Hu, ZY; Zhao, Y, 2014
)
0.4
" Furthermore, the infection reduced absorption of orally administered enrofloxacin, significantly decreased Cmax (0."( E. coli infection modulates the pharmacokinetics of oral enrofloxacin by targeting P-glycoprotein in small intestine and CYP450 3A in liver and kidney of broilers.
Bughio, S; Dai, X; Guo, M; Ren, W; Sun, Y; Wang, L; Zhang, Y, 2014
)
0.4
" Pharmacokinetic sampling for pasireotide SC and verapamil was done during days 18 to 25 and days 15 to 21, respectively."( Effect of verapamil on the pharmacokinetics of pasireotide in healthy volunteers.
Hu, K; Kornberger, R; Nesheiwat, D; Passos, VQ; Rodrigues, H; Ting, LS; Tripathi, AP, 2014
)
1.06
" Even though, pharmacokinetic data regarding the interaction between both drugs have been published, their use is limited to semiquantitative applications."( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
0.64
"Eligible pharmacokinetic interaction study between simvastatin and verapamil in humans was selected from PubMed database."( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
0.88
" The final model adequately describes pharmacokinetic interaction between simvastatin and verapamil which can be helpful in prediction of rhabdomyolysis in patients with concurrent use of these drugs."( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
0.86
"We applied physiologically based pharmacokinetic (PBPK) modeling to study the dose-dependent metabolism and excretion of verapamil and its preformed metabolite, norverapamil, to unravel the kinetics of norverapamil formation via N-demethylation."( PBPK modeling to unravel nonlinear pharmacokinetics of verapamil to estimate the fractional clearance for verapamil N-demethylation in the recirculating rat liver preparation.
Chow, EC; Pang, KS; Si, L; Sveigaard, HH; Tang, H; Yang, QJ, 2015
)
0.87
" Moreover, the pharmacokinetic profiles of orally administered triptolide with and without pretreatment with verapamil were determined in rats."( Influence of Verapamil on Pharmacokinetics of Triptolide in Rats.
Lei, X; Li, J; Liu, G; Liu, M; Yang, M; Zhang, T; Zhang, Y, 2016
)
1.02
"The current study was designed to cross-validate rat liver microsomes (RLM), suspended rat hepatocytes (SRH) and the isolated perfused rat liver (IPRL) model against in vivo pharmacokinetic data, using verapamil as a model drug."( Verapamil hepatic clearance in four preclinical rat models: towards activity-based scaling.
Annaert, P; Augustijns, P; De Bruyn, T; Keemink, J; Nicolaï, J; Van Veldhoven, PP, 2015
)
2.05
" The results indicated that, when the rats were pretreated with verapamil, the peak concentration of pristimerin increased from 189."( Influence of verapamil on pharmacokinetics of pristimerin in rats.
Gao, X; Liu, S; Wang, Y; Zhang, Y, 2016
)
1.04
" Noncompartmental pharmacokinetic analysis was performed using the WinNonlin program."( Influence of verapamil on the pharmacokinetics of oxcarbazepine and of the enantiomers of its 10-hydroxy metabolite in healthy volunteers.
Alexandre Junior, V; Antunes, Nde J; Coelho, EB; Della Pasqua, O; Lanchote, VL; Marques, MP; Takayanagui, OM; Tozatto, E; Wichert-Ana, L, 2016
)
0.8
"Patients receiving anti-retroviral drug treatment are sometimes simultaneously taking herbal remedies, which may result in pharmacokinetic herb-drug interactions."( Herb-Drug Pharmacokinetic Interactions: Transport and Metabolism of Indinavir in the Presence of Selected Herbal Products.
Abay, E; Calitz, C; Gouws, C; Hamman, J; Steenekamp, J; Viljoen, J; Wiesner, L, 2015
)
0.42
" Standard pharmacokinetic parameters were calculated in all studies."( Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies.
Baluom, M; Brealey, C; Craven, K; Gillen, M; Grossbard, EB; Lau, D; Mant, T; Martin, P; Millson, D; Oliver, S; Sweeny, D, 2016
)
0.69
" These results were confirmed by an in vivo pharmacokinetic study of oral administered FEX (10mg/kg) in rats."( Effect of resveratrol on the pharmacokinetics of fexofenadine in rats: Involvement of P-glycoprotein inhibition.
Bedada, SK; Neerati, P; Yellu, NR, 2016
)
0.43
" In comparison with FEX alone, RSV pretreatment significantly increased maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC), while there was no significant change was observed in T1/2 and Tmax of FEX."( Effect of resveratrol on the pharmacokinetics of fexofenadine in rats: Involvement of P-glycoprotein inhibition.
Bedada, SK; Neerati, P; Yellu, NR, 2016
)
0.43
"RSV significantly enhanced the exposure of FEX in rats likely by the inhibition of P-glycoprotein (P-gp) mediated efflux during the intestinal absorption, suggesting that there is a potential pharmacokinetic interaction between RSV and FEX."( Effect of resveratrol on the pharmacokinetics of fexofenadine in rats: Involvement of P-glycoprotein inhibition.
Bedada, SK; Neerati, P; Yellu, NR, 2016
)
0.43
" The compounds were designed with the objective of improving pharmacokinetic properties."( Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
Abdelghany, TM; Bayoumi, SA; Disouky, AM; El-Morsy, A; Elshafeey, A; Mancy, AS; Mayhoub, AS; Mohammad, H; Seleem, MA; Seleem, MN, 2016
)
0.43
" The hypothesis that pharmacokinetic differences underlie the differential efficacies of taccalonolides AF and AJ was tested."( Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
Benavides, R; Cichewicz, RH; Du, L; Kuhn, JG; Li, J; Mooberry, SL; Risinger, AL; Robles, AJ, 2017
)
0.46
" The effects of verapamil, an inhibitor of the efflux pump P-gp, on the pharmacokinetic profile of peficitinib were assessed in this open-label, single-center, single-sequence, crossover drug-interaction study."( The Effect of Verapamil, a P-Glycoprotein Inhibitor, on the Pharmacokinetics of Peficitinib, an Orally Administered, Once-Daily JAK Inhibitor.
Fisniku, O; Garg, JP; Han, D; Howieson, C; Keirns, J; Wojtkowski, T; Zhu, T, 2017
)
1.16
" To quantify the impacts of concomitant verapamil administration and renal impairment on rivaroxaban pharmacokinetics, a minimal physiologically based pharmacokinetic model system was developed and used to evaluate potential increases in rivaroxaban exposure and the consequent increase in risk of major bleeding."( Minimal Physiologically Based Pharmacokinetic and Drug-Drug-Disease Interaction Model of Rivaroxaban and Verapamil in Healthy and Renally Impaired Subjects.
Chow, CR; Ismail, M; Lee, VH; Rubino, CM, 2018
)
0.96
" We conducted virtual drug-drug interactions studies between DABE and the P-glycoprotein inhibitor verapamil in RI populations using physiologically based pharmacokinetic modeling."( Assessing Potential Drug-Drug Interactions Between Dabigatran Etexilate and a P-Glycoprotein Inhibitor in Renal Impairment Populations Using Physiologically Based Pharmacokinetic Modeling.
Doki, K; Homma, M; Neuhoff, S; Rostami-Hodjegan, A, 2019
)
0.73
" In vitro and preclinical in vivo pharmacokinetic (PK) properties of tozadenant were studied through the developed bioanalytical methods, and human PK profiles were predicted using physiologically based pharmacokinetic (PBPK) modeling based on these values."( Quantitative Analysis of Tozadenant Using Liquid Chromatography-Mass Spectrometric Method in Rat Plasma and Its Human Pharmacokinetics Prediction Using Physiologically Based Pharmacokinetic Modeling.
Byeon, JJ; Choi, J; Kim, N; Lee, BI; Park, MH; Park, Y; Shin, SH; Shin, YG, 2019
)
0.51
" Upon systematic model verification, physiologically based pharmacokinetic (PBPK) models are qualified for the quantitative rationalization of complex drug-drug-disease interactions (DDDIs)."( Systematic Development and Verification of a Physiologically Based Pharmacokinetic Model of Rivaroxaban.
Chan, ECY; Cheong, EJY; Chua, DXY; Teo, DWX, 2019
)
0.51
" The validated lesinurad plasma quantification method was successfully applied for the pharmacokinetic evaluations to support the clinical studies in renal impaired patients."( The Effects of Special Patient Population Plasma on Pharmacokinetic Quantifications Using LC-MS/MS.
Nguyen, M; Sun, L; Wilson, DM; Yeh, LT; Zhou, D, 2019
)
0.51
" With the confirmation that there is no impact on quantification from the matrix, the bioanalytical method can be used to support the pharmacokinetic evaluations for clinical studies in special populations."( The Effects of Special Patient Population Plasma on Pharmacokinetic Quantifications Using LC-MS/MS.
Nguyen, M; Sun, L; Wilson, DM; Yeh, LT; Zhou, D, 2019
)
0.51
" To develop a semi-physiologically based pharmacokinetic (semi-PBPK) model for assessing their contributions."( Short-chain fatty acids oppositely altered expressions and functions of intestinal cytochrome P4503A and P-glycoprotein and affected pharmacokinetics of verapamil following oral administration to rats.
Chen, Y; Kong, W; Liu, L; Liu, X; Wang, S; Wang, Z; Xie, Q; Zhang, J; Zhao, K, 2020
)
0.76
" A physiologically based pharmacokinetic (PBPK) model incorporating the metabolites was developed to predict the effect of other strong and moderate CYP3A4 inhibitors and inducers."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" Values for total clearance of compounds from plasma should be one of the most important pharmacokinetic parameters for predictions."( Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data.
Ito, S; Iwamoto, K; Kamimura, H; Mizunaga, M; Nakayama, K; Negoro, T; Nishiwaki, M; Nomura, Y; Suemizu, H; Yamazaki, H; Yoneda, N, 2020
)
0.56
" We report on how 2 acumapimod clinical DDI studies and a physiologically-based pharmacokinetic (PBPK) model assessing how co-administration of a weak (azithromycin) and strong (itraconazole) CYP3A4 inhibitor affected acumapimod systemic exposure, informed decision making and supported concomitant use of CYP3A4 and P-gp inhibitors."( A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor.
Agyemang, A; Farrell, C; Moore, W; Parkin, J, 2021
)
0.62
"This phase I, open-label study evaluated the effect of a potential drug-drug interaction of verapamil-a known P-glycoprotein (P-gp) inhibitor-with omadacycline on the pharmacokinetic profile of omadacycline in healthy adults."( The Effect of Verapamil, a P-gp Inhibitor, on the Pharmacokinetics, Safety, and Tolerability of Omadacycline in Healthy Adults: A Phase I, Open-Label, Single-Sequence Study.
Bai, S; Chitra, S; Hunt, TL; Manley, A; McGovern, PC; Tzanis, E, 2021
)
1.2
"3%) of the 12 participants enrolled in the study completed the study, and all enrolled participants were included in the safety and pharmacokinetic populations."( The Effect of Verapamil, a P-gp Inhibitor, on the Pharmacokinetics, Safety, and Tolerability of Omadacycline in Healthy Adults: A Phase I, Open-Label, Single-Sequence Study.
Bai, S; Chitra, S; Hunt, TL; Manley, A; McGovern, PC; Tzanis, E, 2021
)
0.98
" The maximum concentration (Cmax), half-life time (T1/2) and time to peak (Tmax) were 683."( Determination of Verapamil Hydrochloride and Norverapamil Hydrochloride in Rat Plasma by Capillary Electrophoresis With End-Column Electrochemiluminescence Detection and Their Pharmacokinetics Study.
Deng, B; Sun, S; Tang, L; Wang, H; Wei, Y, 2021
)
0.96
"These findings indicated that verapamil could significantly affect the pharmacokinetic profiles of RA in rats."( Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism.
Ci, X; Gu, Y; Liu, C; Ma, H; Shang, H; Si, D; Sun, Y; Wang, Z, 2021
)
1.28
"As one of the key components in model-informed drug discovery and development, physiologically-based pharmacokinetic (PBPK) modeling linked with in vitro-to-in vivo extrapolation (IVIVE) is widely applied to quantitatively predict drug-drug interactions (DDIs) on drug-metabolizing enzymes and transporters."( Physiologically-based pharmacokinetic modeling to evaluate in vitro-to-in vivo extrapolation for intestinal P-glycoprotein inhibition.
De Zwart, L; Evers, R; Yamazaki, S, 2022
)
0.72
" The systems information gathered on intestine, liver and blood proteins and other physiological parameters was incorporated into a physiologically based pharmacokinetic (PBPK) platform to create a virtual population of CD patients, with a view for guiding dose adjustment in the absence of clinical data in CD."( Altered Bioavailability and Pharmacokinetics in Crohn's Disease: Capturing Systems Parameters for PBPK to Assist with Predicting the Fate of Orally Administered Drugs.
Alrubia, S; Barber, J; Chen, Y; Mao, J; Rostami-Hodjegan, A, 2022
)
0.72
"A rapid, sensitive, and specific LC-MS/MS method was developed and fully validated for the detection of paeoniflorin only in rat plasma, and applied to pharmacokinetic studies, including intravenous, multi-dose oral and combined administrations with verapamil."( Quantification of Paeoniflorin by Fully Validated LC-MS/MS Method: Its Application to Pharmacokinetic Interaction between Paeoniflorin and Verapamil.
Bao, B; Gong, H; Shi, S; Wang, H; Wang, S; Zhao, Y, 2022
)
1.1

Compound-Compound Interactions

The potential for the modification of the pharmacokinetics of doxorubicin (DOX) concurrently administered with high-dose verapamil (VER) has been investigated in 17 patients with advanced neoplasms refractory to drugs belonging to the multidrug resistance spectrum. We therefore studied its functional and metabolic effects in closed chest rats when given in combination with prazosin, verAPamil or metoprolol, all of which have direct effects on the circulation.

ExcerptReferenceRelevance
"Two groups each consisting of twelve healthy students received Fenoterol (0,03 microgram/kg/min) alone or in combination with Verapamil (1,2 micrograms/kg/min) intravenously."( [Cardiac effect of fenoterol alone or combined with Verapamil (author's transl)].
Hofstetter, R; Krebs, W; Lang, D; Schmidt, HP; von Bernuth, G, 1979
)
0.72
" The results showed that a temporary relative hypoglycaemia occured in the newborns in short term as well as long term treatment with Partusisten or Partusisten in combination with Isoptin."( [Behaviour of serum concentrations of glucose, immunoreactive insulin and potassium ions in newborns after long term or crash treatments with Partusisten or Partusisten in combination with Isoptin (author's transl)].
Haller, K; Hiltmann, WD; Mohr, D; Vogel, M; Weidinger, H, 1976
)
0.26
"0 micrograms/ml in combination with diminazene aceturate or isometamidium chloride."( The effect of verapamil alone and in combination with trypanocides on multidrug-resistant Trypanosoma brucei brucei.
Kaminsky, R; Zweygarth, E, 1991
)
0.64
" Inosine in combination with ADA antagonized the noradrenaline-induced positive inotropic effect and the increase in cardiac output."( Hemodynamic effects of inosine in combination with positive and negative inotropic drugs: studies on rats in vivo.
Seesko, RC; Zimmer, HG, 1990
)
0.28
" Therefore, the effects of the anthracycline antibiotics on skin tumor promotion were evaluated in combination with the Ca2+ antagonist verapamil (VRP) and the protein kinase C (PKC) inhibitor palmitoylcarnitine (PC), compounds known to circumvent drug resistance."( Inhibition of mouse skin tumor promotion by adriamycin and daunomycin in combination with verapamil or palmitoylcarnitine.
Perchellet, JP; Satyamoorthy, K, 1990
)
0.7
" We therefore studied its functional and metabolic effects in closed chest rats when given in combination with prazosin, verapamil or metoprolol, all of which have direct effects on the circulation."( Functional and metabolic effects of ribose in combination with prazosin, verapamil and metoprolol in rats in vivo.
Lortet, S; Zimmer, HG, 1989
)
0.72
"The response to verapamil alone and combined with isosorbide dinitrate in a group of 12 patients with severe ischemic heart disease and stable effort angina was assessed by means of serial treadmill testing."( [Evaluation using serial exercise tests of verapamil alone and combined with isosorbide dinitrate in exertional angina].
Colman, T; González-Vílchez, F; Pajarón, A; Ruano, J; Vázquez de Prada, JA; Zueco, J, 1989
)
0.89
" The combination with verapamil may be effective in those who do not respond to etozolin alone."( Etozolin monotherapy and combination with verapamil in essential hypertension.
Agabiti-Rosei, E; Muiesan, G, 1989
)
0.86
" The calcium antagonist finoptin used in combination with alpha-tocopherol made it possible to decrease lipid hydroperoxide levels in low density lipoproteins and malondialdehyde concentrations in platelets, to prevent abnormal cyclic nucleotide metabolism in them and to increase tolerance to physical exercise."( [Effect of alpha-tocopherol combined with finoptin on the level of lipid hydroperoxides in plasma lipoproteins and on the functional activity of thrombocytes in patients with exertion-induced stable stenocardia].
Boklashchuk, MN; Gereliuk, IP; Levchenklo, VA; Serediuk, NN; Vakaliuk, IP, 1989
)
0.28
"Rifampin, a potent inducer of the hepatic microsomal system, has been shown to cause clinically important interactions when combined with other drugs, including oral anticoagulants, oral contraceptives, digitoxin, methadone hydrochloride, sulfonylureas, and barbiturates."( Update on rifampin drug interactions.
Baciewicz, AM; Bekemeyer, WB; Self, TH, 1987
)
0.27
" Verapamil was effective in combination with 5-FU, VCR or PEP on HSGc and with DTIC, VCR or PEP on KB."( [Chemo-sensitivity of a human salivary adenocarcinoma cell line to several anti-cancer drugs and enhancement of the antitumor effects by combination with filipin or verapamil].
Matsuya, T; Okura, M; Shirasuna, K; Sugiyama, M; Watatani, K, 1989
)
1.38
"To evaluate the hypotensive efficacy of Verapamil alone and combined with diuretic, in the treatment of essential hypertension in elderly patients, we studied 54 patients, mean age 67."( [Hypotensive efficacy of verapamil alone and in combination with a diuretic in the treatment of essential hypertension in geriatric patients].
Achilli, L; D'Amico, F; Latini, R; Lombi, V; Pierandrei, G, 1987
)
0.84
"The influence of verapamil (V) and of V combined with glucose-insulin-potassium (VG) on ischemic injured myocardium was investigated in dogs after ligation of the left anterior descending coronary artery."( Influence of verapamil and its combination with glucose-insulin-potassium-infusion on acute myocardial ischemia in dogs.
Beyerdörfer, I; Buller, G; Goos, H; Graff, J; Krause, EG; Lindenau, KF; Nöhring, J; Pissarek, M, 1987
)
0.98
" Verapamil alone had no protective effect on reperfused myocardium, whereas dibunol, and particularly its combination with verapamil, essentially limited the size of necrosis, reduced plasma CPK activity and animal mortality rate and maintained ultrastructural integrity of cardiomyocytes, which was accompanied by a decrease of plasma lipid peroxidation products and a stabilization of cardiomyocyte sarcolemma."( [Prevention of myocardial damage during reperfusion of the coronary artery in dogs using dibunol combined with verapamil].
Golikov, AP; Konorev, EA; Pichugin, VV; Polumiskov, VIu; Sharov, VG, 1987
)
1.39
"The cytotoxic effect of bouvardin (BVD) a protein synthesis inhibitor was studied separately and in combination with verapamil (VRP), a vasodilator and hyperthermia (43 degrees C) against Sarcoma 180 (S 180) and Ehrlich ascites carcinoma (EAC) tumour cells in vitro."( Enhancement of the in vitro cytotoxicity of bouvardin by verapamil alone and combined with hyperthermia in Sarcoma 180 and Ehrlich ascites carcinoma cells.
Adwankar, MK; Chitnis, MP, 1986
)
0.73
" Since IAHQ has only modest activity against L1210 leukemia in mice, it was tested in combination with methotrexate (MTX), probenecid, or verapamil in an effort to enhance efficacy."( Effects of 5,8-dideazaisopteroylglutamate (IAHQ) on L1210 leukemia in mice when given alone and in combination with methotrexate, probenecid, or verapamil.
Gale, GR; Hynes, JB; Smith, AB, 1986
)
0.67
" However, when propranolol was combined with the lower levels of verapamil or diltiazem, the result was decreased heart rate, blood pressure, left ventricular maximum rate of tension development (dP/dt), and cardiac index with increased systemic vascular resistance."( The cardiovascular and adrenergic actions of verapamil or diltiazem in combination with propranolol during halothane anesthesia in the dog.
Fung, DM; Kapur, PA; Matarazzo, DA; Sullivan, KB, 1987
)
0.77
"Twelve patients with variant angina combined with angina of effort were examined."( [Comparative study of the effectiveness of korinfar, izoptin and obzidan in patients with variant stenocardia combined with effort stenocardia].
Borisova, GA; Peres Peres, A; Shevchenko, OP; Sidorenko, BA, 1984
)
0.27
"Our purpose was to investigate modulation of multidrug resistance by liposome-encapsulated vincristine (VCR) in a drug-resistant human colon cancer cell line HT-29mdr1 and the potentiation of this modulation in combination with monoclonal antibody MRK-16 or verapamil."( Reversal of multidrug resistance in human colon cancer cells expressing the human MDR1 gene by liposomes in combination with monoclonal antibody or verapamil.
Husain, SR; Longo, DL; Pearson, JW; Rahman, A; Sela, S, 1995
)
0.67
"HT-29 parental cells and HT-29mdr1 cells were exposed to free VCR or liposome-encapsulated VCR alone or in combination with MRK-16 or verapamil."( Reversal of multidrug resistance in human colon cancer cells expressing the human MDR1 gene by liposomes in combination with monoclonal antibody or verapamil.
Husain, SR; Longo, DL; Pearson, JW; Rahman, A; Sela, S, 1995
)
0.69
"The potential for the modification of the pharmacokinetics of doxorubicin (DOX) concurrently administered with high-dose verapamil (VER) has been investigated in 17 patients with advanced neoplasms refractory to drugs belonging to the multidrug resistance spectrum."( Pharmacokinetics of doxorubicin co-administered with high-dose verapamil.
Boiocchi, M; Gigante, M; Toffoli, G, 1995
)
0.74
" We have evaluated the antitumor activity of a new highly potent vinca-alkaloid derivative, S 12363, in comparison with the activity of the reference compound vinblastine (VLB), when used alone or in combination with verapamil (VRP)."( Antitumor activity of the new vinca-alkaloid S 12363 alone or in combination with verapamil on a human multidrug resistant renal carcinoma xenograft.
Arvelo, F; Berlion, M; Bizzari, JP; Bourgeois, Y; Leonce, S; Poupon, MF; Rigaudy, P,
)
0.54
" Susceptibility patterns of sensitive and resistant parasites were evaluated against calcium antagonists of several chemical classes (verapamil, cyproheptidine, desipramine and chlopromazine), alone and in combination with suramin, diminazene aceturate or melarsen oxide cyteamine."( Trypanocidal resistance in Trypanosoma evansi in vitro: effects of verapamil, cyproheptidine, desipramine and chlorpromazine alone and in combination with trypanocides.
Anene, BM; Anika, SM; Chukwu, CC; Ross, CA, 1996
)
0.73
"The metabolic effects of verapamil alone and in combination with captopril were investigated in rats."( Metabolic effects in rats of verapamil alone and in combination with captopril.
Lopez, R; San Miguel, A; Taboada, C, 1997
)
0.89
" In some cases of atrial fibrillation digoxin is used in combination with verapamil."( P-glycoprotein system as a determinant of drug interactions: the case of digoxin-verapamil.
Beijnen, JH; Koks, CH; Schellens, JH; Verschraagen, M, 1999
)
0.76
"To evaluate the clinical efficacy and safety of a new antihypertensive drug combination of trandolapril/verapamil compared to monotherapy with verapamil or trandolapril, in patients with mild to moderate primary hypertension."( Efficacy and safety of a new long-acting drug combination, trandolapril/verapamil as compared to monotherapy in primary hypertension. Swedish TARKA trialists.
Andrup, M; Karlberg, BE; Odén, A, 2000
)
0.75
"The new fixed drug combination trandolapril/verapamil was superior to monotherapy with either of these drugs alone regarding reduction of both BP and rate pressure product."( Efficacy and safety of a new long-acting drug combination, trandolapril/verapamil as compared to monotherapy in primary hypertension. Swedish TARKA trialists.
Andrup, M; Karlberg, BE; Odén, A, 2000
)
0.8
"To study the intrinsic parameters of P-glycoprotein (P-gp) transport and drug-drug interactions at the blood-brain barrier (BBB), as few quantitative in vivo data are available."( In situ transport of vinblastine and selected P-glycoprotein substrates: implications for drug-drug interactions at the mouse blood-brain barrier.
Cisternino, S; Debray, M; Rousselle, C; Scherrmann, JM, 2004
)
0.32
" Drug-drug interactions were examined using vinblastine and compounds that bind to P-gp sites (verapamil, progesterone, PSC833) other than the vinblastine site to take into account the multispecific drug P-gp recognition."( In situ transport of vinblastine and selected P-glycoprotein substrates: implications for drug-drug interactions at the mouse blood-brain barrier.
Cisternino, S; Debray, M; Rousselle, C; Scherrmann, JM, 2004
)
0.54
" In situ perfusion of mdr1a(-/-) and wild-type mouse brains could be used to predict drug-drug interactions for P-gp at the mouse BBB."( In situ transport of vinblastine and selected P-glycoprotein substrates: implications for drug-drug interactions at the mouse blood-brain barrier.
Cisternino, S; Debray, M; Rousselle, C; Scherrmann, JM, 2004
)
0.32
" Importantly, using freshly isolated PBCECs in suspension in combination with fluorescence-activated cell sorting analysis reduced experimental time to 4hrs vs 7d with cultured PBCECs monolayers, while retaining and even improving feasibility, reliability, specificity, and sensitivity of the assay."( Rapid assessment of p-glycoprotein-drug interactions at the blood-brain barrier.
Bubik, M; Fricker, G; Mahringer, A; Ott, M, 2006
)
0.33
"5 degrees C) combined with two reversal agents (Interferon alpha and Verapamil) in MCF-7/ADR (ADM-resistant MCF-7 breast cancer cell line), and its relevant molecular mechanism of action."( Reversing adriamycin resistance of human breast cancer cells by hyperthermia combined with Interferon alpha and Verapamil.
Hao, XS; Liu, HY; Niu, RF; Shi, YR; Wei, XY; Yang, Y; Zhang, L, 2007
)
0.79
"To reverse the multidrug resistance of MCF-7/ADM cell line by thermochemotherapy combined with verapamil (VRP)."( [Experimental study on thermochemotherapy combined with verapamil for reversing the multidrug resistance responsible to breast cancer cell].
Hou, M; Li, SF; Liu, YY; Yan, X, 2008
)
0.81
"It is suggested that thermochemotherapy combined with Verapamil could be used as a way to overcome the multidrug resistance."( [Experimental study on thermochemotherapy combined with verapamil for reversing the multidrug resistance responsible to breast cancer cell].
Hou, M; Li, SF; Liu, YY; Yan, X, 2008
)
0.84
" The aim of this study was to compare the effect of trandolapril (T) and its fixed-dose combination with verapamil (FDTV) on SAM levels in hypertensive type-2 diabetic patients."( The effect of trandolapril and its fixed-dose combination with verapamil on circulating adhesion molecules levels in hypertensive patients with type 2 diabetes.
Escalante-Acosta, BA; Rodriguez-Lopez, L; Rubio-Guerra, AF; Vargas-Ayala, G; Vargas-Robles, H, 2008
)
0.8
"Nowadays, evaluation of potential risk of metabolic drug-drug interactions (mDDIs) is of high importance within the pharmaceutical industry, in order to improve safety and reduce the attrition rate of new drugs."( Predictions of metabolic drug-drug interactions using physiologically based modelling: Two cytochrome P450 3A4 substrates coadministered with ketoconazole or verapamil.
Blasco, H; Bouzom, F; Cazade, F; Chenel, M; Perdaems, N; Vinson, C; Whalley, S, 2010
)
0.56
" In combination with an increased throughput (up to 300%) and a reduced animal use (up to 50%), the enhanced power of the differential approach improves the utility of the biorelevant in situ perfusion technique with mesenteric blood sampling to elucidate the intestinal interaction profile of drugs and drug candidates."( Validation of a differential in situ perfusion method with mesenteric blood sampling in rats for intestinal drug interaction profiling.
Annaert, P; Augustijns, P; Brouwers, J; Mols, R, 2010
)
0.36
" Inhibition or induction of P-gp can cause drug-drug interactions and thus influence the effects of P-gp substrate drugs."( 20(S)-ginsenoside Rh2 noncompetitively inhibits P-glycoprotein in vitro and in vivo: a case for herb-drug interactions.
Ai, H; Gu, Y; Hao, G; Li, Y; Peng, Y; Sun, J; Wang, G; Wu, X; Zhang, J; Zhang, X; Zheng, Y; Zhou, F, 2010
)
0.36
"The aim of this study was to compare the effect of trandolapril (T) and its fixed-dose combination with verapamil (FDTV) on adiponectin levels in hypertensive type 2 diabetic patients."( Impact of trandolapril therapy and its combination with a calcium channel blocker on plasma adiponectin levels in patients with type 2 diabetes and hypertension.
Castro-Serna, D; Escalante-Acosta, BA; Rodríguez-Lopez, L; Rubio-Guerra, AF; Vargas-Ayala, G; Vargas-Robles, H, 2011
)
0.58
"Verapamil-sensitive idiopathic left ventricular tachycardia (ILVT) combined with a left accessory pathway (AP) is a relatively rare condition."( The characteristics of verapamil-sensitive idiopathic left ventricular tachycardia combined with a left accessory pathway and the effect of radiofrequency catheter ablation.
Hou, Y; Hu, JQ; Liao, ZL; Ma, J; Yang, Q; Zhang, S, 2012
)
2.13
"Drug-drug interactions (DDIs) can occur when two drugs interact with the same gene product."( Discovery and explanation of drug-drug interactions via text mining.
Altman, RB; Garten, Y; Percha, B, 2012
)
0.38
" The estimated k(inact) and K(I) values for each time-dependent inhibitor were compared with those obtained using human liver microsomes and used to estimate the magnitude of clinical pharmacokinetic drug-drug interaction (DDI)."( Time-dependent inhibition and estimation of CYP3A clinical pharmacokinetic drug-drug interactions using plated human cell systems.
Albaugh, DR; Fisher, MB; Fullenwider, CL; Hutzler, JM, 2012
)
0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" In carefully selected subgroup of SVG lesions without visible macrothrombus, a strategy of prophylactic intra-graft administration of abciximab and verapamil, combined with direct stenting of the graft lesion without pre-dilatation, can be safely accomplished without any significant risk of slow-flow/no-reflow phenomenon."( Intra-graft abciximab and verapamil combined with direct stenting is a safe and effective strategy to prevent slow-flow and no-reflow phenomenon in saphenous vein graft lesions not associated with thrombus.
Bhambi, BK; Lardizabal, JA; Sandhu, R; Sharma, S; Singh, S, 2012
)
0.88
"To date, the in vitro-in vivo correlation (IVIVC) of P-glycoprotein (P-gp)-mediated drug-drug interaction (DDI) at the blood-brain barrier (BBB) in rats indicated that the cutoff value to significantly affect the brain penetration of digoxin was [I,unbound/Ki] of 1, where I,unbound is the unbound plasma concentration of P-gp inhibitors."( Retrospective analysis of P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier in humans.
Amano, N; Hirabayashi, H; Moriwaki, T; Sugimoto, H, 2013
)
0.39
"The goal of this study was to investigate potential drug-drug interactions between empagliflozin and verapamil, ramipril, and digoxin in healthy volunteers."( Lack of clinically relevant drug-drug interaction between empagliflozin, a sodium glucose cotransporter 2 inhibitor, and verapamil, ramipril, or digoxin in healthy volunteers.
Broedl, UC; Macha, S; Pinnetti, S; Rose, P; Schoene, K; Sennewald, R; Woerle, HJ, 2013
)
0.81
"The potential drug-drug interactions were evaluated in 3 separate trials."( Lack of clinically relevant drug-drug interaction between empagliflozin, a sodium glucose cotransporter 2 inhibitor, and verapamil, ramipril, or digoxin in healthy volunteers.
Broedl, UC; Macha, S; Pinnetti, S; Rose, P; Schoene, K; Sennewald, R; Woerle, HJ, 2013
)
0.6
"Digoxin is the recommended substrate for assessment of P-glycoprotein (P-gp)-mediated drug-drug interactions (DDIs) in vivo."( Application of permeability-limited physiologically-based pharmacokinetic models: part II - prediction of P-glycoprotein mediated drug-drug interactions with digoxin.
Barter, Z; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Turner, DB; Yeo, KR, 2013
)
0.39
"The present study evaluated the efficacy of chemotherapy combined with targeted arterial infusion of verapamil in patients with advanced gastric cancer."( Efficacy of chemotherapy combined with targeted arterial infusion of verapamil in patients with advanced gastric cancer.
Chen, D; Duan, Q; Fan, G; Fan, P; Liu, A; Ning, Z; Zhang, T, 2014
)
0.85
"The present study aims to determine if an in vivo rat model of drug-drug interaction (DDI) could be useful to discriminate a sensitive (buspirone) from a 'non-sensitive' (verapamil) CYP3A substrate, using ketoconazole and ritonavir as perpetrator drugs."( Assessment of CYP3A-mediated drug-drug interaction potential for victim drugs using an in vivo rat model.
Bellavance, E; Bourg, S; Duan, J; Garneau, M; Ribadeneira, MD; Rioux, N, 2013
)
0.58
"In vitro inhibitory potency (Ki )-based predictions of P-glycoprotein (P-gp)-mediated drug-drug interactions (DDIs) are hampered by the substantial variability in inhibitory potency."( Physiologically based pharmacokinetic modelling and in vivo [I]/K(i) accurately predict P-glycoprotein-mediated drug-drug interactions with dabigatran etexilate.
Hu, ZY; Zhao, Y, 2014
)
0.4
" Drug-drug interactions involving voclosporin and CYP3A substrates are not expected."( Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR, 2014
)
0.4
"Modulation of drug transporters via herbal medicines which have been widely used in combination with conventional prescription drugs may result in herb-drug interactions in clinical practice."( Inhibitory effects of herbal constituents on P-glycoprotein in vitro and in vivo: herb-drug interactions mediated via P-gp.
Hu, J; Li, X; Li, Y; Liu, Z; Sheng, L; Wang, B; Yang, S, 2014
)
0.4
"New verapamil analogues were synthesized and their inhibitory activities against Mycobacterium tuberculosis H37Rv determined in vitro alone and in combination with rifampicin (RIF)."( Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
Chibale, K; Kumar, M; Naran, K; Pavadai, E; Ruminski, PG; Singh, K; Warner, DF, 2014
)
1.3
" Therefore, we aimed to develop a mathematical model describing drug-drug interaction between simvastatin and verapamil in humans."( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
0.85
"The drug-drug interaction between simvastatin and verapamil was modeled simultaneously with a two compartment model for verapamil with its active metabolite, norverapamil and a one compartment model for simvastatin with its active form, simvastatin hydroxy acid."( A pharmacokinetic drug-drug interaction model of simvastatin and verapamil in humans.
Chamnansua, M; Kaewdang, N; Lohitnavy, M; Methaneethorn, J, 2014
)
0.89
" The permeability of nalfurafine across human P-glycoprotein (P-gp)-expressing LLC-PK1 cells was investigated to evaluate drug-drug interactions (DDI) involving the P-gp efflux transporter of nalfurafine."( Drug-Drug Interactions of a Novel κ-Opioid Receptor Agonist, Nalfurafine Hydrochloride, Involving the P-Glycoprotein.
Ando, A; Miyamoto, Y; Ohzone, Y; Sasago, S, 2016
)
0.43
" ABCB1 may be involved in drug-drug interactions (DDIs) at the BBB, which may lead to changes in brain distribution and central nervous system side effects of drugs."( Factors Governing P-Glycoprotein-Mediated Drug-Drug Interactions at the Blood-Brain Barrier Measured with Positron Emission Tomography.
Bauer, F; Erker, T; Filip, T; Kuntner, C; Langer, O; Löscher, W; Mairinger, S; Müller, M; Pahnke, J; Römermann, K; Sauberer, M; Stanek, J; Traxl, A; Wanek, T, 2015
)
0.42
" Drug-drug interactions (DDIs) based on P-gp/CYP3A interplay are of clinical importance and require preclinical investigation."( The Consequence of Drug-Drug Interactions Influencing the Interplay between P-Glycoprotein and Cytochrome P450 3a: An Ex Vivo Study with Rat Precision-Cut Intestinal Slices.
de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; Siissalo, S; van Dam, A, 2016
)
0.43
" The mean maximum QTcF increase from baseline was 407, 487, and 437 milliseconds for AZD1305, alone and in combination with verapamil or ketoconazole, respectively."( In Silico Predictions and In Vivo Results of Drug-Drug Interactions by Ketoconazole and Verapamil on AZD1305, a Combined Ion Channel Blocker and a Sensitive CYP3A4 Substrate.
Aunes, M; Cullberg, M; Edvardsson, N; Frison, L; Johansson, S; Löfberg, B; Lunde, H, 2016
)
0.86
"The purpose of the present study is to demonstrate a useful approach (isotope-IV method) for analyzing drug-drug interactions (DDIs) following the oral administration of drugs using stable isotope-labeled compounds."( Quantitative analysis of pharmacokinetic profiles of verapamil and drug-drug interactions induced by a CYP inhibitor using a stable isotope-labeled compound.
Higashino, H; Kataoka, M; Kojima, C; Minami, K; Mutaguchi, K; Sakuma, S; Togashi, K; Ueda, K; Yamashita, S, 2016
)
0.68
"Intestinal P-gp and CYP3A4 work coordinately to reduce the intracellular concentration of drugs, and drug-drug interactions (DDIs) based on this interplay are of clinical importance and require pre-clinical investigation."( The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo.
de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; van de Steeg, E, 2017
)
0.46
" The model drug combination was verapamil-irbesartan (VER-IRB), which is widely used in clinic to treat hypertension."( The application of a novel high-resolution mass spectrometry-based analytical strategy to rapid metabolite profiling of a dual drug combination in humans.
Liu, H; Xing, J; Zang, M, 2017
)
0.74
" Data from a phase 1, drug-drug interaction study were used to qualify the minimal physiologically based pharmacokinetic model system."( Minimal Physiologically Based Pharmacokinetic and Drug-Drug-Disease Interaction Model of Rivaroxaban and Verapamil in Healthy and Renally Impaired Subjects.
Chow, CR; Ismail, M; Lee, VH; Rubino, CM, 2018
)
0.69
"We analyzed the clinical observations of target arterial infusion of verapamil combined with chemotherapy as therapy for advanced gastric cancer."( The clinical observation of verapamil in combination with interventional chemotherapy in advanced gastric cancer.
Dai, HB; Duan, QH; Fan, GF; Fan, PS; Huang, J; Liu, M; Liu, YB; Pan, JJ; Tang, LL; Weng, CT; Wu, Y; Yang, GH; Zhang, TY; Zhu, ZQ, 2018
)
1.01
" The target artery in the control group was perfused with chemotherapy drugs only, and the target artery in the therapy group was injected with verapamil combined with chemotherapy drugs."( The clinical observation of verapamil in combination with interventional chemotherapy in advanced gastric cancer.
Dai, HB; Duan, QH; Fan, GF; Fan, PS; Huang, J; Liu, M; Liu, YB; Pan, JJ; Tang, LL; Weng, CT; Wu, Y; Yang, GH; Zhang, TY; Zhu, ZQ, 2018
)
0.98
"Target arterial infusion of verapamil combined with chemotherapy drugs for advanced gastric cancer can significantly improve the efficacy of chemotherapy drugs and prolong the survival of patients."( The clinical observation of verapamil in combination with interventional chemotherapy in advanced gastric cancer.
Dai, HB; Duan, QH; Fan, GF; Fan, PS; Huang, J; Liu, M; Liu, YB; Pan, JJ; Tang, LL; Weng, CT; Wu, Y; Yang, GH; Zhang, TY; Zhu, ZQ, 2018
)
1.07
" Using drugs with potential to be repurposed, combined with 5-fluorouracil, the aim of this project was to investigate whether this combination led to therapeutic benefits, comparing with the isolated drugs."( Study of New Therapeutic Strategies to Combat Breast Cancer Using Drug Combinations.
Correia, A; Gärtner, F; Silva, D; Vale, N; Vilanova, M, 2018
)
0.48
" Because the combined effects of drug-drug interactions and RI have not been evaluated by means of clinical studies, the decision of DABE dosing for RI patients receiving P-glycoprotein inhibitors is empirical at its best."( Assessing Potential Drug-Drug Interactions Between Dabigatran Etexilate and a P-Glycoprotein Inhibitor in Renal Impairment Populations Using Physiologically Based Pharmacokinetic Modeling.
Doki, K; Homma, M; Neuhoff, S; Rostami-Hodjegan, A, 2019
)
0.51
" The aim of this study was to better understand the drug-drug interaction (DDI) potential of CYP3A and P-gp inhibitors."( PBPK modeling of CYP3A and P-gp substrates to predict drug-drug interactions in patients undergoing Roux-en-Y gastric bypass surgery.
Chan, LN; Chen, KF; Lin, YS, 2020
)
0.56
"Objectives For revealing the peculiarities of the drug-drug interaction of rivaroxaban (substrate CYP3A4 and P-gp) and calcium channel blockers (CCBs) (verapamil - inhibitor CYP3A4 and P-gp and amlodipine - substrate CYP3A4) in patients 80 years and older with nonvalvular atrial fibrillation (NAF) we studied 128 patients."( Drug-drug interaction of rivaroxaban and calcium channel blockers in patients aged 80 years and older with nonvalvular atrial fibrillation.
Bahteeva, D; Bochkov, P; Cherniaeva, M; Golovina, O; Gorbatenkova, S; Kulikova, M; Mirzaev, K; Ostroumova, O; Rytkin, E; Shevchenko, R; Sychev, D, 2020
)
0.76
" Concerns about drug-drug interactions (DDIs) have meant patients receiving drugs that inhibit CYP3A4 were ineligible for acumapimod trials."( A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor.
Agyemang, A; Farrell, C; Moore, W; Parkin, J, 2021
)
0.62
" Clinical management of DDIs in Chinese older adults in the absence of complex polypharmacy can a priori be similar to the EHRA guideline but routine monitoring of bleeding risk is encouraged when dabigatran etexilate given with verapamil and clarithromycin."( Physiologically-based pharmacokinetic modeling to predict drug-drug interactions of dabigatran etexilate and rivaroxaban in the Chinese older adults.
Cui, C; Lai, X; Li, H; Liu, D; Sia, JEV; Wu, X; Zhang, F, 2023
)
1.09

Bioavailability

The relative bioavailability of a new formulation of verapamil (CAS 52-53-9, Veramex 40) in comparison to a standard formulation was investigated in an open two-period cross-over study in 16 healthy volunteers.

ExcerptReferenceRelevance
" The bioavailability was only 22."( Pharmacokinetics of verapamil in man.
Koike, Y; Saito, H; Shimamura, K; Shudo, I, 1979
)
0.58
" Despite its almost complete absorption after oral administration verapamil was shown to undergo extensive first pass metabolism as the bioavailability was only 10 to 22%."( Physiological disposition of verapamil in man.
Eichelbaum, M; Schomerus, M; Spiegelhalder, B; Stieren, B, 1976
)
0.78
" The pharmacodnaymics of verapamil evaluated with regard to a single well-known pharmacological effect, have not necessarily to be identical with the pharmacokinetics and the bioavailability of the drug."( The pharmacodynamics of orally taken verapamil and verapamil retard as judged by their negative dromotropic effects.
Schlepper, M; Schwarz, F; Thormann, J, 1975
)
0.83
"Relative bioavailability and bioequivalence of two oral verapamil preparations were investigated (dosage 80 mg, film-coated tablets as reference, dragées as test formulation)."( Bioavailability study of two different verapamil formulations.
Blume, H; Horne, C; Knauf, H; Mutschler, E; Stenzhorn, G, 1992
)
0.8
" Bioavailability of SLV was 58."( Comparison of the pharmacokinetics and electrocardiographic effects of sublingual and intravenous verapamil.
Bauman, JL; Beckman, K; Berk, SI; Hariman, RJ; Hoon, TJ; Hu, D; Siegel, FP, 1992
)
0.5
"Twelve healthy male subjects completed this randomized, placebo controlled, four-period crossover trial to determine the effect of verapamil, diltiazem, and labetalol on the bioavailability and metabolism of imipramine."( Comparison of verapamil, diltiazem, and labetalol on the bioavailability and metabolism of imipramine.
Danis, M; Dukes, GE; Hak, LJ; Han, YH; Hermann, DJ; Hussey, EK; Krol, TF; Powell, JR, 1992
)
0.85
"The absolute bioavailability F and response (prolongation of the PR interval) of verapamil after single doses of the same oral formulation administered on two different days were investigated in 16 male subjects with an 80 mg fast dissolving and a 240 mg controlled-release preparation and compared with a bolus injection of 5 mg of verapamil."( Pharmacodynamic profile of verapamil in relation to absolute bioavailability: investigations with a conventional and a controlled-release formulation.
Blume, H; Harder, S; Huber, T; Rietbrock, N; Siewert, M; Thürmann, P, 1991
)
0.8
" The terminal elimination rate constant, clearance, volume of distribution, and bioavailability of verapamil were not significantly different between the two groups of subjects."( The pharmacokinetics of racemic verapamil in patients with impaired renal function.
Frantz, RP; Kurtz, SB; McCarthy, JT; Moyer, TP; Smith, RL; Theobald, HM; Zachariah, PK, 1991
)
0.78
"The bioavailability of 2 slow release formulations (test (P) and reference (R)) of verapamil was investigated in a study with a randomised cross over design, 20 healthy male subjects were included."( [Bioavailability of two slow-release formulations of verapamil].
Keller-Stanislawski, B; Rietbrock, N, 1990
)
0.75
"The effects of food on the bioavailability of a sustained-release (SR) formulation of verapamil (SR-verapamil; Isoptin SR) were determined in an open, three-way single-dose study involving 12 volunteers receiving (in randomized order) the SR preparation (1 X 240 mg) either fasting or with food and a conventional formulation of verapamil (3 X 80 mg) fasting."( Influence of food on the bioavailability of a sustained-release verapamil preparation.
Conway, EL; Drummer, OH; Louis, WJ; Phillips, PA, 1990
)
0.74
"2 mM Ca2+ groups did not show a significant change in absorption rate from their respective control rates."( The effect of calcium on gallbladder absorption.
Bastidas, JA; Lillemoe, KD; Magnuson, TH; May, CA; Pitt, HA; Scheeres, DE, 1990
)
0.28
" Metabolite 17 levels were increased in a parallel fashion, suggesting that altered CsA bioavailability rather than decreased metabolism may have caused the higher CsA levels in verapamil-treated patients."( The effects of calcium channel blockers on cyclosporine and its metabolites in renal transplant recipients.
Awni, WM; Heim-Duthoy, KL; Kasiske, BL; Rao, KV; Tortorice, KL, 1990
)
0.47
" In part, this appears to be related to the cardioinhibitory and negative chronotropic action of verapamil, but it is also likely to depend on increases in bioavailability of prazosin and higher plasma levels when the drug is given with verapamil."( Clinical pharmacological studies on the interaction between alpha-adrenoceptors and calcium antagonists.
Elliott, HL; Meredith, PA; Pasanisi, F; Reid, JL, 1985
)
0.49
" The overall effect is partly due to an increase in the apparent bioavailability of prazosin but may also reflect a synergistic effect on reducing peripheral vascular resistance."( Verapamil and prazosin in essential hypertension: evidence of a synergistic combination?
Elliott, HL; Meredith, PA; Reid, JL, 1987
)
1.72
" The mean bioavailability of the 120-mg tablet relative to the 240-mg tablet was 107%, with 95% confidence limits of 81 and 142%, indicating that the amount of verapamil available from the two tablets was similar."( Sustained-release verapamil: multiple-dose pharmacokinetic comparison of 120-mg and 240-mg tablets and the effect of halving a 240-mg tablet.
Durnin, C; McEwen, J; McMurdo, ME; Moreland, TA, 1989
)
0.81
"As part of a multiple dose bioavailability study, 80-mg verapamil hydrochloride tablets were administered to healthy subjects every 8 hours for 15 doses."( Differences in oral verapamil absorption as a function of time of day.
Battle, MM; Colburn, WA; Eldon, MA; Voigtman, RE, 1989
)
0.85
" During the evening dosage schedule a significantly greater bioavailability (AUC) and a prolonged time to peak concentration was found."( Circadian variation in the pharmacokinetics of verapamil.
Frederiksen, M; Hansen, JF; Jespersen, CM; Klitgaard, NA; Sørum, C, 1989
)
0.53
"A stable isotope technique has been used to assess the bioavailability of sustained release verapamil products."( Assessment of bioavailability of experimental single-unit sustained release tablets of verapamil hydrochloride using the stable isotope technique.
Kannikoski, A; Marvola, M; Ottoila, P; Taskinen, J, 1985
)
0.71
" The absorption rate of the sustained release formulation was significantly slower than for the conventional formulation."( Pharmacokinetics of verapamil and norverapamil in patients with hypertension: a comparison of oral conventional and sustained release formulations.
Jørgensen, NP; Walstad, RA, 1988
)
0.6
" The bioavailability of slow release formulations with a zero order release kinetic is lower than standard release formulations and related to the dissolution rate in vitro."( Drug input rate from the GI-tract. Michaelis-Menten kinetics and the bioavailability of slow release verapamil and nifedipine.
Fischer, A; Köhne, H; Menke, G; Rietbrock, N; Woodcock, BG, 1988
)
0.49
" Further measurements were made during a series of intensive study days, and the most important additional finding was a pharmacokinetic interaction that resulted in increased peak concentrations and bioavailability of prazosin."( The combination of prazosin and verapamil in the treatment of essential hypertension.
Campbell, L; Elliott, HL; Meredith, PA; Reid, JL, 1988
)
0.56
" The mean time of maximum plasma concentrations of verapamil were significantly prolonged and the absorption rate constants significantly reduced after sustained release verapamil on both day 1 and day 10."( Pharmacokinetics and pharmacodynamics of two formulations of verapamil.
Henry, JA; Hla, KK; Latham, AN, 1987
)
0.77
" During long term treatment, oral clearance decreases and bioavailability increases due to saturation of hepatic first-pass metabolism."( Clinical pharmacokinetics of verapamil, nifedipine and diltiazem.
Echizen, H; Eichelbaum, M,
)
0.42
" As compared to untreated subjects, the antituberculosis drugs greatly reduced the bioavailability of the calcium antagonist."( The influence of antituberculosis drugs on the plasma level of verapamil.
Böhm, R; Mooy, J; Rahn, KH; van Baak, M; van Kemenade, J; vd Vet, A, 1987
)
0.51
" In practice the important pharmacokinetic properties of verapamil are low bioavailability (20%), predominant elimination by metabolism (greater than 95%) and a relatively short half-life (t1/2, beta is 3-5 h)."( Pharmacokinetics of conventional and slow-release verapamil.
Bühler, F; Follath, F; Ha, HR; Schütz, E, 1986
)
0.77
" This inadequate bioavailability was caused by very slow absorption."( Pharmacokinetics of sustained-release verapamil after a single administration and at steady state.
Männistö, P; Mäntylä, R; Mattila, J; Taskinen, J,
)
0.4
" These products are well absorbed from the gastrointestinal tract but undergo variable degrees of transformation during the first passage through the liver."( [Clinical pharmacology of calcium inhibitors].
Martre, H; Singlas, E; Taburet, AM, 1985
)
0.27
" The extent of verapamil bioavailability was directly measured in one patient receiving an intravenous dose as well as an oral one and was found to be 42."( Disposition kinetics and urinary excretion of verapamil and some of its primary metabolites after oral administration in patients with angina pectoris.
Metelitsa, VI; Nikolenko, SA; Piotrovskii, VK; Riabokon, OS; Rumiantsev, DO, 1986
)
0.88
" Following a dose of the slow-release preparation, the drug concentration curves were smoother and the mean bioavailability was lower in comparison with the conventional preparation."( Plasma levels and urinary excretion of verapamil, norverapamil, N-dealkylverapamil (D617), N-dealkylnorverapamil (D620) following oral administration of a slow-release preparation.
Barbieri, E; Cargnelli, G; Ferrari, M; Padrini, R; Piovan, D; Toffoli, M; Trevi, G, 1985
)
0.54
" 506 +/- 82 ng/ml X hr) and absolute bioavailability (35% +/- 7% vs."( Lack of interaction between verapamil and cimetidine.
Abernethy, DR; Schwartz, JB; Todd, EL, 1985
)
0.56
" The present results suggest that 5-ISMN shows a high bioavailability and a potency comparable to ISDN, especially in the case of peroral administration."( [Effects of isosorbide 5-mononitrate on cardiovascular function. (I). Effects on the left ventricular system].
Kogi, K; Saito, T, 1985
)
0.27
" Bioavailability (corrected for dose and elimination rate constant) following intranasal administration (36% +/- 7%) was approximately 3 fold that after oral administration (13% +/- 3%)."( Pharmacodynamics of acute intranasal administration of verapamil: comparison with i.v. and oral administration.
Arnold, TH; Tackett, RL; Vallner, JJ,
)
0.38
" The bioavailability of diltiazem and nifedipine has not been well studied, and no investigations of the absolute bioavailability of these compounds have been reported."( Calcium antagonists. Pharmacokinetic properties.
Kates, RE, 1983
)
0.27
" Verapamil, nifedipine, and diltiazem are absorbed well after oral dosing, but absolute bioavailability of each is reduced substantially by a first-pass effect."( Update on calcium-channel blocking agents.
Bussey, HI; Talbert, RL,
)
1.04
" The high hepatic extraction results in low systemic bioavailability (20%) after oral drug administration."( Clinical pharmacokinetics of verapamil.
Blouin, RA; Hamann, SR; McAllister, RG,
)
0.42
" Our data suggest that the greater hypotensive activity of the combination results at least in part from a kinetic interaction that enhances the bioavailability of prazosin, but it is possible that a dynamic interaction at the level of vascular smooth muscle or compensatory cardiac activity also plays a role."( Combined alpha adrenoceptor antagonism and calcium channel blockade in normal subjects.
Elliott, HL; McSharry, DR; Meredith, PA; Pasanisi, F; Reid, JL, 1984
)
0.27
" Either a higher bioavailability of the drug or an extremely increased sensitivity of the receptors can explain such a marked electrophysiological effect at a moderate drug dosage."( Conversion of longstanding atrial flutter to sinus rhythm and transient complete A-V block following oral administration of verapamil. Report of a case.
Di Giacomo, M; Di Giacomo, V; Tedeschi, A, 1984
)
0.47
" The absolute bioavailability of the buccal preparation (37%) was slightly greater than the oral capsule (33%) and both had higher bioavailability than observed in earlier studies on verapamil dragees (10-20%)."( Verapamil disposition and effect on PQ-intervals after buccal, oral and intravenous administration.
Asthana, OP; Frömming, KH; Rietbrock, N; Schwabe, L; Wenchel, M; Woodcock, BG, 1984
)
1.9
"05) decrease in the clearance and an increase in the apparent bioavailability of verapamil during chronic administration, although no difference in the half-life was found."( Inter- and intra-subject variation in the first-pass elimination of highly cleared drugs during chronic dosing. Studies with deuterated verapamil.
Eichelbaum, M; Somogyi, A, 1984
)
0.7
" Thus, it can be anticipated that following oral administration of racemic verapamil bioavailability of (-)-verapamil will be substantially less."( Pharmacokinetics of (+)-, (-)- and (+/-)-verapamil after intravenous administration.
Eichelbaum, M; Mikus, G; Vogelgesang, B, 1984
)
0.76
" Diltiazem's oral bioavailability is good (90% reaches systemic circulation), but there is significant interindividual variability between administered dose and resulting plasma concentration."( Calcium-channel blocking agents.
Leonard, RG; Talbert, RL,
)
0.13
" Verapamil bioavailability was not dose dependent and averaged 19."( The pharmacology of verapamil. IV. Kinetic and dynamic effects after single intravenous and oral doses.
Kirsten, EB; McAllister, RG, 1982
)
1.5
"For drugs with a high hepatic clearance, bioavailability is low due to the so-called "first pass effect"."( Prediction of bioavailability for drugs with a high first-pass effect using oral clearance data.
Eichelbaum, M; Gugler, R; Somogyi, A, 1982
)
0.26
"The pharmacokinetic parameters and oral bioavailability of the antiarrhythmic drug verapamil were determined in six patients with atrial fibrillation."( Clinical pharmacokinetics of verapamil in patients with atrial fibrillation.
Anderson, P; BondessoN, U; Sylvén, C, 1982
)
0.78
" These data suggest that verapamil, and partially amrinone, inhibit histamine-induced tracheal contractions by reducing the bioavailability of intracellular Ca2+."( Relaxant effects of amrinone upon pulmonary smooth muscle.
Buck, DC; Mielens, ZE, 1982
)
0.57
"Although the absorption of verapamil is almost complete after oral administration, its bioavailability is low due to extensive hepatic first-pass metabolism."( Superiority of stable isotope techniques in the assessment of the bioavailability of drugs undergoing extensive first pass elimination. Studies of the relative bioavailability of verapamil tablets.
Dengler, HJ; Eichelbaum, M; Somogyi, A; von Unruh, GE, 1981
)
0.75
" Although absorption was almost complete after oral administration, absolute bioavailability (20%) was low, due to extensive hepatic first-pass metabolism."( Simultaneous determination of the intravenous and oral pharmacokinetic parameters of D,L-verapamil using stable isotope-labelled verapamil.
Dengler, HJ; Eichelbaum, M; Somogyi, A; von Unruh, GE, 1981
)
0.48
" The bioavailability of oral verapamil was 35 +/- 16%."( Verapamil disposition kinetics in chronic atrial fibrillation.
Harapat, S; Harrison, DC; Kates, RE; Keefe, DL; Kirsten, EB; Schwartz, J, 1981
)
2
"1 The pharmacokinetics, bioavailability and ECG response of verapamil was investigated in seven patients with liver cirrhosis and compared with six normal subjects, using stable labelled techniques whereby both the intravenous and oral dose are given simultaneously."( Pharmacokinetics, bioavailability and ECG response of verapamil in patients with liver cirrhosis.
Albrecht, M; Eichelbaum, M; Kliems, G; Schäfer, K; Somogyi, A, 1981
)
0.75
" The bioavailability of the oral dose averaged 22% (17 to 29%)."( Systemic availability of oral verapamil and effect on PR interval in man.
Burgess, CD; Hamer, J; Johnston, A, 1981
)
0.55
" After a single oral dose the bioavailability was only 24%, probably because of the first-pass metabolism."( Verapamil kinetics in normal subjects and patients with coronary artery spasm.
Ashley, JJ; Freedman, SB; Kelly, DT; Richmond, DR, 1981
)
1.71
" Areas under the concentration-time curves (AUCs) after intravenous 5-mg and oral 80-mg doses were used to calculate systemic blood clearance, intrinsic blood clearance, and bioavailability of verapamil in patients and to calculate apparent hepatic blood flow."( Verapamil disposition in liver disease and intensive-care patients: kinetics, clearance, and apparent blood flow relationships.
Rietbrock, I; Rietbrock, N; Vöhringer, HF; Woodcock, BG, 1981
)
1.9
" The mean extent of total verapamil bioavailability from the sustained-release formulation was 73."( Verapamil stereoisomerism: enantiomeric ratios in plasma dependent on peak concentrations, oral input rate, or both.
Karim, A; Piergies, A, 1995
)
2.03
" The technique was evaluated with verapamil and a well-absorbed 5-lipoxygenase inhibitor, A-79035."( Method to estimate the rate and extent of intestinal absorption in conscious rats using an absorption probe and portal blood sampling.
Borre, A; Hoffman, DJ; Nellans, HN; Seifert, T, 1995
)
0.57
" Absorption rate constants, estimated from initial appearance rates in portal blood, were used to monitor factors that affect drug absorption."( Method to estimate the rate and extent of intestinal absorption in conscious rats using an absorption probe and portal blood sampling.
Borre, A; Hoffman, DJ; Nellans, HN; Seifert, T, 1995
)
0.29
" Pharmacokinetic interactions, including an increase in the bioavailability of T when V was added, did not correlate with the degree of orthostasis."( Combined terazosin and verapamil therapy in essential hypertension. Hemodynamic and pharmacokinetic interactions.
Johnston, W; Laddu, AR; Lenz, ML; Pool, JL; Taylor, AA; Varghese, A, 1995
)
0.6
" The bioavailability of tablet C relative to B and A was 101."( [Study on dissolution test in vitro and bioavailability of oral osmotic pump of verapamil hydrochloride].
Cao, DS; Guo, JL; He, HY; Jing, GW; Li, YQ; Li, Z; Ling, LX, 1993
)
0.51
"To determine if there are greater differences in bioavailability of generic verapamil at steady state in elderly patients than in healthy young subjects."( Differences in serum concentrations of and responses to generic verapamil in the elderly.
Carter, BL; Demmler, RW; Noyes, MA,
)
0.6
" There was, however, a great deal of variability in the bioavailability of the generic products."( Differences in serum concentrations of and responses to generic verapamil in the elderly.
Carter, BL; Demmler, RW; Noyes, MA,
)
0.37
" This may have been because of increased bioavailability of the drug or increased sensitivity of the receptors."( Acute verapamil toxicity in a patient with chronic toxicity: possible interaction with ceftriaxone and clindamycin.
Jonas, E; Kishore, K; Misra, V; Raina, A,
)
0.61
" The apparent bioavailability of (+)-(R)-verapamil was over 14 times that of (-)-(S)-verapamil."( Pharmacokinetics of the enantiomers of verapamil in the dog.
Bai, SA; Johnson, LM; Lankford, SM, 1993
)
0.82
" Two subjects achieved measurable verapamil concentrations after intranasal administration with a mean bioavailability of 16."( Comparison of intranasal versus intravenous verapamil bioavailability.
Engelhardt, J; Gal, P; Johnson, M; Kandrotas, R; Kroboth, P; Smith, H; Watling, S, 1993
)
0.83
" Thus the interpretation of results of clinical 'modulator' trials should consider the decreased bioavailability of MDR-reversing agents."( Decreased potency of MDR-modulators under serum conditions determined by a functional assay.
Eisterer, W; Hilbe, W; Hofmann, J; Ludescher, C; Thaler, J, 1995
)
0.29
"The intestinal absorption of DMP 728, a cyclic peptide fibrinogen antagonist, was examined with the goals of identifying the cause(s) of its low oral bioavailability and understanding the mechanisms of its intestinal transport."( Intestinal absorption barriers and transport mechanisms, including secretory transport, for a cyclic peptide, fibrinogen antagonist.
Aungst, BJ; Saitoh, H, 1996
)
0.29
" It is concluded that tacrolimus is metabolized in the intestine, that the metabolites are able to re-enter the gut lumen and also enter into the portal vein and that small intestinal metabolism and transport is at least in part responsible for the low oral bioavailability of tacrolimus."( Metabolism of the macrolide immunosuppressant, tacrolimus, by the pig gut mucosa in the Ussing chamber.
Bader, A; Christians, U; Gonschior, AK; Hackbarth, I; Lampen, A; Sewing, KF; von Engelhardt, W, 1996
)
0.29
" We hypothesized that this assumption was invalid for highly variable drugs such as verapamil and tested it by comparing bioavailability for the brand vs itself."( High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.
Gordon, P; Hems, J; Pop, R; Spino, M; Tsang, YC, 1996
)
0.73
"To avoid any contribution from potential formulation differences, we evaluated bioavailability for isoptin SR 240 mg tablets in 9 healthy volunteers on 2 occasions separated by 1 week as part of a larger study."( High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.
Gordon, P; Hems, J; Pop, R; Spino, M; Tsang, YC, 1996
)
0.51
" Systemic clearance and bioavailability of the verapamil enantiomers were determined by coadministering deuterated verapamil intravenously on day 4, on day 16, and on day 24."( Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin.
Busse, D; Eichelbaum, M; Fromm, MF; Kroemer, HK, 1996
)
0.79
"The effects of high-protein food on the bioavailability of both the racemate and individual enantiomers of verapamil were investigated in 12 healthy volunteers using a randomized crossover design."( No effect of high-protein food on the stereoselective bioavailability and pharmacokinetics of verapamil.
Amamoto, T; Handa, T; Hashiguchi, M; Hirashima, Y; Irie, S; Ishii, S; Kimura, R; Maeda, A; Mori, Y; Ogata, H; Otsuka, N; Urae, A; Urae, R, 1996
)
0.73
" With calcium antagonists in particular, an assessment of the rate of absorption and of the maximum concentration is important, as those characteristics may have implications for the safety profile with this class of drugs."( Bioequivalence of controlled-release calcium antagonists.
Luus, HG; Müller, FO; Müller, FR; Schall, R, 1997
)
0.3
"The relative bioavailability of a new formulation of verapamil (CAS 52-53-9, Veramex 40) in comparison to a standard formulation was investigated in an open two-period cross-over study in 16 healthy volunteers under steady state conditions of 7 days duration each."( [Bioavailability of two verapamil formulations following repeated administration in steady-state conditions. An open, two-period, crossover study].
Heintz, B; Hutt, HJ; Lenhard, G; Müller, A; Schütz, M, 1996
)
0.85
" Saturable clearance may cause higher bioavailability and slower elimination of verapamil after acute oral overdoses."( Non-linear pharmacokinetics of high-dose intravenous verapamil.
Boiocchi, M; De Cicco, M; Fantin, D; Frustaci, S; Gigante, M; Nicolosi, GL; Robieux, I; Toffoli, G, 1997
)
0.77
"A novel method is described for assessing drug bioavailability from pharmacologic data."( Bioavailability assessment from pharmacologic data: method and clinical evaluation.
Gillespie, WR; Liu, Y; Shepherd, AM; Stagni, G, 1997
)
0.3
" bioavailability are of particular interest, also in drug development."( P-glycoprotein transporters and the gastrointestinal tract: evaluation of the potential in vivo relevance of in vitro data employing talinolol as model compound.
Ader, P; Baktir, G; Hanafy, A; Langguth, P; Okyar, A; Radschuweit, A; Spahn-Langguth, H; Terhaag, B, 1998
)
0.3
" Although some volunteer studies have shown substantial decreases in the bioavailability of ingested drugs, no controlled clinical trials have been performed and there is no conclusive evidence that WBI improves the outcome of the poisoned patient."( Position statement: whole bowel irrigation. American Academy of Clinical Toxicology; European Association of Poisons Centres and Clinical Toxicologists.
Tenenbein, M, 1997
)
0.3
"To investigate in vitro the mechanisms involved in the gastro-intestinal absorption of the HIV protease inhibitor, saquinavir mesylate (Invirase), whose oral bioavailability is low, variable, and significantly increased by co-administration with ritonavir, also an HIV protease inhibitor but with higher oral bioavailability."( Active apical secretory efflux of the HIV protease inhibitors saquinavir and ritonavir in Caco-2 cell monolayers.
Alex, R; Alsenz, J; Steffen, H, 1998
)
0.3
" Together with sensitivity to gutwall metabolism by cytochrome P-450 3A, this may partially account for the low and variable oral bioavailability of saquinavir in clinical studies and for its increased bioavailability after co-administration with ritonavir."( Active apical secretory efflux of the HIV protease inhibitors saquinavir and ritonavir in Caco-2 cell monolayers.
Alex, R; Alsenz, J; Steffen, H, 1998
)
0.3
" Inhibition of intestinal P-gp function using MDR reversing agents may enhance the oral bioavailability of some chemotherapeutic agents."( Comparison of effects of surfactants with other MDR reversing agents on intracellular uptake of epirubicin in Caco-2 cell line.
Hsu, CY; Huang, JD; Lo, YL,
)
0.13
" Concomitant intake of rifampicin (600 mg/die) induced especially the presystemic (prehepatic) metabolism of verapamil so that oral bioavailability approached zero and PD effects almost diminished."( Effect of age on pharmacokinetics and pharmacodynamics in man.
Klotz, U, 1998
)
0.51
"The objective of this study was to investigate whether the decrease in artemisinin bioavailability after repeated oral dosing in humans can be a result of increased efflux of artemisinin by P-glycoprotein or decreased membrane transport at the intestinal barrier."( High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement.
Ashton, M; Carlborg, O; Lennernäs, H; Sandström, R; Svensson, US, 1999
)
0.3
" The nasal bioavailability of nicardipine from plain buffered solution was 44%, and increased steadily to 56-79% in direct proportion to the amount of PEG 400 added."( Evaluation of the effect of polyethylene glycol 400 on the nasal absorption of nicardipine and verapamil in the rat.
Lau-Cam, CA; Rahman, M, 1999
)
0.52
"This is the first study to show a decreased oral bioavailability of a P-glycoprotein substrate (talinolol) in humans as a result of coadministration of verapamil."( Unexpected effect of verapamil on oral bioavailability of the beta-blocker talinolol in humans.
Berndt, A; Gramatté, T; Kirch, W; Krappweis, J; Oertel, R; Schwarz, UI; von Richter, O, 1999
)
0.82
" The rate of absorption into plasma of (R)- and (S)-verapamil increased despite the low dose of ketoconazole added, indicating an inhibition of the gut wall metabolism of (R/S)-verapamil by ketoconazole."( The effect of ketoconazole on the jejunal permeability and CYP3A metabolism of (R/S)-verapamil in humans.
Jansson, B; Knutson, L; Knutson, TW; Lennernäs, H; Sandström, R, 1999
)
0.78
" Intra- and inter-patient variations in methadone bioavailability have been observed after oral methadone treatment and this makes it difficult to predict a dosing regimen."( The roles of P-glycoprotein and intracellular metabolism in the intestinal absorption of methadone: in vitro studies using the rat everted intestinal sac.
Barthe, L; Bouër, R; Houin, G; Philibert, C; Tournaire, C; Woodley, J, 1999
)
0.3
" This gives further rationale for P-glycoprotein-mediated intestinal drug secretion as a cause for incomplete oral bioavailability and for drug interactions during intestinal absorption."( Intestinal secretion of intravenous talinolol is inhibited by luminal R-verapamil.
Gramatté, T; Oertel, R, 1999
)
0.54
" Bioavailability was higher in women (0."( Gender-specific effects on verapamil pharmacokinetics and pharmacodynamics in humans.
Barnas, CR; Jones, MP; Krecic-Shepard, ME; Schwartz, JB; Slimko, J, 2000
)
0.6
" From these findings, we concluded that a reduction of CsA bioavailability during ARF is caused by depression in bile excretion and renal function-dependent depression of uptake from intestinal tract via maybe P-gLycoprotein in enterocytes."( Factors that affect absorption behavior of cyclosporin a in gentamicin-induced acute renal failure in rats.
Hoshino, N; Minouchi, T; Morimoto, J; Shibata, N; Yamaji, A, 2000
)
0.31
" The large amount of calcein leakage induced by enhancers was consistent with an enhancement of bioavailability of verapamil and insulin following nasal administration (oleic acid < SG < Sit-G)."( The enhancing effect of soybean-derived sterylglucoside and beta-sitosterol beta-D-glucoside on nasal absorption in rabbits.
Kamata, K; Maitani, Y; Nagai, T; Nakamura, K; Suenaga, H; Takayama, K, 2000
)
0.52
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Greater verapamil and norverapamil bioavailability after administration of regular- compared with sustained-release verapamil also suggests saturable processes at the intestinal level."( Faster clearance of sustained release verapamil in men versus women: continuing observations on sex-specific differences after oral administration of verapamil.
Barnas, CR; Krecic-Shepard, ME; Schwartz, JB; Slimko, J, 2000
)
1
" In addition, its role in modifying the bioavailability of orally administered drugs via induction or inhibition has been also been demonstrated in various studies."( Multidrug resistance (MDR) in cancer. Mechanisms, reversal using modulators of MDR and the role of MDR modulators in influencing the pharmacokinetics of anticancer drugs.
Krishna, R; Mayer, LD, 2000
)
0.31
"The goals of this study were to examine whether formulations, capable of releasing sulpiride (SP) in synchrony with the p-Glycoprotein (P-gp) inhibitors, verapamil (Ver) or quinidine (Qn) can increase SP relative bioavailability and to suggest a rationale approach for oral administration of SP."( Improved intestinal absorption of sulpiride in rats with synchronized oral delivery systems.
Baluom, M; Friedman, M; Rubinstein, A, 2001
)
0.51
" It was used successfully in pharmacokinetic and bioavailability studies of verapamil administration in drug formulations alternative to tablets: buccal and flotation ones."( A validated method for the determination of verapamil and norverapamil in human plasma.
Sawicki, W, 2001
)
0.8
"Irinotecan (CPT-11) is a camptothecin analog with low (about 10--20%) and variable oral bioavailability in animal models."( Active transepithelial transport of irinotecan (CPT-11) and its metabolites by human intestinal Caco-2 cells.
de Bruijn, P; de Jonge, MJ; Kurihara, M; Nishiyama, M; Sparreboom, A; Takano, H; Verweij, J; Yamamoto, W, 2001
)
0.31
" This may lead to increased bioavailability of coadministered compounds."( Methadone inhibits rhodamine123 transport in Caco-2 cells.
Greenblatt, DJ; Perloff, MD; Störmer, E; von Moltke, LL, 2001
)
0.31
" This leads to a secretion-limited peroral absorption of salbutamol, which contributes to the poor oral bioavailability of the drug."( The influence of active secretion processes on intestinal absorption of salbutamol in the rat.
Casabó, VG; Martín-Villodre, A; Nácher, A; Valenzuela, B, 2001
)
0.31
" However, NFZ is an inhibitor of P-gp activity at clinically relevant in vivo concentrations and may have the potential to increase bioavailability of coadministered compounds that are substrates for transport."( P-glycoprotein interactions of nefazodone and trazodone in cell culture.
Greenblatt, DJ; Perloff, MD; Störmer, E; von Moltke, LL, 2001
)
0.31
" At a perfusate concentration of 1 mM, verapamil caused a dramatic increase in [(3)H]digoxin absorption rate from duodenum and jejunum, while the effect in colon was insignificant."( The role of P-glycoprotein in limiting intestinal regional absorption of digoxin in rats.
Borgå, O; Hultkvist-Bengtsson, U; Sababi, M, 2001
)
0.58
"The contribution of the gastrointestinal tract in comparison with the liver for the low and variable bioavailability of orally administered drugs is still poorly understood."( Determination of in vivo absorption, metabolism, and transport of drugs by the human intestinal wall and liver with a novel perfusion technique.
Barclay, ML; Dent, J; Eichelbaum, M; Fraser, R; Fromm, MF; Greiner, B; Omari, T; Somogyi, AA; von Richter, O, 2001
)
0.31
" Bioavailability was low (19."( Determination of in vivo absorption, metabolism, and transport of drugs by the human intestinal wall and liver with a novel perfusion technique.
Barclay, ML; Dent, J; Eichelbaum, M; Fraser, R; Fromm, MF; Greiner, B; Omari, T; Somogyi, AA; von Richter, O, 2001
)
0.31
"First-pass metabolism by the intestinal wall is extensive and contributes to the same extent as the liver to low bioavailability of some drugs such as verapamil."( Determination of in vivo absorption, metabolism, and transport of drugs by the human intestinal wall and liver with a novel perfusion technique.
Barclay, ML; Dent, J; Eichelbaum, M; Fraser, R; Fromm, MF; Greiner, B; Omari, T; Somogyi, AA; von Richter, O, 2001
)
0.51
" Chronic use of Saint John's wort (SJW) has been shown to lower the bioavailability for a variety of co-administered drugs including indinavir, cyclosporin, and digoxin."( Saint John's wort: an in vitro analysis of P-glycoprotein induction due to extended exposure.
Greenblatt, DJ; Perloff, MD; Shader, RI; Störmer, E; von Moltke, LL, 2001
)
0.31
"It has been suggested that cytochrome P450 3A4 (CYP3A4) and MDR1 P-glycoprotein (P-gp) act synergistically to limit the bioavailability of orally administered agents."( Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4.
Achira, M; Ito, K; Sugiyama, Y; Suzuki, H, 1999
)
0.3
" Bioavailability studies were carried out in 12 healthy volunteers including six men and six women."( Pharmacokinetics of verapamil and norverapamil from controlled release floating pellets in humans.
Sawicki, W, 2002
)
0.64
"This paper describes a graphical model for simplifying in vitro absorption, metabolism, distribution, and elimination (ADME) data analysis through the estimation of oral bioavailability (%F) of drugs in humans and other species."( Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates.
Hwang, KK; Mandagere, AK; Thompson, TN, 2002
)
0.31
"The liver had a high intrinsic capacity for clearing VL because the absolute bioavailability (BA) of VL was 21."( Differentiation of gut and hepatic first-pass effect of drugs: 1. Studies of verapamil in ported dogs.
Kunta, JR; Lee, HS; Lee, YH; Perry, BA; Sinko, PJ; Sutyak, JP, 2001
)
0.54
" Following oral administration, the bioavailability (F) of I (17%) was much higher than that of II (1%)."( Differences in the absorption, metabolism and biliary excretion of a diastereomeric pair of alphavbeta3-antagonists in rat: limited role of P-glycoprotein.
Duggan, ME; Hochman, J; Leppert, P; Lin, JH; Ma, B; Meissner, R; Meng, Y; Perkins, J; Prueksaritanont, T; Tang, C; Zrada, M, 2002
)
0.31
" Bioavailability was determined by a crossover method in 12 healthy volunteers."( Pharmacokinetics of verapamil and its metabolite norverapamil from a buccal drug formulation.
Janicki, S; Sawicki, W, 2002
)
0.64
" Oral bioavailability of M6G and the fraction of M6G deglucuronidated to morphine were estimated from areas under the plasma-concentration vs."( Verapamil decreases glucuronidase activity in the gut.
Geisslinger, G; Kroemer, HK; Lötsch, J; Sperker, B, 2002
)
1.76
"Berberine is an important ingredient in a number of traditional Chinese medicines but has been shown to have poor bioavailability in the dog."( The involvement of P-glycoprotein in berberine absorption.
Fawcett, JP; Liu, XD; Pan, GY; Wang, GJ; Xie, YY, 2002
)
0.31
"In an attempt to improve the oral bioavailability of paclitaxel, a novel P-glycoprotein inhibitor, KR30031, which is verapamil analog with fewer cardiovascular effects, was coadministered with paclitaxel, and to elucidate other possible causes of the low oral bioavailability of paclitaxel, an inhibitor of hepatic metabolism, ketoconazole, was also coadministered with paclitaxel."( Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031.
Hwang, SJ; Lee, CH; Shim, CK; Woo, JS, 2003
)
0.53
" Thus, the bioavailability of paclitaxel could be enhanced by coadministration of a P-glycoprotein inhibitor, KR-30031."( Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031.
Hwang, SJ; Lee, CH; Shim, CK; Woo, JS, 2003
)
0.32
"The human multidrug transporter P-glycoprotein (Pgp, ABCB1) contributes to the poor bioavailability of many anticancer and antimicrobial agents as well as to drug resistance at the cellular level."( Allosteric modulation of human P-glycoprotein. Inhibition of transport by preventing substrate translocation and dissociation.
Dey, S; Hafkemeyer, P; Maki, N, 2003
)
0.32
"Weakly basic drugs, such as verapamil hydrochloride, that are poorly soluble in neutral/alkaline medium may have poor oral bioavailability due to reduced solubility in the small intestine and colon."( Film coated pellets containing verapamil hydrochloride: enhanced dissolution into neutral medium.
Munday, DL, 2003
)
0.9
"The mdr1 gene product P-glycoprotein (P-gp) is involved in the bioavailability and pharmacokinetics of various drugs."( (R)- and (S)-[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation.
Boellaard, R; Franssen, EJ; Keizer, H; Lammertsma, AA; Luurtsema, G; Molthoff, CF; Smit, JW; Windhorst, AD, 2003
)
0.65
"Our objective was to investigate the main in vivo transport mechanisms of fexofenadine involved in the intestinal absorption and bioavailability of the drug in humans."( Multiple transport mechanisms involved in the intestinal absorption and first-pass extraction of fexofenadine.
Bondesson, U; Hedeland, M; Knutson, L; Lennernäs, H; Petri, N; Tannergren, C, 2003
)
0.32
"In this in vivo perfusion study verapamil increased the bioavailability of fexofenadine."( Multiple transport mechanisms involved in the intestinal absorption and first-pass extraction of fexofenadine.
Bondesson, U; Hedeland, M; Knutson, L; Lennernäs, H; Petri, N; Tannergren, C, 2003
)
0.6
" Cellular and animal data suggest that ethanol confers beneficial effects on the vascular endothelium and increases the bioavailability of nitric oxide."( Direct effect of ethanol on human vascular function.
Creager, MA; Omland, T; Tawakol, A, 2004
)
0.32
"Repeated administration of St John's wort significantly decreased the bioavailability of R- and S-verapamil."( St John's wort decreases the bioavailability of R- and S-verapamil through induction of the first-pass metabolism.
Bondesson, U; Engman, H; Hedeland, M; Knutson, L; Lennernäs, H; Tannergren, C, 2004
)
0.79
" The presented method was successfully applied to an in vivo intestinal absorption and bioavailability study in humans, using the Loc-I-Gut method."( Simultaneous quantification of the enantiomers of verapamil and its N-demethylated metabolite in human plasma using liquid chromatography-tandem mass spectrometry.
Bondesson, U; Fredriksson, E; Hedeland, M; Lennernäs, H, 2004
)
0.58
"Low and varied oral bioavailability (BA) of some drugs has been attributed to extraction by the intestine and liver."( Differentiation of gut and hepatic first-pass loss of verapamil in intestinal and vascular access-ported (IVAP) rabbits.
Kunta, JR; Lee, SH; Lee, YH; Perry, BA; Sinko, PJ, 2004
)
0.57
" Species differences were observed in the systemic clearance of theophylline (approximately 5-fold higher in CHPs), a low clearance compound, and the bioavailability of propranolol and verapamil (lower in CHPs), both high clearance compounds."( The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application.
Bai, SA; Christ, DD; Diamond, S; Grace, JE; Grossman, SJ; He, K; Qian, M; Wong, H; Wright, MR; Yeleswaram, K, 2004
)
0.51
" The absolute bioavailability of paclitaxel with verapamil (3."( The effect of verapamil on the pharmacokinetics of paclitaxel in rats.
Choi, JS; Li, X, 2005
)
0.94
"This study suggests that verapamil increases fexofenadine exposure probably because of an increase in bioavailability through P-glycoprotein inhibition and that probenecid slightly increases the area under the plasma concentration-time curve of fexofenadine as a result of a pronounced reduction in renal clearance."( Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.
Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.88
" Thus, to accurately determine the absorption rate of Rho123, it was necessary to measure the water movement."( Regional difference in P-glycoprotein function in rat intestine.
Hayashi, M; Iida, A; Tomita, M, 2005
)
0.33
" The absolute bioavailability (F(A."( Pharmacokinetics of verapamil and its major metabolite, norverapamil from oral administration of verapamil in rabbits with hepatic failure induced by carbon tetrachloride.
Burm, JP; Choi, JS, 2005
)
0.65
"This study demonstrated that the bioavailability of risperidone was increased by verapamil, suggesting in vivo involvement of P-glycoprotein in the pharmacokinetics of risperidone."( Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.
Kaneo, S; Nakagami, T; Saito, M; Tateishi, T; Yasui-Furukori, N, 2005
)
0.96
" As Pgp varies from person to person to an extent of 2-8-fold, it can be one direct reason for the interindividual variable bioavailability shown by rifampicin."( Evidence of efflux-mediated and saturable absorption of rifampicin in rat intestine using the ligated loop and everted gut sac techniques.
Mariappan, TT; Singh, S,
)
0.13
"The efflux transporter, P-glycoprotein (P-gp), located in the brush-border membrane of intestinal absorptive cells, reduces the bioavailability of a wide range of orally administered drugs."( Construction of a functional transporter analysis system using MDR1 knockdown Caco-2 cells.
Onuki, R; Sugiyama, Y; Taira, K; Watanabe, T; Yamashita, S, 2005
)
0.33
" Our previous studies demonstrated that sinomenine could significantly improve the bioavailability of paeoniflorin in rats, but the underlying mechanisms remain unknown."( The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xu, HX; Zhou, H, 2006
)
0.33
" The hypotensive effect of isosorbid dinitrate, commonly used as a vasodilatator, was weaker at the onset of AW, being associated with the decreased bioavailability of the drug."( Responses to cardiovascular drugs during alcohol withdrawal.
Kähkönen, S,
)
0.13
" The test formulation was found to be comparable with the Herbesser SR in the extent of bioavailability but differ in the rate of absorption, the test formulation being less sustained."( In vivo performance of controlled release pellets of diltiazem HCl.
Jia Woei, W; K H, Y, 2005
)
0.33
" These results indicate that the mechanism of the pharmacokinetic interaction between oral ximelagatran and erythromycin may involve inhibition of transport proteins, possibly P-gp, resulting in decreased melagatran biliary excretion and increased bioavailability of melagatran."( Influence of erythromycin on the pharmacokinetics of ximelagatran may involve inhibition of P-glycoprotein-mediated excretion.
Dorani, H; Eriksson, UG; Fritsch, H; Hoffmann, KJ; Karlsson, J; Olsson, L; Sarich, TC; Schützer, KM; Wall, U, 2006
)
0.33
" The apparent absorption rate constant (ka) of [(14)C]bepotastine in the small intestine was greatly increased by cyclosporin A and verapamil, especially in the distal portion, and the site-specific absorption of [(14)C]bepotastine disappeared."( Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate.
Fukuda, H; Kamikozawa, Y; Ohashi, R; Sugiura, M; Tamai, I; Yabuuchi, H, 2006
)
0.54
"The significance of intestinal P-glycoprotein (P-gp) in determining the oral bioavailability of tacrolimus has been still controversial."( Limited interaction between tacrolimus and P-glycoprotein in the rat small intestine.
Achiwa, K; Aungst, BJ; Kobayashi, M; Oda, M; Saikachi, Y; Saitoh, H; Tadano, K; Takahashi, Y; Yamaguchi, M; Yuhki, Y, 2006
)
0.33
" In conclusion, pretreatment of naringin enhanced the oral bioavailability of verapamil."( Effect of naringin pretreatment on bioavailability of verapamil in rabbits.
Choi, JS; Yeum, CH, 2006
)
0.81
" It was found that oral bioavailability increases after administration of higher doses of talinolol."( In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.
Bolger, MB; Langguth, P; Spahn-Langguth, H; Tubic, M; Wagner, D, 2006
)
0.33
" Spline functions in convolutional modeling of verapamil formulation bioavailability and bioequivalence, as shown in the numerical simulation investigation, are very powerful additional tools for assessing the quality of new verapamil formulations in order to ensure that they are of the same quality as already registered formulations of the drug."( Spline functions in convolutional modeling of verapamil bioavailability and bioequivalence. I: conceptual and numerical issues.
Popović, J,
)
0.65
" Bioavailability of the new peroral retard formulation ranged from 19."( Spline functions in convolutional modeling of verapamil bioavailability and bioequivalence. II: study in healthy volunteers.
Daković-Svajcer, K; Jakovljević, V; Mikov, M; Mitić, R; Popović, J; Sabo, A,
)
0.39
" To compare the pharmacokinetic characteristics and bioavailability in six Beagle dogs after oral administration of VH-COERP and verapamil hydrochloride delayed-release pellets (VH-DRP) as reference."( [Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].
Chen, HX; Chen, XJ; Chen, ZP; Li, LR; Xiao, YY; Zhu, JB, 2006
)
0.88
" Compared with the VH-DRP, VH-COERP in vivo has an obviously lag time (4 h) , Tmax was also delayed (8 h) and the relative bioavailability was (94."( [Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].
Chen, HX; Chen, XJ; Chen, ZP; Li, LR; Xiao, YY; Zhu, JB, 2006
)
0.68
"The bioavailability of a new retard tablet formulation of verapamil was investigated in a randomized cross-over bioequivalence study on 12 healthy subjects."( Validation of the hepatic blood flow rate model for verapamil first-pass metabolism.
Popović, J,
)
0.63
" Co-administration with carvedilol increased ciclosporin bioavailability from 33% to 70%."( Carvedilol increases ciclosporin bioavailability by inhibiting P-glycoprotein-mediated transport.
Amioka, K; Ejiri, M; Kushihara, H; Kuzuya, T; Nabeshima, T; Nitta, A, 2007
)
0.34
"05) increased the bioavailability of verapamil in rats."( Effect of atorvastatin on the intravenous and oral pharmacokinetics of verapamil in rats.
Chang, KS; Choi, DH; Choi, JS; Han, HK; Hong, SP, 2008
)
0.85
" The oral bioavailability of verapamil was 32."( Effects of liver fibrosis on verapamil pharmacokinetics in rats.
Chen, M; Hu, XL; Wang, H; Xu, D, 2008
)
0.93
" To compare the relative effects of co-administration of P-gp/CYP modulators on intestinal lymphatic transport versus systemic bioavailability of saquinavir."( An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
Griffin, BT; O'Driscoll, CM, 2008
)
0.35
" A comparison of the relative enhancement of lymphatic transport and plasma bioavailability compared to control (i."( An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
Griffin, BT; O'Driscoll, CM, 2008
)
0.35
" Thus, a functional interplay between membrane Gb3 and MDR1 provides a more physiologically based approach to MDR1 regulation to increase the bioavailability of chemotherapeutic drugs."( Inhibition of multidrug resistance by adamantylgb3, a globotriaosylceramide analog.
Ackerley, C; Clarke, DM; De Rosa, MF; Ito, S; Lingwood, C; Wang, B, 2008
)
0.35
" Thus, the relative bioavailability increased by the same magnitude with atorvastatin."( Drug interaction between oral atorvastatin and verapamil in healthy subjects: effects of atorvastatin on the pharmacokinetics of verapamil and norverapamil.
Choi, DH; Choi, JS; Shin, WG, 2008
)
0.6
" The efflux of Mrp2, not P-gp, in the intestinal of the rats may be one of the reasons that lead to the low oral bioavailability of scutellarin."( Mrp2-related efflux of scutellarin in the intestinal absorption in rats.
Cao, F; Guo, J; Ping, Q; Zhang, H, 2008
)
0.35
" This accounted for the lower bioavailability of the compound in humans than in rats."( Identification of intestinal loss of a drug through physiologically based pharmacokinetic simulation of plasma concentration-time profiles.
Peters, SA, 2008
)
0.35
" Consequently hesperidin significantly enhanced bioavailability of verapamil in rats."( Enhanced bioavailability of verapamil after oral administration with hesperidin in rats.
Choi, JS; Piao, YJ, 2008
)
0.88
" The hepatic bioavailability of VP showed saturable metabolism, and the hepatic bioavailability of R-VP was higher than that of S-VP."( Stereoselective first-pass metabolism of verapamil in the small intestine and liver in rats.
Hanada, K; Ikemi, Y; Kukita, K; Mihara, K; Ogata, H, 2008
)
0.61
"Hypoxis hemerocallidea and l-canavanine interact with the efflux of nevirapine across intestinal epithelial cells and therefore can potentially increase the bioavailability of this antiretroviral drug when taken concomitantly."( Impact of traditional medicinal plant extracts on antiretroviral drug absorption.
Brown, D; Brown, L; Hamman, JH; Heyneke, O; van Wyk, JP, 2008
)
0.35
" The poor bioavailability of buagafuran may be partially due to the effect of P-gp on its absorption and transportation in intestinal lumen."( [Effect of P-glycoprotein on the absorption of buagafuran in rat intestinal lumen].
Li, E; Li, Y, 2008
)
0.35
" Although the effects of Echinacea purpurea on systemic P-gp mediated drug transport are probably limited, an influence on drug bioavailability can not be excluded."( Echinacea purpurea and P-glycoprotein drug transport in Caco-2 cells.
Hansen, TS; Nilsen, OG, 2009
)
0.35
"1 min and high clearance values suggesting that drug bioavailability will be considerably reduced, consequently affecting drug response and efficacy."( Quantitative determination of capsaicin, a transient receptor potential channel vanilloid 1 agonist, by liquid chromatography quadrupole ion trap mass spectrometry: evaluation of in vitro metabolic stability.
Beaudry, F; Vachon, P, 2009
)
0.35
" In continuation of the tests investigating the factors limiting bioavailability of boswellic acids, the present study examined the permeability of KBA and AKBA in human Caco-2 cell lines."( Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2.
Abdel-Tawab, M; Fricker, G; Hummel, J; Kanzer, J; Krüger, P; Schubert-Zsilavecz, M, 2009
)
0.35
"Oral bioavailability is one of the important criteria for development of a drug-lead candidate."( Involvement of P-glycoprotein and multidrug resistance associated protein 1 on the transepithelial transport of a mercaptoacetamide-based histone-deacetylase inhibitor in Caco-2 cells.
Jung, M; Konsoula, Z, 2009
)
0.35
" However, compared with the controls, both the AUC and the relative bioavailability of verapamil were significantly (p<0."( Effects of oral epigallocatechin gallate on the oral pharmacokinetics of verapamil in rats.
Choi, DH; Choi, JS; Chung, JH, 2009
)
0.81
" The absorption rate was jejunum > ileum > colon."( [Absorption of extractive Radix Paeoniae Alba in rat everted gut sacs and its interaction with P-glycoprotein].
Dong, Y; Li, Y; Yang, Q; Zhang, Y; Zhu, X, 2009
)
0.35
" After oral administration of diammonium glycyrrhizinate (50 mg kg(-1)), the peak plasma concentration (C(max)), area under the plasma concentration-time curve from zero to time tau (AUC(0-tau)), and absolute bioavailability of aconitine (0."( Effects of diammonium glycyrrhizinate on the pharmacokinetics of aconitine in rats and the potential mechanism.
Chen, L; Chen, YX; Davey, AK; Liu, XQ; Wang, JP; Yang, J, 2009
)
0.35
"This study was to investigate the effect of lovastatin on the bioavailability or pharmacokinetics of verapamil and its major metabolite, norverapamil, in rats."( Effects of lovastatin on the pharmacokinetics of verapamil and its active metabolite, norverapamil in rats: possible role of P-glycoprotein inhibition by lovastatin.
Chang, KS; Choi, DH; Choi, JS; Hong, SP; Koh, YY, 2009
)
0.82
" Consequently, the relative bioavailability of verapamil was also significantly increased (by 76."( Pharmacokinetic interaction between oral lovastatin and verapamil in healthy subjects: role of P-glycoprotein inhibition by lovastatin.
Choi, DH; Choi, JS; Chung, JH, 2010
)
0.86
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" Consequently, the absolute bioavailability (A."( Effects of simvastatin on the pharmacokinetics of verapamil and its main metabolite, norverapamil, in rats.
Choi, DH; Choi, JS; Li, C,
)
0.38
" HLJDD treatment increased the bioavailability of verapamil partly via inhibiting first-pass verapamil metabolism in the intestine."( Effect of Huang-Lian-Jie-Du-Decoction on pharmacokinetics of verapamil in rats.
Hu, N; Jing, XY; Liu, CH; Liu, XD; Wang, GJ; Xie, L; Xie, SS, 2010
)
0.86
" This model also has application for the screening of drug candidates for effects on oral bioavailability via effects on the subcellular distribution and trafficking of P-gp."( Characterization of PXR mediated P-glycoprotein regulation in intestinal LS174T cells.
Allen, J; Bebawy, M; Kota, BP; Roufogalis, BD; Tran, VH, 2010
)
0.36
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described."( Importance of physicochemical properties for the design of new pesticides.
Akamatsu, M, 2011
)
0.37
" Although the relative bioavailability of colonic administration of diclofenac, metformin and cevimeline compared to oral administration was similar regardless of the drug doses in the colon, colonic absorption of diltiazem varied according to the doses."( The relationship between the drug concentration profiles in plasma and the drug doses in the colon.
Hosoi, Y; Kanamaru, T; Konno, T; Nakagami, H; Tajiri, S; Yada, S; Yoshida, K, 2010
)
0.36
"P-glycoprotein is an efflux pump belonging to the ATP-binding cassette super-family that influences the bioavailability and disposition of many drugs."( Tumor necrosis factor alpha increases P-glycoprotein expression in a BME-UV in vitro model of mammary epithelial cells.
Al-Bataineh, MM; Gehring, R; Schultz, BD; van der Merwe, D, 2010
)
0.36
" The absolute bioavailability of verapamil was higher than that of control rats."( Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
Chen, G; Hu, N; Liu, H; Liu, L; Liu, X; Pan, X; Wang, G; Wang, X; Xie, L; Xie, S; Zhang, L, 2011
)
0.86
" PDE-310 exhibited high oral bioavailability (>70%) and was distributed well to various tissues except brain and testis."( Preclinical pharmacokinetics of PDE-310, a novel PDE4 inhibitor.
Ahn, SH; Bae, MA; Cheon, HG; Jeon, DJ; Kim, MS; Kwon, KI; Lee, BH; Park, JS; Rho, HJ; Seo, JW; Song, JS, 2011
)
0.37
"P-glycoprotein (P-gp), expressed in the apical membranes of the epithelial cells of the intestine, can reduce the oral bioavailability of a wide range of drugs."( Enhancing effect of N-octyl-O-sulfate chitosan on etoposide absorption.
Mo, R; Ping, Q; Sun, M; Xiao, Y; Zhang, C, 2011
)
0.37
" Thus, this study suggests that (thiolated) polymers display a promising potential to inhibit cytochrome P450s activity and might turn out to be potentially valuable tools for improving the oral bioavailability of actively secreted compounds by avoiding intestinal metabolism."( Thiomers: Inhibition of cytochrome P450 activity.
Bernkop-Schnürch, A; Iqbal, J; Sakloetsakun, D, 2011
)
0.37
" In vivo, the oral bioavailability of PTX loaded in NOSC micelles (PTX-M) was 6-fold improved in comparison with that of an orally dosed Taxol(®)."( The mechanism of enhancement on oral absorption of paclitaxel by N-octyl-O-sulfate chitosan micelles.
Jin, X; Ju, C; Li, N; Mo, R; Ping, Q; Sun, M; Zhang, C, 2011
)
0.37
" Apparent permeability values (Papp) and absorption rate constant (Ka) of baicalin in the duodenum increased gradually with higher concentrations."( [The enhancing effect of Angelica dahurica extracts on absorption of baicalin--the active composition of Scutellaria].
Cao, YC; Chen, XL; Liang, XL; Liao, ZG; Wang, GF; Yang, M; Zhao, GW; Zhu, JY, 2011
)
0.37
" The absorption rate of flavonoid glycoside was lower than that of aglycone; the flavonoids from Abelmoschus manihot flowers could be absorbed in all of the intestinal segments."( [Absorption of flavonoids from Abelmoschus manihot extract by in situ intestinal perfusion].
Duan, JA; Guo, JM; Qian, DW; Shu, Y; Xue, CF, 2011
)
0.37
" The goals of this study were to determine the mechanisms responsible for its poor oral absorption and to improve its bioavailability by overcoming the barrier to its absorption."( Enhancement of oral bioavailability of 20(S)-ginsenoside Rh2 through improved understanding of its absorption and efflux mechanisms.
Gao, S; Hu, M; Jiang, Z; Teng, Y; Wang, J; Wu, B; Yang, Z; Yin, T; You, M, 2011
)
0.37
"P-glycoprotein (P-gp) is an efflux transporter that regulates bioavailability of orally administered drugs at the intestinal epithelium."( Real-time analysis of P-glycoprotein-mediated drug transport across primary intestinal epithelium three-dimensionally cultured in vitro.
Fukuda, M; Mizutani, T; Mochizuki, W; Morikawa, R; Nagaishi, T; Nakamura, T; Nemoto, Y; Nozaki, K; Okamoto, R; Tsuchiya, K; Watanabe, M; Yamauchi, Y; Yui, S, 2012
)
0.38
" These observations indicated that the three alkaloids may not only be P-gp inhibitors but also its substrates; they interact with each other and can potentially enhance their own bioavailability when taken concomitantly."( Intestinal transport of pure diester-type alkaloids from an aconite extract across the Caco-2 cell monolayer model.
Li, N; Liu, Z; Ma, J; Sui, Z; Tsao, R, 2012
)
0.38
" In conclusion, the low bioavailability of FB2 is believed to be partially due to the P-gp mediated active efflux and first-pass metabolism in the rat intestine."( Role of P-glycoprotein in intestinal absorption of FB2, a promising Abl/Src dual tyrosine kinase inhibitor.
Hu, J; Huang, K; Li, X; Li, Y, 2012
)
0.38
" The P-gp efflux and CYP3A4 metabolism were involved in the poor intestinal absorption and low bioavailability of limonin."( [Transport of limonin in rat intestine in situ and Caco-2 cells in vitro].
He, L; Ke, X; Tian, JL; Zhang, XY, 2012
)
0.38
" In our preliminary study, notoginsenoside R₁ was able significantly to improve the bioavailability of geniposide in beagle dogs, but the underlying mechanisms remain unknown."( The effects of notoginsenoside R₁ on the intestinal absorption of geniposide by the everted rat gut sac model.
Chula, S; Hang, L; Jianning, S; Shi, R; Yinying, B, 2012
)
0.38
"Ginsenoside compound K (CK) is a bioactive compound with poor oral bioavailability due to its high polarity, while its novel ester prodrugs, the butyl and octyl ester (CK-B and CK-O), are more lipophilic than the original drug and have an excellent bioavailability."( Absorption mechanism of ginsenoside compound K and its butyl and octyl ester prodrugs in Caco-2 cells.
Deng, ZY; Hu, JN; Li, HY; Li, W; Liu, XR; Luo, T; Ye, H; Zhang, B; Zheng, YN; Zhu, XM, 2012
)
0.38
"The oral (po) bioavailability of gemifloxacin mesylate in rats and its possible association with efflux transporters was investigated."( Transport of gemifloxacin, a 4th generation quinolone antibiotic, in the Caco-2 and engineered MDCKII cells, and potential involvement of efflux transporters in the intestinal absorption of the drug.
Chong, S; Chung, SJ; Jin, HE; Kim, DD; Kim, SB; Shim, CK; Shim, WS; Song, B, 2013
)
0.39
"To study the absorption of baicalin (BA), baicalin-phospholipid complex (BA-PC), and two kinds of self-microemulsifying drug delivery system (SMEDDS) of BA-PC (BA-PC-NE-SMEDDS with natural emulsifier and BA-PC-NS-SMEDDS with nonionic surfactants) and predict the ability of improving bioavailability through changing the formulation of BA."( [Drug delivery systems of baicalin, baicalin-phospholipid complex and self-microemulsifying drug across Caco-2 cell model].
Chen, L; Huang, SH; Long, XY; Pan, SJ; Wu, HY, 2012
)
0.38
" A good correlation between the dissolution profiles and bioavailability indicated a linear relationship between in vitro - in vivo data."( Modulation of drug release by utilizing pH-independent matrix system comprising water soluble drug verapamil hydrochloride.
Baviskar, D; Jain, D; Sharma, R, 2013
)
0.61
"It may be concluded that BCRP plays an important role in the intestinal efflux of MED-5 and limits the bioavailability after oral administration of MED-15."( Evaluation of intestinal absorption of amtolmetin guacyl in rats: breast cancer resistant protein as a primary barrier of oral bioavailability.
Li, X; Liu, D; Rong, Z; Xiang, D; Xu, Y; Zhang, C, 2013
)
0.39
" Etoposide SMEDDS were orally administered to rats for in vivo bioavailability investigation."( Enhanced intestinal absorption of etoposide by self-microemulsifying drug delivery systems: roles of P-glycoprotein and cytochrome P450 3A inhibition.
Huang, J; Li, G; Si, L; Xue, K; Zhao, G, 2013
)
0.39
" The aim of the present study was to develop and characterize chitosan mucoadhesive microspheres of verapamil hydrochloride (VRP) for intranasal delivery as an alternative to oral VRP which suffers low bioavailability (20%) due to extensive first pass effect."( Bioavailability enhancement of verapamil HCl via intranasal chitosan microspheres.
Abdel Mouez, M; Geneidi, AS; Mansour, S; Zaki, NM, 2014
)
0.9
"One of the key factors in drug discovery is related to the metabolic properties of the lead compound, which may influence the bioavailability of the drug, its therapeutic window, and unwanted side-effects of its metabolites."( High-throughput, computer assisted, specific MetID. A revolution for drug discovery.
Fontaine, F; Plasencia, G; Serra, B; Zamora, I, 2013
)
0.39
" Rise in oral bioavailability of PCT after pre-treatment by cyclosporine was lower than ibuprofen."( Enhanced oral bioavailability of paclitaxel by concomitant use of absorption enhancers and P-glycoprotein inhibitors in rats.
Ahmadi, F; Mohammadi-Samani, S; Montaseri, H; Sobhani, Z; Zarea, B, 2013
)
0.39
" In this study, we systematically evaluated the potential role of P-glycoprotein (P-gp) in the mechanisms underlying the low and variable bioavailability of oral AC."( P-glycoprotein is responsible for the poor intestinal absorption and low toxicity of oral aconitine: in vitro, in situ, in vivo and in silico studies.
Li, Z; Liu, F; Liu, K; Ruan, J; Xu, L; Yang, C; Zhang, T; Zhang, Z, 2013
)
0.39
" Its oral bioavailability is low and its intestinal absorption mechanism is not clear."( Intestinal absorption of raltitrexed and evaluation of the effects of absorption enhancers.
Li, X; Lu, Y; Yin, Z; Yu, Y; Zhao, X, 2013
)
0.39
"Various potential molecules with putative positive role in stroke pathology have failed to confer neuro-protection in animal models due to their insufficient bioavailability in brain."( Verapamil augments the neuroprotectant action of berberine in rat model of transient global cerebral ischemia.
Chopra, K; Singh, DP, 2013
)
1.83
" In summary, our results clearly demonstrate, for the first time, that poor bioavailability of these three prenylated flavonoids is the result of poor intrinsic permeability and efflux by apical efflux transporters."( Study on the mechanism of intestinal absorption of epimedins a, B and C in the Caco-2 cell model.
Chen, Y; Gao, X; Liu, C; Qu, D; Wang, Y; Zhou, J, 2014
)
0.4
" Coadministration of a mixture of linoleic acid-monoolein significantly increased the extent of intestinal lymphatic transport of PTX, but it had little impact on the absolute oral bioavailability of PTX."( Effects of lipid vehicle and P-glycoprotein inhibition on the mesenteric lymphatic transport of paclitaxel in unconscious, lymph duct-cannulated rats.
An, D; Cai, Q; Deng, X; Li, Z; Shen, T; Zhong, M, 2016
)
0.43
" However, its oral bioavailability has not been known."( Permeability of rhynchophylline across human intestinal cell in vitro.
Li, M; Ma, B; Sun, G; Sun, J; Sun, X; Wang, J; Xu, H, 2014
)
0.4
" This led to the identification of selected triazolopyrimidines and phenylpyrimidines that are orally bioavailable and brain-penetrant without disruption of Pgp function."( Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
Ballatore, C; Brunden, KR; Cornec, AS; Gay, B; Hoye, AT; Hyde, E; James, MJ; Lee, VM; Lou, K; Smith, AB; Trojanowski, JQ; Yao, Y, 2014
)
0.4
" Moreover, pharmacokinetic studies were performed in animal models to evaluate the absolute bioavailability of oral doses (Foral) of different compounds."( Development, validation, and application of a novel 7-day Caco-2 cell culture system.
Bi, H; Cai, Y; Chen, P; Hu, J; Hu, R; Huang, M; Xu, C,
)
0.13
" Furthermore, pharmacokinetic studies of several compounds performed in animal models revealed that the absolute bioavailability of oral doses in vivo was well correlated with the Caco-2 permeability in vitro."( Development, validation, and application of a novel 7-day Caco-2 cell culture system.
Bi, H; Cai, Y; Chen, P; Hu, J; Hu, R; Huang, M; Xu, C,
)
0.13
" Although the anticancer activity of PPI has been well demonstrated, information regarding the pharmacokinetics and bioavailability is limited."( Study on the pharmacokinetics profiles of polyphyllin I and its bioavailability enhancement through co-administration with P-glycoprotein inhibitors by LC-MS/MS method.
Ding, CH; Li, SL; Long, MH; Mao, Q; Shakya, S; Zhu, H; Zhu, SC, 2015
)
0.42
"Bazedoxifene, a novel selective estrogen receptor modulator, has complex pharmacokinetics with rapid absorption, high metabolic clearance, low oral bioavailability (6."( Efflux and uptake transporters involved in the disposition of bazedoxifene.
Berginc, K; Kristl, A; Lušin, TT; Mrhar, A; Stieger, B; Trontelj, J, 2016
)
0.43
"To evaluate the effect of Radix euphorbiae pekinensis extract on the permeability and bioavailability of paclitaxel co-administered orally."( [Effect of Radix euphorbiae pekinensis extract on bioavailability of paclitaxel after their oral co-administration].
Li, M; Liu, S; Peng, L; Wang, S; Yang, F, 2015
)
0.42
"Based on Ussing Chamber and in vivo experiment, the permeability and bioavailability of paclitaxel were evaluated after oral co-administration with radix euphorbiae pekinensis in rats."( [Effect of Radix euphorbiae pekinensis extract on bioavailability of paclitaxel after their oral co-administration].
Li, M; Liu, S; Peng, L; Wang, S; Yang, F, 2015
)
0.42
"Co-administration of Radix euphorbiae pekinensis extract can increase the bioavailability of orally administered paclitaxel."( [Effect of Radix euphorbiae pekinensis extract on bioavailability of paclitaxel after their oral co-administration].
Li, M; Liu, S; Peng, L; Wang, S; Yang, F, 2015
)
0.42
" Metoprolol and Verapamil absorption rate coefficients were determined using the in situ closed loop perfusion model in four strains of rats and in both genders."( Drug gastrointestinal absorption in rat: Strain and gender differences.
Bermejo, M; Colon-Useche, S; González-Álvarez, I; González-Álvarez, M; Mangas-Sanjuan, V; Oltra-Noguera, D, 2015
)
0.76
" The absolute oral bioavailability of pristimerin is 28."( Absorption and metabolism characteristics of pristimerin as determined by a sensitive and reliable LC-MS/MS method.
Dong, C; Gao, Y; Liu, H; Peng, J; Xu, C; Xu, S, 2015
)
0.42
"This present study investigated the absorption kinetics of echinacoside (ECH) in situ and in vitro and its oral bioavailability in rats."( Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil.
Kou, JP; Li, F; Shen, JY; Yang, XL; Yang, ZL, 2015
)
0.65
" Pharmacokinetics study was performed to investigate the influences of verapamil and clove oil on ECH bioavailability in vivo."( Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil.
Kou, JP; Li, F; Shen, JY; Yang, XL; Yang, ZL, 2015
)
0.89
"The absorption and bioavailability of ECH were enhanced by verapamil and clove oil, respectively, both in vitro and in vivo."( Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil.
Kou, JP; Li, F; Shen, JY; Yang, XL; Yang, ZL, 2015
)
0.9
" As a result of this, a significant decrease in the intestinal uptake and peroral bioavailability of the P-glycoprotein substrates (verapamil and atorvastatin) was observed along with the progression of diabetes as compared to normal animals."( Increased intestinal P-glycoprotein expression and activity with progression of diabetes and its modulation by epigallocatechin-3-gallate: Evidence from pharmacokinetic studies.
Agarwal, M; Dash, RP; Ellendula, B; Nivsarkar, M, 2015
)
0.62
" Unfortunately, due to the low bioavailability and consequently low blood level, they cannot be used for cancer therapy."( Anthocyanidins but not anthocyanins inhibit P-glycoprotein-mediated calcein extrusion - possible implication for orally administered drugs.
Vrzal, R, 2016
)
0.43
" Similarly absorption rate constant (Ka), fraction absorbed (Fab) and effective permeability (Peff) of FEX were increased significantly in ileum of RSV and VER pretreated groups when compared to FEX alone group."( Effect of resveratrol on the pharmacokinetics of fexofenadine in rats: Involvement of P-glycoprotein inhibition.
Bedada, SK; Neerati, P; Yellu, NR, 2016
)
0.43
" P-gp inhibitors could serve as helpful tools to enhance the oral bioavailability of those substances."( The application of P-gp inhibiting phospholipids as novel oral bioavailability enhancers - An in vitro and in vivo comparison.
Burhenne, J; Fricker, G; Mylius, P; Schubert, R; Weinheimer, M, 2017
)
0.46
" The chitosan composite transfersomal formulation exhibited absolute bioavailability of 81."( Composite chitosan-transfersomal vesicles for improved transnasal permeation and bioavailability of verapamil.
Abdel-Mottaleb, M; Geneidi, AS; Mansour, S; Mouez, MA; Nasr, M, 2016
)
0.65
"P-glycoprotein (P-gp), an important efflux transporter in intestine, regulates the bioavailability of orally taken drugs."( A Novel Model of P-Glycoprotein Inhibitor Screening Using Human Small Intestinal Organoids.
Li, D; Liu, M; Sun, J; Wang, X; Zeng, Z; Zhang, X; Zhang, Y; Zhao, J, 2017
)
0.46
" These results indicate that 4,8-sphingadienine that originates from the glucosylceramide of higher plants is poorly absorbed in the intestine because of efflux by P-glycoprotein and can be incorporated into a ceramide moiety, at least in part, in intestinal endothelial cells."( Selective Absorption of Dietary Sphingoid Bases from the Intestine via Efflux by P-Glycoprotein in Rats.
Aida, K; Fujii, A; Hirata, T; Manabe, Y; Sugawara, T; Tsuduki, T, 2017
)
0.46
" Co-administration of verapamil resulted in a modest increase of the apparent bioavailability of oxcarbazepine by 12% (10-28), but did not affect parent or metabolite clearances."( Population pharmacokinetics of oxcarbazepine and its metabolite 10-hydroxycarbazepine in healthy subjects.
Alexandre Junior, V; Antunes, NJ; Coelho, EB; Della Pasqua, O; Lanchote, VL; Takayanagui, OM; Tozatto, E; van Dijkman, SC; van Hasselt, JGC; Wichert-Ana, L, 2017
)
0.77
"Herein, thioglycolic acid modified N-octyl-O, N'-glycol chitosan (N-mercapto acetyl-N'-octyl-O, N″-glycol chitosan, abbreviated as SH-OGC) was synthesized to improve the oral bioavailability of paclitaxel (PTX)."( N-mercapto acetyl-N'-octyl-O, N″-glycol chitosan as an efficiency oral delivery system of paclitaxel.
Chen, Q; Fu, Y; Huo, M; Li, L; Liu, Y; Mu, Y; Xu, W; Yin, T; Zhou, J, 2018
)
0.48
" Pharmacokinetic experiments show oral bioavailability through gastric absorption."( Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
Cescon, DW; Hansen, MD; Hoj, JP; Siddiqui-Jain, A, 2018
)
0.48
" Compound 12g with MIC values of 5 μg/ml as a representative may possess better oral bioavailability and indicated high permeability by the parallel artificial membrane permeation assay of the blood-brain barrier (PAMPA-BBB)."( Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
An, Q; Deng, Y; Liu, P; Luo, Y; Sang, Z; Tang, Y; Wang, T; Yang, T; Yang, Y; Zhang, T, 2018
)
0.48
" In vivo and in vitro studies were performed to assess absolute bioavailability of finerenone, the effect of metabolic enzyme inhibitors on the pharmacokinetics of finerenone and its metabolites, the quantitative contribution of the involved enzymes cytochrome P450 (CYP) 3A4 and CYP2C8 and the relevance of gut wall versus liver metabolism."( Pharmacokinetics of the Novel, Selective, Non-steroidal Mineralocorticoid Receptor Antagonist Finerenone in Healthy Volunteers: Results from an Absolute Bioavailability Study and Drug-Drug Interaction Studies In Vitro and In Vivo.
Engelen, A; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2018
)
0.48
" Absolute bioavailability was assessed in volunteers receiving finerenone orally and by intravenous infusion (n = 15) and the effects of erythromycin (n = 15), verapamil (n = 13) and gemfibrozil (n = 16) on finerenone pharmacokinetics were investigated."( Pharmacokinetics of the Novel, Selective, Non-steroidal Mineralocorticoid Receptor Antagonist Finerenone in Healthy Volunteers: Results from an Absolute Bioavailability Study and Drug-Drug Interaction Studies In Vitro and In Vivo.
Engelen, A; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2018
)
0.68
" Pharmacokinetic studies indicate that 1 has an oral bioavailability with an average F-value of 27."( An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
Eslamimehr, S; Franzblau, SG; Kong, Y; Kurosu, M; Lemieux, MR; Mitachi, K; Park, F; Pressly, JD; Siricilla, S; Wang, Y; Yang, D, 2018
)
0.48
" Pharmacokinetic results indicate that PTX-loaded CR PMs could significantly enhance the oral bioavailability of PTX."( Preparation and evaluation of carboxymethyl chitosan-rhein polymeric micelles with synergistic antitumor effect for oral delivery of paclitaxel.
Chu, K; Guo, Y; Han, L; Li, T; Ouyang, H; Qiu, L; Wang, X; Xu, W, 2019
)
0.51
" PTX/OPPC micelles possessed improved intestinal epithelial permeability and oral bioavailability of PTX evaluated by in situ perfusion and pharmacokinetic studies."( Self-assembled micelles based on N-octyl-N'-phthalyl-O-phosphoryl chitosan derivative as an effective oral carrier of paclitaxel.
Hou, S; Ju, C; Qu, D; Qu, G; Tian, C; Xue, L; Zhang, C; Zhu, J, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"In oral bioavailability studies, evaluation of the absorption and transport of drugs and food components across the intestinal barrier is crucial."( Dynamic in vitro intestinal barrier model coupled to chip-based liquid chromatography mass spectrometry for oral bioavailability studies.
Bouwmeester, H; Gerssen, A; Nielen, MWF; Santbergen, MJC; van der Zande, M, 2020
)
0.56
" An absolute bioavailability study informed the hepatic and gastric availability."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
"We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity."( Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia.
Kondratenko, SN; Kovachevich, IV; Kukes, VG; Polyakov, AV; Repenkova, LG; Savelyeva, MI; Svistunov, AA, 2020
)
0.81
" The simulations suggest that for highly soluble drugs, such as verapamil, the predicted bioavailability was comparable pre- and post-RYGBS."( PBPK modeling of CYP3A and P-gp substrates to predict drug-drug interactions in patients undergoing Roux-en-Y gastric bypass surgery.
Chan, LN; Chen, KF; Lin, YS, 2020
)
0.8
" The poor bioavailability limits its further development and potential clinic application."( Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism.
Ci, X; Gu, Y; Liu, C; Ma, H; Shang, H; Si, D; Sun, Y; Wang, Z, 2021
)
0.99
" It was demonstrated that P-gp and CYP3A were involved in the transport and metabolism of RA, which might contribute to the low oral bioavailability of RA."( Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism.
Ci, X; Gu, Y; Liu, C; Ma, H; Shang, H; Si, D; Sun, Y; Wang, Z, 2021
)
0.99
"A novel, integrated, in vitro gastrointestinal (GI) system is presented to study oral bioavailability parameters of small molecules."( A versatile, compartmentalised gut-on-a-chip system for pharmacological and toxicological analyses.
Bouwmeester, H; de Haan, P; Nielen, MWF; Santbergen, MJC; van der Zande, M; Verpoorte, E, 2021
)
0.62
"P-glycoprotein (P-gp) over-expression plays a vital role in not only systemic drug bioavailability but also cancer multi-drug resistance (MDR)."( A novel flavonoid from Fissistigma cupreonitens, 5‑hydroxy‑7,8‑dimethoxyflavanone, competitively inhibited the efflux function of human P-glycoprotein and reversed cancer multi-drug resistance.
Hung, CC; Lan, YH; Lin, KI; Lin, YC; Teng, YN; Thang, TD, 2021
)
0.62
" However, the limited oral bioavailability of irinotecan poses a problem for its oral delivery."( Possible roles of intestinal P-glycoprotein and cytochrome P450 3A on the limited oral absorption of irinotecan.
Arimori, K; Furuya, Y; Hidaka, M; Kawano, Y; Ono, H; Yamasaki, K, 2021
)
0.62
" Indeed, the oral bioavailability of irinotecan was increased when verapamil was orally pre-administered."( Possible roles of intestinal P-glycoprotein and cytochrome P450 3A on the limited oral absorption of irinotecan.
Arimori, K; Furuya, Y; Hidaka, M; Kawano, Y; Ono, H; Yamasaki, K, 2021
)
0.86
" Additionally, an ∼85% correlation was obtained between PAMPA pH 5 permeability and in vivo oral bioavailability in mice and rats."( Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability.
Itkin, M; Kabir, M; Mathé, EA; Nguyễn, ÐT; Padilha, EC; Shah, P; Shinn, P; Siramshetty, V; Wang, AQ; Williams, J; Xu, X; Yu, KR; Zhao, T, 2022
)
0.72
" Multiple-target inhibitors of efflux transporter can be overcome the resistance and improve the oral bioavailability of chemotherapy drugs."( Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
Cai, Z; Ghaleb, H; Huang, W; Jiang, Y; Liu, Y; Qian, H; Qiu, Q; Shi, W; Yin, Z; Zhang, P; Zhou, J; Zou, F, 2022
)
0.72
"Niclosamide, a widely-used anthelmintic drug, inhibits SARS-CoV-2 virus entry through TMEM16F inhibition and replication through autophagy induction, but the relatively high cytotoxicity and poor oral bioavailability limited its application."( Design, synthesis and biological evaluations of niclosamide analogues against SARS-CoV-2.
Chang, SY; Chao, TL; Chou, YT; Jan, JT; Juang, YP; Liang, PH; Lin, RX; Ma, HH, 2022
)
0.72
"To study the pharmacokinetics and relative bioavailability of drugs of different chemical structure and pharmacological action under conditions simulating the effects of some factors of spaceflight, as well as the peculiarities of the pharmacokinetics of acetaminophen under long-term spaceflight conditions."( Study of the pharmacokinetics of various drugs under conditions of antiorthostatic hypokinesia and the pharmacokinetics of acetaminophen under long-term spaceflight conditions.
Badriddinova, LY; Kondratenko, SN; Kovachevich, IV; Polyakov, AV; Repenkova, LG; Savelyeva, MI; Shikh, EV; Svistunov, AA, 2021
)
0.62
"Verapamil, a calcium channel blocker has poor bioavailability (20-30%) owing to extensive hepatic first-pass metabolism."( Verapamil hydrochloride loaded solid lipid nanoparticles: Preparation, optimization, characterisation, and assessment of cardioprotective effect in experimental model of myocardial infarcted rats.
Agnihotri, VV; Agrawal, YO; Goyal, SN; Husain, M; Mahajan, HS; Ojha, S; Patil, KD; Patil, TS; Sharma, C; Sodgir, V, 2022
)
3.61
" The changes to the integrity of the intestine and its drug metabolising enzymes and transporters (DMETs) can alter the oral bioavailability of drugs."( Altered Bioavailability and Pharmacokinetics in Crohn's Disease: Capturing Systems Parameters for PBPK to Assist with Predicting the Fate of Orally Administered Drugs.
Alrubia, S; Barber, J; Chen, Y; Mao, J; Rostami-Hodjegan, A, 2022
)
0.72
" LP and VPH have low bioavailability and long half-life."( Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization.
Chen, WB; Chen, YS; Liu, YQ; Qin, ZC; Sun, YY; Zhang, SY, 2022
)
1.03
"The ATP-binding cassette transporter P-glycoprotein (P-gp) limits the oral bioavailability of many drugs."( Characterization of P-glycoprotein orthologs from human, sheep, pig, dog, and cat.
Azimi, M; Brett, CM; Giacomini, CP; Giacomini, KM; Riselli, A; Silva, DB; Yee, SW, 2023
)
0.91

Dosage Studied

50 µg R/S-(14)C-verapamil was dosed intravenously to human volunteers. No significant differences in pharmacokinetics (AUCpo, Cmax, tmax, CLo, F and R/ S enantiomer ratio) between morning and evening treatment.

ExcerptRelevanceReference
"The effect of diazoxide, verapamil and compound D600 on calcium and isoproterenol dose-response relationships was investigated in isolated rabbit atrial preparations."( Effect of diazoxide, verapamil and compound D600 on isoproterenol and calcium-mediated dose-response relationships in isolated rabbit atrium.
Bristow, MR; Green, RD, 1977
)
0.88
"53% of total tissue content, showed parallelism when serial dilutions were compared to the immunoassay dose-response curve and eluted similarly to synthetic somatostatin on Sephadex G-25 (f) chromatography."( Immunoreactive somatostatin release from rat spinal cord in vitro.
Adams, C; Kronheim, S; Pimstone, B; Sheppard, M, 1979
)
0.26
" The dosage was 3 x 80 mg/die during 4 weeks."( [Exertion-electrocardiographic and hemodynamic studies with oral verapamil in chronic ischemic heart disease].
Assmann, I; Fiehring, H; Oltmanns, G; Schwela, H, 1978
)
0.5
"Evidence of selective inhibition, differences in dose-response relationships, and cross-tachyphylaxis studies suggest that separate receptors and/or mechanisms may be involved in responses to angiotensin (Ang), [Sar1]Ang II, and Ang III (= des-Asp1-Ang II)."( Demonstration of different contractile mechanisms for angiotensin II and des-Asp1-angiotensin II in rabbit aortic strips.
Ackerly, JA; Moore, AF; Peach, MJ, 1977
)
0.26
" The dosage varied according to the weight of the infant."( Effect of verapamil in infants with paroxysmal supraventricular tachycardia.
Cabrera, A; Iglesias-Berengué, J; Permanyer-Miralda, G; Roca-Llop, J; Sagristá-Sauleda, J; Sauleda-Parés, J; Soler-Soler, J, 1979
)
0.66
" The average clinical dosage amounts to 1 (0,5--2) mcg/kg/min."( [Diaplacental transfer of verapamil in guinea pigs (author's transl)].
Blümel, G; Erhardt, W; Hege, HG; Strigl, R, 1979
)
0.56
" It is important to know how the pharmacokinetics of a drug vary with different disease states so that appropriate adjustments to dosage can be made."( Series on pharmacology in practice. 2. Antiarrhythmic drug therapy.
Federman, J; Vlietstra, RE, 1979
)
0.26
"The effect of inhibiting isoprenaline-induced intracellular calcium accumulation on the degree of damage produced in the rat myocardium by this amine has been investigated by simultaneously dosing rats with the calcium antagonistic drug D600."( The effect of a calcium antagonist (D600) on isoprenaline-induced myocardial necrosis in the rat.
Powell, T; Rowles, PM; Steen, E; Woolf, N, 1979
)
0.26
"Fifty pregnant women admitted consecutively on account of threatened abortion or premature labour and treated with Ritodrine and Verapamil intravenously in the usual dosage were investigated with respect to creatine kinase activity and, in the event of a raised level, its isoenzyme creatine kinase--MB."( [Does myocardial damage arise as a result of administration of tocolytic drugs? (author's transl)].
Dienstl, F; Lechner, W, 1979
)
0.46
"Fifty pregnant women admitted consecutively on account of threatened abortion or premature labour and treated with Ritodrine and Verapamil intravenously in the usual dosage were investigated with respect to creatine kinase activity and, in the event of a raised level, its isoenzyme creatine kinase--MB."( [Does myocardial damage arise as a result of administration of tocolytic drugs? (author's transl)].
Dienstl, F; Lechner, W, 1979
)
0.46
" It can be concluded that verapamil in a dosage sufficient to terminate the arrhythmia did not exhibit additional negative inotropic effects."( Haemodynamic effects of supraventricular tachycardias and their alterations by electrically and verapamil induced termination.
Merle, H; Schlepper, M; Weppner, HG, 1978
)
0.78
" The dose-response relationship for the inhibitory action of verapamil is shifted to higher concentrations of the drug when the concentration of calcium in the perfusate is increased."( Calcium antagonists and islet function. II. Interaction of theophylline and verapamil.
Devis, G; Malaisse, WJ; Somers, G; Van Obberghen, E, 1976
)
0.73
" The dose-response relation with regard to the maximum rate of rise of the Ca spike showed no noticeable difference in effect between D600 and verapamil."( The effects of D600 and verapamil on action potential in the X-organ neuron of the crayfish.
Kuroda, T, 1976
)
0.76
" It can be concluded that echocardiography is a feasible tool in determining changes of left ventricular dynamics during administration of vasoactive drugs, in indicating the individual dosage of a vasoactive drug in each patient and the follow-up the course of the therapeutic success."( [Echocardiographic evaluation of left ventricular function during therapy with cardiovascularly effective drugs].
Stefan, G, 1976
)
0.26
" Quinidine (10(-6) M to 10(-1) M) produced a prompt reduction in Na influx, maximum after 30 seconds of exposure, and dose-dependent along a sigmoid log dose-response curve."( Effect of quinidine and temperature on sodium uptake and contraction frequency of cultured rat myocardial cells.
McCall, D, 1976
)
0.26
" infusion of the isomers, at a dosage inducing identical reduction of maximum follow frequency, is accompanied by a decrease in left ventricular dp/dtmax with (-)verapamil, whereas with the (+)isomer a significant increase of dp/dtmax is observed at a certain dose level."( Relationship of antiarrhythmic to inotropic activity and antiarrhythmic qualities of the optical isomers of verapamil.
Raschack, M, 1976
)
0.66
" The slope of the dose-response curve of nifedipine is, however, significantly less steep than that of verapamil."( Differences in the cardiac actions of the calcium antagonists verapamil and nifedipine.
Raschack, M, 1976
)
0.71
" The dose-response curve for phenylephrine was markedly shifted to the right by raising the temperature (pD2=0."( Influence of temperature on the positive inotropic effects mediated by alpha-and-beta-adrenoceptors in the isolated rabbit papillary muscle.
Endoh, M; Schümann, HJ; Wagner, J, 1975
)
0.25
"Mechanical activity of the isolated portal vein and thoracic aorta of the guinea-pig was recorded and the effects of verapamil and D 600 (methoxy-verapamil) on the dose-response curves to noradrenaline were measured."( Differentiation of calcium activation mechanisms in vascular smooth muscle by selective suppression with verapamil and D 600-1.
Golenhofen, K; Hermstein, N, 1975
)
0.68
" The effects of phenylephrine and isoprenaline on the isometric contraction of guinea-pig ventricle were compared over the whole range of their respective dose-response curves."( Studies on the positive inotropic effect of phenylephrine: a comparison with isoprenaline.
Ledda, F; Marchetti, P; Mugelli, A, 1975
)
0.25
" In equipotent dosage its duration of action is clearly superior to that of conventional verapamil dragées."( [Demonstration of the long term action of an oral retard preparation of verapamil in the conscious dog].
Raschack, M, 1975
)
0.71
" Current data suggest that only early stages of coronary atheromatosis may be affected by treatment with calcium antagonists; however, optimum drug, dosage and suitable patients are yet to be defined."( Can the coronary atherosclerotic process be influenced by calcium antagonists?
Cieslinski, G; Kaltenbach, M; Kober, G; Schneider, W, 1992
)
0.28
" The dosage was titrated upward until the goal blood pressure was achieved."( Enalapril and verapamil in the treatment of isolated systolic hypertension in the elderly.
Bruner, DE; Davis, JR; Espinel, CH; Williams, JL,
)
0.49
" Since most authors take as optimal therapeutic level of verapamil in blood the range of 100-200 ng/ml, it seems that dosage regimen of 2 x 80 mg/day can be recommended."( [Pharmacokinetic investigations of verapamil used as a concomitant drug in treatment of premature labor].
Jankowski, A; Kotzbach, R; Skublicki, S; Szymański, W, 1992
)
0.81
" The maximal binding and Kd values for skeletal muscle PN 200-110 binding were increased only at the highest dosage for 8 weeks duration."( Effect of chronic administration of verapamil on Ca++ channel density in rat tissue.
Czubryt, MP; Docherty, JC; Dubo, DF; Gilchrist, JS; Lonsberry, BB; Maddaford, TG; Pierce, GN, 1992
)
0.56
" Verapamil, given for 1 week at a dosage of 240 mg orally to eight healthy volunteers, induced a significant elevation of basal PRL levels (17."( Effects of calcium channel blockade with verapamil on the prolactin responses to TRH, L-dopa, and bromocriptine.
Kamal, TJ; Molitch, ME, 1992
)
1.46
" Correlations between log plasma verapamil concentration and percentage increase in PR interval were greater after sublingual compared with oral dosing in all volunteers."( Pharmacokinetics and pharmacodynamics of verapamil following sublingual and oral administration to healthy volunteers.
Fort, S; John, DN; Lewis, MJ; Luscombe, DK, 1992
)
0.83
" Left ventricular ejection fractions at rest or exercise were not significantly changed following either acute intravenous (rest 33%; exercise 38%) or chronic oral dosing with verapamil (rest 35%; exercise 43%) when compared with placebo (rest 34%; exercise 42%)."( Low-dose verapamil in middle-aged and elderly patients with angina pectoris: no evidence of increased susceptibility to the cardiac effects.
Ahmed, JH; Elliott, HL; Meredith, PA; Reid, JL, 1992
)
0.89
" Islets from both genetic models showed a left-shifted glucose dose-response curve for insulin release (concentrations for half-maximal release, 5 to 6 mmol/L v 12 to 13 mmol/L in LA/N lean littermates and 3 mmol/L v 10 mmol/L in lean SHR/N)."( Genetically obese rats with (SHR/N-cp) and without diabetes (LA/N-cp) share abnormal islet responses to glucose.
Recant, L; Timmers, KI; Voyles, NR, 1992
)
0.28
" Dose-response curves for all the drugs tested were similar and a significant dose-dependent antinociceptive action was evident in the formalin and writhing tests."( Antinociceptive effects of Ca2+ channel blockers.
Bustamante, D; Fernandez, E; Kramer, V; Miranda, HF; Paeile, C; Pelissier, T; Pinardi, G; Saavedra, H, 1992
)
0.28
" We are currently studying treatment of tumor-bearing animals with a cumulative dosage regimen of doxorubicin in the presence and absence of verapamil."( Effects of verapamil on the acute toxicity of doxorubicin in vivo.
Anderson, J; Baker, PB; Desai, P; Dwivedi, C; Engineer, FN; Sharma, HM; Sridhar, R, 1992
)
0.87
" Although specific recommendations for calcium dosing in the overdose situation have not been rigorously studied, maintenance of a normal serum ionized calcium concentration is suggested."( Verapamil overdose: case report and review of the literature.
Crain, JL; Edwards, TD; Stiller, RA; Watling, SM, 1992
)
1.73
" With the portal vein isolated, the parathyroid hormone shifted the dose-response curves of KCl and acetylcholine to the right."( Responsiveness to synthetic parathyroid hormone in the portal vein of portal hypertensive rats.
Chao, TW; Kuo, JS; Pang, PK; Yang, MC; Yu, PC, 1992
)
0.28
"The effect of verapamil therapy in a dosage of 120 thrice daily on the mortality and re-infarction from the time of admission and for the subsequent six months was investigated in a double-blind, randomized, placebo-controlled, multicentre investigation (The Danish Verapamil Infarction Trial (DAVIT I))."( [Verapamil therapy improves the prognosis after acute myocardial infarction. A review over the Danish studies of verapamil therapy during and after acute myocardial infarction].
Hansen, JF, 1992
)
1.55
"A stability-indicating reversed phase high-performance liquid chromatographic assay for prazosin was developed to investigate the feasibility of a transdermal dosage form."( High-performance liquid chromatographic assay of prazosin for transdermal screening studies.
Tenjarla, SN; Tseggai, A, 1992
)
0.28
" An increase in the dosage (360 mg/24 hours in two subdoses) could be made during the first month of treatment if the diastolic blood pressure remained greater than or equal to 95 mmHg."( [Sustained-released verapamil and ambulatory recording of blood pressure in mild to moderate essential hypertension].
Bernadet, P; Durand, D; Galey, C; Maarek-Charbit, M; Suc, JM, 1992
)
0.61
" Dose-response studies indicated that exceedingly high doses of DTIC were necessary to produce antimetastatic effects even when drug treatment was combined with the calcium channel blocker verapamil."( Efficacy of dacarbazine (DTIC) in preventing metastases arising from intraocular melanomas in mice.
Gamel, JW; Niederkorn, JY; Sanborn, GE, 1992
)
0.47
"Spontaneous motor activity was measured in six baboons during chronic oral dosing with a diuretic (hydrochlorothiazide/triamterene), a calcium channel blocker (verapamil), and a combination of the two drugs."( Chronic hydrochlorothiazide and verapamil effects on motor activity in hypertensive baboons.
Allen, RP; Hienz, RD; Turkkan, JS, 1992
)
0.76
" The dose-response curves for nifedipine, with respect to the reduction of contractile force and contracture, were identical."( The polycationic compound gentamicin inhibits the calcium paradox in guinea-pig hearts.
Gödicke, J; Jacobsen, L; Lüllmann, H; Mülder, G, 1992
)
0.28
" This product allows for once-daily dosing up to 240 mg/d; however, when higher doses are needed, this sustained-release formulation should be administered twice daily."( Sustained-release verapamil formulations for treating hypertension.
Frishman, WH; Lazar, EJ, 1992
)
0.62
"Behavioral performances of normotensive and hypertensive adult male baboons were tested before, during, and following chronic oral dosing with verapamil."( Behavioral performance effects of verapamil in normotensive and renovascular hypertensive baboons.
Hienz, RD; Turkkan, JS,
)
0.61
" Dose-response relationships with phenytoin supported the hypothesis that the voltage dependence of tonic block resulted from the higher affinity of the drugs for inactivated than for resting channels."( Frequency and voltage-dependent inhibition of type IIA Na+ channels, expressed in a mammalian cell line, by local anesthetic, antiarrhythmic, and anticonvulsant drugs.
Catterall, WA; Ragsdale, DS; Scheuer, T, 1991
)
0.28
" The absolute bioavailability was 23% in both investigations for the 80 mg preparation and 32% in both investigations for the 240 mg dosage form."( Pharmacodynamic profile of verapamil in relation to absolute bioavailability: investigations with a conventional and a controlled-release formulation.
Blume, H; Harder, S; Huber, T; Rietbrock, N; Siewert, M; Thürmann, P, 1991
)
0.58
" Dose-response curves were obtained with intravenous injection of the four drugs."( Hemodynamic profile of Ro 40-5967 in conscious rats: comparison with diltiazem, verapamil, and amlodipine.
Clozel, JP; Hess, P; Véniant, M; Wolfgang, R, 1991
)
0.51
" Hepatic effects can be either protective or toxic depending on the drug dosage and course duration."( [Effects of verapamil on the functional state of the liver in ischemic heart disease].
Makarovskiĭ, VV; Makeeva, LG; Shafranskiĭ, IuA; Svetova, SD; Vertkina, NV; Zharov, EI, 1991
)
0.66
"The relatively short half life of verapamil necessitates divided daily dosing in the treatment of angina, hypertension and arrhythmia."( Dose proportionality of pharmacokinetics with a cr-verapamil formulation.
Devane, J; Martin, M; Mulligan, S, 1991
)
0.81
" The clinical syndrome was controlled by verapamil in 16 cases out of 20 (80% of cases) at the dosage of 360 mg/d in 14 patients and of 480 mg/d in two."( [Unstable angina and infarction without Q wave treated with verapamil: value of the early exercise test].
Ghadanfar, M; Guyon, P; Haiat, R; Halphen, C; Leroy, G; Richecoeur, J; Stoltz, JP, 1991
)
0.79
"Antiarrhythmic therapy was chosen for 3-7 days by modified chronic electrophysiological study at three stages: (1) the efficacy of a drug, its action onset and termination were defined; (2) a dosage was chosen on an individual basis and the duration of drug potency was specified; (3) the dosage regimen of a drug given as a course therapy was confirmed by the results of trials."( [Evaluation of the possibility of selection of individual anti-arrhythmia therapy].
Antonchenko, IV; Borisova, EV; Chekhov, AM; Gimrikh, EO; Plekhanov, IG; Popov, SV; Savenkova, GM, 1991
)
0.28
" Different preparations were used to obtain cumulative dose-response curves (0."( [Comparison of negative chronotropic action of nitrendipine, nifedipine and verapamil on the isolated right atrium of normotensive and renovascular hypertensive rats].
de Faria, MG; Leite, CM; Mill, JG; Pires, JG, 1991
)
0.51
" This is associated with a decrease in reactivity of the vessels of the above mentioned brain structures determined by the dilatory reaction to the dosed inhalation of carbon dioxide."( [The effect of nimodipine and verapamil on the blood supply and vascular reactivity of the brain].
Beketov, AI; Polevik, IV,
)
0.42
"Behavioral performances of six baboons were tested during chronic oral dosing with diuretic (hydrochlorothiazide/triamterene), a calcium channel blocker (verapamil), and a combination of the two drugs."( Behavioral effects of chronic, orally administered diuretic and verapamil in baboons.
Hienz, RD; Turkkan, JS, 1991
)
0.72
" From the investigations to date, changing the digoxin dosage prior to initiating calcium antagonist therapy is, however, not justifiable."( [Interaction between calcium antagonists and digoxin].
Christensen, C, 1991
)
0.28
" Hyposmotic stress during added verapamil dosage (50 mumol/L) also resulted in 23% greater cell swelling compared with control."( Involvement of cell calcium and transmembrane potential in control of hepatocyte volume.
Khalbuss, WE; Wondergem, R, 1991
)
0.56
" Furthermore, this study does not indicate that any change in dosage is necessary when single doses of verapamil are administered to patients with renal failure."( The pharmacokinetics of racemic verapamil in patients with impaired renal function.
Frantz, RP; Kurtz, SB; McCarthy, JT; Moyer, TP; Smith, RL; Theobald, HM; Zachariah, PK, 1991
)
0.78
"The antihypertensive action of sustained release verapamil is, in the majority of cases, obtained with a dosage of 240 mg per day."( [Randomized double-blind study of delayed-action verapamil as a single dose versus 2 doses daily in patients with moderate hypertension].
Chapelon-Abric, C; Godeau, P; Villarroya, A; Wajman, A, 1991
)
0.79
" In other groups of rabbits, the effect of the same dosage of verapamil on the size of myocardial infarct after 20 or 30 min ischaemia and 72 h reperfusion was examined."( Does verapamil limit myocardial infarct size in a heart deficient in xanthine oxidase?
Adachi, T; Goto, M; Iimura, O; Iwamoto, T; Miura, T; Noto, T; Ogawa, T; Ooiwa, H; Tsuchida, A, 1990
)
1.03
" DSPM at higher dosage also lowered the normal myocardial Ca2+ content."( [Protective effect of 2-[p-(dimethylamino) styryl] pyridine methiodide (DSPM) on acute experimental myocardial ischemia].
Wang, XF; Wang, XW; Wei, Y; Zhang, KJ; Zhou, CM, 1990
)
0.28
" This study shows that the acute effects of verapamil on portal hypertension may vary with the dosage used."( Effect of verapamil on splanchnic haemodynamics in a portal hypertensive rat model.
Chen, HI; Chien, S; Lay, CS; Lo, KJ; Simchon, S; Tsai, YT; Yang, CM,
)
0.79
" The dose-response curve of SNP was shifted to the right, and the relaxation to verapamil was slightly reduced."( Endothelium-derived relaxing factor influences renal vascular resistance.
Förstermann, U; Frölich, JC; Radermacher, J, 1990
)
0.51
" No change in slope of the phenylephrine dose-response curve was noted; however, consistent with the dose ratio, verapamil shifted the curve to the right with a decrease in the y intercept determined by linear regression (60."( Forearm vascular alpha 1-adrenergic blockade by verapamil.
Abernethy, DR; Winterbottom, LM, 1990
)
0.75
" Dose-response curves for the effect of carbachol on the formations of IP2 and IP3 showed that high K+ medium selectively decreased the ED50 value of carbachol for IP2 formation about 3-fold."( Effect of membrane depolarization by high K+ on carbachol-stimulated phosphoinositides hydrolysis in guinea pig cerebral cortical slices.
Mizushima, A; Uchida, S; Yoshida, H; Zhou, XM, 1990
)
0.28
" If the desired effect is not obtained, the dosage may be increased first to 360 mg at bedtime and then to 240 mg morning and evening."( [Isoptin Retard. Pharmacokinetics and pharmacodynamics in patients with angina pectoris].
Jespersen, CM, 1990
)
0.28
" Patients treated with cyclosporine and prednisone alone had their cyclosporine dosage adjusted to maintain their cyclosporine level between 400 and 900 ng/mL between 1 and 6 months following transplantation."( The effect of calcium channel blockers on the cyclosporine dose requirement in renal transplant recipients.
Babcock, S; Chan, L; Howard, RL; Shapiro, JI, 1990
)
0.28
"The purpose of this study was to determine the dose-response relationship between verapamil HCl and creatine kinase (CK) release from isolated rat slow (soleus, S) and fast (flexor digitorum profundus, F) skeletal muscles."( Verapamil-induced creatine kinase loss from rat slow and fast muscles.
Armstrong, RB; Glenn, GM; Hayes, DA, 1990
)
1.95
" The fact that enhancement was 6-10 fold greater in resistant then in sensitive cells, as well as the loss of biphasic properties of adriamycin on dose-response curves after combined treatment, indicate that cepharanthine may play a role in overcoming drug resistance in some tumor cells."( Enhancement of adriamycin cytotoxicity in sensitive and resistant sublines of human tumor cells by calcium antagonists.
Mircheva, J; Tsuruo, T, 1990
)
0.28
"We studied the dose-response relationship for hydrochlorothiazide + triameterene and verapamil, comparing monotherapy with combined treatment in 216 hypertensive patients over 3 weeks of active treatment following a 2-week washout period with placebo."( Dose-response curves in antihypertensive combination therapy: results of a controlled clinical trial.
Bluemner, E; Letzel, H, 1990
)
0.5
" Blood pressure (BP) was lower with E after half the maximum dosage compared with V, but similar BP reductions were obtained after 2 months with the maximum dosage."( Antihypertensive and renal effects of enalapril and slow-release verapamil in essential hypertension. A double-blind, randomized study.
Fagher, B; Henningsen, N; Hulthén, L; Katzman, P; Thulin, T, 1990
)
0.52
" administration of verapamil (30-120 micrograms/mouse) and diltiazem (60-120 micrograms/mouse) significantly enhanced, in a dose-dependent way, the analgesic effects of morphine and produced a parallel displacement to the left of the morphine log dose-response line."( Analgesic effects of diltiazem and verapamil after central and peripheral administration in the hot-plate test.
Baeyens, JM; Del Pozo, E; Ruiz-García, C, 1990
)
0.88
" A dose-response relationship was observed for cis-platinum and an 5-fold increase of concentration converted the drug resistant tumor into a drug-sensitive one."( [In vitro drug-resistance decrease of ovarian cancer cells].
Lu, SM, 1990
)
0.28
" dosing of rats with gallopamil or verapamil, 13 and 2% of the dose, respectively, appeared in the bile as the N-glucuronide of the secondary amine metabolite over an 8-hr period."( Synthesis and identification of the N-glucuronides of norgallopamil and norverapamil, unusual metabolites of gallopamil and verapamil.
Mutlib, AE; Nelson, WL, 1990
)
0.79
" After 8 days, arterial pressure and dose-response relationships to norepinephrine, angiotensin II, and bradykinin were measured in conscious animals."( Altered pressor responses to NE and ANG II during cyclosporin A administration to conscious rats.
Smith-Powell, L; Telles, T; Textor, SC, 1990
)
0.28
" For each substance and each incubation time a dose-response curve was established and the D50 determined."( Toxicity of novel anthracycline derivatives towards normal myeloid bone marrow progenitor cells (CFU-GM) is not increased by verapamil.
Busch, FW; Ehninger, G; Schmittele, U, 1990
)
0.49
" Thus, a single predialysis dosage of verapamil has no effect on intradialytic blood pressure in an unselected hemodialysis population."( Effect of predialysis verapamil on intradialytic blood pressure in chronic hemodialysis patients.
Casale, P; Cody, R; Horton, MW; Sherman, RA,
)
0.72
" The patients were continuously treated with verapamil for two periods of two weeks at two dosage levels, 120 mg/d and 240 mg/d, whereafter verapamil was withdrawn."( Verapamil-digoxin interaction in chronic hemodialysis patients.
Halck, S; Johannessen, AC; Klitgaard, NA; Rendtorff, C, 1990
)
1.98
" After 4 days oral treatment, both verapamil and nisoldipine significantly attenuated the responses to angiotensin II with three- to fivefold rightward shifts of the mean pressor dose-response curves."( Effect of calcium channel blockers on adrenergic and nonadrenergic vascular responses in man.
Elliott, HL; Meredith, PA; Pasanisi, F; Reid, JL; Sumner, DJ,
)
0.41
" Thus, the protective action of calcium had a bell-shaped dose-response curve, with the optimum at 5 mmol/L."( Effect of gradual rise in plasma calcium concentration on the impairment of atrioventricular nodal conduction due to verapamil.
el Chebly, M; Faucon, G; Lang, J; Timour-Chah, Q,
)
0.34
" In the estrogen- and estrogen+progesterone-treated uteri, the dose-response curves by verapamil were shifted to the left in a parallel manner."( Calcium channel, Ca++ mobilization, and mechanical reactivity of estrogen- and progesterone-treated rat uterus.
Ando, J; Ishii, K; Kano, T, 1986
)
0.49
" The dose-response curves for VIP- and PHI-stimulated cAMP accumulation were superimposable on those for PRL secretion."( Vasoactive intestinal peptide and peptide with N-terminal histidine and C-terminal isoleucine increase prolactin secretion in cultured rat pituitary cells (GH4C1) via a cAMP-dependent mechanism which involves transient elevation of intracellular Ca2+.
Bjøro, T; Gautvik, KM; Gordeladze, J; Haug, E; Iversen, JG; Ostberg, BC; Sand, O; Torjesen, PA, 1987
)
0.27
" Bay K 8644 caused a leftward shift of the dose-response curve of the potassium-induced decrease in renin release."( Inhibitory effects of calcium channel agonists on renin release from rat kidney cortical slices.
Matsumura, Y; Morimoto, S; Sasaki, Y; Shinyama, H; Uriu, T, 1987
)
0.27
" Lowering the holding potential to -80 mV shifted the dose-response curve to the right."( Blocking actions of Ca2+ antagonists on the Ca2+ channels in the smooth muscle cell membrane of rabbit small intestine.
Kitamura, K; Kuriyama, H; Terada, K, 1987
)
0.27
" The dose-response curves on electrically paced isolated dog ventricular trabeculae on contractile force were determined with single as well as cumulative dosages of milrinone."( Effect of milrinone (Corotrope) on the contractility of isolated dog ventricular muscle.
Bentley, R; Canniff, PC; Farah, AE; Kaiser, LD, 1987
)
0.27
" Calcium induced a concentration dependent increase in dF/dt in normal and diabetic hearts, but in diabetes the dose-response curve to calcium chloride was shifted to the left."( Hypersensitivity to calcium associated with an increased sarcolemmal Ca2+-ATPase activity in diabetic rat heart.
Borda, E; Pascual, J; Sterin-Borda, L; Wald, M, 1988
)
0.27
" Cumulative forearm blood flow dose-response curves to three cumulative infusion rates (3 min each) of NE (0."( Verapamil and alpha-mediated vasoconstriction in human forearm: a comparison between norepinephrine and selective alpha 1- and alpha 2-adrenergic agonists.
Graziadei, L; Pana-Race, G; Pedrinelli, R; Salvetti, A; Taddei, S, 1987
)
1.72
"1 microM) to isolated hearts, or when given intravenously (2 mg kg-1 body weight 1 h before the animals were killed), anipamil displaced the dose-response curves for the positive inotropic effect of (0."( The Ca2+ -antagonist and binding properties of the phenylalkylamine, anipamil.
Dillon, JS; Nayler, WG, 1988
)
0.27
" In addition, verapamil shifted the dose-response curves for both 5-HT and PE to the right in parallel, indicative of competitive antagonism."( Studies on the site of the interaction between alpha 1-adrenoceptors and 5-HT2 receptors in rat tail arteries.
Marwood, JF, 1988
)
0.64
" The purpose of the present experiments has been to investigate a possible similar dose-response curve with a calcium channel activator, Bay k 8644."( Biphasic dose-response relationship observed with Bay k 8644 on atrioventricular nodal conduction inhibited by verapamil.
Aupetit, JF; Faucon, G; Lançon, JP; Lang, J; Timour, Q, 1988
)
0.49
" Dosage of each agent was titrated to achieve optimal clinic BP control and this dose was maintained for the duration of the study."( The efficacy and duration of action of sustained-release verapamil in essential hypertension.
Atkins, N; Latham, AN; McCormack, PM; Mee, F; O'Brien, ET; O'Malley, K, 1989
)
0.52
" The dosage of the drug was adjusted to the therapeutic response; in 88."( Efficacy and safety of verapamil SR 240 mg in essential hypertension: results of a multicentric phase IV study.
Pfennigsdorf, G; Schumacher, A; Sosna, J; Speders, S, 1989
)
0.59
" Plasma samples were collected for 24 h after dosing on day 8 of each phase and assayed for verapamil and norverapamil by high-performance liquid chromatography."( Sustained-release verapamil: multiple-dose pharmacokinetic comparison of 120-mg and 240-mg tablets and the effect of halving a 240-mg tablet.
Durnin, C; McEwen, J; McMurdo, ME; Moreland, TA, 1989
)
0.83
" In explanted rat hypothalami maintained viable in vitro, PAF stimulated immunoreactive CRH secretion in a bell-shaped dose-response fashion."( The alkyl-ether phospholipid platelet-activating factor is a stimulator of the hypothalamic-pituitary-adrenal axis in the rat.
Bernardini, R; Brucke, T; Calogero, AE; Chrousos, GP; Ehrlich, YH; Gold, PW, 1989
)
0.28
" IBI at 10(-6) M shifted the dose-response curve of phenylephrine to the right with reduction in maxima."( Paradoxical effects of isothiocyanate analog of tolazoline on rat aorta and human platelets.
Feller, DR; Hamada, A; Miller, DD; Patil, PN; Shams, G; Venkataraman, BV, 1989
)
0.28
" Verapamil dosing resulted in progressive prolongation of the PR interval as plasma drug levels increased from 40 to 250 ng/ml; at higher drug levels, complete atrioventricular block occurred."( Pharmacodynamic comparison of verapamil and nifedipine in anesthetized dogs.
Hamann, SR; Kaltenborn, KE; McAllister, RG,
)
1.33
" Its aim was to determine the effective dosage of slow release verapamil (V) in the treatment of mild to moderate hypertension and to compare plasma concentrations of V with blood pressure effects."( [Slow-release verapamil 240 mg and treatment of mild to moderate hypertension].
Amabile, G; Bory, M; Hulin, P; Serradimigni, A; Wajman, A,
)
0.73
" Statistically significant successive decreases in verapamil maximum plasma concentrations (Cmax) and area under the concentration-time curve (AUC) values were observed corresponding to dosing at 8 AM, 4 PM, and 12 AM."( Differences in oral verapamil absorption as a function of time of day.
Battle, MM; Colburn, WA; Eldon, MA; Voigtman, RE, 1989
)
0.85
" During the evening dosage schedule a significantly greater bioavailability (AUC) and a prolonged time to peak concentration was found."( Circadian variation in the pharmacokinetics of verapamil.
Frederiksen, M; Hansen, JF; Jespersen, CM; Klitgaard, NA; Sørum, C, 1989
)
0.53
" At their maximal safe dosage in humans, methysergide and verapamil suggest no role for serotonin and calcium ions."( Ventilatory response to sustained hypoxia: effect of methysergide and verapamil.
Anthonisen, NR; Balakumar, M; Easton, PA; Filuk, R; Long, GR, 1989
)
0.76
" Research comparing 240 mg/day with 320 mg/day dosing found 320 mg/day significantly more effective in reducing migraine frequency."( Verapamil in migraine prophylaxis--a five-year review.
Solomon, GD, 1989
)
1.72
" A cumulative dose-response curve to endothelin was obtained and the curves were shifted to the right after both verapamil and nifedipine administration."( Vasoconstrictor effect of endothelin on the canine coronary artery: is a novel endogenous peptide involved in regulating myocardial blood flow and coronary spasm?
Aizawa, Y; Ebe, K; Igarashi, Y; Shibata, A; Tamura, M; Yamaguchi, T, 1989
)
0.49
"The dose-response relationship of verapamil-SR was studied in 221 hypertensive patients."( The relationship of dose to the antihypertensive response of verapamil-sustained release in patients with mild to moderate essential hypertension. The Verapamil-SR Study Group.
McMahon, FG; Reder, RF, 1989
)
0.8
" The resulting dose-survival curve was identical to the dose-response curve of RS cells treated with R123 alone."( Relationship between cellular accumulation of rhodamine 123 (R123) and cytotoxicity in B16 melanoma cells.
Gan, L; Krag, DN; Tao, SZ; Theon, AP; Wardell, J, 1989
)
0.28
" The mean Cmax after dosing with whole tablets, 143 (95 per cent confidence limits 91."( Multiple dose comparison of a whole 240 mg verapamil sustained-release tablet with two half tablets.
McEwen, J; McMurdo, ME; Moreland, TA,
)
0.39
" We have characterized, in vivo, the pharmacokinetics and dose-response interactions between nifedipine and cisplatin."( In vivo characterization of combination antitumor chemotherapy with calcium channel blockers and cis-diamminedichloroplatinum(II).
Honn, KV; Nelson, KK; Onoda, JM; Taylor, JD, 1989
)
0.28
" In contrast to agonist affinity, phentolamine affinity, determined from Schild-plot analysis, was not different from controls, even for the highest daily dosage of verapamil."( Effects of chronic treatment with verapamil on adrenoceptor-mediated contraction of rabbit aorta.
Aceto, JF; Tallarida, RJ,
)
0.61
" In aorta strips depleted of Ca2+ by several applications of noradrenaline (10(-6) M), Sr2+ induced a dose-response contraction in a Ca2+-free solution."( Study of the strontium response in isolated rat aorta.
Anselmi, E; Barreda, A,
)
0.13
" A multiple instant-release dosage regime can now be replaced by once daily administration of the sustained-release preparation."( Sustained-release and instant-release verapamil in treatment of angina pectoris.
Hansen, JF; Jespersen, CM; Klitgaard, NA; Nielsen, H, 1989
)
0.55
" Oral dosage ranged from 825 mg to 1,100 mg for quinidine polygalacturonate and 240 mg to 320 mg for verapamil."( [Combination of quinidine and verapamil in auricular fibrillation].
Calvo, L; Maté, I; Mesa, JM; Moreno, I; Plaza, I; Rico, J; Sobrino, JA, 1989
)
0.78
" A preliminary approach of the dosage of verapamil showed that a total dose of 120-240 mg daily could achieve satisfactory result clinically in most patients."( [Therapeutic effect of verapamil in hypertension: an analysis of 52 cases].
Wang, JJ; Wen, ZB; Zong, JL, 1989
)
0.85
" THP and Ver shifted the KCl, CaCl2, norepinephrine (NE) and 15-methyl prostaglandin F2 alpha dose-response curves to the right in a non-parallel fashion, and decreased the maximal response, showing noncompetitive antagonism."( [Effects of l-tetrahydropalmatine on isolated rabbit arterial strips].
Li, DX; Sun, F, 1989
)
0.28
" DI and VE shifted dose-response curves for phenylephrine and clonidine to the right with suppression of maximal responses."( Effects of calcium antagonists on alpha-adrenoceptor mediated vasoconstrictions of the canine intermediate auricular artery.
Chiba, S; Ito, T, 1987
)
0.27
" Dose-response curves to calcium in SHR aortae treated with 10(-3) mol/l ouabain were shifted to the left of those in WKY."( Calcium and contractile responses to ouabain and potassium-free solution in aortae from spontaneously hypertensive rats.
Lamb, FS; Moreland, RS; Webb, RC, 1988
)
0.27
" Thus, when verapamil is introduced or discontinued in patients on ciclosporin, close monitoring of ciclosporin levels and dosage adjustment are necessary."( [Effect of enalapril, furosemide and verapamil on cyclosporin concentration in whole blood].
Angermann, CE; Anthuber, M; Kemkes, BM; Spes, CH; Theisen, K, 1988
)
0.93
" After the first doses of each drug and after 4 days continued treatment both verapamil and nisoldipine significantly attenuated the responses to angiotensin II with three- to fivefold rightward shifts of the pressor dose-response curves."( The effect of calcium channel blockers on alpha 1- and alpha 2-adrenoceptor-mediated vascular responsiveness in man.
Elliott, HL; Pasanisi, F; Reid, JL; Sumner, DJ, 1985
)
0.5
" However, as dosage adjustment and close observation may be necessary to minimise side effects, the use of this combination should be limited to hospital practice."( Tolerability of combined treatment with verapamil and beta-blockers in angina resistant to monotherapy.
McGourty, JC; Silas, JH; Solomon, SA, 1985
)
0.54
" In most cases the dose-response curves were biphasic and changes in coronary flow paralleled those in oxygen consumption."( The effect of cholinergic agonists on coronary flow rate and oxygen consumption in isolated perfused rat heart.
Erecińska, M; Nuutinen, EM; Wilson, DF, 1985
)
0.27
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
" Two patients with mild symptoms were rechallenged with a lower verapamil dosage (120 mg twice a day) and showed similar rises in CBZ concentration and recurrent neurotoxic symptoms."( Verapamil potentiates carbamazepine neurotoxicity: a clinically important inhibitory interaction.
Brodie, MJ; Macphee, GJ; McInnes, GT; Thompson, GG, 1986
)
1.95
" Cumulative dose-response curves to intra-arterial methoxamine or B-HT 933 were obtained during saline or two different rates of verapamil infusion (0."( Verapamil antagonizes forearm vasoconstriction mediated by selective alpha 1- and alpha 2-agonists in hypertensive patients.
Graziadei, L; Panarace, G; Pedrinelli, R; Salvetti, A; Taddei, S, 1986
)
1.92
"Intravenous administration of verapamil at low dosage was effective in reversal of atrial tachycardia of unknown origin in a dog."( Reversal of atrial tachycardia with intravenous administration of verapamil in a dog.
Foodman, MS; Macintire, D, 1989
)
0.8
" Tityustoxin caused a slight leftward shift of the dose-response curves to adrenaline and norepinephrine and a large potentiation of the frequency-response curves to electrical stimulation."( Effects of tityustoxin on the rat isolated tail artery.
Catanzaro, OL; Savino, EA, 1985
)
0.27
" The pharmacokinetics of verapamil and of one of its metabolites, norverapamil, is changed after multiple oral dosing as has been described in patients with supraventricular tachyarrhythmias, angina pectoris or in patients with essential hypertension."( Pharmacokinetics of calcium channel blocking agents.
Anderson, P, 1986
)
0.57
" The response was characterized by dose-response and kinetics investigations."( The proliferative T-lymphocyte response to streptokinase.
Bruserud, O; Jørgensen, PF; Sollid, L, 1986
)
0.27
" The dose-response curves for both adenosine and L-PIA were shifted to the right in the presence of aminophylline (13 and 32 mumol l-1)."( [Comparative effects of adenosine and L-N-phenylisopropyladenosine (L-PIA) on the spontaneous contraction of the isolated atrium in the guinea-pig].
Prostran, M; Varagić, VM, 1986
)
0.27
" After a stable control period, dose-response curves were constructed for each drug with hemodynamics measured 10 minutes after intravenous boluses."( Comparative hemodynamic dose-response effects of five slow calcium channel-blocking agents in coronary artery disease.
Frais, MA; Jackson, N; Midtbo, KA; Reynolds, G; Sharma, S; Silke, B; Taylor, SH; Verma, SP, 1987
)
0.27
"Inhibition of platelet aggregation was observed after 4 days of oral dosing with the calcium antagonists, verapamil (160 mg) or nisoldipine (20 mg) but not following acute dosing."( Effects of verapamil and nisoldipine on human platelets: in vivo and in vitro studies.
Elliott, HL; Jones, CR; Pasanisi, F; Reid, JL, 1985
)
0.87
" The GH responses to the combined addition of TRH with all doses of GRF or DBcAMP were fully additive, causing parallel elevations of the dose-response curves."( TRH and GRF stimulate release of growth hormone through different mechanisms.
Szabo, M, 1986
)
0.27
" Insulin secretory dose-response curves utilizing static incubations fit a single binding site model and established that glyburide (ED50 = 112 +/- 18 nM) is a more potent secretagogue than tolbutamide (ED50 = 15 +/- 3 microM)."( Increased cytosolic calcium. A signal for sulfonylurea-stimulated insulin release from beta cells.
Berg, M; Boyd, AE; Gaines, KL; Nelson, TY; Rajan, AS, 1987
)
0.27
" It is concluded that at the dosage level used in this study propranolol and verapamil were equally effective, but there were individual variations in best response to one or the other of these two drugs."( [Comparative study of the effects of verapamil and propranolol therapy in 16 cases of obstructive hypertrophic myocardiopathy].
Casset, D; Cosnay, P; Fauchier, JP; Itti, R; Lang, M; Lavigne, G; Raynaud, P, 1987
)
0.77
" A similar dose-response relationship was observed for verapamil in increasing net intracellular doxorubicin accumulation."( Verapamil reversal of doxorubicin resistance in multidrug-resistant human myeloma cells and association with drug accumulation and DNA damage.
Alberts, DS; Bellamy, WT; Dalton, WS; Dorr, RT; Gleason, MC; Kailey, JM; McCloskey, TM, 1988
)
1.96
" Renal clearance of atenolol was shown to be decreased by more than 25% in 2 subjects studied using intravenous dosing of atenolol."( Extent and pharmacokinetic mechanisms of oral atenolol-verapamil interaction in man.
Harper, RW; Harrison, PM; Keech, AC; McLean, AJ; Pitt, A, 1988
)
0.52
" The norepinephrine- and methoxamine-induced dose-response curves were similar in both SAD and SO groups on day 3, but shifted to the left on days 7 and 15 and demonstrated a tendency to shift to the right at 30 days."( Contractile reactivity of the perfused mesenteric vascular bed from sinoaortic denervated rats to norepinephrine, methoxamine and verapamil.
Bissoli, NS; Cabral, AM; Moyses, MR; Vasquez, EC, 1988
)
0.48
" In the presence of a standard concentration of verapamil (73 nmol l-1), the dose-response curves for NECA, both for the isometric contraction and the atrial rate, were significantly shifted to the left."( Interactions of 5'-N-ethylcarboxamide adenosine (NECA), aminophylline and dipropyl-phenyl-xanthine (XAC) on the isolated guinea-pig atria.
Prostran, M; Varagic, VM,
)
0.39
" In addition, (a) the presence of non-linear absorption kinetics offers a further explanation for the considerable inter-patient variability in AUC since the ability of drug to cross the liver is a function of the concentrations attained in portal blood which will be dependent on dissolution conditions prevailing in the GI-tract, (b) depending on the choice of the dose and dosage interval of the conventional release formulation used for comparison and as a consequence of Michaelis-Menten first pass metabolism it is possible to obtain relative bioavailability data showing superiority, equivalence or bioavailability loss with the slow release form."( Drug input rate from the GI-tract. Michaelis-Menten kinetics and the bioavailability of slow release verapamil and nifedipine.
Fischer, A; Köhne, H; Menke, G; Rietbrock, N; Woodcock, BG, 1988
)
0.49
" The second episode of calcium uptake was unaffected by lectin dosage and only moderately affected by the duration of lectin exposure."( Two episodes of calcium uptake associated with T-lymphocyte activation.
Gamaz, N; Kimball, PM; Sell, S, 1988
)
0.27
" Denuding caused a parallel shift of the dose-response curve of adenosine to the right by a factor of five in comparison with intact aorta."( Partially endothelium-dependent vasodilator effect of adenosine in rat aorta.
Chiou, WF; Wu, CC; Yen, MH, 1988
)
0.27
" In vitro dissolution studies have proved to be of little value in determining the clinical activity of these new dosage forms."( Controlled-release formulations of propranolol and verapamil.
Dunn, J, 1987
)
0.52
" No correlation could be found between the change in clinical symptoms and electrocardiographic, echocardiographic or hemodynamic data, nor to the dosage of V or P administered."( Long-term treatment of hypertrophic cardiomyopathy with verapamil or propranolol in matched pairs of patients: results of a multicenter study.
Biamino, G; Bubenheimer, P; Förster, K; Hanrath, P; Hopf, R; Kaltenbach, M; Kober, G; Kuck, KH; Schlepper, M; von Olshausen, KE, 1987
)
0.52
" These effects of DMDP were greater than those of another calcium channel blocker, verapamil, and occurred at one-half the dosage levels."( The effects of verapamil and a tiapamil analogue, DMDP, on adriamycin-induced cytotoxicity in P388 adriamycin-resistant and -sensitive leukemia in vitro and in vivo.
Bankusli, I; Mayhew, E; Radel, S; Rustum, YM, 1988
)
0.85
" Transient atrioventricular dissociation occurred in two patients 2 h after dosing with verapamil and propranolol or atenolol."( The effect of combined therapy on the pharmacokinetics and pharmacodynamics of verapamil and propranolol in patients with angina pectoris.
Lennard, MS; McCourty, JC; Silas, JH; Tucker, GT, 1988
)
0.72
" Studies with a representative Chinese hamster line (CHO) and a single-step multidrug resistant (MDR) mutant of human (HeLa) cells show that: (i) In comparison to the sensitive human cells, both cell lines show a comparable degree of resistance to the above mentioned drugs; (ii) In the presence of non-toxic dosage of verapamil, the drug-resistance phenotype of both cell lines is completely reversed; (iii) Both these cell lines showed greatly reduced uptake/intracellular levels of 3H-daunomycin, 3H-puromycin and 3H-vinblastine, which was restored to sensitive human cell's level in the presence of non-toxic doses of verapamil."( Intrinsic multidrug resistance phenotype of Chinese hamster (rodent) cells in comparison to human cells.
Gupta, RS, 1988
)
0.45
" Trough serum concentration of verapamil did not differ during the two dosage regimens (59 ng/ml - conventional formulation and 49."( 24-hour antiarrhythmic effect of conventional and slow-release verapamil in chronic atrial fibrillation.
Bjerregaard, P; Jørgensen, HS; Klitgaard, NA; Mølgaard, H, 1987
)
0.8
" There were no differences between formulations other than a significantly longer PR interval following the conventional formulation 2 h after dosing on day 10."( Pharmacokinetics and pharmacodynamics of two formulations of verapamil.
Henry, JA; Hla, KK; Latham, AN, 1987
)
0.51
" Treatment with verapamil elicited biphasic dose-response effects on rat locomotor activity: doses equimolar to CRF treatment slightly increased CRF-stimulated locomotion, while doses of verapamil ten times greater slightly depressed CRF-stimulated locomotion."( The effects of verapamil on the locomotor-activating properties of corticotropin releasing factor (CRF) in the rat.
Aldenhoff, JB; Koob, GF; Swerdlow, NR, 1986
)
0.97
" The elimination half-life of all 3 prototypical calcium antagonists is probably significantly prolonged during long-term dosing with clinically effective regimens."( Kinetics and dynamics of calcium entry antagonists in systemic hypertension.
Hamann, SR; McAllister, RG; Schloemer, GL, 1986
)
0.27
" The recently developed sustained formulation of the drug renders a simple dosage regimen possible."( Instant and sustained-release verapamil in the treatment of essential hypertension.
Hals, O; Lauve, O; Midtbø, K; Storstein, L; van der Meer, J, 1986
)
0.56
" The differences in the concentrations of the D- and L-isomers after oral vs intravenous dosing may contribute to the relatively lower efficacy of orally administered verapamil in the treatment of PSVT."( The pharmacodynamic and pharmacokinetic differences of the D- and L-isomers of verapamil: implications in the treatment of paroxysmal supraventricular tachycardia.
Bauman, JL; Gallestegui, J; Hariman, RJ; Hoon, TJ; Rodvold, KA, 1986
)
0.69
" There was no significant correlation between plasma drug concentrations and BP reduction, but the dosage regimens with the highest mean plasma drug concentrations were associated with the greatest mean reduction in BP."( Studies on verapamil in the treatment of essential hypertension: a review.
Hals, O; Lauve, O; Midtbø, K; Storstein, L; van der Meer, J, 1986
)
0.66
"The antihypertensive effect of a new sustained-release matrix formulation of verapamil 200 mg was investigated in a dose-response study in patients with mild to moderate essential hypertension."( Sustained release verapamil in hypertension. Results from a noninvasive ambulatory blood pressure monitoring and a clinical study.
Gordin, A; Koistinen, A; Nissinen, A; Sundberg, S; Tuomilehto, J, 1986
)
0.83
" We have compared the effect on heart rate variability, of doubling the digoxin dosage or adding verapamil 120 mg daily in a randomized cross-over study in 14 patients."( Towards improved control of atrial fibrillation.
Channer, KS; James, MA; Papouchado, M; Pitcher, DW; Rees, JR, 1987
)
0.49
" The cumulative log dose-response curves of Vp, acyano-Vp and nor-Vp were sigmoidal."( Evidence that uncharged verapamil inhibits myocardial contractility.
Cohen, L; Kezdy, FJ; Retzinger, GS; Vereault, D; Wasserstrom, JA, 1987
)
0.58
" In an anesthetized dog model, dosing regimens which produced stable plasma concentrations of either verapamil and/or pindolol resulted in drug effects which were closely related to the plasma levels of the individual agents."( Hemodynamic and pharmacokinetic aspects of the interactions between verapamil and pindolol.
Hamann, SR; Kaltenborn, KE; McAllister, RG, 1987
)
0.72
" Twelve patients were not receiving therapy or were receiving very low dosage therapy, including 8 with asymptomatic periods of more than 1 year."( Late follow-up (41 to 102 months) of medically treated patients with coronary artery spasm and minor atherosclerotic coronary obstructions.
Alwyn, M; Freedman, SB; Kelly, DT; Richmond, DR, 1986
)
0.27
" This dosage resulted in plasma concentrations of verapamil in the same range as the usual therapeutic levels in humans."( Effect of verapamil on accumulation of free and esterified cholesterol in the thoracic aorta of cholesterol-fed rabbits.
Haugegaard, M; Kjeldsen, K; Ravn, H; Stender, S, 1986
)
0.93
" The dosage of adriamycin was 50 mg/M2 every 3 weeks."( Verapamil reversal of clinical doxorubicin resistance in human cancer. A Wilshire Oncology Medical Group pilot phase I-II study.
Bouzaglou, A; Gala, K; Kennedy, PS; Naessig, V; Presant, CA; Wiseman, C; Wyres, M, 1986
)
1.71
"05) shifts to the right of the histamine dose-response curve in normal physiological salt solution (PSS)."( Differential effects of adenosine and verapamil on histamine vascular contractions.
Merrill, GF; Tozzi, CA, 1986
)
0.54
" Verapamil elimination was also found to be impaired after chronic dosing as compared to single administration."( The effect of oral verapamil therapy on antipyrine clearance.
Kokurina, EV; Metelitsa, VI; Piotrovskii, VK; Riabokon, OS; Rumiantsev, DO; Slastnikova, ID, 1986
)
1.51
" The apparent oral clearance of verapamil was decreased after both the twice and thrice daily dosage regimens (1."( Pharmacokinetics of verapamil in patients with hypertension.
Anderson, P; Bondesson, U; de Faire, U, 1986
)
0.88
" This could be attributed to a relatively low dosage and slow infusion speed."( Effects of four antiarrhythmic drugs on the induction and termination of paroxysmal supraventricular tachycardia.
Ishinaga, T; Komatsu, C; Tateishi, O; Tokuhisa, Y; Yoshimura, S, 1986
)
0.27
" The dosage of Verapamil necessary for maintaining an effective concentration for enhancement of the anti-tumor drug was determined and the influences of bladder instillation of Verapamil on the cardiovascular system and on the bladder were studied."( [Bladder instillation of verapamil as a means of enhancing the efficacy of chemotherapy in superficial bladder carcinoma: influence of bladder instillation of verapamil on the cardiovascular system].
Horiuchi, S; Kaneoya, F; Nakame, Y; Negishi, T; Saitoh, H; Takahashi, T; Yoshida, K, 1987
)
0.93
" These data lead us to conclude that verapamil can reverse DNR resistance completely, but that verapamil at non-toxic dosage only reduces DNR resistance by 50% in vivo."( Effect of verapamil on daunorubicin accumulation in Ehrlich ascites tumor cells.
Friche, E; Nissen, NI; Skovsgaard, T, 1987
)
0.95
" Such information assists in development of safe dosing regimens, prediction of abnormal handling of drugs in states of disease and disorder and anticipation of drug interactions."( Pharmacokinetics of calcium-entry blockers.
Blouin, RA; Hamann, SR; McAllister, RG, 1985
)
0.27
" Patients failing to convert to sinus rhythm after 12 days had dosage reduced to 180 mg/d of diltiazem or 240 mg/d of verapamil, and quinidine, 750 mg/d, was coadministered for another six days (part III)."( Diltiazem, verapamil, and quinidine in patients with chronic atrial fibrillation.
Anda, L; Eichelbaum, M; Greenblatt, DJ; Ochs, HR, 1985
)
0.87
" Nevertheless, this procedure may provide useful information for optimizing the dosage regimen of each patient as the pathological condition and drug therapy may be quite complex."( Pharmacokinetics of diltiazem and other calcium entry blockers.
Hermann, P; Morselli, PL, 1985
)
0.27
"To determine whether verapamil, diltiazem, or nifedipine affect digitoxin kinetics, glycoside plasma concentrations and renal excretion were measured before and during steady-state dosing in 30 patients with cardiac insufficiency."( Effects of verapamil, diltiazem, and nifedipine on plasma levels and renal excretion of digitoxin.
Kuhlmann, J, 1985
)
0.98
" We conclude therefore that verapamil may prevent post-transplant acute renal failure, but its optimal dosage and route of administration remain to be determined."( Verapamil prevents post-transplant oliguric renal failure.
Charlesworth, JA; Duggan, KA; Macdonald, GJ; Pussell, BA, 1985
)
2.01
" Preconstriction was induced with norepinephrine and cumulative dose-response curves were obtained for the vasodilators."( Effects of magnesium on the action of vasodilatory agents.
Arnold, TH; Tackett, RL, 1985
)
0.27
" Pretreatment of aortic rings with high concentrations of nifedipine (5 X 10(-7) M) or verapamil (10(-5) M) caused a comparable displacement to the right (2-3 times) in the relaxant dose-response curve for acetylcholine, A23187 and sodium nitroprusside with little or no changes in the maximal relaxation obtained with these vasodilators."( Blockade of endothelium-dependent relaxation by the amiloride analog dichlorobenzamil: possible role of Na+/Ca++ exchange in the release of endothelium-derived relaxant factor.
Bunting, PB; Schofield, TL; Winquist, RJ, 1985
)
0.49
" In 13 the dosage was decreased to 120 mg 2 times a day."( Short- and long-term treatment of mild to moderate hypertension with verapamil.
Dallocchio, M; Gosse, P; Roudaut, R; Wicker, P, 1986
)
0.51
" In the second part of the study, dogs received identical dosage sequences, but verapamil preceded dantrolene administration."( Effects of dantrolene and verapamil on atrioventricular conduction and cardiovascular performance in dogs.
Althaus, JS; Durbin, CG; Fisher, NA; Lynch, C; Veselis, RA, 1986
)
0.8
" These data indicate the safety and utility of twice-daily verapamil administration for the treatment of essential hypertension and suggest the value of obtaining verapamil plasma levels as a guide to dosage determination."( Twice-daily administration of oral verapamil in the treatment of essential hypertension.
Charlap, S; Dorsa, F; Frishman, W; Kimmel, B; Monuszko, E; Pollack, S; Saltzberg, S; Stroh, J; Weinberg, P; Wiezner, J, 1986
)
0.79
" Both doses of both anesthetics increased plasma verapamil levels compared with the same verapamil dosing regimen awake."( Cardiovascular effects of and interaction between calcium blocking drugs and anesthetics in chronically instrumented dogs. II. Verapamil, enflurane, and isoflurane.
Chelly, JE; Hartley, C; Hysing, ES; Merin, RG; Rogers, K; Taylor, A, 1986
)
0.73
" In 2 patients, verapamil caused weakness, lightheadedness, and severe sinus bradycardia (40 to 48 beats/min), and the dosage was reduced (blindly) to 240 mg/day, with the alleviation of bradycardia and associated symptoms."( Propranolol-verapamil versus propranolol-nifedipine in severe angina pectoris of effort: a randomized, double-blind, crossover study.
Corbett, JR; Croft, CH; Fulton, KL; Hillis, LD; Winniford, MD, 1985
)
0.99
"The accumulation of verapamil during regular dosing conditions was studied."( An investigation of the cause of accumulation of verapamil during regular dosing in patients.
Abernethy, DR; Mitchell, JR; Schwartz, JB; Taylor, AA, 1985
)
0.85
"Submaximal histamine dose-response curves were obtained on 34 dogs divided into six groups."( Interaction of verapamil hydrochloride and atropine sulphate on histamine-induced bronchoconstriction.
Brandt, HD; Bunn, AE; Krivoy, N, 1985
)
0.62
" Compared with the concentration after intravenous injection, the total verapamil concentration after oral dosing consisted of a substantially smaller proportion of the more potent l-isomer."( Effects of d,l-verapamil on atrioventricular conduction in relation to its stereoselective first-pass metabolism.
Echizen, H; Eichelbaum, M; Vogelgesang, B, 1985
)
0.85
" Dosing regimens were used that produced steady state plasma levels of both drugs, and the observed effects were clearly related to the plasma concentrations of the agents."( Cardiovascular and pharmacokinetic consequences of combined administration of verapamil and propranolol in dogs.
Hamann, SR; Kaltenborn, KE; McAllister, RG; Tan, TG; Vore, M, 1985
)
0.5
"A linear dose-response curve was produced by the addition of ouabain (10(-8)-10(-6) M) to the media bathing segments of porcine right coronary arteries."( Insurmountable antagonism of ouabain-induced coronary constriction by prazosin.
Fairfax, CA; Tanz, RD, 1985
)
0.27
" Nicardipine given by three different dosing schedules to baboons markedly limited myocardial infarction over a 6 h period of LAD occlusion."( Nicardipine in models of myocardial infarction.
Alps, BJ; Calder, C; Wilson, A, 1985
)
0.27
"1 to 1 mM) or verapamil (3 to 30 nM) induced parallel, concentration-dependent rightward displacements of the dose-response curves to Ca2+ (0."( Ketamine-inhibition of calcium-induced contractions in depolarized rat uterus: a comparison with other calcium antagonists.
Calixto, JB; Loch, S, 1985
)
0.63
"Nine healthy normal subjects received verapamil, 10 mg iv, before (control) and during cimetidine dosing (300 mg every 6 hours), and verapamil, 120 mg po, twice in the same manner."( Lack of interaction between verapamil and cimetidine.
Abernethy, DR; Schwartz, JB; Todd, EL, 1985
)
0.83
" Dose-response curves were constructed for five agents."( The effectiveness of local injections of vasodilating agents to produce vasodilation in subcutaneous tissue in rabbits.
DeYoung, NJ; Duncan, HJ; Faris, IB, 1985
)
0.27
" The steep dose-response relationships in other lines support the rationale for high-dose therapy either by intraperitoneal or systemic administration of drugs."( Pharmacologic reversal of drug resistance in ovarian cancer.
Ozols, RF, 1985
)
0.27
" Puppies had a greater area under concentration (AUC) after oral dosing than adults, indicating a greater amount of the dose reaching the systemic circulation."( Age-related changes in the pharmacodynamics of verapamil.
Arnold, TH; Tackett, RL; Vallner, JJ, 1985
)
0.53
" At the higher dosage verapamil produced a significant improvement in frequency of angina, trinitrin consumption, and exercise tolerance, and had a favourable and significant effect on the amount and duration of ischaemic S-T depression occurring in the electrocardiogram during exercise."( Clinical evaluation of verapamil in angina pectoris.
Clayton, GA; Sandler, G; Thornicroft, SG, 1968
)
0.87
" Dose-response curves were constructed correlating decreases in renal blood flow with doses of phenylephrine, clonidine, and guanabenz injected as boluses into renal arteries of anesthetized dogs."( Renal alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in dogs: comparison of phenylephrine, clonidine, and guanabenz.
Buckalew, VM; Strandhoy, JW; Wolff, DW, 1984
)
0.27
" Then prazosin or yohimbine were administered intra-arterially and dose-response curves repeated."( Renal alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in dogs.
Buckalew, VM; Strandhoy, JW; Wolff, DW, 1984
)
0.27
" According to the known dosage curve, the dosage of Verapamil would have to be increased multifold to achieve an effect, which is hardly possible due to the cardiodepression and peripheral circulation drop with hypotension that this would entail."( Does the administration of the calcium-antagonist verapamil in tocolysis with beta-sympathicomimetics still make sense?
Blümel, G; Erhardt, W; Fischbach, F; Krieglsteiner, P; Pfeiffer, U; Strigl, R, 1981
)
0.77
"Verapamil is effective primary therapy for angina pectoris at a dosage of about 120 mg three times a day."( Calcium channel blocking drugs for chronic, stable angina. Verapamil.
Kelly, DT, 1982
)
1.95
"5 micrograms/kg per min) that was continued while dose-response curves to M-7 and cirazoline were generated."( Differential inhibition of vascular smooth muscle responses to alpha 1- and alpha 2-adrenoceptor agonists by diltiazem and verapamil.
Cavero, I; Langer, SZ; Lefèvre-Borg, F; Shepperson, N, 1983
)
0.47
" Special consideration, however, must be given with regard to drug selection and dosage in order to avoid adverse effects on the mother and fetus."( Antiarrhythmic drug therapy during pregnancy.
Elkayam, U; Frishman, W; Rotmensch, HH, 1983
)
0.27
"Nifedipine is a strong calcium antagonist; it blocks the excitation-contraction coupling, yet at therapeutic dosage levels it has few side effects."( What is preferable in unstable angina, beta-blockade or calcium-inhibition?
Hugenholtz, PG; Serruys, PW; Simoons, ML, 1983
)
0.27
" The dose-response curve to dopamine was shifted to the right by both sulpiride and verapamil, indicative of competitive inhibition."( Dopamine antagonist effect of verapamil on isolated perfused rabbit ear artery.
Johnson, CE; Scriabine, A; Steinsland, OS, 1983
)
0.78
" Cumulative histamine dose-response curves were obtained on three groups each consisting of six dogs."( Different, dose-dependent effects of verapamil inhalation on histamine-induced bronchoconstriction in anaesthetized dogs.
Brandt, HD; Bunn, AE; Krivoy, N, 1984
)
0.54
"6 mg/kg) shifted the norepinephrine pressor dose-response curve to the right but were ineffective in alpha 2-blocked animals."( Interference of calcium entry blockade in vivo with pressor responses to alpha-adrenergic stimulation: effects of two unrelated blockers on responses to both exogenous and endogenously released norepinephrine.
Pedrinelli, R; Tarazi, RC, 1984
)
0.27
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
" Norverapamil concentrations were higher than those of the parent drug throughout the entire dosage interval."( Serum concentration and antihypertensive effect of slow-release verapamil.
Bühler, FR; Follath, F; Ha, HR; Schütz, E, 1982
)
1.06
" Dose-response curves for the physiological effects of the drugs are observed over the same range of concentrations as their inhibition of [3H]nitrendipine binding to its receptor."( Activation of the voltage-dependent Ca2+ channel in rat heart cells by dihydropyridine derivatives.
Lazdunski, M; Méaux, JP; Renaud, JF; Romey, G; Schmid, A, 1984
)
0.27
" There was a dose-response relationship between both moieties of PTH and the rise in heart beats, but the effect of 1-84 PTH was significantly greater than that of 1-34 moiety."( Effect of parathyroid hormone on rat heart cells.
Bogin, E; Harary, I; Massry, SG, 1981
)
0.26
" Finally, in a dosage which blocked degranulation, verapamil inhibited calcium uptake."( Role of extracellular calcium and neutrophil degranulation responses to 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine.
Lees, CJ; McCall, CE; O'Flaherty, JT; Swendsen, CL, 1981
)
0.51
" But the dose-response curve for Ca2+ in the presence of A23187 (3 X 10(-5) M), a Ca ionophore, was not affected at all by verapamil (10(-6) M)."( Contractile response of the rabbit aorta to maitotoxin, the most potent marine toxin.
Ohizumi, Y; Yasumoto, T, 1983
)
0.47
" The effect of dosage on twitch reduction was far more pronounced for indirect than direct stimulation."( Neuromuscular blocking action of verapamil in cats.
Gintautas, J; Kraynack, BJ; Lawson, NW, 1983
)
0.55
"An understanding of the pharmacokinetics of the calcium antagonists (slow-channel blocking drugs) is essential in order to design appropriate dosage regimens which will provide optimum therapeutic efficacy with these agents."( Calcium antagonists. Pharmacokinetic properties.
Kates, RE, 1983
)
0.27
" These investigations demonstrate that verapamil is safe and effective when evaluated after 1 year of continuous therapy using a dosage of 480 mg/day."( Efficacy and safety of verapamil in patients with angina pectoris after 1 year of continuous, high-dose therapy.
Creager, MA; Cutler, SS; Klein, MD; McCabe, CH; Ryan, TJ; Weiner, DA, 1983
)
0.85
" Because of the complex pharmacokinetics associated with multiple-dose administration and the variation in individual patient responsiveness to the drug, 'standard' dosing recommendations are difficult to determine; use of verapamil must be titrated to a clinical end-point."( Clinical pharmacokinetics of verapamil.
Blouin, RA; Hamann, SR; McAllister, RG,
)
0.61
" Drug dosage was twice daily and titrated according to casual clinic pressures (propranolol, 40 to 240 mg twice a day; verapamil, 120 to 240 mg twice a day)."( Propranolol versus verapamil for the treatment of essential hypertension.
Gould, BA; Hornung, RS; Jones, RI; Raftery, EB; Sonecha, T, 1984
)
0.8
"Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs."( Reliability of antiarrhythmic drug plasma concentration monitoring.
Follath, F; Ganzinger, U; Schuetz, E,
)
0.13
" A dose-response relationship resulted when explants were challenged with methacholine in nutrient medium containing varied calcium concentrations (0."( The calcium dependency of mucus glycoconjugate secretion by canine tracheal explants.
Barbieri, EJ; Bobyock, E; Chernick, WS; McMichael, RF, 1984
)
0.27
" Peak BP responses were blunted by a maximal dosage of 120 mg of verapamil administered twice daily during static activity."( Effects of nifedipine and verapamil on isometric and dynamic exercise in normal subjects.
Bravo, EL; Falkner, B; Hare, TW; Lowenthal, DT; Porter, RS; Stein, DT, 1984
)
0.81
"Inhalation histamine dose-response curves were constructed 15 minutes after inhalation of saline placebo or verapamil (4 mg) for eight patients with mild atopic asthma in a double blind, random manner."( Effects of calcium channel blockade on histamine induced bronchoconstriction in mild asthma.
Banks, J; Davies, BH; Fennerty, A; Walters, EH, 1984
)
0.48
" bolus/infusion dosing regimens were used for each drug to achieve and maintain stable drug concentrations in four different ranges rapidly."( Effects of hemodynamic changes on the elimination kinetics of verapamil and nifedipine.
Blouin, RA; Chang, SL; Hamann, SR; Kaltenborn, KE; McAllister, RG; Tan, TG, 1984
)
0.51
" PY decreased the maximum inotropic and chronotropic responses to isoprenaline and caused a dose-response parallel shift of the Ca dose-response curve."( Inotropic and electrophysiological effects of PY 108-068 on isolated cardiac preparations.
Delgado, C; Diez, J; Tamargo, J; Tejerina, MT, 1984
)
0.27
"In a patient with ischaemic heart disease chronic atrial flutter reverted to sinus rhythm during treatment with oral Verapamil, given at dosage of 240 mg once a day in order to prevent spontaneous angina."( Conversion of longstanding atrial flutter to sinus rhythm and transient complete A-V block following oral administration of verapamil. Report of a case.
Di Giacomo, M; Di Giacomo, V; Tedeschi, A, 1984
)
0.68
"As an aid to clinical therapeutic decisions, the haemodynamic dose-response effects following intravenous verapamil were evaluated in ten male patients with angiographically confirmed and stable coronary artery disease."( Haemodynamic dose-response effects of i.v. verapamil in coronary artery disease.
Ahuja, RC; Hussain, M; Nelson, GI; Silke, B; Taylor, SH; Verma, SP, 1984
)
0.74
" The most frequently applied dosage was 1 film-coated tablet of gallopamil 50 mg 2-3 times daily."( [Multicenter long-term study of gallopamil in patients with coronary heart disease].
Schiemann, J; Sućić, M, 1984
)
0.27
" These findings imply that verapamil dosage should be reduced in patients with impaired renal function and elderly patients."( Pharmacokinetics of calcium blockers in patients with renal insufficiency and in geriatric patients.
Larsen, A; Midtbø, K; Saevareid, L; Storstein, L, 1984
)
0.56
" In this dosage nifedipine did not show any significant change in exercise duration and the variables obtained using computer assisted exercise testing when compared to placebo."( Evaluation of verapamil and high dose nifedipine in patients with chronic stable angina with objective methods.
Bowles, MJ; Davies, AB; Khurmi, NS; Raftery, EB; Subramanian, VB, 1984
)
0.63
" One-fifth of the D10 value (concentration of drug that reduced colony-formation ability to 10% that of control) for each isoprenoid was calculated from dose-response curves of Chinese hamster V79 cells or human HeLa cells in culture."( Potentiation of anticancer agents by new synthetic isoprenoids. I. Inhibition of the growth of cultured mammalian cells.
Fukawa, H; Ikezaki, K; Kishiye, T; Komiyama, S; Koyama, H; Miyazaki, C; Tahara, Y; Takahashi, T; Ueda, H; Yamaguchi, T, 1984
)
0.27
" Following sinoaortic baroreflex denervation the dose-response curve for the calcium antagonist-induced fall in blood pressure and total peripheral resistance was shifted to the left."( Calcium antagonists: systemic and regional haemodynamic effects in conscious spontaneously hypertensive rats (SHR).
Nievelstein, HM; Smits, JF; Struyker-Boudier, HA; van Essen, H, 1984
)
0.27
" It is therefore concluded that continuous control of water intake and analysis of the stability of the drug is essential for the establishment of proper dose-response relationships."( Drinking water and drug dosage in rat studies.
Jakobsen, P; Jespersen, LT; Mikkelsen, EO; Pedersen, OL, 1983
)
0.27
"The relaxant effects of five organic calcium antagonists (nicardipine, diltiazem, PY 108068, verapamil and bepridil) on guinea-pig isolated trachea were tested against contractions induced by acetylcholine, histamine, 5-hydroxytryptamine, potassium chloride (KCl) and tetraethylammonium (TEA) in a medium containing the normal amount of calcium and against calcium dose-response curves in a calcium-free, potassium-enriched medium."( Effects of five different organic calcium antagonists on guinea-pig isolated trachea.
Advenier, C; Cerrina, J; Duroux, P; Floch, A; Renier, A, 1984
)
0.49
" Adjustments in anesthetic dosage may be necessary in patients receiving verapamil."( Verapamil decreases MAC for halothane in dogs.
Kates, RE; Mason, DM; Maze, M, 1983
)
1.94
" No clinically useful benefit was found with verapamil in the dosage used in this group of patients and the value of calcium antagonists in the treatment of patients with chronic obstructive lung disease requires further clarification."( Effects of verapamil on pulmonary haemodynamics during hypoxaemia, at rest, and during exercise in patients with chronic obstructive pulmonary disease.
Blair, GP; Brown, SE; King, RR; Light, RW; Linden, GS; Stansbury, DW, 1983
)
0.92
" Furthermore, occurrence of tachycardia was uniformly distributed throughout a dosing interval; there was no predilection for tachycardia to occur late in a dosing interval when plasma drug levels were presumed to be lowest."( The spontaneous occurrence of paroxysmal supraventricular tachycardia.
Lee, KL; McCarthy, EA; Pritchett, EL; Smith, MS, 1984
)
0.27
" At a dosage of 20 mg/kg/day, drug therapy in each case significantly prolonged the functional ability of the dystrophic chickens as quantitated regularly by a standardized test for righting ability."( In vivo effects of three calcium blockers on chickens with inherited muscular dystrophy.
Heffner, RR; Hudecki, MS; Pollina, CM, 1984
)
0.27
" The dose-response curve for verapamil was bell-shaped and the activity resided in the l form."( An inhibitory effect of verapamil and diltiazem on the release of noradrenaline from ischaemic and reperfused hearts.
Nayler, WG; Sturrock, WJ, 1984
)
0.87
" In the presence of 1 X 10(-3) M fusaric acid, the dose-response curves of cerebral arteries for 15-HPAA were antagonized in a noncompetitive manner."( Contractile responses of mammalian cerebral arteries to 15-hydroperoxyarachidonic acid vary in the presence of fusaric acid and verapamil.
Asano, M; Hidaka, H; Matsuda, T; Suzuki, Y, 1984
)
0.47
" An increased pressor responsiveness to noradrenaline was indicated by a shift of the noradrenaline dose-response curve to the left in group A rats as compared with group C rats."( Vascular hypersensitivity to noradrenaline: a possible mechanism of hypertension in rats with chronic uraemia.
Chaichenco, Y; Chaimovitz, C; Goligorsky, M; Kaplanski, J; Rapoport, J; Zimlichman, RR, 1984
)
0.27
" Dose-response curves for the relaxation of muscle to these drugs were all in parallel."( Mechanisms of slow contracture induced by potassium and caffeine in skeletal muscle of the dog.
Aoyama, T; Ono, H; Sato, T, 1984
)
0.27
" Dosing guidelines for all drugs are given in the paper."( Diagnosis and treatment of Prinzmetal's variant angina.
Greenberg, B; McMahon, MT; McPherson, MA; Sheaffer, SL; Talbert, RL,
)
0.13
" Verapamil caused no side effects forcing a reduction in dosage or a discontinuation."( A controlled trial of verapamil for Prinzmetal's variant angina.
Hillis, LD; Johnson, SM; Mauritson, DR; Willerson, JT, 1981
)
1.49
" When verapamil was administered to the healthy volunteers at the dosage commonly used, inhibition of platelet aggregation was observed 2 hrs after the drug ingestion."( Inhibition of human platelet functions by verapamil.
Ando, Y; Ikeda, Y; Kikuchi, M; Toyama, K; Watanabe, K, 1981
)
1.01
" The main limiting factor in dosage was hypotension."( Verapamil in the long-term treatment of angina pectoris.
Raftos, J, 1982
)
1.71
" In normal calcium Krebs solution, dose-response curves to histamine were markedly reduced by verapamil while acetylcholine responses were relatively unaffected."( The effect of prostaglandin E2 on histamine-stimulated calcium mobilization as a possible explanation for histamine tachyphylaxis in canine tracheal smooth muscle.
Anderson, WH; Krzanowski, JJ; Polson, JB; Szentivanyi, A, 1983
)
0.48
" Follow-up study with oral verapamil at the same dosage in 13 patients for 7 +/- 5 months (+/- SD) revealed that the six patients with induction of echo beats alone have been free of symptomatic arrhythmia, while six of the remaining eight patients had occasional attacks of sustained tachycardia."( Effects of oral verapamil in patients with atrioventricular reentrant tachycardia incorporating an accessory pathway.
Hung, JS; Kou, HC; Lin, FC; Wu, D; Yeh, SJ, 1983
)
0.91
" These results suggest that verapamil, at the dosage used, did not prevent allergic bronchoconstriction by a direct action on smooth muscle and therefore was effective by inhibiting the release of mast cell mediators."( Modification of allergic bronchoconstriction by a calcium antagonist: mode of action.
Abraham, WM; Ahmed, T; Marchette, B; Russi, EW; Yerger, L, 1983
)
0.56
" When the relationship between serum concentration at the end of the dosing interval and angina frequency was studied, it was observed that patients in whom angina was completely suppressed had concentrations greater than 160 ng/ml and patients with poor control (greater than 5 anginal episodes per week) had concentrations less than 60 ng/ml."( Pharmacokinetics of verapamil and norverapamil during long-term oral therapy.
Lopez, LL; Mehta, J; Pieper, JA; Tartaglione, TA, 1983
)
0.59
" Of 26 patients who completed the single-blind dose titration, 16 were improved (greater than 1 minute) at a dosage of 240 or 360 mg/day."( Verapamil versus placebo in relieving stable angina pectoris.
Bailly, DJ; Butman, S; Citron, PD; Landa, DW; Pine, MB; Plasencia, GO; Wong, RK, 1982
)
1.71
" Patients in the first two categories were evaluated both by open-label dosage titration and by a randomized, double-blind, cross-over protocol."( Clinical use of oral verapamil in chronic and paroxysmal atrial fibrillation.
Guerrero, J; King, BD; Pitchon, R; Schneider, RR; Stern, EH; Wiener, I, 1982
)
0.58
" Verapamil was well tolerated in both dosage forms by all subjects."( The pharmacology of verapamil. IV. Kinetic and dynamic effects after single intravenous and oral doses.
Kirsten, EB; McAllister, RG, 1982
)
1.5
" In the 20 patients with hypertension for whom full dose-response curves were determined, the dilator response to verapamil was significantly greater than that in the normal controls, whereas the response to sodium nitroprusside was reduced."( Response of forearm resistance vessels to verapamil and sodium nitroprusside in normotensive and hypertensive men: evidence for a functional abnormality of vascular smooth muscle in primary hypertension.
Bayley, S; Dobbs, RJ; Robinson, BF, 1982
)
0.74
" Flunarizine at a small dose shifted to the right the dose-response curve for Ca2+ of the phasic contraction due to electric stimuli in rabbit basilar strips, while in a large dose, flunarizine reduced the maximum tension and slope of the dose-response curve."( Selective abolition of Ca-dependent responses of smooth and cardiac muscles by flunarizine.
Kasuya, Y; Nakayama, K, 1980
)
0.26
"Verapamil kinetics after intravenous and single and long-term oral dosing were studied in 12 patients with coronary artery spasm and four normal subjects."( Verapamil kinetics in normal subjects and patients with coronary artery spasm.
Ashley, JJ; Freedman, SB; Kelly, DT; Richmond, DR, 1981
)
3.15
" After 2 weeks, aortic and portal vein strips were prepared from each rat for studies of cumulative dose-response curves to norepinephrine (NE) in Krebs' solution containing normal (2."( Effect of chronic treatment of spontaneously hypertensive rats with D 600.
Pang, CC; Sutter, MC,
)
0.13
" All three drugs inhibited norepinephrine (NE) and KCl dose-response curves in a concentration-dependent manner."( Spasmolytic action of verapamil, D600 and cinchocaine on the rat vas deferens.
Lin, CS; Swamy, VC, 1980
)
0.58
" The main limiting factor in dosage was hypotension."( Verapamil in the long-term treatment of angina pectoris.
Raftos, J, 1980
)
1.7
" Group III animals were given verapamil orally in the dosage of 4 mg/kg, three times a day, 10 days before coronary ligation."( Experimental myocardial infarction in rhesus monkeys. Verapamil pretreatment in the reduction of infarct size.
Anand, IS; Chakravarti, RN; Sharma, PL; Wahi, PL, 1980
)
0.8
" The results of in vivo protein binding studies using plasma samples collected during a steady-state dosing interval from a patient receiving 80 mg of verapamil orally every 6 hr were similar to those obtained from vitro binding studies."( Factors affecting the plasma protein binding of verapamil and norverapamil in man.
Bates, TR; Kunka, RL; Yong, CL, 1980
)
0.72
" Nifedipine released during Days 11-14 elicited an inverted U-shaped dose-response curve in the VDI with a peak increase of 30."( Calcium entry blockers stimulate vasoproliferation on the chick chorioallantoic membrane.
Dusseau, J; Hutchins, PM, 1993
)
0.29
" However, the concentrations at which these calcium channel blockers elicit antiproliferative effects may not be attainable during therapeutic dosing in humans."( Effect of calcium channel blockers on the growth of human vascular smooth muscle cells derived from saphenous vein and vascular graft stenoses.
Betteridge, L; Chan, P; Gallagher, K; Munro, E; Patel, M; Schachter, M; Sever, P; Wolfe, J, 1994
)
0.29
" Dose-response curves were constructed before and during intra-arterial infusion of the NO synthase inhibitor NG-monomethyl-L-arginine (L-NMMA) (2 mg/min, n = 6) or vehicle (n = 6)."( Endothelial release of nitric oxide contributes to the vasodilator effect of adenosine in humans.
Banitt, P; Creager, MA; Lipson, DE; Rongen, GA; Smits, P; Williams, SB, 1995
)
0.29
" In both tissues, variations in perfusate [Ca2+] had similar effects: threshold contractile concentrations of 5-HT were unaffected, and the upper ends of the 5-HT dose-response curves were augmented or decreased by increased or decreased [Ca2+], respectively."( Interaction between Ca2+, verapamil, and ketanserin in rat tail artery and aorta.
Marwood, JF; Okoro, EO; Stokes, GS, 1995
)
0.59
" Relative resistance was not significantly changed by co-incubation with a non-cytotoxic dosage of these inhibitors."( Role of sodium pump systems to determine sensitivity to mitomycin C in non-small cell lung cancer cell lines.
Bando, T; Fujimura, M; Kasahara, K; Matsuda, T; Nakatsumi, Y; Numata, Y; Shibata, K,
)
0.13
" Both of them inhibited the contraction of the left atrium and reversed the frequency-contraction response from positive to negative staircase in the higher dosage (500 and 1 mumol."( Effects of osthole on isolated guinea pig heart atria.
Li, L; Yang, L; Zhang, CL; Zhao, DK; Zhao, GS; Zhuang, FE, 1995
)
0.29
"The technique detailed here allows reliable, direct measurement of intestinal absorption which may assist in characterizing oral dosing for novel therapeutic agents."( Method to estimate the rate and extent of intestinal absorption in conscious rats using an absorption probe and portal blood sampling.
Borre, A; Hoffman, DJ; Nellans, HN; Seifert, T, 1995
)
0.29
"This study investigated the effect of verapamil metabolites on R- and S-verapamil protein binding in plasma samples collected from subjects prior to rac-verapamil dosing and following single dose and steady state rac-verapamil dosing."( Influence of metabolites on protein binding of verapamil enantiomers.
Akers, WS; Johnson, JA, 1995
)
0.82
" In combined intraperitoneal injection with vinblastine (200 micrograms kg-1) into P388/ADR-bearing mice, NA-382 in a suspension form (10 mg kg-1) prolonged the life-span of the mice near to that of P388/S-bearing mice treated with vinblastine alone, but verapamil even at the maximum tolerated dosage (30 mg kg-1) barely affected the in-vivo antitumour effect of vinblastine."( Antitumour effects and pharmacokinetics of combination of vinblastine with a staurosporine derivative, NA-382, in P388/ADR-bearing mice.
Koga, K; Miyamoto, K; Ohshima, T; Takeda, K; Wakusawa, S, 1995
)
0.47
" Initial dose-response studies for anipamil (0."( Effects of anipamil, a long acting analog of verapamil, in pigs subjected to myocardial ischemia.
Guppy, LJ; Harvie, CJ; Pugsley, MK; Ries, CR; Walker, MJ, 1995
)
0.55
" Although apoptosis occurred when its multidrugs resistance had been reversed by verapamil, compared with sensitive HL-60 cells, the time at which apoptosis happened delayed and the drug dosage increased."( [Apoptosis resistance and its reversal in harringtonine resistant cell line].
Chi, XS; Fang, M; Pang, DB; Xue, SB; Zhang, HQ, 1994
)
0.51
" This verapamil formulation can be clinically titrated within a 180 to 540 mg dosing range, permitting effective once-daily administration for the treatment of chronic stable angina."( Placebo-controlled evaluation of three doses of a controlled-onset, extended-release formulation of verapamil in the treatment of stable angina pectoris.
Anders, RJ; Awan, NA; Bultas, J; Cutler, NR; Jhee, SS; Lahiri, A; Sramek, JJ; Woroszylska, M, 1995
)
0.99
" Dose-response relations were also consistent with independent binding of transcainide to two separate sites on the channel."( Transcainide causes two modes of open-channel block with different voltage sensitivities in batrachotoxin-activated sodium channels.
French, RJ; Zamponi, GW, 1994
)
0.29
" If sinus rhythm could not be established at that time, electric cardioversion was performed and the drug was continued in lower dosage thereafter."( [Sotalol and quinidine/verapamil (Cordichin) in chronic atrial fibrillation--conversion and 12-month follow-up--a randomized comparison].
Betz, P; Kalusche, D; Roskamm, H; Stockinger, J, 1994
)
0.6
" Dose-response curves were generated for the response to intravenous administration of acetylcholine (ACh), phenylephrine (PE), or salbutamol (SAL) (10(-8) to 10(-4) mol/kg)."( Effect of cyclic phenyl saligenin phosphate and paraoxon treatment on vascular response to adrenergic and cholinergic agents in hens.
Ehrich, M; Lee, JC; McCain, WC; Wilcke, J, 1995
)
0.29
" Lid shifted the dose-response curves for KCl and NA to the right nonparallelly and depressed their maximal responses."( [Effects of lidocaine on contraction of isolated rabbit aortic rings].
Bu, X; Jiang, MZ; Li, ST; Wen, Y; Zhang, ZH, 1994
)
0.29
" A dose-response relationship was established for the effect of VER on efflux."( Kinetics of daunorubicin transport in Ehrlich ascites tumor cells with different expression of P-glycoprotein.
Maare, C; Nielsen, D; Skovsgaard, T, 1994
)
0.29
" Most antihypertensives can be given once or twice daily without the need for sustained-release dosage forms."( Selected factors that influence responses to antihypertensives. Choosing therapy for the uncomplicated patient.
Carter, BL; Elliott, WJ; Frohlich, ED; Mann, RJ; Moore, MA; Roberts, RW, 1994
)
0.29
" In summary, aging decreases clearance of both S- and R-verapamil during steady-state intravenous dosing of racemic verapamil with preserved stereoselective clearance of verapamil with aging."( Verapamil stereoisomers during racemic verapamil administration: effects of aging and comparisons to administration of individual stereoisomers.
Capili, H; Schwartz, JB; Wainer, IW, 1994
)
1.98
"HCl in eight volunteers following single and multiple oral doses of these dosage forms were determined using HPLC method."( [Study on dissolution test in vitro and bioavailability of oral osmotic pump of verapamil hydrochloride].
Cao, DS; Guo, JL; He, HY; Jing, GW; Li, YQ; Li, Z; Ling, LX, 1993
)
0.51
" Finally, verapamil, a calcium/potassium channel blocker displaced the dose-response curve for Cd2+ toxicity as well as metallothionein-IIA and heat shock protein 70 gene expression to higher Cd2+ concentrations."( Modulation of stress proteins by Cd2+ in a human T cell line.
Benveniste, J; Davenas, E; Manuel, Y; Morin, L; Pellegrini, O; Thomas, Y; Tsangaris, GT, 1994
)
0.69
" Forearm blood flow was determined by venous occlusion plethysmography, and dose-response curves were generated for each drug."( Impaired endothelium-dependent vasodilation in patients with insulin-dependent diabetes mellitus.
Creager, MA; Creager, SJ; Cusco, JA; Johnstone, MT; Lee, BK; Scales, KM, 1993
)
0.29
" These changes were more pronounced by increasing the dosage of histamine."( Effects of calcium channel and H1-receptor blockers on the responses of slowly adapting pulmonary stretch receptors to histamine in vagotomized rabbits.
Kanno, T; Matsumoto, S; Nagayama, T; Shimizu, T; Yamasaki, M, 1993
)
0.29
"In vitro prospective, repeated-measures, dose-response study."( Effect of calcium to reverse the electrocardiographic effects of hyperkalemia in the isolated rat heart: a prospective, dose-response study.
Bisogno, JL; Langley, A; Von Dreele, MM, 1994
)
0.29
" As the phosphate concentration was increased, the biphasic fluoride dose-response curve was shifted to a lower range of fluoride concentrations."( Fluoride increases net 45Ca uptake by SaOS-2 cells: The effect is phosphate dependent.
Farley, JR; Hall, SL; Herring, S; Tanner, MA, 1993
)
0.29
" The pharmacokinetic parameters of verapamil indicated a two-fold increase in AUC and Cmax at trial B and C when compared with the single dose application, but AUC and Cmax were considerably lesser during the afternoon dosing interval (trial D)."( Concentration/effect analysis of verapamil: evaluation of different approaches.
Harder, S; Rietbrock, S; Thürmann, P, 1993
)
0.84
"Recent pharmacotherapeutic advances in the treatment of hypertension have included the development of sustained-release (SR) dosage formulations, providing patients with the convenience of once daily administration."( Utility of a sustained-release formulation for antihypertensive therapy.
Markowski, DJ; Sclar, DA; Skaer, TL; Won, JK, 1993
)
0.29
" The time-course of the ocular effects of topical verapamil and nifedipine as well as the dose-response relationship, were studied in conscious, normotensive rabbits."( The topical application of verapamil and nifedipine lowers intraocular pressure in conscious rabbits.
Garrido, M; Martínez de Ibarreta, MJ; Santafé, J; Segarra, J, 1993
)
0.84
" The nurse's monitoring and evaluation of the desired and adverse effects helps the team to titrate the dosage according to the patient's response."( Continuous verapamil infusion: the nurse's role in monitoring patient outcomes.
Jozefiak, E; Molchany, CA; Swavely, DA,
)
0.52
" After 500 and 1000 mg R-verapamil there were significant prolongations in PR interval, maximal at 1-2 h after dosing and coincident with peak plasma drug concentrations, but these were not significantly different from the maximum prolongation obtained with 240 mg racemic verapamil."( R-verapamil: pharmacokinetics and effects on PR interval, blood pressure and heart rate.
Ahmed, JH; Elliott, HL; Godden, J; Meredith, PA, 1993
)
1.31
"5 mg/kg) and oral (5 mg/kg) dose kinetics of verapamil were studied in 6 dogs during steady-state oral verapamil dosing (5 mg/kg every 8 h for 3 days)."( Pharmacokinetics of the enantiomers of verapamil in the dog.
Bai, SA; Johnson, LM; Lankford, SM, 1993
)
0.82
" In the taenia coli, lower concentrations of both the extract and verapamil induced a parallel displacement of the dose-response curves to calcium (0."( Inhibition of calcium-dependent contractions of the isolated guinea-pig ileal longitudinal muscle and taenia coli by the total glycosidic extract of the plant Sarcolobus globosus.
Mustafa, MR, 1993
)
0.52
" Development of a concentrated dosage form is necessary to assess bioavailability."( Comparison of intranasal versus intravenous verapamil bioavailability.
Engelhardt, J; Gal, P; Johnson, M; Kandrotas, R; Kroboth, P; Smith, H; Watling, S, 1993
)
0.55
" Both gallopamil and verapamil inhibited the Ach-induced contractions of ovine tracheal smooth muscle, by shifting the dose-response curves to Ach to the right."( Ovine tracheal muscle contraction in vitro: inhibition by calcium channel blockers gallopamil and verapamil.
Abraham, WM; Ahmed, T; Chapman, GA; Jackowski, J, 1993
)
0.82
" R56865 was given before ischemia and with the onset of reperfusion, applying different dosing schedules, including an initial loading dose."( R56865 is antifibrillatory in reperfused ischemic guinea-pig hearts, even when given only during reperfusion.
Guttmann, I; Mozes, A; Scheufler, E; Wilffert, B, 1995
)
0.29
" Forearm blood flow dose-response curves were determined for each drug before and during concomitant intraarterial administration of vitamin C (24 mg/min)."( Vitamin C improves endothelium-dependent vasodilation in patients with non-insulin-dependent diabetes mellitus.
Boles, KS; Creager, MA; Creager, SJ; Ganz, P; Timimi, FK; Ting, HH, 1996
)
0.29
"Twelve patients meeting DSM-IIIR criteria for mania received verapamil over a 2-week period, with dosing up to 360 mg/day."( Treatment of mania: relationship between response to verapamil and changes in plasma calcium and magnesium levels.
Goodnick, PJ, 1996
)
0.78
" Forearm blood flow was determined by venous occlusion plethysmography, and dose-response curves were generated for each agent."( Impaired nitric oxide-mediated vasodilation in patients with non-insulin-dependent diabetes mellitus.
Creager, MA; Cusco, JA; Johnstone, MT; Roddy, MA; Williams, SB, 1996
)
0.29
" Both dosage regimens were continued for 1 week with a minimum 1-week period between the two drug treatments."( Pharmacokinetics of verapamil and norverapamil enantiomers after administration of immediate and controlled-release formulations to humans:evidence suggesting input-rate determined stereoselectivity.
Bhatti, MM; Foster, RT; Lewanczuk, RZ; Pasutto, FM, 1995
)
0.61
" Plasma verapamil concentrations were measured at steady state over the dosing interval."( The effect of food, time of dosing, and body position on the pharmacokinetics and pharmacodynamics of verapamil and norverapamil.
Atkinson, L; Gupta, SK; Longstreth, J; Yih, BM, 1995
)
0.94
" Antihypertensive therapy has been traditionally dosed in the morning after awakening, and in recent years most of the newly developed antihypertensive agents have been once-daily, long-acting preparations."( A chronotherapeutic approach to the management of hypertension.
White, WB, 1996
)
0.29
" LFLX (100 microM) shifted the dose-response curve of glucose-induced insulin release to the left without altering the maximal response."( Increase in insulin release from rat pancreatic islets by quinolone antibiotics.
Iguchi, A; Maeda, N; Miura, H; Niki, I; Nonogaki, K; Ozawa, K; Tamagawa, T; Uemura, K; Watanabe, G, 1996
)
0.29
" The dose-response curves of adenosine on AV nodal conduction were almost identical in the control state and after verapamil, propranolol, or procainamide injection."( Effects of verapamil, propranolol, and procainamide on adenosine-induced negative dromotropism in human beings.
Lai, WT; Lee, CS; Sheu, SH; Wu, JC; Wu, SN, 1996
)
0.89
" Dose-response curves were fitted with a nonlinear regression microcomputer programme."( A complex interaction between topical verapamil and timolol on intraocular pressure in conscious rabbits.
Garrido, M; Martínez de Ibarreta, MJ; Melena, J; Santafé, J; Segarra, J, 1996
)
0.57
" After 1-week recovery, dogs underwent control euglycemic insulin dose-response studies (n = 6) in the conscious state: at 1,000 mU/mm insulin infusion rate, myocardial glucose and lactate extraction increased seven- and threefold, respectively with no change in coronary artery blood flow or ventricular elasticity and end-systole (Ees)."( Myocardial metabolism during graded intraportal verapamil infusion in awake dogs.
Kline, JA; Leonova, E; Schroeder, JD; Watts, JA; Williams, TC, 1996
)
0.55
" Further studies are needed to determine the dose-response and the efficacy of the drug in nonhuman primates."( The effects of subconjunctival verapamil on filtering blebs in rabbits.
Agarwala, A; Edward, DP; Gupta, B; Moy, JJ, 1996
)
0.58
"The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied."( Stability of labetalol hydrochloride, metoprolol tartrate, verapamil hydrochloride, and spironolactone with hydrochlorothiazide in extemporaneously compounded oral liquids.
Allen, LV; Erickson, MA, 1996
)
0.54
" The 48 study subjects received verapamil daily during each of the 4 sequential 5-day dosing segments."( Simultaneous first-order and capacity-limited elimination kinetics after oral administration of verapamil.
Atkinson, L; Gupta, SK; Hwang, S; Longstreth, J, 1996
)
0.8
" Dose-response curves to insulin (2 to 2000 microU/ml) were compared for extraluminal (EL), intraluminal (IL), and combined IL-EL application."( Direct vasodilatory effect of insulin on isolated retinal arterioles.
Alder, VA; Cringle, SJ; Su, EN; Yu, DY; Yu, PK, 1996
)
0.29
" Exposure to EL insulin while the IL K+ contraction dose-response curve was measured had no effect."( Direct vasodilatory effect of insulin on isolated retinal arterioles.
Alder, VA; Cringle, SJ; Su, EN; Yu, DY; Yu, PK, 1996
)
0.29
"Since the balance between the positive and the negative effects of vasodilation may be delicate in ischemic diseases a dose-response study (dose range, 120 to 480 mg) was established to determine optimal, individual dosages of slow-release verapamil in 44 patients with stable intermittent claudication (Fontaine classification stage II) with respect to walking capacity."( Effect of verapamil in intermittent claudication A randomized, double-blind, placebo-controlled, cross-over study after individual dose-response assessment.
Bagger, JP; Helligsoe, P; Jensen, BS; Kimose, HH; Randsbaek, F, 1997
)
0.88
" Individual optimization of drug dosage should be considered an option both in trials and in the clinical setting in these patients."( Effect of verapamil in intermittent claudication A randomized, double-blind, placebo-controlled, cross-over study after individual dose-response assessment.
Bagger, JP; Helligsoe, P; Jensen, BS; Kimose, HH; Randsbaek, F, 1997
)
0.7
" This study was undertaken in adult male New Zealand rabbits to assess the effect of 3 weeks of dosing with NIS (1 mg."( A high cholesterol diet blocks the effect of calcium channel blockers on the uptake of sugars in rabbit intestine.
Hyson, DH; Kappagoda, CT; Keelan, M; Thomson, AB, 1997
)
0.3
" It is concluded that the combination doses tested showed a sustained and marked antihypertensive effect throughout the 24-hour dosing interval, and the starting dose (verapamil 180 mg plus trandolapril 2 mg) seems appropriate in this group of patients."( Once-daily fixed dose combinations of verapamil and trandolapril in black patients with mild to moderate hypertension: a new choice for first line treatment.
Hlatswayo, Z; Radevski, I; Sareli, P; Skoularigis, J; Strugo, V, 1997
)
0.76
" In this situation, the selection of a correct assay dosage to study the MDR modulation mechanism was a problem."( Simultaneous determination of cytotoxic (adriamycin, vincristine) and modulator of resistance (verapamil, S 9788) drugs in human cells by high-performance liquid chromatography and ultraviolet detection.
Atassi, G; Dubois, J; Hanocq, M; Tassin, JP, 1997
)
0.52
" This may be explained by the inconsistent efficacy of Mg2+, partly in relationship to a given plasma Mg(2+)-concentration, partly caused by the uncertainty regarding the dosage and injection rate or the unawareness of the clinical effects of the cation."( [Clinico-electrophysiologic effects of magnesium, especially in supraventricular tachycardia].
Vester, EG, 1997
)
0.3
" The dose-response curves constructed in the presence of 17 beta E (2 x 10(-5) mol/l) produced a rightward shift and a reduction in the maximum response showing inhibitory activity."( In vitro administration of 17 beta-estradiol inhibits drug-induced contractions of the rat isolated seminal vesicle.
Chandranath, SI, 1997
)
0.3
" In the in vivo study, the dose-response curve for the 50% lethal dose (LD50) of bupivacaine was determined for rats."( The effects of verapamil and nimodipine on bupivacaine-induced cardiotoxicity in rats: an in vivo and in vitro study.
Adsan, H; Onaran, O; Tulunay, M, 1998
)
0.65
" After a 4-week single-blind placebo phase, patients received one of the following daily dosage regimens in a double-blind fashion for 6 weeks: placebo, 4 mg of trandolapril, 240 mg of verapamil SR, or a combination of 4 mg of trandolapril and 240 mg of verapamil SR."( Effects of verapamil and trandolapril in the treatment of hypertension. Trandolapril Study Group.
Elliott, WJ; Frishman, WH; Messerli, F, 1998
)
0.88
" A rightward shift in the dose-response curve for InsP3-induced Ca2+ release was observed in permeabilized monolayers of vasopressin-pretreated A7r5 cells (EC50 630 nM and 400 nM for pretreated and non-pretreated cells, respectively)."( Agonist-induced down-regulation of type 1 and type 3 inositol 1,4,5-trisphosphate receptors in A7r5 and DDT1 MF-2 smooth muscle cells.
Casteels, R; Deelman, L; Henning, RH; Missiaen, L; Parys, JB; Sipma, H; Smedt, HD; Vanlingen, S, 1998
)
0.3
" Furthermore, a low incidence of side effects, particularly ankle edema and optimal pharmacokinetics allowing once-daily dosing would be desirable."( Comparative pharmacological properties among calcium channel blockers: T-channel versus L-channel blockade.
Lüscher, TF; Noll, G, 1998
)
0.3
" Dose-response studies revealed procaine hydrochloride pretreated 3 min before KCN, at doses of 18."( Effect of procaine hydrochloride on cyanide intoxication and its effect on neuronal calcium in mice.
Jiang, S; Liu, Z; Zhuang, X, 1998
)
0.3
"To investigate the dose-response relationship and contribution of verapamil SR and trandolapril given in combination once a day for the treatment of essential hypertension."( Verapamil SR and trandolapril combination therapy in hypertension--a clinical trial of factorial design. German Hypertension Study Group.
Compagnone, D; Scholze, J; Zilles, P, 1998
)
1.98
"All dosage combinations of verapamil SR and trandolapril produced significantly greater reduction of blood pressure than the monotherapy at the same dosage."( Verapamil SR and trandolapril combination therapy in hypertension--a clinical trial of factorial design. German Hypertension Study Group.
Compagnone, D; Scholze, J; Zilles, P, 1998
)
2.04
" As an alternative, the dosage of simvastatin should be reduced considerably, that is, by about 50% to 80%, at least when a simvastatin dosage higher than 20 mg/day is used."( Erythromycin and verapamil considerably increase serum simvastatin and simvastatin acid concentrations.
Kantola, T; Kivistö, KT; Neuvonen, PJ, 1998
)
0.64
" Higher dosage of verapamil are needed to block Na+ channels in adult avian heart as reported for mammalian myocardium."( Verapamil and TTX inhibit +Vmax but differentially alter the duration of action potential of adult chicken ventricular myocardium.
Prakash, P; Tripathi, O, 1998
)
2.08
" Independent, duplicate assessments were made of patient outcomes and trial characteristics (including study design, treatment dosage and schedule, duration of treatment, inclusion criteria, and sample size)."( Verapamil use in patients with cardiovascular disease: an overview of randomized trials.
Faich, G; Makuch, R; Pepine, CJ, 1998
)
1.74
"We compared the cumulative dose-response relations of verapamil (0."( Effects of the optical isomers of verapamil on electrophysiological properties of the heart in conscious dogs.
Bosnjak, ZJ; Krolikowski, JG; Lathrop, DA; McCallum, JB; Takahata, O, 1998
)
0.83
" Animals in group 2 (n = 10) with artificially-induced pancreatitis received the same dosage of saline in the same manner."( Continuous calcium channel blocker infusion in experimentally induced acute pancreatitis: effects on pancreas and liver function.
Ciner, I; Ciner, L; Soran, A; Yücel, E, 1998
)
0.3
" Hypothermia shifted the dose-response curves to the right for the negative chronotropic and inotropic effects of verapamil and for the negative chronotropic and positive inotropic effects of zatebradine, but not for the negative chronotropic and positive inotropic effects of E-4031."( Effects of low temperature on the chronotropic and inotropic responses to zatebradine, E-4031 and verapamil in isolated perfused dog atria.
Chiba, S; Furukawa, Y; Hoyano, Y; Kasama, M; Oguchi, T, 1998
)
0.73
" This fact permits the use of high Drol Z dosage in order to achieve a relevant modulating effect in vivo and to use this drug in combination with a further modulator so as to reach maximum efficacy with tolerable side effects."( In vitro efficacy of known P-glycoprotein modulators compared to droloxifene E and Z: studies on a human T-cell leukemia cell line and their resistant variants.
Gieseler, F; Gullis, E; Hasmann, M; Löser, R; Nüssler, V; Pelka-Fleisc, R; Stötzer, O; Wilmanns, W; Zwierzina, H, 1998
)
0.3
"The objective of this study was to investigate whether the decrease in artemisinin bioavailability after repeated oral dosing in humans can be a result of increased efflux of artemisinin by P-glycoprotein or decreased membrane transport at the intestinal barrier."( High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement.
Ashton, M; Carlborg, O; Lennernäs, H; Sandström, R; Svensson, US, 1999
)
0.3
" In this article, we show that the effect of verapamil and diltiazem on cyclosporine levels appears to be independent of dosage within their usual prescription range."( Absence of a dose-response of cyclosporine levels to clinically used doses of diltiazem and verapamil.
Chan, L; Jacob, LP; Malhotra, D; Shapiro, JI, 1999
)
0.78
"This multicenter, randomized, double-blind, parallel group, placebo lead-in, placebo-controlled study compared the antianginal and anti-ischemic effects of once-daily bedtime dosing of controlled-onset extended-release (COER-24) verapamil to a once-daily morning dosing of amlodipine +/- atenolol in patients with chronic stable angina."( Comparison of controlled-onset, extended-release verapamil with amlodipine and amlodipine plus atenolol on exercise performance and ambulatory ischemia in patients with chronic stable angina pectoris.
Deedwania, PC; Fakouhi, TD; Frishman, WH; Glasser, S; Johnson, M; Stone, P, 1999
)
0.74
"1 mg/kg) into the carotid artery directly after infliction of dosed craniocerebral injury improve energy metabolism and limit the intensity of lipid peroxidation in the brain during the first hour of the posttraumatic period."( [Use of neoton and finoptin to correct metabolic disorders of the brain in craniocerebral injuries].
Dolgikh, VT; Ivanov, SR; Zakharov, IV,
)
0.13
"We observed no significant differences in pharmacokinetics (AUCpo, Cmax, tmax, CLo, F and R/S enantiomer ratio) between morning and evening treatment with modified release verapamil and there was no influence of time of dosing on mean prolongation of PR interval."( Chronopharmacology of intravenous and oral modified release verapamil.
Dilger, K; Eckhardt, K; Eichelbaum, M; Hofmann, U; Kucher, K; Mikus, G, 1999
)
0.74
"Time of dosing has no significant influence on pharmacokinetics and pharmacodynamics of this new modified release formulation of verapamil."( Chronopharmacology of intravenous and oral modified release verapamil.
Dilger, K; Eckhardt, K; Eichelbaum, M; Hofmann, U; Kucher, K; Mikus, G, 1999
)
0.75
" At doses of 10(-6)-3 x 10(-5) M, propiverine caused both a rightward shift and inhibition of the maximum response in the acetylcholine (ACh) dose-response curve."( [Effects of propiverine hydrochloride (propiverine) on isolated rat and dog urinary bladder].
Kaneko, S; Nakano, D; Nishimori, T; Ohara, M, 1999
)
0.3
"Intravenous and oral verapamil clearance values were significantly correlated, and cumulative dextromethorphan/3-methoxymorphinan urinary ratios correlated with both plasma AUC(norverapamil)/AUC(verapamil) after oral verapamil dosing and with oral and intravenous verapamil clearance."( In vivo comparison of putative probes of CYP3A4/5 activity: erythromycin, dextromethorphan, and verapamil.
Barnas, CR; Gorski, JC; Krecic-Shepard, ME; Schwartz, JB; Slimko, J; Wainer, IW, 1999
)
0.84
" Intra- and inter-patient variations in methadone bioavailability have been observed after oral methadone treatment and this makes it difficult to predict a dosing regimen."( The roles of P-glycoprotein and intracellular metabolism in the intestinal absorption of methadone: in vitro studies using the rat everted intestinal sac.
Barthe, L; Bouër, R; Houin, G; Philibert, C; Tournaire, C; Woodley, J, 1999
)
0.3
" Our findings raise important questions concerning the need for a dosage adjustment of IDA when MDR modulators are coadministered."( Multidrug resistance modulation in vivo: the effect of cyclosporin A alone or with dexverapamil on idarubicin pharmacokinetics in acute leukemia.
Baccarani, M; Baraldo, M; Damiani, D; Ermacora, A; Fanin, R; Furlanut, M; Michieli, M; Pea, F; Russo, D, 1999
)
0.53
" The effect of MIB on the dose-response curve of externally applied noradrenaline was also studied."( Evidence for a sympatholytic effect of mibefradil in the pithed rat preparation.
Mathy, MJ; Pfaffendorf, M; van der Lee, R; van Zwieten, PA, 2000
)
0.31
" Liver blood flow through individual hepatic vessels was measured up to 8 hours after dosage administration using a duplex Doppler ultrasound technique."( Effect of metoprolol and verapamil administered separately and concurrently after single doses on liver blood flow and drug disposition.
Bauer, LA; Easterling, TR; Horn, JR; Maxon, MS; Shen, DD; Strandness, DE, 2000
)
0.61
" Cocaine shifted the dose-response curve of noradrenaline to the left and enhanced its maximal effects."( Post-junctional mechanisms involved in the potentiation of cardiac adrenergic responses by cocaine.
Bechara, G; El-Bizri, NM; Khoury, HA; Sabra, R; Sharaf, LH, 2000
)
0.31
"A high-performance liquid chromatographic procedure with two detectors is presented for the determination of verapamil in pharmaceutical dosage forms."( High-performance liquid chromatographic analysis of verapamil and its application to determination in tablet dosage forms and to drug dissolution studies.
Biryol, I; Ozkan, SA; Ozkan, Y; Yilmaz, N, 2000
)
0.77
"A novel verapamil chronotherapeutic oral drug absorption system (CODAS-Verapamil) designed for bedtime dosing and with controlled onset and extended-release properties was evaluated in 257 patients with mild-to-moderate essential hypertension in an 8-week, double-blind, placebo-controlled trial."( A new chronotherapeutic oral drug absorption system for verapamil optimizes blood pressure control in the morning.
Neutel, JM; Smith, DH; Weber, MA, 2001
)
0.99
" While repetitive verapamil and talinolol dosing had no statistically significant exsorption-inducing effect, vinblastine and rifampicin pretreatments resulted in decreased intestinal talinolol permeabilities in the three tested gut segments, duodenum, jejunum, and colon [e."( Pretreatment with potent P-glycoprotein ligands may increase intestinal secretion in rats.
Hanafy, A; Langguth, P; Spahn-Langguth, H, 2001
)
0.64
" Verapamil SR/trandolapril 180/2 mg combination produces the best dose-response ratio of different dose combinations of these two drugs."( The fixed combination of verapamil SR/trandolapril.
Widimský, J, 2000
)
1.52
"To compare the steady state pharmacokinetics of the 200 mg verapamil PM CODAS (chronotherapeutic oral drug absorption system) formulation dosed nightly versus immediate-acting verapamil 80 mg tablets dosed three times daily, an open-label, single-dose, two-treatment, two-period, two-sequence, balanced, randomized crossover study was performed with a 7-day washout between two treatment periods."( A steady-state evaluation of the bioavailability of chronotherapeutic oral drug absorption system verapamil PM after nighttime dosing versus immediate-acting verapamil dosed every eight hours.
Butler, J; Devane, JG; Prisant, LM, 2000
)
0.77
" Efficacy was assessed as change from baseline in blood pressure (BP), heart rate, and rate-pressure product during four time periods throughout the dosing interval."( Chronotherapeutic delivery of verapamil in obese versus non-obese patients with essential hypertension.
Black, HR; Elliott, WJ; Johnson, MF; White, WB, 2001
)
0.6
" The dose-response curve for NE (0."( Lead-cadmium interaction effect on the responsiveness of rat mesenteric vessels to norepinephrine and angiotensin II.
Andrzejak, R; Skoczyńska, A; Wróbel, J, 2001
)
0.31
" Concentrations of NFZ and TZD achieved in the intestine after chronic oral dosing may induce P-gp expression and reduce absorption of coadministered drugs."( P-glycoprotein interactions of nefazodone and trazodone in cell culture.
Greenblatt, DJ; Perloff, MD; Störmer, E; von Moltke, LL, 2001
)
0.31
" This relatively small interactive effect occurred only while peak plasma drug concentrations were developing at 1 to 3 hours after dosing and is probably caused by the known effect of verapamil to increase hepatic and portal bloodflow."( Transient kinetic and dynamic interactions between verapamil and dofetilide, a class III antiarrhythmic.
Cheng, SL; Johnson, BF; Venitz, J, 2001
)
0.75
" Inhibitory concentration (IC50) values for a number of compounds were calculated as means +/- SEM from dose-response determinations."( Second messengers in platelet aggregation evoked by serotonin and A23187, a calcium ionophore.
Cheema, M; Connor, JD; Gilani, AH; Rasheed, H; Rizvi, Z; Saeed, SA, 2001
)
0.31
" On day 7, concentrations of verapamil and norverapamil enantiomers were determined during one dosing interval, and model independent pharmacokinetic parameters were estimated."( Effects of grapefruit juice and smoking on verapamil concentrations in steady state.
Fuhr, U; Harder, S; Jünemann, M; Kern, R; Lopez-Rojas, P; Müller-Peltzer, H; Staib, AH, 2002
)
0.87
" Buccal formulation has previously been designed as an alternative form of dosing verapamil."( Pharmacokinetics of verapamil and its metabolite norverapamil from a buccal drug formulation.
Janicki, S; Sawicki, W, 2002
)
0.86
"We studied the effects of a chronotherapeutic delivery system of verapamil (controlled-onset extended release [COER]-24 system) dosed at bedtime versus conventional morning administration of both enalapril and losartan on the blood pressure (BP), heart rate, and the heart rate systolic BP product during the first 4 hours after awakening in a placebo-controlled, forced-titration trial."( Preventing increases in early-morning blood pressure, heart rate, and the rate-pressure product with controlled onset extended release verapamil at bedtime versus enalapril, losartan, and placebo on arising.
Anders, RJ; Calhoun, D; Mansoor, GA; Sica, DA; White, WB, 2002
)
0.76
"Bedtime administration of an agent designed to parallel the circadian rhythm of BP and heart rate led to significantly greater early morning hemodynamic effects compared with other conventional once-daily antihypertensive agents dosed in the morning."( Preventing increases in early-morning blood pressure, heart rate, and the rate-pressure product with controlled onset extended release verapamil at bedtime versus enalapril, losartan, and placebo on arising.
Anders, RJ; Calhoun, D; Mansoor, GA; Sica, DA; White, WB, 2002
)
0.52
" Verapamil, administered at a dosage corresponding to a typical cardiovascular posology in humans, significantly increased doxorubicin toxicity."( Toxicologic and pharmacokinetic study of low doses of verapamil combined with doxorubicin.
Bartoli, F; Candussio, L; Crivellato, E; Decorti, G; Giraldi, T; Granzotto, M; Rosati, A, 2002
)
1.47
" After 4-year treatment, verapamil has been substituted for its retard dosage form--isoptin retard."( [Verapamil retard as a medication for the prevention of affective and schizoaffective psychosis relapses].
Raiushkin, VA, 2002
)
1.53
" FDA's newly issued guidance on bioequivalence recommends the use of individual bioequivalence (IBE) for highly variable drugs and possibly for modified release dosage forms."( Assessing individual bioequivalence with high-order cross-over designs: a unified procedure.
Hsuan, FC; Reeve, R, 2003
)
0.32
" The higher the dosage used, the higher the regression of the atherosclerotic lesions."( Planimetric and histological study of the aortae in atherosclerotic chickens treated with nifedipine, verapamil and diltiazem.
Ayala, I; Ballesta, J; Castells, MT; Fernández Pardo, J; García Pérez, B; Madrid, JF; Ortega, JV; Ortega, MR; Valdés, M, 2003
)
0.53
" Additionally, a time control experiment was conducted, during which the methacholine dose-response curve was measured twice during vehicle infusions (n = 5)."( Direct effect of ethanol on human vascular function.
Creager, MA; Omland, T; Tawakol, A, 2004
)
0.32
"High dosage of NIF, VER and DIL has an inhibitory effect on the entrance of extracellular Ca2+ into islet cells and thus reduces insulin secretion."( [The effect of Ca2+ channel blocker on insulin secretion in rat pancreatic islet cells].
Gao, SW; Yin, W; Zhu, TH, 2004
)
0.32
" Ouabain shifted the NE dose-response curve to the left without changing in the maxium response."( [Effect of ouabain on the aortic rings of guinea pig and its interactions with Ca2+, norepinephrine].
Cheng, L; Gong, XR; Wang, F; Yao, WX; Zhou, HY, 2003
)
0.32
" At a sub-effective dose, pargyline could cause a leftward shift in the dose-response curve of 5-HTP-induced antinociception."( L-type calcium channel blockers enhance 5-HTP-induced antinociception in mice.
Chen, B; Han, R; Li, JX; Liang, JH; Lu, Y; Wang, XH; Ye, XF; Zhang, P, 2004
)
0.32
" After starting 200 mg/d at bedtime, dosing was titrated to a maximum of 400 mg/d at 4-week intervals to achieve a target blood pressure of <140/<90 mm Hg using morning blood pressure measurements."( Treatment of elderly hypertensive patients with a delayed-release verapamil formulation in a community-based trial.
Black, HR; Messerli, FH; Prisant, LM; Weber, MA,
)
0.37
" The method has been successfully applied to the determination of the drug in commercial dosage forms."( Spectrophotometric method for the determination of verapamil hydrochloride in pharmaceutical formulations using N-bromosuccinimide as oxidant.
Hejaz Azmi, SN; Rahman, N, 2004
)
0.58
" In clinical practice we found we needed to adapt dosage to individual's time of attacks, in particular giving higher doses before going to bed to suppress severe nocturnal episodes."( Individualizing treatment with verapamil for cluster headache patients.
Blau, JN; Engel, HO,
)
0.42
"To find the minimum dose of verapamil required to prevent episodic and chronic cluster headaches by supervising each individual and adjusting the dosage accordingly."( Individualizing treatment with verapamil for cluster headache patients.
Blau, JN; Engel, HO,
)
0.71
"Providing the dosage for each individual is adequate, preventing CH with verapamil is highly effective, taken three (occasionally with higher doses, four) times a day."( Individualizing treatment with verapamil for cluster headache patients.
Blau, JN; Engel, HO,
)
0.65
" Thus, it is possible to formulate a single-unit, controlled-release dosage form of verapamil for oral administration at least once every 12 hours using the polymers CA and EC."( Preparation and evaluation of verapamil hydrochloride microcapsules.
Mahanti, B; Mahapatra, S; Mukherjee, B; Panda, P,
)
0.64
" Using propranolol as a model compound the effect of formulation and dosing variables was explored as a means to characterize the limiting parameters of this model."( A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol, verapamil and captopril.
Dali, MM; Heran, CL; Mathias, NR; Moench, PA; Smith, RL; Stetsko, PI, 2006
)
0.55
" Dose-response curves for transport and the ratio of dye concentration in the secreted fluid to that in the bathing medium (S/M) were determined for Texas Red as well as for P-gp substrates (rhodamine 123, daunorubicin), the organic anion fluorescein and the organic cation quinacrine."( Transepithelial transport of fluorescent p-glycoprotein and MRP2 substrates by insect Malpighian tubules: confocal microscopic analysis of secreted fluid droplets.
Leader, JP; O'Donnell, MJ, 2005
)
0.33
" Dose-response curves to benzodiazepines on peak [Ca2+]i and shortening were not affected by pretreatment with Bay K 8644 (0."( Effects of L-type Ca2+ channel modulation on direct myocardial effects of diazepam and midazolam in adult rat ventricular myocytes.
Damron, DS; Kanaya, N; Murray, PA, 2006
)
0.33
" Based on these results, the verapamil dosage should be adjusted when given with naringin or a naringin-containing dietary supplement."( Effect of naringin pretreatment on bioavailability of verapamil in rabbits.
Choi, JS; Yeum, CH, 2006
)
0.87
"00105) and 10-day dosing (102 +/- 40 L/h, P = ."( The effect of short- and long-term administration of verapamil on the disposition of cytochrome P450 3A and P-glycoprotein substrates.
Gorski, JC; Hall, SD; Hamman, MA; Lemma, GL; Wang, Z; Zaheer, NA, 2006
)
0.58
"5 nmol dose of [3H]-verapamil (infused within 1 min) in the absence and presence of the amiodarone (1 microM) in perfusate, as well as using a double dosing regimen (0."( Modeling cardiac uptake and negative inotropic response of verapamil in rat heart: effect of amiodarone.
Abdelrahman, O; Sermsappasuk, P; Weiss, M, 2007
)
0.91
"0 mg/mL) caused a rightward shift in the Ca(++) dose-response curves similar to that caused by verapamil, a standard calcium channel blocker."( Antispasmodic effect of Acorus calamus Linn. is mediated through calcium channel blockade.
Ahmad, M; Gilani, AU; Shah, AJ; Shaheen, F, 2006
)
0.55
" Abbreviated dosing of verapamil prior to cardioversion improves outcome at 1 week postcardioversion."( Signal-averaged P wave reflects change in atrial electrophysiological substrate afforded by verapamil following cardioversion from atrial fibrillation.
Lane, J; Redfearn, DP; Skanes, AC; Stafford, PJ, 2006
)
0.86
" CCAs can be safely used in children with renal insufficiency or failure and as a general rule there is no need to modify drug dosage in this population."( A review of calcium channel antagonists in the treatment of pediatric hypertension.
Sahney, S, 2006
)
0.33
"The dose-response studies revealed that intracarotid administration of nicardipine, compared with verapamil, was more effective in augmenting cerebral blood flow."( Augmentation of cerebral blood flow and reversal of endothelin-1-induced vasospasm: a comparison of intracarotid nicardipine and verapamil.
Etu, JJ; Joshi, S; Lavine, SD; Meyers, PM; Wang, M, 2007
)
0.76
" In the long asymptomatic period, it is imperative to select a proper dosing regimen for drugs that are applicable to hepatic fibrosis."( Establishment of rat precision-cut fibrotic liver slice technique and its application in verapamil metabolism.
Guo, Y; Wang, H; Zhang, C,
)
0.35
" Verapamil pharmacokinetics and pharmacodynamics were determined after 7 days of dosing with 240 mg daily."( Cytochrome P450 3A5 genotype is associated with verapamil response in healthy subjects.
Hall, SD; Hamman, MA; Hilligoss, J; Jin, Y; Kovacs, RJ; Li, L; Marunde, R; Miao, J; Philips, S; Phillips, S; Wang, YH, 2007
)
1.51
"4% in rats, with non-linear pharmacokinetics when its dosage increased."( Role of P-glycoprotein in the intestinal absorption of tanshinone IIA, a major active ingredient in the root of Salvia miltiorrhiza Bunge.
Chen, X; Chowbay, B; Duan, W; Li, CG; Liang, J; Lin, SG; Liu, PQ; Wen, JY; Yu, XY; Zhou, SF; Zhou, ZW, 2007
)
0.34
" To achieve BP target a combination of antihypertensives will be needed, and the use of long-acting drugs that are able to provide 24-hour efficacy with a once-daily dosing confers the noteworthy advantages of compliance improvement and BP variation lessening."( Trandolapril/verapamil combination in hypertensive diabetic patients.
García Donaire, JA; Ruilope, LM, 2007
)
0.71
" Dose-response curves revealed IC(50) values of 199+/-19 microM for verapamil, 466+/-151 microM for gallopamil and 326+/-67 microM for diltiazem."( Effects of phenylalkylamines and benzothiazepines on Ca(v)1.3-mediated Ca2+ currents in neonatal mouse inner hair cells.
Engel, J; Lacinova, L; Tarabova, B, 2007
)
0.58
" In the long asymptomatic period, it is imperative to select a proper dosing regimen for drugs that are applicable to hepatic fibrosis owing to altered pharmacokinetics and bioavailability."( Effects of liver fibrosis on verapamil pharmacokinetics in rats.
Chen, M; Hu, XL; Wang, H; Xu, D, 2008
)
0.64
"A cremophor mixed micelle formulation of saquinavir alone, or co-administered with P-gp/CYP modulators, verapamil, ketoconazole or cyclosporine, was dosed intraduodenally in the mesenteric lymph duct cannulated anaesthetized rat model."( An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
Griffin, BT; O'Driscoll, CM, 2008
)
0.56
" We build upon our previous findings and generated a simple index for the adequate administration dosage of beta-methyldigoxin based on variable degrees of renal function and the serum trough level of beta-methyldigoxin."( [Pharmaceutical support in the cardiovascular and cardiovascular surgery ward].
Kataoka, Y; Machida, S; Masuda, K, 2007
)
0.34
"A clear reduction of BP values was recorded after both the first and the second month of treatment with kanrenoate, with the maximal effect obtained when the dosage titration at 100 mg/day was accomplished."( Menopause not aldosterone-to-renin ratio predicts blood pressure response to a mineralocorticoid receptor antagonist in primary care hypertensive patients.
Blengio, GS; Ciacciarelli, A; Corrocher, R; Falcone, S; Olivieri, O; Pizzolo, F; Signorelli, D, 2008
)
0.35
" This may explain some of the beneficial effects of this fixed dosed combination that are non-related to its antihypertensive effects."( The effect of trandolapril and its fixed-dose combination with verapamil on circulating adhesion molecules levels in hypertensive patients with type 2 diabetes.
Escalante-Acosta, BA; Rodriguez-Lopez, L; Rubio-Guerra, AF; Vargas-Ayala, G; Vargas-Robles, H, 2008
)
0.59
" Marketed Verapamil is a calcium channel blocker, mainly used as antihypertensive and anti-anginal drug and available in various dose and dosage forms."( Ethanol effects on drug release from Verapamil Meltrex, an innovative melt extruded formulation.
Breitenbach, J; Brennan, D; Burst, A; Roth, W; Sellers, E; Setnik, B; Zietsch, M, 2009
)
1.03
" The increased bioavailability of etoposide in the presence of verapamil should be taken into consideration for dosage regimens due to a potential drug interaction (DI)."( Effects of verapamil on etoposide pharmacokinetics after intravenous and oral administration in rats.
Choi, JS; Li, X; Piao, YJ,
)
0.76
" In this case sustained ventricular tachycardia was developed suddenly a year later after ablation, despite the treatment with low dosage verapamil (80 mg/tid)."( A case report. A patient with idiopathic ventricular tachycardia.
Avaliani, I; Kacharava, G; Rahmat, B; Venkata, KI, 2008
)
0.55
" Verapamil (25mg/kg) was administered orally 2h before irinotecan oral (80 mg/kg) or intravenous (20mg/kg) dosing in female Wistar rats."( Effect of P-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of irinotecan in rats.
Bansal, T; Jaggi, M; Khar, RK; Mishra, G; Talegaonkar, S, 2009
)
1.54
"The release of verapamil hydrochloride from tablets with Eudragit RLPO or Kollidon SR with different drug-to-polymer ratios were investigated with a view to develop twice-daily sustained-release dosage form by solid dispersion (SD) technique."( Formulation of sustained-release dosage form of verapamil hydrochloride by solid dispersion technique using Eudragit RLPO or Kollidon SR.
Biswal, S; Murthy, PN; Sahoo, J, 2009
)
0.96
"A novel gastro retentive controlled release drug delivery system of verapamil HCl was formulated in an effort to increase the gastric retention time of the dosage form and to control drug release."( Development and in vivo floating behavior of verapamil HCl intragastric floating tablets.
Modasiya, M; Patel, A; Patel, V; Shah, D, 2009
)
0.85
" A clopidogrel maintenance dosage of 150 mg daily for 1 week resulted in greater platelet inhibition than 75 mg daily (50 +/- 28% vs."( The antiplatelet effect of higher loading and maintenance dose regimens of clopidogrel: the PRINC (Plavix Response in Coronary Intervention) trial.
Armstrong, G; Dahl, ML; El-Jack, S; Farrell, H; Gladding, P; Gunes, A; Kay, P; Ormiston, J; Ruygrok, P; Scott, D; Stewart, J; Webster, M; Zeng, I, 2008
)
0.35
" A maintenance dosage of 150 mg daily produces greater platelet inhibition than 75 mg daily."( The antiplatelet effect of higher loading and maintenance dose regimens of clopidogrel: the PRINC (Plavix Response in Coronary Intervention) trial.
Armstrong, G; Dahl, ML; El-Jack, S; Farrell, H; Gladding, P; Gunes, A; Kay, P; Ormiston, J; Ruygrok, P; Scott, D; Stewart, J; Webster, M; Zeng, I, 2008
)
0.35
"To examine the effects of verapamil on the intracellular drug pharmacokinetics of epirubicin using alternative dosing schedules."( Time-lapse live cell imaging and flow analysis of multidrug resistance reversal by verapamil in bladder cancer cell lines.
Birch, BR; Cooper, AJ; Featherstone, JM; Hayes, MC; Lwaleed, BA; Speers, AG, 2009
)
0.88
" Flow cytometry was performed after the alternative dosing regimens."( Time-lapse live cell imaging and flow analysis of multidrug resistance reversal by verapamil in bladder cancer cell lines.
Birch, BR; Cooper, AJ; Featherstone, JM; Hayes, MC; Lwaleed, BA; Speers, AG, 2009
)
0.58
" The present results highlight the need for additional clinical trials of drug dosing and scheduling for combination intravesical chemotherapy regimens."( Time-lapse live cell imaging and flow analysis of multidrug resistance reversal by verapamil in bladder cancer cell lines.
Birch, BR; Cooper, AJ; Featherstone, JM; Hayes, MC; Lwaleed, BA; Speers, AG, 2009
)
0.58
" In a randomized, two-phase, crossover design, verapamil was dosed 80 mg three times daily (with total daily doses of 240 mg) for 6 days, and on day 6, a single 120-mg dose of fexofenadine was administered along with an 80-mg dose of verapamil."( Enantioselective disposition of fexofenadine with the P-glycoprotein inhibitor verapamil.
Hokama, N; Miura, M; Sakugawa, T; Suzuki, T; Tateishi, T; Uno, T, 2009
)
0.84
" NOX-1 also significantly antagonized cumulative dose-response effect of norepinephrine, phenylephrine, KCl or calcium with reduction in submaximal contractions."( Vasorelaxant effect in rat aortic rings through calcium channel blockage: a preliminary in vitro assessment of a 1,3,4-oxadiazole derivative.
Bankar, GR; Chamallamudi, MR; Nampurath, GK; Nandakumar, K; Nayak, PG; Thakur, A, 2009
)
0.35
" These results suggest that caution be exercised when these solubilizing agents are included in preclinical oral dosing solutions as the perturbation of drug absorption barriers may heighten the risk of incorrectly classifying drug candidate PK-parameters."( Absorption barriers in the rat intestinal mucosa. 3: Effects of polyethoxylated solubilizing agents on drug permeation and metabolism.
Borchardt, RT; Mudra, DR, 2010
)
0.36
" An individualized dosage regimen design incorporating such information may improve the efficacy of the drug whilst reducing adverse reactions."( Influence of ABCB1 gene polymorphisms on the pharmacokinetics of verapamil among healthy Chinese Han ethnic subjects.
He, XJ; Li-Ling, J; Qiu, F; Sun, YX; Zhao, LM, 2009
)
0.59
" Cumulative levobupivacaine dose-response curves over a range of 10(-6) to 3 x 10(-4) M were constructed in 1) aortic rings with no drug pretreatment; 2) endothelium-denuded rings pretreated with quinacrine dihydrochloride (nonspecific phospholipase A(2) inhibitor: 2 x 10(-5), 4 x 10(-5) M), nordihydroguaiaretic acid (NDGA) (lipoxygenase inhibitor: 10(-5), 3 x 10(-5) M), indomethacin (nonspecific cyclooxygenase inhibitor: 10(-5) M), AA-861 (5-lipoxygenase inhibitor: 10(-5), 5 x 10(-5) M), fluconazole (cytochrome P450 epoxygenase inhibitor: 10(-5) M), verapamil (10(-5) M), or calcium-free solution; and 3) endothelium-intact rings pretreated with N(omega)-nitro-L-arginine methyl ester (L-NAME) (nitric oxide synthase inhibitor: 5 x 10(-5) M), indomethacin, or fluconazole."( The direct effect of levobupivacaine in isolated rat aorta involves lipoxygenase pathway activation and endothelial nitric oxide release.
Choi, YS; Hah, YS; Hwang, EM; Jeong, YS; Lee, SH; Ok, SH; Park, JY; Shin, IW; Sohn, JT, 2010
)
0.52
" The aim of this study was to evaluate the dose-response relationship of two potent P-gp inhibitors and to investigate if increased brain uptake of VPM mediated by P-gp inhibition can be used to assess regional differences in P-gp activity."( Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.
Bankstahl, JP; Bankstahl, M; Brauner, R; Ding, X; Karch, R; Kuntner, C; Langer, O; Löscher, W; Meier, M; Müller, M; Stanek, J; Stundner, G; Wanek, T, 2010
)
0.56
" Verapamil heart tissue and plasma levels after intraperitoneal dosing of spontaneously hypertensive and normotensive rats were investigated."( Impaired tissue clearance of verapamil in rat cardiac hypertrophy results in transcriptional repression of ion channels.
Borlak, J; Zwadlo, C, 2010
)
1.56
" After rats were injected intrathecally with verapamil and diltiazem, dose-response curves were constructed."( The dose-dependent study of verapamil and diltiazem on spinal anesthesia in the rat.
Chen, YC; Chen, YW; Chu, CC; Hung, CH; Wang, JJ, 2010
)
0.91
" Subcutaneous ECG leads were implanted, and 2 days following the second injection, each rat was dosed with 25 mg·kg(-1) verapamil per os, and an ECG was recorded over 4 h after dosing."( Drug-disease interaction: reduced verapamil response in isoproterenol-induced myocardial injury in rats.
El-Kadi, AO; Hanafy, S; Jamali, F, 2010
)
0.85
"After the dosing of an extended-release (ER) formulation, compounds may exist in solutions at various concentrations in the colon because the drugs are released at various speeds from the ER dosage form."( The relationship between the drug concentration profiles in plasma and the drug doses in the colon.
Hosoi, Y; Kanamaru, T; Konno, T; Nakagami, H; Tajiri, S; Yada, S; Yoshida, K, 2010
)
0.36
" Combination therapy can reduce the dosage of each drug but achieve equal or better efficacy than monotherapy, reducing the side effects of a single drug."( The effect of combined steroid and calcium channel blocker injection on human hypertrophic scars in animal model: a new strategy for the treatment of hypertrophic scars.
Huang, CY; Yang, JY, 2010
)
0.36
"A microdose study was performed where 50 µg R/S-(14)C-verapamil was dosed intravenously to human volunteers."( Development of 2D chiral chromatography with accelerator mass spectrometry for quantification of (14)C-labeled R- and S-verapamil in plasma.
Keely, BJ; Lappin, G; Simpson, M, 2010
)
0.82
" Therefore, we had to limit the dosage to 1-1."( Add-on treatment with verapamil in pharmacoresistant canine epilepsy.
Jambroszyk, M; Potschka, H; Tipold, A, 2011
)
0.68
"The failure of the maximum tolerated dosage to improve seizure control in dogs with phenobarbital-resistant epilepsy argues against the suitability of verapamil add-on treatment to overcome pharmacoresistance."( Add-on treatment with verapamil in pharmacoresistant canine epilepsy.
Jambroszyk, M; Potschka, H; Tipold, A, 2011
)
0.88
" Thus, the proposed method is simple and suitable for the simultaneous analysis of active ingredients in dosage forms and human serum."( Simultaneous determination of gliquidone, pioglitazone hydrochloride, and verapamil in formulation and human serum by RP-HPLC.
Arayne, MS; Mirza, AZ; Sultana, N, 2011
)
0.6
" In vivo, the oral bioavailability of PTX loaded in NOSC micelles (PTX-M) was 6-fold improved in comparison with that of an orally dosed Taxol(®)."( The mechanism of enhancement on oral absorption of paclitaxel by N-octyl-O-sulfate chitosan micelles.
Jin, X; Ju, C; Li, N; Mo, R; Ping, Q; Sun, M; Zhang, C, 2011
)
0.37
" The average of recovery in synthetic samples as well as dosage forms was 98."( Rapid inexpensive assay method for verapamil by spectrophotometric sequential injection analysis.
Abulkibash, AM; Ibrahim, AE; Ibrahim, KE; Idris, AM; Saleh, TA, 2011
)
0.65
" The cardiomyocytes showed a chronotropic dose-response (0."( Pharmacological response of human cardiomyocytes derived from virus-free induced pluripotent stem cells.
Atan, S; Chung, YY; Dusting, G; Iskandar, F; Mehta, A; Ng, A; Shim, W; Sun, W; Wei, H; Wong, P, 2011
)
0.37
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" An in vivo study, verapamil (25mg/kg, per oral) was administered 2h before phenytoin (30mg/kg, per oral) dosing in male Wistar rats."( Study on in situ and in vivo absorption kinetics of phenytoin by modulating P-glycoprotein with verapamil in rats.
Bedada, SK; Ganji, D; Neerati, P, 2011
)
0.92
" For dose-response studies, LS-180 cells were treated with different concentrations of the selected drugs followed by P-gp protein and gene expressions analyses."( Exposure of LS-180 cells to drugs of diverse physicochemical and therapeutic properties up-regulates P-glycoprotein expression and activity.
Abuznait, AH; Kaddoumi, A; Patrick, SG, 2011
)
0.37
" Toxicity studies with Diclofenac, Paracetamol and Verapamil in both cell lines show dose-response characteristics and EC(50) values similar to hHeps."( Comparative analysis of phase I and II enzyme activities in 5 hepatic cell lines identifies Huh-7 and HCC-T cells with the highest potential to study drug metabolism.
Dooley, S; Ehnert, S; Hao, L; Lin, J; Liu, L; Mühl-Benninghaus, R; Neumann, J; Nussler, AK; Nussler, N; Schyschka, L; Stöckle, U, 2012
)
0.63
" A concentration- or dose-response relationship was shown between the concentration and dose of CH and Rho123 accumulation or the antitumor activity."( Using rhodamine 123 accumulation in CD8 cells as a surrogate indicator to study the P-glycoprotein modulating effect of cepharanthine hydrochloride in vivo.
Cai-Hong, Z; Fang, M; Jin-Hua, J; Li, H; Ning, W; Qing-Duan, W; Xiao-Juan, G; Yan, Z, 2011
)
0.37
" Once a day dosage forms for drugs differing in solubility have been developed using a single polymer matrix which is easy to manufacture."( pH Sensitive graft copolymers for zero order drug release: a mechanistic analysis.
Kulkarni, MG; Muthusamy, R, 2012
)
0.38
" We compared the dose-response relationship of tariquidar in humans with data obtained in rats using a similar methodology."( Pgp-mediated interaction between (R)-[11C]verapamil and tariquidar at the human blood-brain barrier: a comparison with rat data.
Bankstahl, JP; Bauer, M; Böhmdorfer, M; Jäger, W; Karch, R; Koepp, M; Kuntner, C; Langer, O; Löscher, W; Matzneller, P; Mitterhauser, M; Müller, M; Stanek, J; Wadsak, W; Zeitlinger, M, 2012
)
0.64
" Further studies in humans are required to determine whether modification of the oral verapamil dosage regimen in HL states is necessary."( Pharmacokinetics of verapamil and its metabolite norverapamil in rats with hyperlipidaemia induced by poloxamer 407.
Kang, HE; Lee, MG; Lee, YS; Yoon, IS; Yoon, JN, 2012
)
0.93
" The exploration of the intestinal absorption mechanism is crucial to the design of dosage form and clinical use of limonin."( [Transport of limonin in rat intestine in situ and Caco-2 cells in vitro].
He, L; Ke, X; Tian, JL; Zhang, XY, 2012
)
0.38
"A couple of days after increasing the dosage of betaadrenergic- and adding calcium channel blockers due to an increased heart rate in atrial fibrillation, a 77 year old female was found in cardiogenic shock."( [The choked heart].
Furrer, F; Giambarba, C, 2012
)
0.38
" Verapamil-poisoned rats received the higher dosing regimen of FDP250."( The effects of fructose-1,6-diphosphate on haemodynamic parameters and survival in a rodent model of propranolol and verapamil poisoning.
Graudins, A; Kalam, Y, 2012
)
1.5
"0-10 mg/mL relaxed high K+ (80 mM) and phenylephrine (PE, 1 μM)-induced contractions and shifted Ca++ dose-response curves to right, similar to that caused by verapamil."( Hypotensive effect of Gentiana floribunda is mediated through Ca++ antagonism pathway.
Khan, AU; Murugan, DD; Mustafa, MR, 2012
)
0.58
" In patients with life-saving use in suicide attempts important role in addition to medication dosage plays an elapsed time of their consumption and speed of action taken to remove and prevent absorbtion the poison", as well as close supervision in the intensive care unit."( [Drugs acting on the heart-conductive system in suicide attempts].
Dabek, J; Jakubowski, D; Rychlik, W; Stachoń, K, 2012
)
0.38
" The absence of stereoselectivity after iv dosing indicates that the first-pass tissue binding effect is an important factor in determining the steroselective PK of R/S-VER after oral administration."( Binding processes determine the stereoselective intestinal and hepatic extraction of verapamil in vivo.
Dickinson, PA; Lennernäs, H; Sjögren, E; Thörn, HA, 2012
)
0.6
"Cassette dosed plasma and brain samples from nine compounds were extracted using a protein precipitation method."( High-throughput liquid chromatography/mass spectrometry method for the quantitation of small molecules using accurate mass technologies in supporting discovery drug screening.
Dean, B; Deshmukh, G; Ding, X; Ghobarah, H; Hop, CE; Jaochico, A; Liederer, BM; Liu, X; Zhang, X, 2013
)
0.39
" Moreover, VPL completely restored susceptibility to ivermectin in a resistant isolate resulting in virtually identical dose-response curves of susceptible and resistant isolates in the presence of VPL."( Potential contribution of P-glycoproteins to macrocyclic lactone resistance in the cattle parasitic nematode Cooperia oncophora.
AlGusbi, S; De Graef, J; Demeler, J; Geldhof, P; Kerboeuf, D; Krücken, J; Pomroy, WE; Ramünke, S; von Samson-Himmelstjerna, G, 2013
)
0.39
"97) or ramipril (AUC over a uniform dosing interval τ at steady state [AUCτ,ss]: GMR, 96."( Lack of clinically relevant drug-drug interaction between empagliflozin, a sodium glucose cotransporter 2 inhibitor, and verapamil, ramipril, or digoxin in healthy volunteers.
Broedl, UC; Macha, S; Pinnetti, S; Rose, P; Schoene, K; Sennewald, R; Woerle, HJ, 2013
)
0.6
" These results may provide a possible explanation for higher methadone dosage requirements in patients carrying variant-type of P-gp and revealed the possible drug-drug interactions in patients who receive concomitant drugs which are also P-gp substrates."( Functional impact of ABCB1 variants on interactions between P-glycoprotein and methadone.
Chiou, MH; Hsieh, YW; Huang, CL; Hung, CC; Lane, HY; Teng, YN, 2013
)
0.39
" IFE therapy is being recommended by US PCCs; protocols and dosing regimens are nearly uniform."( Lipid rescue 911: Are poison centers recommending intravenous fat emulsion therapy for severe poisoning?
Christian, MR; Mycyk, MB; Pallasch, EM; Wahl, M, 2013
)
0.39
" Pharmacokinetic and pharmacodynamic changes depend on the nature and degree of hepatic impairment and on the characteristics of the dosed drug."( [Effect of liver cirrhosis on pharmacokinetics and pharmacodynamics of drugs].
Perlík, F, 2013
)
0.39
"The Biopharmaceutics Drug Disposition Classification System (BDDCS) predicts intestinal transporter effects to be clinically insignificant following oral dosing for highly soluble and highly permeable/metabolized drugs (class 1 drugs)."( Effect of P-glycoprotein on the rat intestinal permeability and metabolism of the BDDCS class 1 drug verapamil.
Benet, LZ; Estudante, M; Maya, M; Morais, JG; Soveral, G, 2013
)
0.61
" The formulation factors such as the viscosity grade of polyethylene oxide as the primary polymer as well as the level and location of osmogen within the bilayer tablets led to a difference in performance of osmotic tablets and hence should be critically evaluated in the design of such dosage forms."( Investigation of critical core formulation and process parameters for osmotic pump oral drug delivery.
Farrell, TP; Huatan, H; Missaghi, S; Patel, P; Rajabi-Siahboomi, AR, 2014
)
0.4
" Prior to the revision of the European Medicines Agency (EMA, formerly EMEA) guideline in 2010, the "dose" in this ratio was consistently defined by the US FDA, the EMA, and the WHO biowaiver guidelines as the highest dosage strength."( The impact of the EMA change in definition of "dose" on the BCS dose-solubility ratio: a review of the biowaiver monographs.
Dressman, J; Kubbinga, M; Langguth, P; Sediq, A, 2014
)
0.4
" These candidates were subjected to a dose-response bioactivity assay, measuring an increase in α-tubulin K40 acetylation in two neuronal cell lines, which yielded five compounds bioactive in both cell lines and eight compounds bioactive in at least one of the cell lines tested."( Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
Choi, SH; Kazantsev, AG; Khanfar, MA; Quinti, L; Silverman, RB; Wang, H, 2014
)
0.4
" Throughout the study, carbamazepine, valproic acid and clobazam levels increased following verapamil intake; minor dosage adjustment was required in one patient on carbamazepine."( A pilot double-blind trial using verapamil as adjuvant therapy for refractory seizures.
Ali, A; Andrade, DM; Borlot, F; Verocai, F; Wither, RG; Wu, N, 2014
)
0.9
"This review aims to identify recent literature on the use of ILE in humans as an antidote and to familiarize emergency providers with the indications, availability, dosing recommendations, and adverse reactions associated with ILE use."( Intravenous lipid emulsion in the emergency department: a systematic review of recent literature.
Cao, D; Foran, M; Heard, K; Koyfman, A, 2015
)
0.42
" ILE should be administered per American Society of Regional Anesthesia and Pain Medicine dosing recommendations."( Intravenous lipid emulsion in the emergency department: a systematic review of recent literature.
Cao, D; Foran, M; Heard, K; Koyfman, A, 2015
)
0.42
" Brain exposure at microdosing agreed with pharmacological dosing conditions for the investigated drugs."( Large Variation in Brain Exposure of Reference CNS Drugs: a PET Study in Nonhuman Primates.
Amini, N; Farde, L; Finnema, SJ; Halldin, C; Lundquist, S; Nakao, R; Schou, M; Takano, A; Varnäs, K, 2015
)
0.42
" To augment the clinical trial results, we performed mouse orthotopic xenograft experiments using similar dosing to test tumor growth, vascularity, and drug bioavailability."( Combined Hydroxyurea and Verapamil in the Clinical Treatment of Refractory Meningioma: Human and Orthotopic Xenograft Studies.
Barth, T; Burt, L; Dunson, W; Gillespie, DL; Hoang, N; Jensen, RL; Karsy, M, 2016
)
0.74
" As a result, proportionally similar strengths of ER dosage forms that meet biowaiver requirements per current regulatory guidelines cannot ensure bioequivalence in all cases."( Influence of Drug Properties and Formulation on In Vitro Drug Release and Biowaiver Regulation of Oral Extended Release Dosage Forms.
Hoag, S; Lin, Z; Qiu, Y; Zhou, D, 2016
)
0.43
"Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of NAs, and combination therapy of NA and MRP inhibitors could reduce the dosage for long-term NA use."( Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of nucleos(t)ide analogues.
Chen, Q; Liu, W; Liu, Y; Lu, M; Song, H; Wang, B; Xu, C; Xu, D; Yang, D; Zhang, W; Zheng, X, 2016
)
0.43
"The measured data and simulations for pharmacologically unstimulated contraction resembled findings in native human heart tissue, while the pharmacological dose-response curves were highly accurate and consistent with reference data."( Mechano-Pharmacological Characterization of Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells.
Artmann, AT; Artmann, GM; Bayer, R; Epple, M; Frotscher, R; Goßmann, M; Linder, P; Neumann, S; Staat, M, 2016
)
0.43
" The extract caused rightward shift of the Ca(++) dose-response curves, similar to that caused by verapamil, indicating that it produced vasorelaxation by inhibiting extracellular Ca(2+) influx."( Antihypertensive activity of 80% methanol seed extract of Calpurnia aurea (Ait.) Benth. subsp. aurea (Fabaceae) is mediated through calcium antagonism induced vasodilation.
Engidawork, E; Getiye, Y; Tolessa, T, 2016
)
0.65
" However, only curcumin could increase the sensitivity of DOX at all dosing levels, therefore used for further studies."( Selection of P-Glycoprotein Inhibitor and Formulation of Combinational Nanoformulation Containing Selected Agent Curcumin and DOX for Reversal of Resistance in K562 Cells.
Dash, TK; Konkimalla, VB, 2017
)
0.46
" There was no apparent association between insulin dosing and severity of hypoglycaemia or hypokalaemia, or in glucose or potassium replacement."( The safety of high-dose insulin euglycaemia therapy in toxin-induced cardiac toxicity.
Isbister, GK; Page, CB; Ryan, NM, 2018
)
0.48
" Modification of recommended dosage may be required in this combination of circumstances to reduce risk to patients."( Impaired Rivaroxaban Clearance in Mild Renal Insufficiency With Verapamil Coadministration: Potential Implications for Bleeding Risk and Dose Selection.
Chow, CR; Greenblatt, DJ; Harmatz, JS; Nicholson, WT; Patel, M; Rubino, CM, 2018
)
0.72
"Current dosing recommendations for rivaroxaban advocate dosage reduction in patients with moderate to severe renal impairment and avoidance of concomitant strong inhibitors of CYP3A or P-glycoprotein."( Minimal Physiologically Based Pharmacokinetic and Drug-Drug-Disease Interaction Model of Rivaroxaban and Verapamil in Healthy and Renally Impaired Subjects.
Chow, CR; Ismail, M; Lee, VH; Rubino, CM, 2018
)
0.69
"The low permeability of anti-malarial drugs must be borne in mind during development of effective dosage regimens of new drugs."( Absorptive and Secretory Transport of Selected Artemisinin Derivatives Across Caco-2 Cell Monolayers.
Gouws, C; Hamman, J; Haynes, RK; Heyns, J; Willers, C; Wong, HN, 2018
)
0.48
" Because the combined effects of drug-drug interactions and RI have not been evaluated by means of clinical studies, the decision of DABE dosing for RI patients receiving P-glycoprotein inhibitors is empirical at its best."( Assessing Potential Drug-Drug Interactions Between Dabigatran Etexilate and a P-Glycoprotein Inhibitor in Renal Impairment Populations Using Physiologically Based Pharmacokinetic Modeling.
Doki, K; Homma, M; Neuhoff, S; Rostami-Hodjegan, A, 2019
)
0.51
" QTc prolongation was observed in the marmosets dosed with sotalol, astemizole, flecainide, quinidine, verapamil and terfenadine."( Telemetered common marmosets is useful for the assessment of electrocardiogram parameters changes induced by multiple cardiac ion channel inhibitors.
Hinoi, E; Miyawaki, I; Tsubouchi, T; Watanabe, K; Yamada, T, 2019
)
0.73
" Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a dabigatran plasma concentration ratio (perpetrator versus placebo)."( Renal Excretion of Dabigatran: The Potential Role of Multidrug and Toxin Extrusion (MATE) Proteins.
Marathe, P; Rodrigues, AD; Shen, H; Sinz, M; Yao, M; Zhu, M, 2019
)
0.51
" The efficacy of MMF as an immunosuppressant and long-term safety in cats of this dosage regimen is unknown."(
Abrams, G; Adolfsson, E; Agarwal, PK; Akkan, AG; Al Alhareth, NS; Alves, VGL; Armentano, R; Bahroos, E; Baig, M; Baldridge, KK; Barman, S; Bartolucci, C; Basit, A; Bertoli, SV; Bian, L; Bigatti, G; Bobenko, AI; Boix, PP; Bokulic, T; Bolink, HJ; Borowiec, J; Bulski, W; Burciaga, J; Butt, NS; Cai, AL; Campos, AM; Cao, G; Cao, Y; Čapo, I; Caruso, ML; Chao, CT; Cheatum, CM; Chelminski, K; Chen, AJW; Chen, C; Chen, CH; Chen, D; Chen, G; Chen, H; Chen, LH; Chen, R; Chen, RX; Chen, X; Cherdtrakulkiat, R; Chirvony, VS; Cho, JG; Chu, K; Ciurlino, D; Coletta, S; Contaldo, G; Crispi, F; Cui, JF; D'Esposito, M; de Biase, S; Demir, B; Deng, W; Deng, Z; Di Pinto, F; Domenech-Ximenos, B; Dong, G; Drácz, L; Du, XJ; Duan, LJ; Duan, Y; Ekendahl, D; Fan, W; Fang, L; Feng, C; Followill, DS; Foreman, SC; Fortunato, G; Frew, R; Fu, M; Gaál, V; Ganzevoort, W; Gao, DM; Gao, X; Gao, ZW; Garcia-Alvarez, A; Garza, MS; Gauthier, L; Gazzaz, ZJ; Ge, RS; Geng, Y; Genovesi, S; Geoffroy, V; Georg, D; Gigli, GL; Gong, J; Gong, Q; Groeneveld, J; Guerra, V; Guo, Q; Guo, X; Güttinger, R; Guyo, U; Haldar, J; Han, DS; Han, S; Hao, W; Hayman, A; He, D; Heidari, A; Heller, S; Ho, CT; Ho, SL; Hong, SN; Hou, YJ; Hu, D; Hu, X; Hu, ZY; Huang, JW; Huang, KC; Huang, Q; Huang, T; Hwang, JK; Izewska, J; Jablonski, CL; Jameel, T; Jeong, HK; Ji, J; Jia, Z; Jiang, W; Jiang, Y; Kalumpha, M; Kang, JH; Kazantsev, P; Kazemier, BM; Kebede, B; Khan, SA; Kiss, J; Kohen, A; Kolbenheyer, E; Konai, MM; Koniarova, I; Kornblith, E; Krawetz, RJ; Kreouzis, T; Kry, SF; Laepple, T; Lalošević, D; Lan, Y; Lawung, R; Lechner, W; Lee, KH; Lee, YH; Leonard, C; Li, C; Li, CF; Li, CM; Li, F; Li, J; Li, L; Li, S; Li, X; Li, Y; Li, YB; Li, Z; Liang, C; Lin, J; Lin, XH; Ling, M; Link, TM; Liu, HH; Liu, J; Liu, M; Liu, W; Liu, YP; Lou, H; Lu, G; Lu, M; Lun, SM; Ma, Z; Mackensen, A; Majumdar, S; Martineau, C; Martínez-Pastor, JP; McQuaid, JR; Mehrabian, H; Meng, Y; Miao, T; Miljković, D; Mo, J; Mohamed, HSH; Mohtadi, M; Mol, BWJ; Moosavi, L; Mosdósi, B; Nabu, S; Nava, E; Ni, L; Novakovic-Agopian, T; Nyamunda, BC; Nyul, Z; Önal, B; Özen, D; Özyazgan, S; Pajkrt, E; Palazon, F; Park, HW; Patai, Á; Patai, ÁV; Patzke, GR; Payette, G; Pedoia, V; Peelen, MJCS; Pellitteri, G; Peng, J; Perea, RJ; Pérez-Del-Rey, D; Popović, DJ; Popović, JK; Popović, KJ; Posecion, L; Povall, J; Prachayasittikul, S; Prachayasittikul, V; Prat-González, S; Qi, B; Qu, B; Rakshit, S; Ravelli, ACJ; Ren, ZG; Rivera, SM; Salo, P; Samaddar, S; Samper, JLA; Samy El Gendy, NM; Schmitt, N; Sekerbayev, KS; Sepúlveda-Martínez, Á; Sessolo, M; Severi, S; Sha, Y; Shen, FF; Shen, X; Shen, Y; Singh, P; Sinthupoom, N; Siri, S; Sitges, M; Slovak, JE; Solymosi, N; Song, H; Song, J; Song, M; Spingler, B; Stewart, I; Su, BL; Su, JF; Suming, L; Sun, JX; Tantimavanich, S; Tashkandi, JM; Taurbayev, TI; Tedgren, AC; Tenhunen, M; Thwaites, DI; Tibrewala, R; Tomsejm, M; Triana, CA; Vakira, FM; Valdez, M; Valente, M; Valentini, AM; Van de Winckel, A; van der Lee, R; Varga, F; Varga, M; Villarino, NF; Villemur, R; Vinatha, SP; Vincenti, A; Voskamp, BJ; Wang, B; Wang, C; Wang, H; Wang, HT; Wang, J; Wang, M; Wang, N; Wang, NC; Wang, Q; Wang, S; Wang, X; Wang, Y; Wang, Z; Wen, N; Wesolowska, P; Willis, M; Wu, C; Wu, D; Wu, L; Wu, X; Wu, Z; Xia, JM; Xia, X; Xia, Y; Xiao, J; Xiao, Y; Xie, CL; Xie, LM; Xie, S; Xing, Z; Xu, C; Xu, J; Yan, D; Yan, K; Yang, S; Yang, X; Yang, XW; Ye, M; Yin, Z; Yoon, N; Yoon, Y; Yu, H; Yu, K; Yu, ZY; Zhang, B; Zhang, GY; Zhang, H; Zhang, J; Zhang, M; Zhang, Q; Zhang, S; Zhang, W; Zhang, X; Zhang, Y; Zhang, YW; Zhang, Z; Zhao, D; Zhao, F; Zhao, P; Zhao, W; Zhao, Z; Zheng, C; Zhi, D; Zhou, C; Zhou, FY; Zhu, D; Zhu, J; Zhu, Q; Zinyama, NP; Zou, M; Zou, Z, 2019
)
0.51
" The daily dosage of verapamil varied from 25 to 50 mg of the drug diluted in 200-400 ml of isotonic sodium chloride solution."( [Intracisternal administration of verapamil for the prevention and treatment of vasospasm in patients after microsurgical treatment of cerebral aneurysms in the acute period of hemorrhage].
Baranich, AI; Belousova, OB; Eliava, SS; Gorozhanin, VA; Kheyreddin, AS; Konovalov, AN; Kurdyumova, NV; Mikeladze, KG; Okishev, DN; Pilipenko, YV; Savin, IA; Shekhtman, OD; Spiru, AM; Tabasaransky, TF; Varyukhina, MD; Vinogradov, EV, 2019
)
1.11
" This review focuses on the various analytical methods reported between 1976 and 2019 for the determination of VER in different biological samples and pharmaceutical dosage forms along with their methodological limitations."( Analytical techniques for the determination of verapamil in biological samples and dosage forms: an overview.
Jouyban, A; Pourkarim, F; Rahimpour, E, 2019
)
0.77
" The current PBPK model, which considers changes in unbound potency-adjusted active species, can be used to inform dosing recommendations when abemaciclib is coadministered with CYP3A4 perpetrators."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" Quantitative thresholds and analysis based on DSA perfusion may assist with real-time dosage estimation and help predict response to treatment, however future prospective analysis is required for validation."( Computational methods for visualizing and measuring verapamil efficacy for cerebral vasospasm.
Abumoussa, A; Flores, A; Ho, J; Lee, YZ; Niethammer, M; Sasaki-Adams, D, 2020
)
0.81
" A medication episode was defined as a timeframe in which the highest dosage at a fixed level of a single drug was used in a patient."( The Efficacy of Anti-Arrhythmic Drugs in Children With Idiopathic Frequent Symptomatic or Asymptomatic Premature Ventricular Complexes With or Without Asymptomatic Ventricular Tachycardia: a Retrospective Multi-Center Study.
Bertels, RA; Blom, NA; Filippini, LH; Kammeraad, JAE; Knobbe, I; Kuipers, IM; Zeelenberg, AM, 2021
)
0.62
" Also, the effect of multiple dosing of parabens on p-gp expression was examined."( Evaluation of the Effect of Isobutyl Paraben and 2-ethyl Hexyl Paraben on P-glycoprotein Functional Expression in Rats: A Pharmacokinetic Study.
Alshogran, OY; Ghraiybah, NFA; I Al-Azzam, S, 2022
)
0.72
" Our simulation results revealed that recommended reduced dosing regimen of dabigatran etexilate during comedication with verapamil and clarithromycin (110 and 75 mg BID for Chinese young and old older adults) will result in exposure (trough concentration) that was either slightly higher or similar to the trough concentration of patients with any bleeding events."( Physiologically-based pharmacokinetic modeling to predict drug-drug interactions of dabigatran etexilate and rivaroxaban in the Chinese older adults.
Cui, C; Lai, X; Li, H; Liu, D; Sia, JEV; Wu, X; Zhang, F, 2023
)
1.12
" However, 4-hourly dosing is a practical limitation and verapamil has been proposed as an alternative."( Verapamil in the treatment of reversible cerebral vasoconstriction syndrome: A systematic review.
Bacchi, S; Bagster, M; Collins, L; Goh, R; Gupta, A; Kleinig, O; Kleinig, T; Kovoor, J; Lam, L; Proudman, W; Schultz, D; Zhang, R, 2023
)
2.6
" The most common oral verapamil dosing regimen was controlled release 120 mg once daily."( Verapamil in the treatment of reversible cerebral vasoconstriction syndrome: A systematic review.
Bacchi, S; Bagster, M; Collins, L; Goh, R; Gupta, A; Kleinig, O; Kleinig, T; Kovoor, J; Lam, L; Proudman, W; Schultz, D; Zhang, R, 2023
)
2.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
polyetherAny ether that contains more than one ether linkage.
nitrileA compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Verapamil Action Pathway478

Protein Targets (74)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency14.12540.01846.806014.1254AID624172
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.39810.100020.879379.4328AID588453
TDP1 proteinHomo sapiens (human)Potency26.51010.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency1.51120.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency26.41930.000221.22318,912.5098AID743035; AID743054; AID743063
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency26.60320.001022.650876.6163AID1224838
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346784
regulator of G-protein signaling 4Homo sapiens (human)Potency9.46620.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.66090.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00540.001310.157742.8575AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.83250.000214.376460.0339AID720691; AID720692
pregnane X nuclear receptorHomo sapiens (human)Potency4.21630.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency31.27180.000229.305416,493.5996AID743069; AID743079; AID743091
GVesicular stomatitis virusPotency37.90830.01238.964839.8107AID1645842
glucocerebrosidaseHomo sapiens (human)Potency28.18380.01268.156944.6684AID2101
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency21.31380.001019.414170.9645AID743094
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
thyroid stimulating hormone receptorHomo sapiens (human)Potency26.60320.001628.015177.1139AID1259385
activating transcription factor 6Homo sapiens (human)Potency0.30110.143427.612159.8106AID1159516
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency50.11870.036619.637650.1187AID2112
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.94330.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency28.22630.000323.4451159.6830AID743065; AID743067
huntingtin isoform 2Homo sapiens (human)Potency35.48130.000618.41981,122.0200AID1688
lamin isoform A-delta10Homo sapiens (human)Potency11.22020.891312.067628.1838AID1487
Interferon betaHomo sapiens (human)Potency37.90830.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency19.95260.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
Ataxin-2Homo sapiens (human)Potency17.78280.011912.222168.7989AID588378
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)6.80000.21005.553710.0000AID386625
Solute carrier family 22 member 1 Homo sapiens (human)Ki2.90000.55004.26507.4600AID681146
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC50 (µMol)41.50000.02201.64228.9000AID1207176
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)0.20000.00032.63119.0000AID1207779
Bile salt export pumpRattus norvegicus (Norway rat)Ki92.50000.30003.10006.1000AID1449629
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.29700.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.15500.00000.887110.0000AID625218
Bile salt export pumpHomo sapiens (human)IC50 (µMol)131.50000.11007.190310.0000AID1443980; AID1473738; AID681139; AID681155
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)2.00000.06404.012610.0000AID150754; AID681128
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)18.71170.00022.318510.0000AID1167512; AID1167513; AID1228905; AID1320724; AID1486951; AID1486971; AID1486973; AID150617; AID150618; AID150752; AID150755; AID1517888; AID1517889; AID1517892; AID1517893; AID1530092; AID1530705; AID1530709; AID1530761; AID154132; AID154133; AID1564095; AID1566020; AID1566022; AID1566024; AID1604133; AID1625252; AID1647652; AID1649243; AID1683978; AID1683991; AID1683996; AID1684000; AID1739808; AID1739810; AID1739812; AID1739814; AID1739816; AID1739818; AID1739820; AID1739822; AID1739824; AID1739826; AID1739828; AID1739830; AID1750901; AID1758181; AID1761208; AID1761209; AID1761210; AID1761211; AID1761212; AID1761213; AID1761214; AID1761215; AID1785069; AID1785075; AID1802151; AID1813139; AID1822202; AID1878311; AID1878312; AID1904130; AID310120; AID310122; AID326367; AID326368; AID326369; AID350540; AID364884; AID365465; AID395103; AID578762; AID643321; AID672543; AID678952; AID679465; AID680136; AID681122; AID681126; AID681127; AID681131; AID681144; AID681162; AID681358; AID681579; AID681580; AID681581; AID681582; AID681618; AID682152; AID701948; AID722220
ATP-dependent translocase ABCB1Homo sapiens (human)Ki3.61140.02002.35948.5900AID150616; AID150735; AID681356; AID681383; AID681611; AID714427; AID714428
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)16.62380.00011.753610.0000AID1350754; AID1649390; AID1683957; AID1785086; AID1833385; AID428564; AID54923
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.57900.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.21700.00010.807410.0000AID625201
Cytochrome P450 2C8Homo sapiens (human)Ki17.50000.00180.38733.3000AID589253
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)22.00000.00002.800510.0000AID1210069
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)3.02000.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.72600.00010.739610.0000AID625190
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)64.33330.20004.713010.0000AID150753; AID1802796; AID681119
Catechol O-methyltransferaseHomo sapiens (human)IC50 (µMol)0.20000.00101.31466.3096AID1207779
Potassium voltage-gated channel subfamily A member 3Homo sapiens (human)IC50 (µMol)8.00000.00203.19698.0000AID717088
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)2.59000.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki2.54700.00062.197310.0000AID625270
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.44200.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.12600.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.29700.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.15500.00010.954910.0000AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)3.02000.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki1.72600.00031.29679.2440AID625190
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.24000.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.12700.00000.70488.1930AID625222
Delta-type opioid receptorMus musculus (house mouse)Ki1.75000.00000.53939.4000AID714427
Multidrug resistance-associated protein 1 Homo sapiens (human)IC50 (µMol)5.59800.00153.71109.6600AID1186756; AID1530762; AID1802151; AID365463; AID643322
Multidrug resistance-associated protein 1 Homo sapiens (human)Ki13.30000.07002.20208.1000AID427738; AID427739
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki1.75000.00000.38458.6000AID714427
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.18600.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.06300.00000.602010.0000AID625254
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki1.75000.00000.20186.4240AID714427
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.16500.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.10500.00030.769310.0000AID625217
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)6.80002.03005.53139.9000AID386625
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)22.00000.01202.53129.4700AID1210069
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)200.00000.00010.54948.4000AID1411805
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)0.20000.00032.59559.0000AID1207779
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.39450.00091.901410.0000AID1054122; AID1207235; AID161281; AID161283; AID1633048; AID1649390; AID1779702; AID240820; AID243151; AID243188; AID408340; AID420668; AID576612; AID82355
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)0.20000.00032.63119.0000AID1207779
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)24.14170.00032.25459.6000AID1207717; AID1207723; AID1207724; AID1207725; AID1207779; AID45602
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)41.50000.00033.64849.2000AID1207176
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)112.66672.41006.343310.0000AID1473739; AID1733379; AID365464
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)192.00010.00401.966610.0000AID1733381; AID364887; AID678801
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50 (µMol)232.00000.05002.37979.7000AID1218863; AID1218864; AID1218865
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki52.00000.04401.36305.0000AID1218867
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminHomo sapiens (human)Kd645.65400.08933.31358.0000AID327170
Muscarinic acetylcholine receptor M2Sus scrofa (pig)EC50 (µMol)30.97420.01351.86256.3096AID142787
ATP-dependent translocase ABCB1Homo sapiens (human)EC50 (µMol)6.41090.01600.67863.1000AID1062339; AID1129602; AID1228907; AID1228908; AID1228909; AID1228910; AID1239235; AID1565849; AID1595499; AID210307; AID271725; AID295523; AID317949; AID321879; AID407205; AID679129; AID755320
Multidrug resistance-associated protein 1 Homo sapiens (human)EC50 (µMol)10.83121.70004.30289.8000AID1168903; AID1414427; AID1565850; AID1595500
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)EC50 (µMol)19.10000.00540.42203.2000AID1168904; AID1565853
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Homo sapiens (human)Activity1.60000.02001.67004.5000AID282999; AID310897
ATP-dependent translocase ABCB1Homo sapiens (human)ED503.00000.05001.52503.0000AID399366
ATP-dependent translocase ABCB1Homo sapiens (human)I0.51.60001.60001.60001.6000AID1565851
ATP-dependent translocase ABCB1Homo sapiens (human)INH1.60001.60001.60001.6000AID464018
ATP-dependent translocase ABCB1Homo sapiens (human)Km13.34330.01403.717210.0000AID239740; AID350526; AID681163; AID681164; AID682516; AID713773
ATP-dependent translocase ABCB1Homo sapiens (human)MIC8.00008.00008.00008.0000AID714426
ATP-dependent translocase ABCB1Mus musculus (house mouse)Km10.000010.000010.000010.0000AID350523
Multidrug resistance-associated protein 1 Homo sapiens (human)Activity2.60002.60002.60002.6000AID427722
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (461)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
behavioral fear responseCatechol O-methyltransferaseHomo sapiens (human)
response to hypoxiaCatechol O-methyltransferaseHomo sapiens (human)
synaptic transmission, dopaminergicCatechol O-methyltransferaseHomo sapiens (human)
startle responseCatechol O-methyltransferaseHomo sapiens (human)
response to amphetamineCatechol O-methyltransferaseHomo sapiens (human)
renin secretion into blood streamCatechol O-methyltransferaseHomo sapiens (human)
glycogen metabolic processCatechol O-methyltransferaseHomo sapiens (human)
prostaglandin metabolic processCatechol O-methyltransferaseHomo sapiens (human)
response to oxidative stressCatechol O-methyltransferaseHomo sapiens (human)
memoryCatechol O-methyltransferaseHomo sapiens (human)
visual learningCatechol O-methyltransferaseHomo sapiens (human)
response to xenobiotic stimulusCatechol O-methyltransferaseHomo sapiens (human)
response to woundingCatechol O-methyltransferaseHomo sapiens (human)
response to toxic substanceCatechol O-methyltransferaseHomo sapiens (human)
response to inorganic substanceCatechol O-methyltransferaseHomo sapiens (human)
gene expressionCatechol O-methyltransferaseHomo sapiens (human)
dopamine secretionCatechol O-methyltransferaseHomo sapiens (human)
cellular response to phosphate starvationCatechol O-methyltransferaseHomo sapiens (human)
cerebellar cortex morphogenesisCatechol O-methyltransferaseHomo sapiens (human)
response to foodCatechol O-methyltransferaseHomo sapiens (human)
methylationCatechol O-methyltransferaseHomo sapiens (human)
glomerulus developmentCatechol O-methyltransferaseHomo sapiens (human)
cholesterol effluxCatechol O-methyltransferaseHomo sapiens (human)
response to cytokineCatechol O-methyltransferaseHomo sapiens (human)
multicellular organism growthCatechol O-methyltransferaseHomo sapiens (human)
exploration behaviorCatechol O-methyltransferaseHomo sapiens (human)
renal sodium excretionCatechol O-methyltransferaseHomo sapiens (human)
norepinephrine metabolic processCatechol O-methyltransferaseHomo sapiens (human)
dopamine catabolic processCatechol O-methyltransferaseHomo sapiens (human)
catecholamine catabolic processCatechol O-methyltransferaseHomo sapiens (human)
habituationCatechol O-methyltransferaseHomo sapiens (human)
norepinephrine secretionCatechol O-methyltransferaseHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painCatechol O-methyltransferaseHomo sapiens (human)
response to corticosteroneCatechol O-methyltransferaseHomo sapiens (human)
artery developmentCatechol O-methyltransferaseHomo sapiens (human)
cellular response to cocaineCatechol O-methyltransferaseHomo sapiens (human)
masticationCatechol O-methyltransferaseHomo sapiens (human)
renal albumin absorptionCatechol O-methyltransferaseHomo sapiens (human)
renal filtrationCatechol O-methyltransferaseHomo sapiens (human)
response to saltCatechol O-methyltransferaseHomo sapiens (human)
response to dopamineCatechol O-methyltransferaseHomo sapiens (human)
response to angiotensinCatechol O-methyltransferaseHomo sapiens (human)
dopamine metabolic processCatechol O-methyltransferaseHomo sapiens (human)
developmental processCatechol O-methyltransferaseHomo sapiens (human)
potassium ion transportPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
optic nerve developmentPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
corpus callosum developmentPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
protein homooligomerizationPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
leukotriene metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
response to xenobiotic stimulusMultidrug resistance-associated protein 1 Homo sapiens (human)
cobalamin transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid biosynthetic processMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to oxidative stressMultidrug resistance-associated protein 1 Homo sapiens (human)
heme catabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transportMultidrug resistance-associated protein 1 Homo sapiens (human)
phospholipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
positive regulation of inflammatory responseMultidrug resistance-associated protein 1 Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cell chemotaxisMultidrug resistance-associated protein 1 Homo sapiens (human)
transepithelial transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cyclic nucleotide transportMultidrug resistance-associated protein 1 Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 1 Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to amyloid-betaMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (181)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C8Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
magnesium ion bindingCatechol O-methyltransferaseHomo sapiens (human)
protein bindingCatechol O-methyltransferaseHomo sapiens (human)
methyltransferase activityCatechol O-methyltransferaseHomo sapiens (human)
O-methyltransferase activityCatechol O-methyltransferaseHomo sapiens (human)
catechol O-methyltransferase activityCatechol O-methyltransferaseHomo sapiens (human)
voltage-gated monoatomic ion channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
outward rectifier potassium channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
ATP bindingMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type vitamin B12 transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (87)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
cytosolCatechol O-methyltransferaseHomo sapiens (human)
plasma membraneCatechol O-methyltransferaseHomo sapiens (human)
membraneCatechol O-methyltransferaseHomo sapiens (human)
intracellular membrane-bounded organelleCatechol O-methyltransferaseHomo sapiens (human)
synapseCatechol O-methyltransferaseHomo sapiens (human)
extracellular exosomeCatechol O-methyltransferaseHomo sapiens (human)
dendriteCatechol O-methyltransferaseHomo sapiens (human)
membraneCatechol O-methyltransferaseHomo sapiens (human)
axonCatechol O-methyltransferaseHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
presynaptic membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
calyx of HeldPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
postsynaptic membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
glutamatergic synapsePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
axonPotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
membranePotassium voltage-gated channel subfamily A member 3Homo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basal plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
lateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
extracellular exosomeMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2796)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1378879Effective permeability of the compound at 100 mg/ml after 16 hrs by UV based PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID1180228Inhibition of L-type calcium channel in Wistar rat aorta rings assessed as reduction in L-type Ba(2+) current at Vh of -50 mV2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1576576Effective permeability of compound by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID379509Reversal of P-glycoprotein-mediated multidrug resistance assessed as ratio of IC50 for human KB-V1 cells to IC50 for human KB-V1 cells in presence of 100 nM vinblastine1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1673441Effect on P-gp expression in human K562/A02 cells overexpressing P-gp at 5 uM after 72 hrs by Western blot analysis2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1502892Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID351903Chemosensitizing activity as 500nM potentiation of chloroquine effect after 72 hrs against chloroquine-resistant transporter 106/1'76T mutant Plasmodium falciparum infected in human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1239240Increase in rhodamine 123 accumulation in human MDA435/LCC6 cells at 2 uM after 2.5 hrs by spectrofluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID1764875Permeability of the compound at 50 uM measured after 4 hrs by PAMPA assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.
AID1486983Inhibition of ABCB1 in human K562/A02 cells assessed as increase in doxorubicin accumulation after 90 mins by rhodamine123 staining based flow cytometric analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1761200Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring cell survival rate at 10 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID1633048Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method
AID230566Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vincristine (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID406534Inhibition of NorA efflux pump in Staphylococcus aureus 1199 assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Citral derived amides as potent bacterial NorA efflux pump inhibitors.
AID726493Inhibition of human MDR1 expressed in mouse L5178Y cells assessed as reduction of rhodamine-123 uptake by measuring fluorescence activity ratio at 1 uM preincubated for 10 mins measured after 40 mins relative to control2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Development of small-molecule P-gp inhibitors of the N-benzyl 1,4-dihydropyridine type: novel aspects in SAR and bioanalytical evaluation of multidrug resistance (MDR) reversal properties.
AID1807362Metabolic stability in mouse liver microsomes assessed as intrinsic clearance in presence of NADPH regenerating system by UPLC-MS analysis
AID167265Electrophysiological effect in isolated rabbit hearts in atrio-His bundle (A-H) interval1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID331503Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected mouse L5178Y cells assessed as fluorescence activity ratio at 4 ug/ml by flow cytometry2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.
AID1900354Stability in pooled human liver microsomes assessed as intrinsic clearance at 8 uM in presence of NADPH measured upto 60 mins by HPLC-MS analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Multitarget Hybrid Fasudil Derivatives as a New Approach to the Potential Treatment of Amyotrophic Lateral Sclerosis.
AID1215169AUC (0 to 90 mins) in Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1776729Inhibition of Multidrug resistance efflux pump in Mycobacterium tuberculosis FURG-2 assessed as relative final fluorescence at 128 ug/ml measured by ethidium bromide accumulation assay2021Bioorganic & medicinal chemistry letters, 06-15, Volume: 422,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis.
AID1322367Metabolic stability in human liver microsomes assessed as compound remaining after 30 mins2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents.
AID1215181Drug metabolism in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestinal microsomes assessed as CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1207204Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1739842Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold change in doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to doxorubicin IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID514303Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as loss of rhodopsin expression at 10 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1429868Permeability of the compound at pH 2 at 50 mM after 4 hrs by PAMPA-GI assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID1288623Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as reduction in adriamycin IC50 at 5 uM after 48 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID472413Inhibition of P-gp-mediated multidrug-resistance in human KB-C2 cells assessed as increase in colchicine-induced cytotoxicity at 1 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
AID143479Inhibitory activity when combined with 5-fluorouracil (uM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID94172Increase in adriamycin uptake in modulator-treated cells relative to untreated KB-A1 cells at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1703749Half life in human liver microsomes at 0.1 uM in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1228904Cytotoxicity against mouse L929 cells after 3 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID680054TP_TRANSPORTER: inhibition of Daunorubicin intracellular accumulation (DMN: 0.05 uM, Verapamil: 100 uM) in MDA435/LCC6 MDR1 cells2003The Journal of pharmacology and experimental therapeutics, Mar, Volume: 304, Issue:3
Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport.
AID1215134Decrease of CYP3A2 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestine by Western blot analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID288565Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-C2 cells at 5 uM after 68 hrs by MTT assay2007Journal of natural products, Jun, Volume: 70, Issue:6
Reversal of P-glycoprotein-mediated multidrug resistance by sipholane triterpenoids.
AID1502866Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1652316Half life in human hepatocytes2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
AID656837Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 24 hrs post washout measured after 72 hrs by MTS assay (Rvb = 52012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID1502792Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to er2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1770544Metabolic stability of the compound in human liver microsomes assessed as half life at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1514559Cytotoxicity against human KBV cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID681441TP_TRANSPORTER: inhibition of TEA uptake by Verapamil at 5mM in Octn1-HRPE cells2000Biochimica et biophysica acta, Jun-01, Volume: 1466, Issue:1-2
Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.
AID1761208Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID1322434Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine influx by measuring mean fluorescence intensity at 10 uM incubated for 20 mins by flow cytometry (Rvb = 1.8 No_unit)2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
AID587815Metabolic stability of the compound in human liver microsome assessed as compound remaining2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Potent farnesyltransferase inhibitors with 1,4-diazepane scaffolds as novel destabilizing microtubule agents in hormone-resistant prostate cancer.
AID1623663Half life in mouse microsomes2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1215347Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by LC-MS/MS analysis in 2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID1273467Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 32 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1352540Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1235737Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 2 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1813151Reversal of P-glycoprotein-mediated paclitaxel resistance in human LCC6/MDR cells assessed as relative fold by measuring paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1548950Unbound hepatic clearance in rat liver microsomes2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of
AID1446267Metabolic stability of human liver microsomes assessed as amount of parent compound remaining at 25 to 100 uM after 1 hr in the presence of NADPH by LC-MS method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Design, Synthesis, and Evaluation of Novel Prodrugs of Transition State Inhibitors of Norovirus 3CL Protease.
AID1351583Tracheorelaxant activity in Wistar rat trachea tonus assessed as reduction in 30 mM KCl-induced contraction at 100 uM after 15 mins relative to control2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID1286275Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay2016Journal of natural products, Jan-22, Volume: 79, Issue:1
Aspidofractinine and Eburnane Alkaloids from a North Borneo Kopsia. Ring-Contracted, Additional Ring-Fused, and Paucidactine-Type Aspidofractinine Alkaloids from K. pauciflora.
AID639368Permeability of the compound by PAMPA assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1595503Ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells incubated for 120 mins by UV spectroscopy2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID1235780Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in isoniazid MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1371163Half life in human liver microsomes in absence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA).
AID324577Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID430563Reversal of ABCB1-mediated multidrug resistance in human KB-3-1 cells assessed as ratio of colchicine IC50 in absence of drug to colchicine IC50 in presence of drug at 10 uM after 68 hrs by MTT assay2009Journal of natural products, Jul, Volume: 72, Issue:7
Sipholane triterpenoids: chemistry, reversal of ABCB1/P-glycoprotein-mediated multidrug resistance, and pharmacophore modeling.
AID1062344Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM after 5 days by MTS assay relative to untreated control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID653458Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 5 uM after 72 hrs by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1604717Stability in human plasma assessed as parent compound remaining level at 5 uM at 37 degC measured at 240 mins by LC-MS analysis2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1649259Potentiation of DOX-induced anti tumor activity against human K562/A02 cells xenografted in BALB/c mouse assessed as tumor size at 3 mg/kg, iv administered every 2 days for 14 days measured during compound dosing by caliper method (Rvb = 610 mm3)2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
AID1460712Cytotoxicity against human MCF7/DX cells incubated for 48 hrs by MTT assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
Isolation, Structure Elucidation, and Absolute Configuration of Syncarpic Acid-Conjugated Terpenoids from Rhodomyrtus tomentosa.
AID389747Inhibition of NorA efflux pump in Staphylococcus aureus 1199B assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1215164Clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1182022Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1246309Half life in human microsomes2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1357218Intrinsic clearance in rat liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID1769164Inhibition of CYP2C19 in human liver microsomes assessed as remaining activity at 1 to 10 uM using (S)-mephenytoin as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID679920TP_TRANSPORTER: inhibition of Saquinavir transepithelial transport (basal to apical)(Saquinavir: 10 uM, Verapamil: 5 uM) in HCT-8 cells1998The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3
Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein.
AID1733395Induction of cell cycle arrest in human KBV cells assessed as accumulation at S phase at 10 uM after 24 hrs by PI/RNaseA staining based flow cytometric analysis (Rvb = 11.32 +/- 0.04%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1129446Half life in mouse microsomes at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1174620Potentiation of adriamycin-induced cytotoxicity against human K562/ADR cells at 10 uM after 48 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities.
AID475688Metabolic stability in human liver microsomes assessed as compound remaining at 5 umol/L after 15 mins by LC/MS/MS analysis2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
AID1429865Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1502712Antimycobacterial activity against Mycobacterium avium isolate MAV3 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1275774Cytotoxicity against CHO cells by MTT assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID406196Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of puromycin2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID1215129Total intrinsic clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID230565Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vincristine (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1235720Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 4 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1352548Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of vincristine-induced cytotoxicity at 10 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID755314Inhibition of p-gp in human KB/VCR cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID326369Inhibition of Pgp by daunorubicin accumulation assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.
AID1459758Potentiation of doxorubicin-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1352544Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity after 48 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID351893Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1524536Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as fold reduction in adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay
AID1459773Inhibition of P-gp in human KBVIN cells assessed as potentiation of paclitaxel-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID681618TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells2003Anti-cancer drugs, Feb, Volume: 14, Issue:2
Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.
AID762398Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as EtBr accumulation measured every 3 mins interval for 45 mins by spectrofluorometric method2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1336845Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of actinomycin D-induced cytotoxicity by measuring fold reduction in actinomycin D EC50 at 5 uM after 72 hrs by MTT assay relative to untreated control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1530709Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM)2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID697544Activation of human recombinant P-glycoprotein using unmetabolized ATP by luminescence based p-gp-glo assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents.
AID1673429Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as fold reduction in doxorubicin IC50 at 5 uM preincubated for 24 hrs followed by compound washout and later incubated with doxorubicin and measured after 2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID345309Intrinsic cytotoxicity against wild type mouse NIH/3T3 cells at 10 uM after 72 hrs by MTT assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID247665Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
AID589253Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant system2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1155075Inhibition of CTR in Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1429863Effective permeability of the compound at pH 5.5 at 200 uM after 4 hrs by PAMPA-GI assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID1502752Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1358241Inhibition of P-gp in human MCF7/ADR cells assessed as assessed as potentiation of doxorubicin-induced antiproliferative activity by measuring doxorubicin antiproliferative activity at 20 uM after 2 days by MTT assay (Rvb = 5.3 +/- 1.1%)2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID679788TP_TRANSPORTER: serosal to mucosal transport in SD rat intestinal segment1995Pharmaceutical research, Sep, Volume: 12, Issue:9
Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine.
AID678746TP_TRANSPORTER: inhibition of Cyclosporin A efflux (CsA: 0.005 uM, Verapamil: 10 uM) in P388/S and P388/ADR cells2000Clinical and experimental pharmacology & physiology, Aug, Volume: 27, Issue:8
Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1502901Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 50 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1273403Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 4 ug/ml after 7 days by microdilution checkerboard2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1330773Effective permeability of the compound by PAMPA2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID1530097Cell cycle arrest in human KBV cells assessed as accumulation at S phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10.03 +/- 0.75%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID509769Inhibition of P-gp expression in human KB cells at 4 to 16 uM after 48 hrs by Western blotting2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity.
AID330505Apparent permeability from apical to basolateral side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
AID1565856Inhibition of of MDR1 (unknown origin) expressed in MDCK-MDR1 cells assessed as decrease in ATP consumption at 1 uM incubated for 2 hrs by ATPlite luminescence assay relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID1215177Total intrinsic clearance in Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil per gram of intestinal mucosa by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1459770Inhibition of P-gp in human KBVIN cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1429934Substrate activity at P-gp in human LoVo/DX cells assessed as ATP consumption at 10 uM after 2 hrs by ATPlite assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity.
AID1273474Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 4 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1496418Intrinsic clearance in human liver microsomes at 3 uM2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
AID1833359Reversal of resistance to paclitaxel-induced cytotoxicity in human KB-C2 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1886.37 +/- 243.05 nM)
AID324585Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1683967Inhibition of [3H]PTX efflux in human SW620 cells at 4 uM pre-incubated for 4 hrs followed by PTX addition and measured after 2 hrs by liquid scintillation counting analysis
AID102856Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, fluorescence activity ratio at 5 ug/mL.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery and biological evaluation of a new family of potent modulators of multidrug resistance: reversal of multidrug resistance of mouse lymphoma cells by new natural jatrophane diterpenoids isolated from Euphorbia species.
AID1750944Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as early apoptotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 22.3%)
AID429849Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as reversal fold after 48 hrs by SRB assay relative to control2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures.
AID681385TP_TRANSPORTER: RT-PCR in HK-2 cell2002Toxicology and applied pharmacology, Sep-01, Volume: 183, Issue:2
Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line.
AID1386183Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation by measuring increase in fluorescence intensity after 24 hrs by fluorescence microscopic analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID1352552Stimulation of human Pgp ATPase activity expressed in cell membranes at 50 uM after 1 hr by P-gp Glo assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1414430Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
AID1502793Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1603237Permeability of the compound assessed as ratio of Kin to Kout by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1584806Permeability of the compound at pH 7.4 by PAMPA2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents.
AID1740406Half life in human microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID154123In vitro relative vinblastin uptake into P388/s (murine leukemia) cells following 10 uM treatment.1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID1225500Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of vinblastine cytotoxic IC50 in absence of compound to vinblastine cytotoxic IC50 in presence of compound at 3 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1168903Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
AID681118TP_TRANSPORTER: transepithelial transport in Caco-2 cells2003International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2
Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.
AID1739812Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 80 +/- 10 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1740449Half life in human hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID1879914Permeability of compound incubated for 3 hrs by UV plate reader based PAMPA assay2022European journal of medicinal chemistry, May-05, Volume: 235Design, synthesis and biological evaluations of niclosamide analogues against SARS-CoV-2.
AID1517887Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as fold reduction in doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1217729Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1502808Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 64 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID717463Potentiation of doxorubicin-mediated cytotoxicity against human KBVIN cells assessed as reduction in doxorubicin IC50 at 10 uM after 72 hrs by SRB method relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity.
AID1733372Reversal of Pgp-mediated paclitaxel resistance in human KBV cells assessed as cell viability at 10 uM in presence of paclitaxel incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1235793Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in amikacin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID185649Compound was tested for the % inhibition rate of infarct size (myoglobin depleted area) on iv administration 15 min prior to the ligation at a dose of 0.1 mg/kg.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.
AID1684000Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72
AID680389TP_TRANSPORTER: inhibition of TEA uptake (TEA: 60 uM, Verapamil: 1000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID1235799Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in ethidium bromide MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1739803Inhibition of human full-length ABCB1 expressed in Flp-In-293 cells assessed as reduction in calcein-AM uptake at 2.5 uM preincubated for 30 mins followed by calcein-AM addition and measured after 30 mins by fluorescence spectrometric assay relative to co2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1903287Potentiation of paclitaxel-induced cytotoxicity against human KBV cells assessed as paclitaxel IC50 at 5 uM for 72 hrs by MTT assay (Rvb = 1199.11 +/- 51.46 nM )2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID75362Nagative chronotropic activity was expressed as percent changes in atrial rate on guinea pig spontaneously beating isolated right atrium at 10 e-5 M1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID159425Tested for beta-2 adrenoceptor blocking activity in anesthetized pigs (n=2) challenged with intravenous injections of isoproterenol.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1566030Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as fold reduction in irinotecan IC50 at 10 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID399196Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 0.1 ug/mL after 2 hrs relative to control2004Journal of natural products, Jan, Volume: 67, Issue:1
Production of biologically active taxoids by a callus culture of Taxus cuspidata.
AID1211795Dissociation constant, pKa of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1418886Inhibition of ABCB1 (unknown origin) expressed in human HEK293T/ABCB1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold reduction in doxorubicin IC50 at 4 uM after 72 hrs by MTT assay relative to doxorubicin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1155074Response modification index, ratio of IC50 for Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles in presence of drug to IC50 for Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles in2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID53614Percent of cell viability remaining after incubating the cells with the modulator alone a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID681337TP_TRANSPORTER: Western blot, HK-2 cells2002Toxicology and applied pharmacology, Sep-01, Volume: 183, Issue:2
Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line.
AID360079Cytotoxicity against human MRP1 expressing hamster BHK21 cells at 10 to 20 uM by MTT assay2007The Journal of biological chemistry, Oct-26, Volume: 282, Issue:43
(R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1.
AID1502822Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1813140Inhibition of P-gp in human LCC6MDR cells assessed as fold increase in intracellular DOX accumulation at 2 uM incubated for 150 mins in presence of doxorubicin by fluorescence microscopy relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1215185AUC (0 to 480 mins) in Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1603225Permeability of the compound assessed as molar fraction in donor well at 0.5 mM measured after 16 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID568588Vasodilatory activity in Sprague-Dawley rat thoracic aorta smooth muscle assessed as inhibition of KCL-induced vasoconstriction2011Journal of natural products, Jan-28, Volume: 74, Issue:1
Macrophyllionium and macrophyllines A and B, oxindole alkaloids from Uncaria macrophylla.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1427528Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1062336Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as induction of doxorubicin accumulation at 1 uM after 150 mins by spectrofluorometric analysis relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID153401Inhibitory activity when combined with taxol (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID683265Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as fold decrease in doxorubicin IC50 for cytotoxic activity at 10 uM after 72 hrs by SRB assay relative to control2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID193258Antiarrhythmic activity against anesthetized rats after peroral administration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1350749Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of [3H]-paclitaxel up to 2 uM preincubated for 4 hrs followed by [3H]-paclitaxel addition measured after 2 hrs by liquid scintillation counting method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1338194Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in rhodamine-123 accumulation at 2 uM measured after 150 mins by fluorescence spectrophotometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID307742Cytotoxicity against human A2780 cells assessed as cell viability at 0.2 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID209801Inhibitory activity when combined with 5-Fluorouracil (uM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID681131TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1174969Resistance factor, ratio of adriamycin IC50 for human K562/A02 cells over-expressing Pgp to adriamycin IC50 for human K562/A02 cells over-expressing Pgp in presence of 5 uM compound incubated for 24 hrs followed by adriamycin treatment post compound washo2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1290697Drug metabolism in human liver microsomes assessed as cytochrome P450-mediated compound oxidation by measuring drug recovery after 1 hr by HPLC analysis2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.
AID53608In vitro activity in DC-3F/AD cell line Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 10 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1761209Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID230393Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with cisplatin (uM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID230558Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with taxol (nM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID27587Partition coefficient (logP)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID681164TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID1228903Cytotoxicity against human MDA435/LCC6MDR cells after 3 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID429848Reversal of p-gp-mediated multidrug-resistance in human MCF7/ADM cells after 48 hrs by SRB assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures.
AID153400Inhibitory activity when combined with doxorubicin (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID696928Cytotoxicity against MDR1 expressing human HCT15 cells2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID1283420Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 10 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID679269TP_TRANSPORTER: transepithelial transport (apical to basal) of Verapamil at a concentration of 11.8 nM in MDR1-expressing LLC-PK1 cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID227601Inhibition of P-glycoprotein, MDR-1, expressed in mouse T-cell lymphoma cell line at 11 uM2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.
AID1502809Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to azithromy2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID379473Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay in presence of vinblastine1999Journal of natural products, Apr, Volume: 62, Issue:4
Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii.
AID306133Effect on calcein accumulation in multidrug-resistant human 2780AD cells at 0.25 ug/ml relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Structure-activity relationships of some taxoids as multidrug resistance modulator.
AID1167550Permeability of the compound in 70:30 PBS:EtOH by PAMPA-BBB assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
AID455720Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as mean fluorescence intensity of rhodamine-123 uptake at 22 uM after 10 mins by flow cytometry2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID105436Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID76007Compound was tested in vitro for ionotropic activity on isolated atria preparations of guinea pig at 10E-6 M concentration1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Verapamil analogues with restricted molecular flexibility.
AID1235749Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 32 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID744440Permeability of the compound by PAMPA2013European journal of medicinal chemistry, May, Volume: 63Functionalized indoleamines as potent, drug-like inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt).
AID1517881Reversal of P-gp mediated multidrug resistance in human HepG2/Dox cells assessed as potentiation of doxorubicin-induced cell growth inhibition at 10 uM measured after 48 hrs by MTT assay (Rvb = 24%)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1904172Effect on P-gp expression in human K562/A02 cells at 5 uM measured by Western blot analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID78477Ability to bind to guinea pig atrial homogenate1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Accumulation of drugs by guinea pig isolated atria. Quantitative correlations.
AID358906Increase in DINIB-induced cytotoxicity against human LOXIMVI at 0.8 to 12.5 ug/mL2001Journal of natural products, Dec, Volume: 64, Issue:12
Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei.
AID1459751Cytotoxicity against human KBVIN assessed as reduction in cell viability by SRB assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1694879Permeability of compound after 16 hrs by PAMPA-BBB assay2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID19468Partition coefficient (logP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID1739808Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 6 +/- 0.2 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1502796Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502834Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID96002percentage of the dead cells of K-562 cells was determined for the concentration of 1 uM of the compound.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID1332153Effective permeability of the compound at pH 7.4 by BBB-PAMPA method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.
AID88410In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 50 uM2000Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18
A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID472409Cytotoxicity against human KB cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
AID294091Cytotoxicity against BHK cells by XTT assay2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Synthesis of dioxane-based antiviral agents and evaluation of their biological activities as inhibitors of Sindbis virus replication.
AID1733402Induction of cell cycle arrest in human KBV cells assessed as accumulation at G1/G0 phase at 10 uM after 24 hrs in presence of 0.1 uM paclitaxel by PI/RNaseA staining based flow cytometric analysis (Rvb = 50.74 +/- 0.07%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID78491Inhibitory concentration of [3H]- nitrendipine binding against guinea pig cerebral cortex membrane1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID1739133Stability of the compound in mouse plasma assessed as half life incubated for 3 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Chemical profiling of HIV-1 capsid-targeting antiviral PF74.
AID1502829Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1673426Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 5 uM preincubated for 24 hrs followed by compound washout and 12 hrs l2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1738696Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as increase in intracellular doxorubicin accumulation at 1 to 10 uM pretreated with compound for 30 mins followed by incubation with doxorubicin for 2 hrs by flow cytometry2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID1336850Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of vinblastine-induced cytotoxicity by measuring compound concentration required for reduction of vinblastine IC50 by half after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1514554Cytotoxicity against HOSEC assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1496041Effective permeability of the compound by PAMPA-BBB assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
AID401293Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 22.0 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID317951Ratio of permeability from apical to basolateral side over basolateral to apical side in human Caco-2 cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
AID1591940Modulation of ABCB1 (unknown origin) expressed in mouse L5178Y-MDR cells assessed as multidrug resistance reversing activity by measuring fluorescence activity ratio at 20 uM by rhodamine-123 accumulation based flow cytometry (Rvb = 1.1 No unit)
AID1502816Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID193719Hypotensive effect in Spontaneously hypertensive rats as maximum decrease in systolic blood pressure at 30 mg/kg, po dose1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID681579TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1207779Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID1215173Intrinsic clearance in Sprague-Dawley rat hepatic microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil per gram of liver by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1569059Intrinsic clearance in rat liver microsomes pre-incubated for 15 mins followed by addition of NADPH regenerating system by LC-MS analysis
AID1703889Permeability of the compound incubated for 8 hrs by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1769165Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM preincubated for 5 mins followed by NADPH regeneration system addition and measured after 30 mins by LC-MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID1281334Inhibition of P-gp in human MCF7/D70 cells assessed as decrease in doxorubicin IC50 at 10 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.906 +/- 0.02 uM)2016European journal of medicinal chemistry, Mar-03, Volume: 110Ligand-based modeling of diverse aryalkylamines yields new potent P-glycoprotein inhibitors.
AID1338182Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vinblastine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1273486Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 4 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1062339Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID1353432Inhibition of P-gp in human K562/Dox cells assessed as increase in nuclear accumulation of pirarubicin by spectrofluorometric method2018European journal of medicinal chemistry, Mar-10, Volume: 147Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents.
AID42314Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1286276Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay in presence of 0.121 uM vincristine2016Journal of natural products, Jan-22, Volume: 79, Issue:1
Aspidofractinine and Eburnane Alkaloids from a North Borneo Kopsia. Ring-Contracted, Additional Ring-Fused, and Paucidactine-Type Aspidofractinine Alkaloids from K. pauciflora.
AID1502795Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1502844Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID379474Ratio of IC50 for human KBV1 cells to IC50 for human KBV1 cells in presence of vinblastine1999Journal of natural products, Apr, Volume: 62, Issue:4
Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii.
AID77930Left ventricular pressure of isolated guinea pig heart at dose 0.005 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID1566016Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring cell survival at 5 uM after 72 hrs by MTT assay (Rvb = 100.58 +/- 7.78%)2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID1568812Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1703887Permeability of the compound incubated for 165 mins by PAMPA-BBB assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID230553Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with doxorubicin (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1566020Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 352.31 +/- 10.9 nM)2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1264447Permeability of the compound by PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID365463Inhibition of human MRP1 in human 2008 cells2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
AID1378333Permeability of the compound in PBS/EtOH at 100 mg/ml after 16 hrs by PAMPA2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.
AID1502877Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxaci2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID1211297Drug recovery in plasma (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1298980Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Jun-15, Volume: 26, Issue:12
Identification of selenocompounds with promising properties to reverse cancer multidrug resistance.
AID1558704Intrinsic clearance in mouse liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis
AID472443Antioxidant activity assessed as superoxide radical-scavenging activity at 1 mM by EPR spectroscopy2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
AID1502798Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1495600Inhibition of voltage gated calcium channel in Wistar rat aorta assessed as relaxation of KCl-precontracted aortic rings by measuring reduction in calcium entry in presence of phentolamine2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
AID1273398Anti-tubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294T after 7 days by mircodilution method2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1733391Effect on Pgp protein expression in human KBV cells at 10 uM after 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1514563Reversal ratio of IC50 for paclitaxel-induced cytotoxicity against human A2780/TAX cells in absence of compound to IC50 paclitaxel-induced cytotoxicity against human A2780/TAX cells in presence of compound2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID365464Inhibition of human MRP2 expressed in dog MDCK2 cells2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
AID1904133Reversal of BCRP-mediated multidrug resistance in dog MDCK-II-BCRP cells assessed as fold reduction in mitoxantrone IC50 at 5 uM measured after 48 hrs by MTT assay relative to mitoxantrone IC50 alone2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID94163MDR-reversal property tested in vitro on KB-A1 cells, resistance was induced by adriamycin1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID1215147Half life in Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1228917Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as restoration of intracellular doxorubicin accumulation after 150 mins by spectrofluorometric analysis relative to parental cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1631744Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate constant at 100 uM by HPLC-UV analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID696005Permeability of the compound after 4 hrs by PAMPA assay2012European journal of medicinal chemistry, Dec, Volume: 58Microwave-assisted synthesis of hydroxyphenyl nitrones with protective action against oxidative stress.
AID1459746Inhibition of ABCB1 (unknown origin) expressed in Flp-In-293 cells assessed as increase in calcein-AM uptake at 5 uM preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by fluorescence spectrometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1353431Inhibition of P-gp in human K562/Dox cells assessed as compound concentration causing 50% increase in nuclear accumulation of pirarubicin by spectrofluorometric method2018European journal of medicinal chemistry, Mar-10, Volume: 147Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents.
AID653306Inhibition of p-glycoprotein in human K562/A02 cells assessed as accumulation of rhodamine 123 at 10 uM by flow cytometry relative to control2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID340946Decrease in intracellular calcium concentration in human THP1 cells at 100 uM after 60 mins2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Modulation of the cellular accumulation and intracellular activity of daptomycin towards phagocytized Staphylococcus aureus by the P-glycoprotein (MDR1) efflux transporter in human THP-1 macrophages and madin-darby canine kidney cells.
AID99501Compound was tested for inhibition of rhodamine 123 efflux in mdr 1 transfectant L5178Y VMDRI C.06 mouse lymphoma cells; nd=Not determined1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.
AID331505Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected mouse L5178Y cells assessed as fluorescence activity ratio at 10 ug/ml by flow cytometry2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.
AID1352547Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of docetaxel-induced cytotoxicity at 10 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID615732Reversal of MDR1-mediated paclitaxel resistance in human NCI-H460 cells assessed as ratio of compound IC50 to IC50 of paclitaxel at 2.5 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1275776Antiplasmodial activity against multidrug resistant Plasmodium falciparum Dd2 by spectroscopic method2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID1481498Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-mediated cytotoxicity by measuring reduction in ADR IC50 at 5 uM preincubated for 24 hrs followed by compound washout and subsequent addition of adriamycin measured after 42017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID653466Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated for 24 hrs followed by adriamycin treated 12 hrs after drug washout by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1352539Cytotoxicity against human MCF7 cells assessed as cell survival at 10 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID453203Lipophilicity, log D of the compound2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1391818Inhibition of P-gp in human K562 cells assessed as increase in Rh123 accumulation at 5 uM after 2.5 hrs by by flow cytometry method2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID1307797Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID364884Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID53616Percent of cell viability remaining after incubating with a 10 uM concentration1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1903291Potentiation of vincristine-induced cytotoxicity against human KBV cells assessed as vincristine IC50 at 5 uM for 72 hrs by MTT assay (Rvb = 1542.76 +/- 827.23 nM )2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID1816741Metabolic stability in human liver microsomes assessed as intrinsic clearance in presence of NADPH at 1 uM by LC-MS/MS analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID714413Inhibition of P-gp-mediated paclitaxel resistance in human LCC6MDR cells assessed as fold decrease in paclitaxel IC50 for cytotoxic activity at 0.5 uM after 5 days by MTS assay relative to parental cells2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1358116Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM up to 30 mins in presence of NADPH by LC-MS/MS analysis
AID146413The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Aminoalkynyldithianes. A new class of calcium channel blockers.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID681122TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1156489Inhibition of p-glycoprotein in human MDA435/LCC6MDR cells assessed as ratio of IC50 for taxol in absence of drug to IC50 for taxol in presence of 1 uM of drug after 5 days by MTS assay2014European journal of medicinal chemistry, Aug-18, Volume: 834,5-Di-substituted benzyl-imidazol-2-substituted amines as the structure template for the design and synthesis of reversal agents against P-gp-mediated multidrug resistance breast cancer cells.
AID1350739Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of paclitaxel-induced cytotoxicity after 72 hrs by MTT assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID150759P-gp activity was measured by a direct transport assay, using polarized LLC-mdr1a epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1365717Half life in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1530100Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cell cycle arrest by measuring accumulation at G0/G1 phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 71.12019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1633078Cytotoxicity against human HepG2/ADM cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay relative to control2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1502800Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1517886Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as fold reduction in doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1502891Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1481497Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-mediated cytotoxicity by measuring reduction in ADR IC50 at 5 uM preincubated for 24 hrs followed by compound washout for 24 hrs and subsequent addition of adriamycin measu2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID1502883Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxa2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1785078Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as colchicine IC50 by measuring reversal fold at 2 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay relative to colchicine
AID103926Compound (1 uM) was evaluated for the inhibition of cell growth in MCF-7/ADR* cell line (over expresses Pgp and is for Doxorubicin resistant) in the presence of Taxol2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
AID29140Apparent value (pKa) calculated with ACD/pKa (experimental pKa value)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID464018Inhibition of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID150364MDR-reversal property tested in vitro on P388/VCR-20 cells, resistance was induced by vincristine1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID1758185Antiproliferative activity against human MCF7/ADR cells assessed as inhibition rate at 10 uM incubated for 48 hrs by CCK-8 assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
AID1813133Reversal of P-glycoprotein mediated drug resistance in human LCC6MDR cells assessed as reversal of paclitaxel resistance measured after 5 days by Cell Titer-Glo luminescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1533103Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 3.12 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID680136TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells2000Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 28, Issue:10
Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in
AID1235753Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 2 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1064671Induction of human recombinant p-glycoprotein ATPase activity using ATP as substrate at 0.5 mM after 40 mins by luciferase-mediated Pgp-Glo assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication.
AID1739814Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 823 +/- 16 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID362950Inhibition of P-glycoprotein expressed in mouse L5178Y cells measured by rhodamine 123 uptake assessed as fluorescence activity ratio relative to wild type mouse L5178 cells at 1 uM2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes.
AID1174968Resistance factor, ratio of adriamycin IC50 for human K562/A02 cells over-expressing Pgp to adriamycin IC50 for human K562/A02 cells over-expressing Pgp in presence of 5 uM compound incubated for 24 hrs prior to adriamycin treatment2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID150618Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID54923Inhibition of human cytochrome P450 3A42003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1502867Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID714427Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Lineweaver-Burk plot analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID289064Effect on calcein accumulation in MDR 2780AD cells at 0.25 ug/mL relative to control2007Journal of natural products, Jun, Volume: 70, Issue:6
Bioactive polyketides from Peperomia duclouxii.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1465293Effective permeability of the compound at 100 ug/ml by PAMPA-BBB assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID406191Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of vinblastine2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID1603235Permeability of the compound assessed as rate constant for partitioning to the membrane by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1365649Permeability of the compound at 100 mg/ml after 16 hrs by BBB-PAMPA method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease.
AID1502762Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1228918Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as restoration of intracellular doxorubicin accumulation at 3 uM after 150 mins by spectrofluorometric analysis relative to parental cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID722211Reversal fold, ratio of doxorubicin IC50 for doxorubicin-resistant human K562 cells in absence of compound to doxorubicin IC50 for doxorubicin-resistant human K562 cells in presence of 20 uM of compound2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID1209593Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1210967Ratio of drug level in brain to plasma of 5/6 nephrectomized Sprague-Dawley rat chronic renal failure model at 0.1 mg/kg, iv after 60 mins by beta-counting method relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Effects of chronic renal failure on brain drug transporters in rats.
AID166816Compound was evaluated for the alpha-Adrenoceptor pA2 blocking activity in vitro in rabbit thoracic aorta1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID158040Concentration required to reduce chloroquine IC50 by 50%2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID306134Effect on calcein accumulation in multidrug-resistant human 2780AD cells at 2.5 ug/ml relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Structure-activity relationships of some taxoids as multidrug resistance modulator.
AID653451Inhibition of p-glycoprotein-mediated rhodamine 123 efflux in human K562/A02 cells at 0.25 to 5 after 60 mins by fluorescence microscopic analysis2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1459772Inhibition of P-gp in human KBVIN cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1785069Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as reduction in paclitaxel IC50 at 2 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1851936Metabolic stability in mouse microsomes assessed as compound remaining measured after 30 mins2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1595499Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1813135Reversal of P-glycoprotein mediated drug resistance in human LCC6MDR cells assessed as reversal of vinblastine resistance measured after 5 days by Cell Titer-Glo luminescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1904176Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability at 50 uM after 48 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID27572Partition coefficient (logD7.0)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID619536Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for daunomycin-induced cytotoxicity in absence of drug to IC50 for daunomycin-induced cytotoxicity in presence of 10 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID76313Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro Negative inotropic potency)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1675373Stimulation of P-gp ATPase activity (unknown origin) assessed as increase in ATP consumption at 10 uM relative to control2020Journal of natural products, 08-28, Volume: 83, Issue:8
Ecdysteroid Derivatives that Reverse P-Glycoprotein-Mediated Drug Resistance.
AID1313195Intrinsic clearance in human liver microsomes assessed per mg of protein at 3 uM in presence of NADPH by LC-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID318687Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of paclitaxel by MTS assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis of curcumin mimics with multidrug resistance reversal activities.
AID1288621Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID1368307Inhibition of P-gp in human K562/Dox cells assessed as maximum increase in nuclear accumulation of pirarubicin by spectrofluorometric assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Design and synthesis of aminoester heterodimers containing flavone or chromone moieties as modulators of P-glycoprotein-based multidrug resistance (MDR).
AID1198506Inhibition of Trypanosoma cruzi cruzaine at 100 uM using mMBz-Pro-Phe-Arg-pNA substrate incubated for for 5 mins by UV-vis spectrophotometry2015European journal of medicinal chemistry, Mar-26, Volume: 93Computer-guided drug repurposing: identification of trypanocidal activity of clofazimine, benidipine and saquinavir.
AID1673437Inhibition of P-gp overexpressed in human K562/A02 cells assessed as increase in doxorubicin accumulation preincubated for 60 mins followed by doxorubicin addition and measured after 90 mins by fluorescence spectrophotometry analysis2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1733389Modulation of Pgp-ATPase activity (unknown origin) assessed as fold increase in ATP consumption at 0.5 mM preincubated for 5 mins followed by Mg-ATP addition and measured after 45 mins by microplate reader analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1530762Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method2019European journal of medicinal chemistry, Jan-01, Volume: 1611,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.
AID1239239Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in doxorubicin accumulation at 2 uM after 2.5 hrs by spectrofluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID1517908Inhibition of P-gp mediated doxorubicin efflux in human MCF7/ADM cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing c2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1190830Cytotoxicity against human KB/VCR cells at 10 uM after 72 hrs by SRB method2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Multidrug resistance-reversal effects of resin glycosides from Dichondra repens.
AID230554Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with taxol (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1167634Blood brain permeability of the compound at donor and acceptor by PAMPA assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1215182Intrinsic clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1351582Tracheorelaxant activity in Wistar rat trachea tonus assessed as reduction in 30 mM KCl-induced contraction after 15 mins2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID332136Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of doxorubicin ED50 without drug to doxorubicin ED50 with drug at 1.5 ug/ml after 6 days by BCA assay1997Journal of natural products, Nov, Volume: 60, Issue:11
Multidrug-resistance modulators from Stephania japonica.
AID653455Cytotoxicity against human K562/A02 cells expressing p-glycoprotein assessed as cell killing at 5 uM after 72 hrs by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1228919Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as restoration of intracellular doxorubicin accumulation at 8 uM after 150 mins by spectrofluorometric analysis relative to parental cells2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1684008Reversal of resistance to paclitaxel-induced cytotoxicity against human SW620 cells by measuring reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1906055Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, May-05, Volume: 235Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells.
AID1750903Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay
AID681163TP_TRANSPORTER: ATP hydrolysis in reconstituted proteoliposomes1996The Journal of biological chemistry, Feb-09, Volume: 271, Issue:6
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.
AID103936Inhibitory activity when combined with 5-fluorouracil (uM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1530092Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 1353.98 +/- 303.33 nM)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID105434Ability of compound to inhibit MDA-435/LCC6-MDR cell growth relative to progesterone.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1785072Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as paclitaxel IC50 by measuring reversal fold at 2 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID1576577Effective permeability of compound incubated for 8 hrs by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID166558Fractional inhibitory concentration (FIC) tested against RCS cells, isolate from Brazil.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum.
AID1062341Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID1334753Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID1429867Effective permeability of the compound at pH 7.4 at 50 uM after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID330503Activation of human P-gp ATPase in human Caco-2 cells at 100 uM2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
AID340721Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Role of the ABC transporter PRP1 (ABCC7) in pentamidine resistance in Leishmania amastigotes.
AID680675TP_TRANSPORTER: increase in saquinavir intracellular accumulation by Verapamil at 100uM in LLC-GA5-COL150 cells2004British journal of pharmacology, Dec, Volume: 143, Issue:7
Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux.
AID492324Inhibition of Pgp expressed in mouse L5178Y cells at 10 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID1237324Inhibition of human P-gp expressed in mouse T-cell lymphoma assessed as ratio of rhodamine 123 uptake in P-gp expressing cells to rhodamine 123 uptake in non P-gp expressing cells at 1 uM by flow cytometric analysis relative to control2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Discovery of substituted 1,4-dihydroquinolines as novel promising class of P-glycoprotein inhibitors: First structure-activity relationships and bioanalytical studies.
AID230556Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with taxol (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1771040Half life in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1683969Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in intracellular concentration of PTX at 4 uM pre-incubated for 4 hrs followed by PTX addition and measured after 2 hrs by liquid scintillation counting analysis
AID1472782Inhibition of human P-gp transfected in HEK293 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 10 uM pre-incubated for 1 hr before paclitaxel addition and measured after 72 hrs by MTT ass2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.
AID1207718Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1502729Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as increase in EtBr accumulation by measuring relative final fluorescence incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1210072Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1502815Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1502872Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 64 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID103923Effective concentration against MCF-7/ADR cells using P-gp-mediated MDR assay using 25 nM actinomycin D which results in 50% of the cells being killed in the presence of particular cytotoxic drug.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin.
AID681907TP_TRANSPORTER: inhibition of MTX uptake (MTX: 20 uM, Verapamil: 30 uM) in membrane vesicles from MRP4-expressing Sf9 cells2002Cancer research, Jun-01, Volume: 62, Issue:11
Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system.
AID619537Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for vinblastine-induced cytotoxicity in absence of drug to IC50 for vinblastine-induced cytotoxicity in presence of 1 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID1413459Permeability of the compound at 50 ug/ml after 16 hrs by PAMPA
AID1739824Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 242 +/- 5 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1589935Half life in rat liver microsomes2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
AID179048Compound was evaluated for the slow action potential blockade in 4 spontaneously hypertensive rats (SHR)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1427564Metabolic stability in rat liver microsomes assessed as parent compound remaining measured after 30 mins in presence of NADPH2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID1459767Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID368371Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1174628Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence microscopy2015European journal of medicinal chemistry, Jan-07, Volume: 89Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities.
AID313273Inhibition of P-glycoprotein in MDR human KBChR-8-5 cells assessed as retention of [3H]VLB after 2 hrs2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells.
AID1235784Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in rifampin MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID88420In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100 (uM) of infected host2000Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18
A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID1617119Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay2019Journal of natural products, 11-22, Volume: 82, Issue:11
Macroline-Sarpagine Bisindole Alkaloids with Antiproliferative Activity from
AID1215162AUC (0 to infinity) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1210070Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1362715Inhibition of LfrA in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as decrease in EtBr MIC at 80 ug/ml after 72 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria.
AID229582Ratio of maximal driving frequency to atrial rate in isolated guinea pig atria1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID77932Left ventricular pressure of isolated guinea pig heart at dose 0.5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID1525470Protein binding in rat plasma2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.
AID1565852Inhibition of P-gp in human K562/DOX cells assessed as drug level causing maximum increase in nuclear pirarubicin concentration incubated for 30 mins by fluorescence based assay relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID1703921Permeability of the compound by PAMPA-BBB assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID73909Potency expressed as EC50 for the negative inotropic activity.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID1833338Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID156089Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID175483Compound was evaluated for the concentration dependent negative ionotropic effect in rat right myocardial ventricular strips1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil.
AID1517907Inhibition of P-gp mediated doxorubicin efflux in human HepG2/Dox cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing 2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID80297Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.03 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID194806Antihypertensive activity as percent maximum (0-6 hr) decrease in blood pressure at 45 umol/kg po (~22 mg/kg) in 4 spontaneously hypertensive rats (SHR)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1459761Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID88407In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 100 uM2000Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18
A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID1235783Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in rifampin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1376831Modulation of human ABCB1 expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 22 uM pretreated for 10 mins followed by rhodamine-123 addition after 20 mins by flow cytometry (Rvb = 0.87 No_unit)2017Journal of natural products, 05-26, Volume: 80, Issue:5
Exploring Jolkinol D Derivatives To Overcome Multidrug Resistance in Cancer.
AID1771041Intrinsic clearance in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID76077Inhibition concentration of vasodilation was calculated from log concentration/response curves1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID481936Inhibition of P-gp-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells by flow cytometry2010Journal of natural products, May-28, Volume: 73, Issue:5
Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells.
AID1459771Inhibition of P-gp in human KBVIN cells assessed as potentiation of vincristine-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1245597Half life in human microsomes at 1 uM in absence of NADPH2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID1702313Inhibition of P-gp in human MDR1-MDCKII cells
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID310122Inhibition of P-glycoprotein by Hoechst assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1709005Permeability of compound at 100 uM at pH 7.4 by PAMPA assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
AID1769163Inhibition of CYP2C9 in human liver microsomes assessed as remaining activity at 1 to 10 uM using diclofenac as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID331513Cytocidal activity against human MDR1 gene transfected mouse L5178Y cells after 48 hrs by MTT method2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.
AID1129441Intrinsic clearance in human microsomes at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1321568Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as mean fluorescence intensity preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry (Rvb = 8.7 to 25.6 No2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID1684011Reversal of resistance to paclitaxel-induced cytotoxicity against human SW620 cells by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
AID1228905Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1533104Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 1.56 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1180205Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction at 100 uM relative to untreated control2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1833374Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/ABCB1 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID1904132Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as fold reduction in adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay relative to adriamycin IC50 alone2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID1235731Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1502869Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502775Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1225496Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of daunomycin cytotoxic IC50 in absence of compound to daunomycin cytotoxic IC50 in presence of compound at 1 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID90298Effect on doxorubicin IC50 against MDR human carcinoma cell line HCT116/VM46 cell line at a dose of 1 uM concentration2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID513628Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1338187Selectivity index, ratio of IC50 for cytotoxicity against mouse L929 cells to EC50 for inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vincristine cytotoxic IC50 by half2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID209999Fractional inhibitory concentration (FIC) tested against TM91C235 isolate.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum.
AID1472789Cytotoxicity in parental HEK293-pcDNA 3.1 transfected cells assessed as cell survival at 10 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.
AID1230203Permeability of the compound using PDVF membrane after 2 hrs 45 mins by PAMPA-BBB assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier.
AID1459765Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of vincristine-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID232671Selectivity ratio of IC50 for [Ca2+] antagonistic activity in aorta / IC50 for suppressive effect on rate of contraction1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID358645Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL2001Journal of natural products, Dec, Volume: 64, Issue:12
Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei.
AID150751Inhibition of P-glycoprotein using ATPase in MDR1 membranes2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1504324Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition measured after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance.
AID251491Multi drug resistance reversal in HCT116/VM46 cell line treated with Doxorubicin2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID307744Cytotoxicity against human A2780 cells assessed as cell viability at 10 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID1264249Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury.
AID695917Inhibition of Staphylococcus aureus SA-1199B NorA expressed in Escherichia coli DH10B assessed as inhibition of Hoechst 33342 dye efflux by spectrofluorometric analysis in presence of 50 uM Mg2+2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID1502839Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID252997Toxicity of compound (10 uM) is expressed as percentage of cell growth inhibition with respect to the control2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID340719Antileishmanial activity against wild-type Leishmania major LV39 promastigotes infected in human THP1 cells by luciferase based assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Role of the ABC transporter PRP1 (ABCC7) in pentamidine resistance in Leishmania amastigotes.
AID1874535Metabolic stability in mouse liver microsomes assessed as half life at 5 uM measured for 60 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits.
AID427726Reversal of MRP1-mediated doxorubicin resistance in doxorubicin co-incubated human 2008/MRP1 cells assessed as minimum concentration required for restoration of doxorubicin accumulation after 120 mins by spectrofluorimetry relative to accumulation in huma2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID80741Evaluated for decrease in contractility in isolated guinea pig atria1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID389919Inhibition of verapamil-induced specific ATPase activity in lipid activated mouse P-glycoprotein mdr3 cys-less mutant assessed as ATP hydrolysis per ug of protein at 100 uM2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID1353449Inhibition of P-gp in human K562/Dox cells assessed as reduction in Rh-123 efflux by measuring mean fluorescence intensity at 3 uM preincubated for 15 mins followed by Rh-123 addition for 30 mins and subsequent replacement in Rh-123 free medium measured a2018European journal of medicinal chemistry, Mar-10, Volume: 147Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents.
AID697007Induction of human MDR1 ATPase activity assessed as inorganic phosphate production2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID351892Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76N mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID43527The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM etoposide1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID1502845Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID236917Apparent permeability of the compound was determined inCaco-2 (human colon carcinoma) cells; Activity = Papp 10E-62005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
In silico prediction of membrane permeability from calculated molecular parameters.
AID1904190Inhibition of P-gp in human Caco-2 cells assessed as reduction in basal to apical transport of paclitaxel at 10 uM measured as apparent permeability after 120 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID43867The reversion potency of compound was measured against P-glycoprotein expressing CCRF-CEM cells and expressed as the ratio of ED50 in the absence and presence of daunomycin1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID1683957Inhibition of CYP3A4 in in human liver microsomes at incubated for 10 mins in presence of CYP3A4 substrate/NADP+ by fluorescence based assay
AID1833377Inhibition of ABCB1-mediated 3H-[PTX] efflux in human SW-620 cells assessed as accumulation of intracellular 3H-[PTX] at 4 uM preincubated for 4 hrs followed by 3H-[PTX] addition and measured after 2 hrs by liquid scintillation analysis
AID217929Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release)2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID1210015Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1502835Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID151341Amount of vincristine (VCR) accumulation in multidrug-resistant human ovarian cancer 2780AD cells at a concentration of 1 ug/mL.1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Modulation of multidrug resistance in tumor cells by taxinine derivatives.
AID594605Resistance modification index, ratio of IC50 for chloroquine in presence of compound to IC50 for chloroquine alone for chloroquine-resistant Plasmodium falciparum W22011European journal of medicinal chemistry, May, Volume: 46, Issue:5
A series of structurally simple chloroquine chemosensitizing dibemethin derivatives that inhibit chloroquine transport by PfCRT.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID283797Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 0.25 ug/mL relative to verapamil2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID1517901Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analy2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID728950Myorelaxant activity in albino rat aorta rings assessed as relaxation of KCl-induced contraction of aorta rings in presence of 10 uM KATP channel blocker glibenclamide2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1459757Potentiation of doxorubicin-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1273451Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 32 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID81852Inhibitory concentration of doxorubicin against the MDR resistant cell line HCT116/VM46 in the presence of 1 mM of the compound2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID1215135Decrease of CYP3A1 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat duodenum by Western blot analysis relative to wild type rat2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1129449Metabolic stability in human microsomes assessed as compound remaining at 1 uM after 60 mins2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID185881Ability to lower blood pressure in the spontaneously hypertensive rat (SHR) at 30 mg/kg (p.o.)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1199783Intrinsic cytotoxicity against human K562 cells assessed as cell survival at 10 uM after 24 hrs by MTT assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID722219Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as maximal increase of pirarubicin accumulation by spectrofluorometric analysis relative to control2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID1486975Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 6 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1604714Permeability assessed as mean mass balance at 200 uM incubated for 4 hrs by PAMPA method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
AID486954Lipophilicity, log P of the compound2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators.
AID1141746Myorelaxant activity in endothelium-free rat thoracic aorta assessed as inhibition of 30 mM of KCl-induced contraction2014European journal of medicinal chemistry, Jun-10, Volume: 80Influence of the alkylsulfonylamino substituent located at the 6-position of 2,2-dimethylchromans structurally related to cromakalim: from potassium channel openers to calcium entry blockers?
AID77259Negative inotropic activity was calculated from log concentration/response curves1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID249669Effect of compound on multidrug resistance in COLO 320 neoplasm at 10 ug/ml concentration; expressed as fluorescence activity ratio (treated/untreated cells)2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
3-Arylidene-1-(4-nitrophenylmethylene)-3,4-dihydro-1H-naphthalen-2-ones and related compounds displaying selective toxicity and reversal of multidrug resistance in neoplastic cells.
AID1502733Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1569060Half-life in human liver microsomes in presence of NADPH regenerating system
AID681162TP_TRANSPORTER: drug resistance (vincristine) in AML-2/D100 cells2004Biochemical and biophysical research communications, Jul-30, Volume: 320, Issue:3
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.
AID1502904Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 50 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1514558Cytotoxicity against human A2780/CDDP cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID562105Chemosensitization of chlorcycloguanil against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1215167Tmax in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1392732Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA
AID1273411Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 32 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1449544Metabolic stability in human intestinal microsomes assessed as compound remaining after 60 mins2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1465314Effective permeability of the compound by PAMPA2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID678839TP_TRANSPORTER: cell accumulation of daunomycin in MDA435/LCC6MDR1 cells2003The Journal of pharmacology and experimental therapeutics, Mar, Volume: 304, Issue:3
Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport.
AID682503Induction of ATPase activity of human His10-tagged P-gp expressed in BHK cells assessed as inorganic phosphate release after 30 mins relative to control2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Chalcogenopyrylium compounds as modulators of the ATP-binding cassette transporters P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1).
AID1761212Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID472444Antioxidant activity assessed as peroxyl radical-scavenging activity at 1 mM by EPR spectroscopy2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
AID509759Reversal of P-glycoprotein-mediated vincristine-resistance in human KB/VCR cells expressing Pgp assessed as ratio of vincristine IC50 to vincristine IC50 in presence of compound at 16 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity.
AID656833Potentiation of adriamycin-induced cytotoxicity against human K562 cells at 2.5 to 10 uM after 72 hrs by MTS assay2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID274751Effect on calcein accumulation in multidrug resistant human 2780 AD cells at 2.5 ug/mL relative to control2007Journal of natural products, Jan, Volume: 70, Issue:1
Bioactive pregnanes from Nerium oleander.
AID1502894Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID77839Heart rate of isolated guinea pig heart at dose 0.05 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID1849434Stability of the compound in simulated intestinal fluid at pH 6 to 8 assessed as half life at 120 mins by LC-MS/MS analysis
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID159424Tested for beta-1 adrenoceptor blocking activity in anesthetized pigs (n=2) challenged with intravenous injections of isoproterenol.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1486987Inhibition of ABCB1 in human K562/A02 cells assessed as rhodamine123 efflux after 90 mins by flow cytometric analysis (Rvb = 0.0231 +/- 0.0058 /s)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID165670In vitro inhibition of development of isometric tension, in response to KCl (60 uM) in rabbit aorta1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1631741Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID330504Apparent permeability from basolateral to apical side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
AID283799Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 25 ug/mL relative to verapamil2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID1750900Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay
AID1558701Half life in rat liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis
AID1673436Inhibition of P-gp overexpressed in human K562/A02 cells assessed as increase doxorubicin accumulation at 5 uM preincubated for 60 mins followed by doxorubicin addition and measured after 90 mins by fluorescence spectrophotometry analysis2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID80316Inhibitory concentration required to suppress the contractile force of guinea pig right atria1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID102848Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, by shrinkage (FSC) at 5 ug/mL.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery and biological evaluation of a new family of potent modulators of multidrug resistance: reversal of multidrug resistance of mouse lymphoma cells by new natural jatrophane diterpenoids isolated from Euphorbia species.
AID681336TP_TRANSPORTER: cell accumulation of 0.05u daunomycin in MCF-7/ADR cells2004Journal of pharmaceutical sciences, Jul, Volume: 93, Issue:7
Effects of benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates on P-glycoprotein- and MRP1-mediated transport.
AID1502771Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID75504Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro negative inotropic activity)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID289065Effect on calcein accumulation in MDR 2780AD cells at 2.5 ug/mL relative to control2007Journal of natural products, Jun, Volume: 70, Issue:6
Bioactive polyketides from Peperomia duclouxii.
AID1243943Metabolic stability in human liver microsomes assessed as compound remaining incubated for 60 mins in presence of NADPH2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1196794Metabolic stability in human microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in absence of NADPH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID283795Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 2.5 ug/mL relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID331367Toxicity in Sprague-Dawley rat assessed as ventricular permeature beat by measuring aconitine nitrate level at 2 mg.kg, iv by echocardiography2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID1411805Inhibition of Vesicular stomatitis Indiana virus envelope glycoprotein G-mediated cell entry in rVSIV-deltaG-G pseudotype virus infected HEK293 cells after 24 hrs post transfection by luciferase reporter gene assay2017MedChemComm, Dec-01, Volume: 8, Issue:12
N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.
AID1446765Half life in human liver microsomes in presence of NADPH by LC-MS/MS method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID23672Partition coefficient (logP)1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Accumulation of drugs by guinea pig isolated atria. Quantitative correlations.
AID1476986Effective permeability of compound at 200 uM after 18 hrs by PAMPA-BBB assay2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.
AID1772562n-Octanol/PBS buffer distribution coefficient, logD of the compound at pH 7.42021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID710065Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes assessed as reduction in [3H]-chloroquine uptake after 1.5 to 2 hrs2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents.
AID248377inhibitory activity of compound against Multidrug resistance HCT116/VM46 cell line treated with Doxorubicin2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
AID294052Antiproliferative activity against human Caco-2 cells assessed as cell viability by MTT assay after 48 hrs2007Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6
New 1,3-dioxolane and 1,3-dioxane derivatives as effective modulators to overcome multidrug resistance.
AID153524In vitro relative vinblastin uptake into P388/ADR (murine leukemia/multidrug resistant) cells following 10 uM treatment.1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID170816Effect (10 mg/kg, po) on coronary reperfusion-induced arrhythmias was assessed in anesthetized rats.(Intervals of ventricular tachycardia (VT)+ventricular fibrillation (VF) within 600 s.1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1295107Permeability of the compound at 100 ug/ml by PAMPA-BBB assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Design, synthesis and evaluation of novel ferulic acid-memoquin hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1486984Inhibition of ABCB1 in human K562/A02 cells assessed as increase in adriamycin accumulation at 0.5 to 2.5 uM pretreated for 60 mins followed by ADR addition after 90 mins by fluorescence spectrophotometric method2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1785086Inhibition of human recombinant CYP3A4 by fluorescence assay
AID594607Inhibition of chloroquine-resistant Plasmodium falciparum D10 CRT expressed in Xenopus laevis oocytes assessed as [3H]-chloroquine uptake after 1 to 2 hrs2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
A series of structurally simple chloroquine chemosensitizing dibemethin derivatives that inhibit chloroquine transport by PfCRT.
AID1666036Effective permeability by PAMPA-BBB penetration assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.
AID1750943Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as viable cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 52.8%)
AID282999Reversal of P-gp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug concentration causing half-maximal increase in nuclear pirarubicin concentration2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Exploratory chemistry toward the identification of a new class of multidrug resistance reverters inspired by pervilleine and verapamil models.
AID1586571Effective permeability of the compound in prisma HT buffer at 10 mM at pH 7.4 after 4 hrs by PAMPA2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1139646Permeability of the compound at 5 mg/mL after 18 hrs by PAMPA2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of (e)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides as novel multifunctional neuroprotective agents.
AID324584Increase in long-lived protein degradation in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID427731Reversal of MRP1-mediated doxorubicin resistance in human 2008/MRP1 cells assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of compound at 0.5 uM2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1235748Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID321883Ratio of apparent permeability from apical to basolateral over basolateral to apical side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID193257Antiarrhythmic activity against anesthetized rats after intravenous administration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1502742Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1378880Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID373867Hepatic clearance in human hepatocytes in absence of fetal calf serum2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
First-principle, structure-based prediction of hepatic metabolic clearance values in human.
AID1529416Cytotoxicity against CHO cells by MTT assay2018MedChemComm, Oct-01, Volume: 9, Issue:10
Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles.
AID1228902Cytotoxicity against human LCC-6 cells after 3 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1502719Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as increase in EtBr accumulation by measuring relative final fluorescence at 1/2 times MIC incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1874534Metabolic stability in human liver microsomes assessed as half life at 5 uM measured for 60 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits.
AID1365725Intrinsic clearance in human liver S9 microsomes at 1 uM in absence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1779702Inhibition of human ERG stably expressed in CHO-K1 cells at -90 mV holding potential by automated Q-patch clamp method
AID1530711Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 10 uM after 72 hrs by MTT assay relative to paclitaxel alone2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID1129167Permeability of the compound by PAMPA2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID7812In vitro rate of absorption observed as Caco-2 permeability in humans2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates.
AID1548638Effective permeability of compound in PBS buffer at pH 7.4 at 200 uM incubated for 17 hrs by PAMPA-BBB assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.
AID286481Inhibition of P-gp in A549 cells assessed as drug concentration required to double baseline fluorescence level by calcein-AM uptake assay2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Development of ruthenium antitumor drugs that overcome multidrug resistance mechanisms.
AID94168Percent of cell viability of KB-A1 human epidermoid carcinoma remaining after inoculation with the modulator alone1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID1502736Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1739844Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold change in vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to vincristine IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID156203Binding to POPC/GMI liposomes using biosensor system2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1168391Cytotoxicity against human HL60/MDR cells assessed as viable cells at 25 uM after 48 hrs by WST assay2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1502730Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1215149Cmax in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1578509Intrinsic clearance in ICR/CD1 mouse hepatocytes at 1 uM measured upto 120 mins by LCMS analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID81857Gain in sensitivity is measured as MDR IC50 (without added drug) / MDR IC50 (with added drug) in MDR HCT116/VM46 cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID151339Amount of vincristine (VCR) accumulation in multidrug-resistant human ovarian cancer 2780AD cells at a concentration of 10 ug/mL.1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Modulation of multidrug resistance in tumor cells by taxinine derivatives.
AID1285114Half life in human liver microsomes at 0.1 uM up to 60 mins by HPLC-MS/MS analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation.
AID1333892Inhibition of P-gp in doxorubicin resistant human K562 cells assessed as increase in accumulation of rhodamine 123 at 10 uM measured after 1 hr by flow cytometry2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
A novel curcumin derivative which inhibits P-glycoprotein, arrests cell cycle and induces apoptosis in multidrug resistance cells.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID106335Compound (1 uM) was evaluated for the inhibition of cell growth in MES-SA/DX5** cell line (over expresses Pgp and is for Doxorubicin resistant) in the presence of taxol2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
AID513655Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74/m-calpain assessed as inhibition of EGFP-HDQ74 aggregation at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1631739Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1225497Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of daunomycin cytotoxic IC50 in absence of compound to daunomycin cytotoxic IC50 in presence of compound at 3 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1623120Effective permeability of the compound by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID351904Chemosensitizing activity as 500nM potentiation of chloroquine effect after 72 hrs against chloroquine-resistant transporter 106/1'76N mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1386186Potentiation of adriamycin-induced cytotoxicity in human MCF7 cells assessed as adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay (Rvb = 1.3 +/- 0.2 uM)2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID165389Antagonistic activity against K+ induced responses in rabbit aorta1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1155071Antiplasmodial activity against Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1273465Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 16 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1502842Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to ciprofl2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1764804Stability in CD1 mouse pooled liver microsomes assessed as parent compound remaining measured at 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1355332Metabolic stability in rat liver microsomes assessed as compound remaining at 0.1 mM after 30 mins in presence of NADPH by HPLC analysis2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity.
AID1215132Increase of CYP3A2 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat liver by Western blot analysis relative to wild type rat2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID472415Inhibition of P-gp-mediated multidrug-resistance in human KB-C2 cells assessed as increase in colchicine-induced cytotoxicity at 5 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
AID91480Ability to bind to human serum albumin (HSA)1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Accumulation of drugs by guinea pig isolated atria. Quantitative correlations.
AID1275781Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as reversal of of choloroquine resistance at 0.5 uM relative to control2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID143484Inhibitory activity when combined with vincristine (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1652317Intrinsic clearance in human hepatocytes assessed per million cells2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
AID344455Antispasmodic activity in guinea pig ileum assessed as inhibition of acetylcholine-induced smooth muscle contraction2008Journal of natural products, Jul, Volume: 71, Issue:7
Chemical constituents of Aristolochia constricta: antispasmodic effects of its constituents in guinea-pig ileum and isolation of a diterpeno-lignan hybrid.
AID227994Inhibition of lipid peroxidation in rat liver microsomes.1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID368404Reversal of P-glycoprotein-mediated doxorubicin resistance in human doxorubicin-resistant K562 cells expressing Pgp assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of parent compound at 3 uM2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1502707Antimycobacterial activity against Mycobacterium avium 104 mc'2 3 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID377593Inhibition of human MDR1-mediated rhodamine efflux in mouse L5178 cells assessed as mean fluorescence intensity at 10 ug/mL by flow cytometry2006Journal of natural products, Jun, Volume: 69, Issue:6
Euphoportlandols A and B, tetracylic diterpene polyesters from Euphorbia portlandica and their anti-MDR effects in cancer cells.
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1502908Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay relati2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1585851Effective permeability of the compound by PAMPA2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1421886Effective permeability of the compound at 25 ug/ml after 18 hrs by BBB-PAMPA method2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID401288Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 1.10 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1207725Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1602181Metabolic stability in mouse liver microsomes at 1 uM in presence of NADPH incubated for 10 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.
AID513630Induction of autophagy in human SK-N-MC cells assessed as increase in LC3-2 level at 0.33 uM after 24 hrs by immunoblotting analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID680871TP_TRANSPORTER: inhibition of Rhodamine 123 efflux (R123: 1 ug/mL, Verapamil: 10 uM) in mdr1b-expressing NIH3T3 cells1997Carcinogenesis, Nov, Volume: 18, Issue:11
Functional characterization of the rat mdr1b encoded P-glycoprotein: not all inducing agents are substrates.
AID1472092n-Octanol-buffer distribution coefficient, log D of the compound at pH 5 incubated for 4 hrs by UV-vis based shake flask method2017Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice.
AID643322Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.
AID1235695Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 days by broth microdilution method2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1602583Intrinsic clearance in ICR/CD1 mouse hepatocytes assessed per million cells at 1 uM up to 120 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1404015Permeability of the compound after 2.5 hrs by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID165392Antagonistic activity against norepinephrine (NE) induced responses in rabbit aorta1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1502705Antimycobacterial activity against Mycobacterium smegmatis str. MC2 155 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1390042Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1460716Reversal of multidrug resistance in human MCF7/DX cells assessed as potentiation doxorubicin-induced cytotoxicity by measuring reduction in doxorubicin IC50 level at 5 uM incubated for 48 hrs by MTT assay relative to untreated control2017Journal of natural products, 04-28, Volume: 80, Issue:4
Isolation, Structure Elucidation, and Absolute Configuration of Syncarpic Acid-Conjugated Terpenoids from Rhodomyrtus tomentosa.
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID475691Oral bioavailability in human2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
AID653308Induction of rhodamine 123 accumulation in human K562 cells at 0.3 to 10 uM by flow cytometry2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1878314Gain in sensitivity, ratio of IC50 for reversal of P-gp mediated doxorubicin resistance in human SW620/AD300 cells overexpressing P-gp by measuring doxorubicin IC50 in absence of compound to IC50 for reversal of P-gp mediated doxorubicin resistance in hum2022Journal of natural products, 02-25, Volume: 85, Issue:2
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived
AID1761213Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID562104Chemosensitization of quinine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1336848Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring compound concentration required for reduction of doxorubicin IC50 by half after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID239740Michaelis-Menten constant for human P-glycoprotein expressed in Sf9 cells2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.
AID45602Inhibition of (-)-[3H]- D-888 binding to L-type calcium channels in kitten heart ventricle membranes1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID1152149Inhibition of MDR1 in MDCK2 cells assessed as inhibition of calcein AM efflux at 8 uM relative to control2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.
AID659301Reversal of p-glycoprotein-mediated multidrug resistance in human vincristine-resistance KB cells assessed as potentiation of vincristine-induced cytotoxicity at 4 uM after 48 hrs by SRB assay2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Anti-AIDS agents 89. Identification of DCX derivatives as anti-HIV and chemosensitizing dual function agents to overcome P-gp-mediated drug resistance for AIDS therapy.
AID72887Increase in the accumulation of vinblastine in multi-drug resistant GC3/Cl (human adenocarcinoma) cell line in vitro.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and chemical characterization of N-substituted phenoxazines directed toward reversing vinca alkaloid resistance in multidrug-resistant cancer cells.
AID1186756Inhibition of MRP1 (unknown origin) expressed in MDCK cells after 30 mins by Calcein-AM assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Trimethoxybenzanilide-based P-glycoprotein modulators: an interesting case of lipophilicity tuning by intramolecular hydrogen bonding.
AID1174636Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence spectrophotometry2015European journal of medicinal chemistry, Jan-07, Volume: 89Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities.
AID502838Reversal of human P-glycoprotein-mediated multidrug resistance in human KB/V cells as reduction of vincristine IC50 at 10 uM2010Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
Synthesis and structure-activity relationships of sinenxan A derivatives as multidrug resistance reversal agents.
AID1530102Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cell cycle arrest by measuring accumulation at G2/M phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 16.352019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1129457Solubility of the compound in PBS buffer after 16 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1210016Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID195197Inhibition of [Ca2+] induced contraction of K+ depolarized rat aorta by 50%1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID349880Permeability across porcine brain lipid coated polyvinylidene fluoride membrane by PAMPA2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID704797Inhibition of MDR1-mediated rhodamine 123 uptake expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 22 ug/mL after 10 mins by flow cytometry relative to parent cells2012Journal of natural products, Nov-26, Volume: 75, Issue:11
Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon adenocarcinoma cells.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID681358TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells2000Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 28, Issue:6
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
AID368370Cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp assessed as cell viability by trypan blue exclusion assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1429869Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID1862043Effective permeability of compound in PBS buffer at pH 7.4 at 200 uM incubated for 17 hrs by PAMPA-BBB assay2022Bioorganic & medicinal chemistry, 09-01, Volume: 692-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors.
AID105429Ability of compound to inhibit MDA-435/LCC6 cell growth relative to progesterone.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID604021Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID230144The P-glycoprotein (Pgp) antagonism score is the percentage of NCI/ADR cells surviving in the absence of vinblastine to that of in the presence of vinblastine.2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists.
AID1351578Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 30 mM KCl-induced contraction after 15 mins in presence of 10 uM glibenclamide2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID1275768Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as reversal of of choloroquine resistance at 1 uM relative to control2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID695916Inhibition of Hoechst 33342 dye in norA-deficient Escherichia coli DH10B expressing pTrc99A at 2 ug/mL by spectrofluorometer analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID376934Reversal of multidrug resistance in human AD10 cells assessed as increase in calcein accumulation at 2.5 ug/ml relative to control2006Journal of natural products, May, Volume: 69, Issue:5
Bioactive secolignans from Peperomia dindygulensis.
AID1750946Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as necrotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 7%)
AID1377752Effective permeability of the compound at 25 ug/ml by PAMPA assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID1739854Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold change in doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to doxorubicin IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1890739Permeability of the compound across blood brain barrier incubated for 18 hrs by UV plate reader based PAMPA assay2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
AID1436079Permeability of compound at 25 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID1179310Inhibition of multidrug resistance efflux pump Rv1258c in Mycobacterium tuberculosis H37Rv assessed as reduction in rifampicin MIC99 by MABA method2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
AID1566028Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as fold reduction in vincristine IC50 at 10 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID717341Inhibition of P-gp-mediated calcein AM efflux in human KBVIN cells assessed as fluorescence intensity at 10 uM incubated for 1 hr prior to calcein AM-addition by fluorimetric analysis (Rvb = 61.9 +/- 7.13)2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity.
AID1769284Inhibition of BCRP (unknown origin) expressed in HEK293/R2 cells assessed as conformational change by measuring increase in 5D3 shift at 1 uM preincubated for 15 mins followed by FITC mouse antihuman BCRP antibody addition measured after 30 mins by flow c2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Flavonoid Monomers as Potent, Nontoxic, and Selective Modulators of the Breast Cancer Resistance Protein (ABCG2).
AID429847Reversal of p-gp-mediated multidrug-resistance in human MCF7/ADM cells assessed as enhancement intensity at 10 ug/mL after 48 hrs by SRB assay relative to adriamycin2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures.
AID1390040Effective permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1517903Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 5 to 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by flow cytometry analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1517904Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 5 to 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by flow cytometry analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID615813Reversal of MDR1-mediated doxorubicin resistance in multidrug resistant human NCI-H460 cells assessed as combination index at 1 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1348614Metabolic stability in human liver microsomes at 5 uM preincubated for 5 mins followed NADPH addition measured after 120 mins by UPLC-MS/MS analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1279139Permeability of the compound at 25 ug/ml at pH 7.4 after 16 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID1215349Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by refined CYP450 IC50 s2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID619541Intrinsic toxicity in mouse NIH/3T3 cells expressing human MDR1 assessed as cell growth at 10 uM relative to control2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID1243939Kinetic solubility of the compound in PBS2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID436088Antioxidant activity against ferrous ion-induced lipid peroxidation in liver microsomes assessed as inhibition rate at 100 uM by TBA method in presence of cysteine2008Journal of natural products, Nov, Volume: 71, Issue:11
Targeted isolation and structure elucidation of stilbene glycosides from the bark of Lysidice brevicalyx Wei guided by biological and chemical screening.
AID153403Inhibitory activity when combined with vincristine (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1386182Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation after 1 hr by flow cytometry2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID1502860Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID75364Nagative inotropic activity was expressed as percent changes in developed tension in isolated guinea pig left atrium at 10 e-5 M1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID1335249Effective permeability of the compound incubated for 2 hrs by PAMPA-BBB assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT
AID722212Reversal fold, ratio of doxorubicin IC50 for doxorubicin-resistant human K562 cells in absence of compound to doxorubicin IC50 for doxorubicin-resistant human K562 cells in presence of 2 uM of compound2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID1565850Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID1587350Half life in mouse liver microsomes at 1 uM in presence of NADP by LC/MS-MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.
AID513176Displacement of [3H]astemizole from free heme crystal at 15 uM after 16 hrs by scintillation counting2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID681119TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID678952TP_TRANSPORTER: transepithelial transport of fexofenadine in Caco-2 cells2004Pharmaceutical research, Aug, Volume: 21, Issue:8
Transport characteristics of fexofenadine in the Caco-2 cell model.
AID603953In-vivo plasma to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
AID90135Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1739830Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 4736 +/- 59 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1537442Permeability of the compound at 100 uM after 6 hrs by PAMPA2019ACS medicinal chemistry letters, Feb-14, Volume: 10, Issue:2
Identification of Portimine B, a New Cell Permeable Spiroimine That Induces Apoptosis in Oral Squamous Cell Carcinoma.
AID45634Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID568587Vasodilatory activity in Sprague-Dawley rat thoracic aorta smooth muscle assessed as inhibition of phenylephrine-induced vasoconstriction2011Journal of natural products, Jan-28, Volume: 74, Issue:1
Macrophyllionium and macrophyllines A and B, oxindole alkaloids from Uncaria macrophylla.
AID679467TP_TRANSPORTER: efflux in MDR1-expressing LLC-PK1 cells2004Biochemical pharmacology, Jan-15, Volume: 67, Issue:2
Variable modulation of opioid brain uptake by P-glycoprotein in mice.
AID167787Myocardial infarction (MI) size was calculated as a percentage of the infarct area to the total area of the left ventricle of male chinchilla rabbits1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis of some hydroxynaphthazarins and their cardioprotective effects under ischemia-reperfusion in vivo.
AID1273455Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 128 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1288620Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID1338185Selectivity index, ratio of IC50 for cytotoxicity against mouse L929 cells to EC50 for inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of doxorubicin cytotoxic IC50 by half2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID165792Inhibition of [Ca2+] influx in response to a stimulus of norepinephrine (NE, 10 uM)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID251492Multi drug resistance reversal in HCT116/VM46 cell line treated with Vinblastine2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
AID252855Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (1 uM) and Daunorubian (DNM)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID159764Fractional inhibitory concentration (FIC) against Plasmodium falciparum W2 of equimolar (1:1) combination dose with chloroquine2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum.
AID43526The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID1357216Intrinsic clearance in mouse liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID1564095Reversal of P-gp-mediated multidrug resistance in human MCF7/Dox cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 12.5 uM after 48 hrs by MTT assay (Rvb = 51.19 +/- 0.95 microM)2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance.
AID510387Inhibition of Staphylococcus aureus 1199 norA efflux pump assessed as potentiation of ciprofloxacin MIC by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus.
AID1155076Inhibition of CTR in Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1174972Inhibition of P-gp mediated efflux in adriamycin-sensitive human K562 cells assessed as intracellular rhodamine-123 accumulation2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1705959Effective permeability of compound at 100 ug/ml incubated for 20 hrs by PAMPA-BBB assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID693226Effective permeability of the compound at pH 7.4 at 30 to 50 uM by PAMPA assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1336843Activity at human P-gp expressed in membranes assessed as stimulation of P-gp ATPase activity at 100 uM after 40 mins in presence of MgATP by luciferase reporter gene assay relative to control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID453204Permeability in human skin after 48 hrs by Franz cell permeability assay2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID680418TP_TRANSPORTER: inhibition of MTX uptake (MTX: 1 uM, Verapamil: 1000 uM) in membrane vesicles from MRP3-expressing HEK293 cells2001Cancer research, Oct-01, Volume: 61, Issue:19
Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport.
AID368554Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID368382Intrinsic cytotoxicity against human doxorubicin-sensitive K562 cells at 1 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1649243Reversal of Pgp-mediated DOX resistance in human SW620/AD300 cells assessed as potentiation of DOX-induced cytotoxicity by measuring DOX IC50 at 1 uM incubated for 48 hrs by SRB assay (Rvb = 33.39 +/- 7.08 uM)2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
AID1200540Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 50 uM relative to untreated control2015European journal of medicinal chemistry, Mar-26, Volume: 93Xanthone analogues as potent modulators of intestinal P-glycoprotein.
AID1762450Metabolic stability in human liver microsomes assessed as parent compound remaining after 120 mins in presence of NADPH regeneration system by UPLC/MS anlaysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters.
AID1770543Metabolic stability of the compound in rat liver microsomes assessed as half life at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID1239234Cytotoxicity against mouse L929 cells assessed as cell survival after 3 days by MTS/PMS assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID427723Reversal of MRP1-mediated doxorubicin resistance in doxorubicin co-incubated human 2008/MRP1 cells assessed as increase in doxorubicin accumulation at 3 uM after 120 mins by spectrofluorimetry relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1215131Increase of CYP3A1 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat liver by Western blot analysis relative to wild type rat2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID230394Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with cisplatin (uM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1228910Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing doxorubicin resistance measured as cell survival after 5 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1530088Cytotoxicity against human KBV cells assessed as cell survival at 10 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1733381Reversal of BCRP-mediated multidrug resistance in human KBV cells assessed as mitoxantrone IC50 at 10 uM after 72 hrs in presence of mitoxantrone by MTT assay (Rvb = 1186.50 +/- 29.24 nM)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID658437Antibacterial activity against Mycobacterium smegmatis mc2 155 after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Compounds of Alpinia katsumadai as potential efflux inhibitors in Mycobacterium smegmatis.
AID604020Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID96336Potency that causes a half maximal increase in nuclear concentration of pirarubicin.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID1071344Permeability of the compound by BBB-PAMPA2014European journal of medicinal chemistry, Feb-12, Volume: 731,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.
AID153398Inhibitory activity when combined with 5-fluorouracil (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1502847Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID331512Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected human Colo 320 cells assessed as fluorescence activity ratio at 10 ug/ml by flow cytometry2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.
AID161283Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.12003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches.
AID1129445Intrinsic clearance in mouse microsomes at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1739433Metabolic stability in human liver microsomes assessed as half life at 100 uM measured upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID376935Reversal of multidrug resistance in human AD10 cells assessed as increase in calcein accumulation at 25 ug/ml relative to control2006Journal of natural products, May, Volume: 69, Issue:5
Bioactive secolignans from Peperomia dindygulensis.
AID1783665Effective permeability of the compound in PBS/EtOH buffer (9:1) at 200 mM after 10 hrs by HPLC-UV based PAMPA-BBB assay2021European journal of medicinal chemistry, Nov-15, Volume: 2241,10-Seco-Eudesmane sesquiterpenoids as a new type of anti-neuroinflammatory agents by suppressing TLR4/NF-κB/MAPK pathways.
AID656832Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring survival rate at 10 uM after 72 hrs by MTS assay (Rvb = 95%)2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID464023Growth inhibition in doxorubicin-resistant human K562 cells overexpressing Pgp at 1 uM after 72 hrs by MTT assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID492325Inhibition of MRP1 expressed in human A2780 cells at 10 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID1392219Effective permeability of the compound by PAMPA assay2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
N
AID1502830Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID252857Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (3 uM) and Daunorubian (DNM)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID246154Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
AID1517867Permeability of compound by PAMPA-BBB assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1647651Antiproliferative activity against human SW620/AD300 cells assessed as reduction in cell viability after 48 hrs by MTT assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus,
AID1683996Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured
AID1235715Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1502849Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1781218Anti-MDR activity in human MCF7-DOX cells assessed as reversal of cell resistance to doxorubicin by measuring reversal fold at 10 uM measured after 48 hrs by MTT assay
AID1181956Stability in human liver microsomes assessed as metabolite formation at 8 uM at 37 degC in absence of NADPH and glucose-6-phosphate2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Straightforward entry to pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones and their ADME properties.
AID434446Passive membrane permeability across the PAMPA using pre coated plate based method2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.
AID1502787Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID371118Displacement of (-)-[3H]devapamil from L-type calcium channel in rabbit smooth skeletal cells relative to verapamil2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile.
AID1862044Effective permeability of the compound at pH 7.4 measured after 18 hrs by PAMPA-BBB assay2022Bioorganic & medicinal chemistry, 09-01, Volume: 692-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors.
AID1209972Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1502732Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID427742Reversal of MRP1-mediated doxorubicin resistance in human 2008/MRP1 cells assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of compound at 20 uM2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1514562Potentiation of vincristine-induced cytotoxicity against human KBV cells assessed as vincristine IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 666.3 nM)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1429862Effective permeability of the compound at pH 2 at 200 uM after 4 hrs by PAMPA-GI assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID7974Metabolic stability observed at 30 min after administration in human liver microsomes2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates.
AID101595Inhibitory activity when combined with vinblastine (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID9983MDR-reversing activity was measured by vincristine accumulation in the multidrug resistant 2780AD, a subline of A2780 ovarian carcinoma cells at 10 mg/mL2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Synthesis and biological activities of hapalosin derivatives with modification at the C12 position.
AID604026Unbound CSF to plasma concentration ratio in human2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID681169TP_TRANSPORTER: uptake in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID324380Induction of light chain 3-GFP level in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID514302Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as decrease in EGFP-HDQ74 aggregation at 10 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1288630Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as reduction in adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID1215175Intrinsic clearance in Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1514560Potentiation of paclitaxel-induced cytotoxicity against human A2780/TAX cells assessed as paclitaxel IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 3970 nM)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID678811TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID703734Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocyte assessed as inhibition of [3H]chloroquine uptake measured from 1 to 2 hrs2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling.
AID389767Inhibition of MDR1 overexpressed in MDCK cells at 25 uM relative to LSN3359842008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID81708Percent reversion was determined in HCT116 cell line (IC50(-)/MDR IC50(+) X 1002003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID513626Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1352542Cytotoxicity against human MCF7/ADR cells assessed as cell survival at 10 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID472414Inhibition of P-gp-mediated multidrug-resistance in human KB-C2 cells assessed as increase in colchicine-induced cytotoxicity at 2 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
AID1595500Inhibition of MRP1 (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID1502805Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID252996Toxicity of compound (3 uM) is expressed as percentage of cell growth inhibition with respect to the control2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID728949Myorelaxant activity in albino rat aorta rings assessed as relaxation of KCl-induced contraction of aorta rings in presence of 1 uM KATP channel blocker glibenclamide2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action.
AID332132Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of doxorubicin ED50 without drug to doxorubicin ED50 with drug at 10 ug/ml after 6 days by BCA assay1997Journal of natural products, Nov, Volume: 60, Issue:11
Multidrug-resistance modulators from Stephania japonica.
AID1338177Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM)2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1215145AUC (0 to 300 mins) in Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1769825Permeability of the compound across basolateral to apical membrane in human Caco-2 cells incubated for 2 hrs by LC-MS/MS analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
AID368374Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing maximum increase in nuclear concentration of pirarubicin by spectrofluorimetry relative to control2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1511119Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID318688Inhibition of Pgp in multidrug resistant human KBV20C cells assessed as increase in intracellular accumulation of Rh1232008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis of curcumin mimics with multidrug resistance reversal activities.
AID608394Permeability of the compound at 100 uM after 5 hrs by PAMPA2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1533116Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1703748Intrinsic clearance in human liver microsomes at 0.1 uM in presence of NADPH measured upto 60 mins by LC/MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1459749Cytotoxicity against human Flp-In-293 cells expressing MDR1 assessed as reduction in cell viability by SRB assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1520012Intrinsic clearance in rat liver microsomes up to 60 mins by HPLC-LC/MS analysis relative to control
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID288983Inhibition of P-glycoprotein in MDR mouse T lymphoma cells using rhodamine 123 assessed as ratio of fluorescent uptake relative to untreated control at 10 uM in MDR reversal assay by flow cytometry2007Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15
Structure-activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors.
AID1625252Inhibition of P-gp in doxorubicin-resistant human MCF7/ADR cells assessed as reversal of doxorubicin resistance by measuring doxorubicin IC50 incubated for 48 hrs by MTT assay (Rvb = doxorubicin alone = 64.8 +/- 2.1 uM)2019Journal of natural products, 04-26, Volume: 82, Issue:4
Jatrophane Diterpenoids from Euphorbia glomerulans.
AID1807359Metabolic stability in human liver microsomes assessed as half life in presence of NADPH regenerating system by UPLC-MS analysis
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1702154Metabolic stability in rat liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID464021Inhibition of P-glycoprotein-mediated in absence of test compound multidrug resistance in human doxorubicin-resistant K562 cells assessed as doxorubicin cytotoxic IC50 to doxorubicin cytotoxic IC50 in presence of test compound at 1 uM after 72 hrs by MTT 2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1739805Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1871990Antimycobacterial activity against non-replicating Mycobacterium tuberculosis H37Rv by time kill kinetic assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID340944Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in MDCK cells over expressing human MADR1 assessed as decrease in CFU at 500 uM in presence of 1 mg/liter daptomycin2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Modulation of the cellular accumulation and intracellular activity of daptomycin towards phagocytized Staphylococcus aureus by the P-glycoprotein (MDR1) efflux transporter in human THP-1 macrophages and madin-darby canine kidney cells.
AID1502880Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to ofloxa2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID653464Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated 24 hrs before adriamycin challenge followed by drug washout by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID94488Increase in the accumulation of vincristine in multi-drug resistant KB8-5 (HeLa variant) cell line in vitro.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and chemical characterization of N-substituted phenoxazines directed toward reversing vinca alkaloid resistance in multidrug-resistant cancer cells.
AID222590% inhibition of twitch contraction at 3 uM in electrically stimulated guinea pig ileum preparation by2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
AID1338196Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in doxorubicin accumulation to half of parental LCC6 cells measured after 150 mins by fluorescence spectrophotometric method2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1502743Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1595501Inhibition of BCRP (unknown origin) in MDCK-MDR1 assessed as inhibtion of hoechst 33342 transport incubated for 30 mins by fluorescence assay2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID1704106Inhibition of P-gp mediated multidrug resistance activity in human A2780T cells assessed as increase in intracellular DOX accumulation at 10 uM incubated for 4 hrs in presence of doxorubicin by flow cytometry2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID389398Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected mouse L5178 cells assessed as mean fluorescence intensity at 10 ug/ml by rhodamine-123 exclusion test2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic interaction between p-glycoprotein modulators and epirubicine on resistant cancer cells.
AID326368Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.
AID1486982Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1525472Stability in human liver microsomes assessed as parent compound remaining level2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.
AID1649244Reversal of Pgp-mediated DOX resistance in human SW620/AD300 cells assessed as potentiation of DOX-induced cytotoxicity by measuring change in DOX IC50 at 1 uM incubated for 48 hrs by SRB assay relative to DOX alone2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
AID195589Compound was evaluated for the displacement of [3H]gallopamil from specific binding sites on rat myocardial membrane particulates1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil.
AID679129TP_TRANSPORTER: reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID513635Induction of autophagy in Atg positive human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID681356TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells2002Pharmaceutical research, Jun, Volume: 19, Issue:6
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?
AID274752Effect on calcein accumulation in multidrug resistant human 2780 AD cells at 25 ug/mL relative to control2007Journal of natural products, Jan, Volume: 70, Issue:1
Bioactive pregnanes from Nerium oleander.
AID1517906Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID714426Inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin after 150 mins by fluorescence spectrophotometric analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID103937Inhibitory activity when combined with cisplatin (uM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID679791TP_TRANSPORTER: increase in Glibenclamide intracellular accumulation (Glibenclamide: 0.0525 uM, Vinblastine: 100 uM) in CC531mdr+ cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID324576Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID546593Cytotoxicity in human KBVIN cells by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Antitumor agents 286. Design, synthesis, and structure-activity relationships of 3'R,4'R-disubstituted-2',2'-dimethyldihydropyrano[2,3-f]chromone (DSP) analogues as potent chemosensitizers to overcome multidrug resistance.
AID395038Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 0.5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1374470Half life in mouse liver microsomes2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
AID1683971Effect on intracellular PTX concentration in human SW620 cells at 4 uM pre-incubated for 4 hrs followed by PTX addition and measured after 2 hrs by liquid scintillation counting analysis
AID1813130Reversal of Pgp-mediated paclitaxel resistance in human LCC6MDR cells assessed as paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay (Rvb = 152.5 +/- 9.7 uM)2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1739822Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 26.50 +/- 4.1 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1564096Inhibition of P-gp-mediated drug resistance in human MCF7/Dox cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring ratio of doxorubicin IC50 in absence of test compound to doxorubicin IC50 in presence of test compound at 12.5 uM2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance.
AID1388649Binding affinity to P-gp (unknown origin)2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment.
AID427196Membrane permeability by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID1904187Inhibition of P-gp in human Caco-2 cells assessed as reduction in basal to apical transport of paclitaxel at 10 uM measured as apparent permeability after 30 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID464019Inhibition of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as maximal increase in nuclear concentration of pirarubicin by spectrofluorimetry relative to sensitive K562 cells2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1273495Modulation factor, ratio of ethidium bromide MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 128 ug/ml in presence of ethidium bromide2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID78279Effect on force of atrial contractions induced by PTX-B in guinea pig (control value)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid A new class of A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid pu
AID1190185Permeability of the compound after 16 hrs by PAMPA2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Multifunctional coumarin derivatives: monoamine oxidase B (MAO-B) inhibition, anti-β-amyloid (Aβ) aggregation and metal chelation properties against Alzheimer's disease.
AID1056992Permeability of the compound by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
AID1362720Inhibition of LfrA in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as decrease in norfloxacin MIC at 150 ug/ml after 72 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria.
AID95592Inhibition of [3H]nitrendipine binding at L-type [Ca2+] channel in rat cortex homogenate by 50%.1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1733401Induction of cell cycle arrest in human KBV cells assessed as accumulation at sub-G1 phase at 10 uM after 24 hrs in presence of 0.1 uM paclitaxel by PI/RNaseA staining based flow cytometric analysis (Rvb = 5.83 +/- 0.31%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1704102Reversal of multidrug resistance activity in P-gp overexpressing human KB-VIN cells assessed as potentiation of VCR-induced cytotoxicity by measuring reversal ratio at 10 uM incubated for 48 hrs in presence of VCR by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID755310Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 1 uM after 2 hrs by microplate fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1459759Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1446268Metabolic stability of mouse liver microsomes assessed as amount of parent compound remaining at 25 to 100 uM after 1 hr in the presence of NADPH by LC-MS method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Design, Synthesis, and Evaluation of Novel Prodrugs of Transition State Inhibitors of Norovirus 3CL Protease.
AID1502871Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 64 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID337112Inhibition of human MDR1 expressed in mouse L5178 cells assessed as fluorescence activity at 23 uM by rhodamine 123 exclusion test2003Journal of natural products, Jul, Volume: 66, Issue:7
Jatrophane diterpenoids from Euphorbia mongolica as modulators of the multidrug resistance of L5128 mouse lymphoma cells.
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1352059Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as increase in intracellular Rh123 accumulation at 10 uM after 1 hr by flow cytometric analysis relative to untreated control2018European journal of medicinal chemistry, Feb-10, Volume: 145Synthesis and biological evaluation of bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potential P-glycoprotein and tumor metastasis inhibitors.
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1352549Inhibition of P-gp mediated efflux in human MCF7/ADR cells at 10 uM after 4 hrs by Rh123 dye-based flow cytometric method2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1903301Potentiation of cisplatin-induced cytotoxicity against human KBV cells assessed as cisplatin IC50 by measuring ratio IC50 as reversal fold at 5 uM for 72 hrs by MTT assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID88851Effect on cellular accumulation of Vincristine in multidrug resistant human ovarian cancer 2780AD cells at 10 ug/mL1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Modulation of multidrug resistance by taxuspine C and other taxoids from Japanese yew.
AID401286Reversal of P-gp-mediated multidrug resistance in human MCF cells assessed as enhancement in cytotoxicity of adriamycin1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1435954Intrinsic clearance in human liver microsomes after 10 to 60 mins in presence of NADPH by LC/MS/MS analysis2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1218865Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID1770546Metabolic stability of the compound in rat liver microsomes assessed as clearance at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID1502714Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis str. MC2 155 assessed as increase in EtBr accumulation by measuring relative final fluorescence at 1/2 times MIC incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1228907Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1502903Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 50 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1437175Permeability of the compound by PAMPA2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1481914Inhibition of P-gp in human K562/A02 cells assessed as accumulation of doxorubicin at 5.0 uM after 150 mins by fluorescence spectrophotometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID1312936Intrinsic half life in human liver microsomes in absence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID615810Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as combination index at 1 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1218864Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID1569058Half-life in rat liver microsomes pre-incubated for 15 mins followed by addition of NADPH regenerating system by LC-MS analysis
AID536762Intrinsic clearance in human liver microsomes at 3 uM measured per mg of protein by LC-MS/MS analysis2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.
AID230563Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vinblastine (nM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1771037Intrinsic clearance in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1772563Apparent permeability of the compound across apical side to basolateral side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID713774Binding affinity to human His10-tagged P-gp expressed in BHK cells assessed as induction of ATPase activity measured as inorganic phosphate release by spectrophotometric analysis relative to control2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Thiorhodamines containing amide and thioamide functionality as inhibitors of the ATP-binding cassette drug transporter P-glycoprotein (ABCB1).
AID1215166AUC (0 to 90 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1502772Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1371162Intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA).
AID656823Inhibition of Pgp-mediated rhodamine 123 efflux in human K562/A02 cells assessed as intracellular rhodamine 123 accumulation at 10 uM preincubated for 30 mins measured after 60 mins by fluorescence microscopy relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID265200Reversal of multi-drug resistance in L5178Y cells transfected with human MDR1 as relative fluorescent rhodamine123 activity at 10 ug/mL2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
New potent P-glycoprotein inhibitors carrying a polycyclic scaffold.
AID1728591Inhibition of human ABCB1 expressed in mouse L5178Y-MDR cells assessed as multidrug resistance reversing activity by measuring fluorescence activity ratio at 20 uM preincubated for 10 mins followed by rhodamine-123 addition and measured after 20 mins by f2021European journal of medicinal chemistry, Jan-15, Volume: 210Alkylated monoterpene indole alkaloid derivatives as potent P-glycoprotein inhibitors in resistant cancer cells.
AID379508Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID379471Cytotoxicity against human KB31 cells after 48 hrs by SRB assay1999Journal of natural products, Apr, Volume: 62, Issue:4
Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii.
AID1273401Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 16 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1481490Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID321881Apparent permeability from basolateral to apical side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID159876Accumulation coefficient of chloroquine at 1 uM-10 uM of DEEA against Plasmodium falciparum W22002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID368401Reversal of P-glycoprotein-mediated doxorubicin resistance in human doxorubicin-sensitive K562 cells assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of parent compound at 3 uM2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1904170Inhibition of P-gp in human K562/A02 cells assessed as rescue of intracellular Rhodamine 123 accumulation at 5 uM incubated for 5 to 120 mins and measured by flow cytometry analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID1358240Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular accumulation of doxorubicin at 20 uM after 2 days by fluorescence assay relative to doxorubicin alone2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell.
AID1647654Reversal of P-gp mediated multidrug resistance in human SW620/AD300 cells assessed as fold-resistance by measuring [IC50 for SW620/AD300 cells to doxorubicin IC50 for SW620 cells] at 2.5 uM after 48 hrs by MTT assay (Rvb = 38 No_unit)2020Journal of natural products, 02-28, Volume: 83, Issue:2
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus,
AID332133Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of doxorubicin ED50 without drug to doxorubicin ED50 with drug at 8 ug/ml after 6 days by BCA assay1997Journal of natural products, Nov, Volume: 60, Issue:11
Multidrug-resistance modulators from Stephania japonica.
AID1502738Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >1024 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1215184Tmax in Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1904130Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID317949Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
AID1769132Inhibition of CYP3A4 in human liver microsomes assessed as remaining activity at 1 to 10 uM using midazolam as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID230392Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with cisplatin (uM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1771038Half life in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1273438Modulation factor, ratio of refampin MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of refampin2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1273463Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 4 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID427402Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as fluorescence activity ratio at 22.2 uM after 10 mins by rhodamine-123 exclusion test2009Journal of natural products, Jun, Volume: 72, Issue:6
Tabernines A-C, beta-carbolines from the leaves of Tabernaemontana elegans.
AID1603231Permeability of the compound assessed as molar fraction in membrane at 0.5 mM measured after 2 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1054122Inhibition of human ERG2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Polypharmacology - foe or friend?
AID1817177Stability of compound in human liver microsomes assessed as compound remaining at 1 uM preincubated for 5 mins followed by addition of NADPH generating system and incubated for 30 mins by LC/MS relative to control2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of G Protein-Biased Ligands against 5-HT
AID1502785Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID514301Protection of neurodegeneration in Drosophila Huntington's disease model assessed as induction autophagy at 2.5 mM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1833362Reversal of resistance to paclitaxel-induced cytotoxicity in human KB-C2 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID1374514Activity at recombinant human Pgp expressed in cell membranes assessed as basal ATPase activity at 200 uM after 200 mins by P-gp Glo assay relative to control2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
MF-8, a novel promising arylpiperazine-hydantoin based 5-HT
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1225502Cytotoxicity against human MDR1 transfected mouse NIH/3T3 MDR1-G185 cells assessed as cell growth at 10 uM after 24 hrs by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1739828Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 1762 +/- 63 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID193139inhibitory activity was tested against anesthetized rats at 10 mg/kg1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID379773Reversal of P-glycoprotein-mediated multidrug resistance assessed as ratio of taxol IC50 for drug-resistant human KB-V1 cells to taxol IC50 for human drug-sensitive KB-3-1 cells at 10 uM after 48 hrs by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1174944Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID693225Binding affinity to truncated human PrP 121-231 at 50 uM by surface plasmon resonance method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1623668Permeability of compound at pH 7.4 by PAMPA2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1502873Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxacin alone2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502920Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1524535Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 89.14 +/- 4.89 uM)
AID1604713Permeability at 200 uM incubated for 4 hrs by PAMPA method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
AID103939Inhibitory activity when combined with vinblastine (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1849433Stability of the compound in simulated intestinal fluid at pH 6 to 8 assessed as compound remaining at 120 mins by LC-MS/MS analysis
AID1215186AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1273479Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 32 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1909448Permeability of the compound by PAMPA-BBB assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
AID1888851Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of norfloxacin-induced antibacterial activity by measuring fractional inhibitory concentration2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1514555Cytotoxicity against HUVEC assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1459762Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID399032Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780 cells assessed as calcein accumulation at 25 ug/ml after 15 mins relative to control2005Journal of natural products, Nov, Volume: 68, Issue:11
Bioactive tetrahydrofuran lignans from Peperomia dindygulensis.
AID1283419Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 3 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID1215163Half life in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1733396Induction of cell cycle arrest in human KBV cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by PI/RNaseA staining based flow cytometric analysis (Rvb = 33.81 +/- 0.57%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1807361Metabolic stability in mouse liver microsomes assessed as half life in presence of NADPH regenerating system by UPLC-MS analysis
AID1604133Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potential Tools for Eradicating HIV Reservoirs in the Brain: Development of Trojan Horse Prodrugs for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity.
AID714415Cytotoxicity against human LCC-6 cells after 72 hrs2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1234531Inhibition of human ABCB1 expressed in mouse L5178Y cells using rhodamine 123 as substrate assessed as ratio of fluorescent intensity in ABCB1 expressing L5178Y cells to wild type L5178Y cells at 10 uM after 20 mins by flow cytometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Discovery of substituted 1,4-dihydroquinolines as novel class of ABCB1 modulators.
AID1235719Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 8 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1330413Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing GFP assessed as growth inhibition at 1 ug/ml measured after 7 days by fluorescence analysis relative to control2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Discovery of novel N-phenyl 1,4-dihydropyridines with a dual mode of antimycobacterial activity.
AID1502820Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1816740Metabolic stability in rat liver microsomes assessed as half life in presence of NADPH at 1 uM by LC-MS/MS analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1888852Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at sub MIC2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1502778Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to erythromy2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1770542Metabolic stability of the compound in mouse liver microsomes assessed as half life at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID510384Inhibition of Staphylococcus aureus 1199B norA efflux pump assessed as potentiation of ciprofloxacin MIC by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus.
AID29338Dissociation constant (pKa)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID1517905Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analys2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1833353Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
AID1816742Metabolic stability in rat liver microsomes assessed as intrinsic clearance in presence of NADPH at 1 uM by LC-MS/MS analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID77643Antagonism of calcium-induced contractions of guinea pig ileal strips1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Aminoalkynyldithianes. A new class of calcium channel blockers.
AID1322437Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring ratio of mean fluorescence intensity in presence and absence of compound at 10 uM incubated for 1 hr by flow cytometry2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
AID1739840Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold change in paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to paclitaxel IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1822204Fold increase ratio, ratio of test compound gain of sensitivity doxorubicin IC50 to verapamil gain of sensitivity doxorubicin IC50 in human SW620/AD300 cells overexpressing P-glycoprotein assessed as reversal of doxorubicin resistance after 48 hrs by MTT 2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore.
AID1602170Metabolic stability in mouse liver microsomes at 1 uM in presence of NADPH incubated for 0 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.
AID728948Myorelaxant activity in albino rat aorta rings assessed as relaxation of 30 mM KCl-induced contraction of aorta rings2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action.
AID1167513Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 2.00 +/- 0.24 uM)2014European journal of medicinal chemistry, Nov-24, Volume: 87Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.
AID546592Inhibition of Pgp-mediated multidrug resistance in human KBVIN cells assessed as chemosensitization activity measured by increase in vincristine-induced cytotoxicity at 1 ug/mL by SRB assay relative to untreated control2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Antitumor agents 286. Design, synthesis, and structure-activity relationships of 3'R,4'R-disubstituted-2',2'-dimethyldihydropyrano[2,3-f]chromone (DSP) analogues as potent chemosensitizers to overcome multidrug resistance.
AID1833365Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/pcDNA3.1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1.93 +/- 0.06 nM
AID158683In vitro inhibitory activity against multidrug-resistant Plasmodium falciparum W2 Indochina2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID499784Activation of phospholipase A2/C in human OC2 cells assessed as increase in intracellular calcium level at 1 uM2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Effect of [6]-shogaol on cytosolic Ca2+ levels and proliferation in human oral cancer cells (OC2).
AID1180220Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings depolarized with 60 mM K+ solution assessed as relaxation of Ca2+-induced contraction at 1 uM (Rvb AUC = 82.7 +/- 8.3 no unit)2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID231934Ratio for antagonistic activity for Pgp/MRP1 was determined2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists.
AID1502784Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1623673Protein binding in human plasma2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1770545Metabolic stability of the compound in mouse liver microsomes assessed as clearance at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID1813134Reversal of P-glycoprotein mediated drug resistance in human LCC6MDR cells assessed as reversal of Dox resistance measured after 5 days by Cell Titer-Glo luminescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1283416Intrinsic cytotoxicity against mouse NIH/3T3 cells transfected with human MDR1 assessed as cell growth at 60 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID324578Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 8 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1245598Half life in human microsomes at 1 uM in presence of NADPH2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID307748Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 10 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID331363Inhibition of Pgp-mediated multidrug resistance activity in rat RBMEC cells assessed as decrease in Rh123 efflux2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID262090Antiarrhythmic activity in iv dosed rat2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Antiarrhythmic activity of 4,6-di(het)aryl-5-nitro-3,4-dihydropyrimidin-(1H)-2-ones and its effects on arterial pressure in rats.
AID1623690Permeability of compound at pH 7.4 assessed as drug retention by PAMPA2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1200541Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 100 uM relative to untreated control2015European journal of medicinal chemistry, Mar-26, Volume: 93Xanthone analogues as potent modulators of intestinal P-glycoprotein.
AID1338180Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of paclitaxel cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1502890Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1374214Effective permeability of the compound in pH 7.4 buffer after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID247607Inhibitory activity against KB cell line after 72 h of drug exposure2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
AID1218863Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID379727Reversal of multidrug resistance in human 2780AD cells assessed as accumulation of calcein at 2.5 ug/mL after 15 mins by fluorescence technique relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii.
AID1273399Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as accumulation of EtBr at 0.5 ug/ml after 3 days by real time fluorometric analysis relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1525471Stability in rat liver microsomes assessed as parent compound remaining level2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.
AID1215152AUC (0 to infinity) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID80864Percent reversion in HCT116 cell line (IC50(-)/MDR IC50(+) X 1002003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID268084Metabolic stability in rat liver microsomes2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID274750Effect on calcein accumulation in multidrug resistant human 2780 AD cells at 0.25 ug/mL relative to control2007Journal of natural products, Jan, Volume: 70, Issue:1
Bioactive pregnanes from Nerium oleander.
AID1322436Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring mean fluorescence intensity at 10 uM incubated for 1 hr by flow cytometry (Rvb = 0.47 No_unit)2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
AID1215153Half life in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1235765Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 32 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1481494Substrate activity at ABCB1 ATPase in human ABCB1 membrane fraction assessed as increase in ATPase activity at 50 uM preincubated with compound followed by addition of MgATP measured after 1 hr by luciferase reporter gene assay relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID1738693Cytotoxicity against human K562/4 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID481441Aqueous diffusivity at 37C2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1446672Displacement of [3H]-azidopine from ABCB1 in human KBV1 cell membranes at IC50 incubated for 20 mins in dark followed by irradiation of UV-light measured after 20 mins by SDS-PAGE based autoradiography relative to control
AID1502766Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1702159Clearance in mouse liver microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1235762Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 256 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID714416Cytotoxicity against mouse L929 cells after 72 hrs2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1168387Inhibition of P-gp-mediated doxorubicin efflux in human HL60/MDR cells assessed as intracellular doxorubicin accumulation at 25 uM preincubated for 15 mins measured after 60 mins by flow cytometry2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition.
AID1288619Inhibition of P-gp in human K562/A02 cells assessed as rate constant for rhodamine 123 efflux at 5 uM after 90 mins by flow cytometry (Rvb = 0.0253 +/- 0.0069/sec)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID1740447Intrinsic clearance in human microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID1480942Permeability of the compound at pH 7.4 at 1 mg/ml after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID1215148Clearance in Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1739834Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold change in paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to paclitaxel IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1371164Aqueous solubility of the compound in PBS after 2 hrs by turbidimetric method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA).
AID1731760Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life at 5 uM preincubated for 5 mins followed by NADPH addition and measured after 60 mins by LCMS analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
AID755320Inhibition of p-gp in human KB/VCR cells assessed as potentiation of 100 nM docetaxel-induced cytotoxicity after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1195137Permeability of the compound in DMSO/Prisma HT buffer at 1:200 ratio after 2 hrs by PAMPA-BBB assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo.
AID680086TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Azidopine: 0.1 uM, Verapamil: 100 uM) in membranes from K562/DOX cells2000Methods and findings in experimental and clinical pharmacology, Jun, Volume: 22, Issue:5
Enhancement of doxorubicin activity in multidrug-resistant cells by mefloquine.
AID1357220Intrinsic clearance in human liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID319361Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID1502857Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID80317Inhibitory concentration required to suppress the rate of contraction of guinea pig right atria1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID1215176Total intrinsic clearance in Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID344454Antispasmodic activity in guinea pig ileum assessed as inhibition of electrically-induced smooth muscle contraction2008Journal of natural products, Jul, Volume: 71, Issue:7
Chemical constituents of Aristolochia constricta: antispasmodic effects of its constituents in guinea-pig ileum and isolation of a diterpeno-lignan hybrid.
AID358651Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL2001Journal of natural products, Dec, Volume: 64, Issue:12
Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei.
AID1483834Half life in human liver microsomes in absence of NADPH by LC-MS/MS analysis2017Journal of natural products, 02-24, Volume: 80, Issue:2
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
AID1411806Selectivity index, ratio of CC50 for HEK293 cells to IC50 for Marburg virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-MarV-GP pseuotype virus infected HEK293 cells2017MedChemComm, Dec-01, Volume: 8, Issue:12
N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.
AID1174966Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs followed by adriamycin treatment 6 hrs post compound washout measured after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1062340Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID562098Chemosensitization of amodiaquin against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1444095Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1429870Permeability of the compound at pH 7.4 at 50 uM by PAMPA-BBB assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID321384Apparent permeability from apical to basolateral side of human Caco-2 cell membrane at pH 7.4 after 21 days2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma.
AID678795TP_TRANSPORTER: uptake in OCTN2-expressing HEK293 cells2001Molecular pharmacology, Feb, Volume: 59, Issue:2
Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2.
AID1514565Reversal ratio of IC50 for vincristine-induced cytotoxicity against human KBV cells cells in absence of compound to IC50 for vincristine-induced cytotoxicity against human KBV cells in presence of compound2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1761222Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as paclitaxel-mediated apoptosis by measuring accumulation of cells in Sub-G1 phase in at 5 uM measured by flowcytometry method (Rvb (paclitaxel)= 2.1%)2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID502262Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
AID306135Effect on calcein accumulation in multidrug-resistant human 2780AD cells at 25 ug/ml relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Structure-activity relationships of some taxoids as multidrug resistance modulator.
AID322362Inhibition of human multidrug resistant gene Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein.
AID475689Metabolic stability in cryopreserved human hepatocytes assessed as compound remaining at 5 umol/L after 240 mins by LC/MS/MS analysis2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1246312Intrinsic clearance in mouse microsomes2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1740448Intrinsic clearance in mouse microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID722615Inhibition of human Pgp-mediated Rhodamine 123 efflux expressed mouse L5178Y cells assessed as fluorescence activity ratio at 22 uM after 10 mins by flow cytometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Enhancing macrocyclic diterpenes as multidrug-resistance reversers: structure-activity studies on jolkinol D derivatives.
AID1174965Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs followed by adriamycin treatment post compound washout measured after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1525469Protein binding in human plasma2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.
AID1625255Inhibition of P-gp in doxorubicin-resistant human MCF7/ADR cells assessed as reversal of doxorubicin resistance by measuring reduction in doxorubicin IC50 incubated for 48 hrs by MTT assay relative to doxorubicin alone2019Journal of natural products, 04-26, Volume: 82, Issue:4
Jatrophane Diterpenoids from Euphorbia glomerulans.
AID1738698Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as increase in doxorubicin accumulation by flow cytometric analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID1649256Effect on recombinant human membrane bound ABCB1 ATPase activity 0.5 mM incubated for 5 mins followed by Mg-ATP addition and measured after 40 mins by luciferase reporter gene based p-gp glo assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
AID1502803Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID345308Intrinsic cytotoxicity against mouse NIH/3T3 cells overexpressing MDR1 at 3 uM after 72 hrs by MTT assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
AID103938Inhibitory activity when combined with taxol (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1168906Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by neutral red dye-based assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
AID1502837Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID230388Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with 5-Fluorouracil (uM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1352555Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity at 10 uM preincubated with cells followed by compound washout and subsequent incubation for 6 hrs prior to addition of doxorubicin and measured after 42018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1783322Inhibition of P-gp in human A549/Taxol cells assessed as increase in rhodamine 123 accumulation at 10 uM preincubated for 4 hrs followed by addition of rhodamine 123 and measured after 1 hr by flow cytometry assay (Rvb = 26.5%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis, computational docking and biological evaluation of celastrol derivatives as dual inhibitors of SERCA and P-glycoprotein in cancer therapy.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID551246Half life in human microsome by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis.
AID1702153Metabolic stability in mouse liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID153399Inhibitory activity when combined with cisplatin (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1235691Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 3 days by broth microdilution method2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1163826Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID1237325Inhibition of human P-gp expressed in mouse T-cell lymphoma assessed as ratio of rhodamine 123 uptake in P-gp expressing cells to rhodamine 123 uptake in non P-gp expressing cells at 10 uM by flow cytometric analysis relative to control2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Discovery of substituted 1,4-dihydroquinolines as novel promising class of P-glycoprotein inhibitors: First structure-activity relationships and bioanalytical studies.
AID1481913Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 5 uM preincubated for 24 hrs followed by doxorubicin addition measured after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID653307Inhibition of p-glycoprotein in human K562/A02 cells assessed as accumulation of rhodamine 123 by flow cytometry2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1764805Half life in CD1 mouse pooled liver microsomes assessed as parent compound remaining measured up to 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID317950Activation of human P-glycoprotein ATPase in Caco-2 cells assessed as ATP depletion at 100 uM2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
AID427738Inhibition of MRP1 in human 2008/MRP1 cells by Lineweaver-Burke plot analysis2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1502859Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1437174Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID753938Inhibition of p-gp in Wistar rat primary hepatocytes assessed as inhibition of rhodamine 123 efflux up to 50 uM after 3 hrs2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Synthesis and pharmacological investigation of new N-hydroxyalkyl-2-aminophenothiazines exhibiting marked MDR inhibitory effect.
AID619534Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as daunomycin efflux at 10 uM after 30 mins by flow cytometry2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID194922Percent Catecholamine-depletion in brain by administering a dose of 2 x 45 umol/kg, perorally to 4 spontaneously hypertensive rats (SHR).1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID481440Dissociation constant, pKa of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1603232Permeability of the compound assessed as molar fraction in membrane at 0.5 mM measured after 16 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID679340TP_TRANSPORTER: increase in brain concentration in mdr1a(-/-) mouse2001Pharmaceutical research, Jul, Volume: 18, Issue:7
Effect of mdr1a P-glycoprotein gene disruption, gender, and substrate concentration on brain uptake of selected compounds.
AID1502745Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID180478Molar concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50%1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID51927Cytotoxicity against Chinese hamster ovary cells2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID619465Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for daunomycin-induced cytotoxicity in absence of drug to IC50 for daunomycin-induced cytotoxicity in presence of 3 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID1635243Intrinsic clearance in human liver microsomes assessed per mg protein at 3 uM preincubated with compound followed by NADPH addition measured after 5 to 45 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Aug-08, Volume: 118Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1273497Modulation factor, ratio of ethidium bromide MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of ethidium bromide2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID324536Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1350734Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of paclitaxel up to 2 uM treated at 2 hrs post paclitaxel treatment for 30 mins in paclitaxel free medium by HPLC analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1179309Inhibition of multidrug resistance efflux pump Rv1258c in Mycobacterium tuberculosis H37Rv assessed as rifampicin MIC99 by MABA method2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
AID1459744Inhibition of ABCB1 (unknown origin) expressed in Flp-In-293 cells assessed as increase in calcein-AM uptake at 2.5 uM preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by fluorescence spectrometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1305711Half life in mouse liver microsomes at 0.1 uM2016Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14
Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents.
AID1310680Inhibition of full length human ABCB1 expressed in Flp-In-293 cells at 5 uM incubated for 30 mins by calcein-AM uptake assay relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis and bioevaluation of novel benzodipyranone derivatives as P-glycoprotein inhibitors for multidrug resistance reversal agents.
AID1235701Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 32 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1307816Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 10'-6 M2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1673424Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 5 uM preincubated for 24 hrs followed by compound washout and 24 hrs l2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1210074Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID252856Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (1 uM) and Vinblastine (VNB)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID588993Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MDR12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID619538Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for vinblastine-induced cytotoxicity in absence of drug to IC50 for vinblastine-induced cytotoxicity in presence of 3 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID1273475Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 8 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID321887Inhibition of human Pgp in adriamycin resistant MCF7 cells assessed as fold increase in accumulation of doxorubicin at 20 uM relative to control2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID1761215Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID324582Increase in long-lived protein degradation in human H4 cells after 1 hr relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID283794Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 0.25 ug/mL relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID1452459Inhibition of MDR1 (unknown origin) expressed in mouse L5178 cells assessed as rhodamine-123 accumulation measured as fluorescence activity ratio at 50 ug/ml preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytome2017European journal of medicinal chemistry, Jul-28, Volume: 135Discovery of potential anticancer multi-targeted ligustrazine based cyclohexanone and oxime analogs overcoming the cancer multidrug resistance.
AID1822202Inhibition of P-glycoprotein overexpressed in human SW620/AD300 cells assessed as reversal of doxorubicin resistance by measuring doxorubicin IC50 at 2.5 uM after 48 hrs by MTT assay2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore.
AID1865862Metabolic stability in rat liver microsomes assessed as parent compound remaining measured after 2 hrs by UPLC-MS analysis
AID681139TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID1738187Effective permeability of compound at 200 uM measured after 4 hrs by PAMPA-BBB assay
AID351905Chemosensitizing activity as 500nM potentiation of chloroquine effect after 72 hrs against chloroquine-resistant transporter 106/1'76I mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID319362Activity of Pgp-ATPase in doxorubicin-resistant human K562 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID1530108Inhibition of P-gp-mediated Rh-123 efflux in human KBV cells assessed as Rh-123 accumulation at 10 uM preincubated for 2 hrs followed by Rh-123 addition measured after 30 mins by flow cytometry2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID669862Inhibition of Pgp-mediated adriamycin efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of adriamycin at 0.33 to 10 uM after 60 mins by FACS flow cytometry2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1502875Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxaci2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1167512Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM)2014European journal of medicinal chemistry, Nov-24, Volume: 87Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.
AID1276882Apparent permeability of the compound in pig LLC-PK1 cells expressing human MDR1 at 1 uM measured at 3 hrs by LC/MS/MS analysis2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID681128TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1502861Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1683999Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring reduction in paclitaxel IC50 pre-incubated for 4 hrs followed by paclitaxel addition and meas
AID449583Inhibition of ABCB1 in human MES-SA/Dx5 cells assessed as potentiation of taxol-induced cytotoxicity after 60 hrs relative to verapamil by MDR reversal assay2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.
AID1502790Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1704103Reversal of multidrug resistance activity in human A2780/CDDP cells assessed as potentiation of CDDP-induced cytotoxicity by measuring CDDP IC50 at 10 uM incubated for 48 hrs in presence of CDDP by MTT assay (Rvb = 43.11 uM)2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1480849Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID643321Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1705925Effective permeability of compound in PBS at pH 7.4 at 100 uM incubated for 5 hrs by PAMPA-BBB based UPLC-MS analysis
AID1273491Modulation factor, ratio of ofloxacin MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of ofloxacin2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID656819Inhibition of Pgp-mediated rhodamine 123 efflux in human K562/A02 cells assessed as intracellular rhodamine 123 accumulation at 10 uM preincubated for 1 hr prior rhodamine 123 addition measured after 30 mins by flow cytometry relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID1486979Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 24 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID351889Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76T mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1312934Intrinsic half life in human liver microsomes in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID615814Reversal of MDR1-mediated doxorubicin resistance in human NCI-H460 cells assessed as ratio of compound IC50 to IC50 of paclitaxel at 5 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1172268Inhibition of human MDR1 expressed in mouse L5178Y cells assessed as Rhodamine-123 accumulation measured as fluorescence activity at 22 uM after 20 mins by flow cytometry relative to control2014Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22
Improving the MDR reversal activity of 6,17-epoxylathyrane diterpenes.
AID1197236Reversal of human MDR1-mediated drug efflux in mouse L5178 cells using rhodamine 123 as substrate assessed as fluorescence activity ratio at 4 uM incubated for 10 mins prior to substrate addition measured after 20 mins by FACScan flow cytometry relative t2015European journal of medicinal chemistry, Mar-06, Volume: 92Design, synthesis and biological profile of new inhibitors of multidrug resistance associated proteins carrying a polycyclic scaffold.
AID1435957Half life in human liver microsomes after 10 to 60 mins in absence of NADPH by LC/MS/MS analysis2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID604025Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1565851Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID1391813Inhibition of P-gp in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring fold reduction in adriamycin IC50 at 5 uM preincubated for 24 hrs followed by adriamycin addition measured after 48 hrs by MTT assay relati2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID513629Cytotoxicity against human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID678801TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells2004Molecular pharmacology, Jun, Volume: 65, Issue:6
High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter.
AID1465450Unbound intrinsic clearance in human liver microsomes at 10 uM preincubated for 5 mins followed by NADPH addition measured after 60 mins by HPLC-UV-MS analysis2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
AID1570001Permeability of compound at 100 ug/ml measured after dilution with PBS/EtOH (70:30) at pH 7.4 after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1235735Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 8 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1362713Growth inhibition of Mycobacterium smegmatis MC2 155 ATCC 700084 after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria.
AID150756Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1330414Inhibition of human ABCB1 expressed in mouse T-lymphoma cells assessed as rhodamine-123 accumulation by measuring fluorescence activity ratio at 1 uM by flow cytometry relative to control2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Discovery of novel N-phenyl 1,4-dihydropyridines with a dual mode of antimycobacterial activity.
AID428564Inhibition of CYP3A42009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
AID1750898Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay
AID1569061Intrinsic clearance in human liver microsomes in presence of NADPH regenerating system
AID464025Growth inhibition in human K562 cells at 1 uM after 72 hrs by MTT assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1351579Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 80 mM KCl-induced contraction after 15 mins2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID1207266Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1483833Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS analysis2017Journal of natural products, 02-24, Volume: 80, Issue:2
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
AID150758P-gp activity was measured by a direct transport assay, using polarized LLC-PK1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1273476Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 16 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1502850Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1225499Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of vinblastine cytotoxic IC50 in absence of compound to vinblastine cytotoxic IC50 in presence of compound at 1 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1623665Half life in human microsomes2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1502763Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1418856Potentiation of paclitaxel-induced cytotoxicity in human SW620 cells assessed as fold reduction in paclitaxel IC50 at 4 uM after 72 hrs by MTT assay relative to paclitaxel alone2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1225501Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of vinblastine cytotoxic IC50 in absence of compound to vinblastine cytotoxic IC50 in presence of compound at 10 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1200585Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 20 uM relative to untreated control2015European journal of medicinal chemistry, Mar-26, Volume: 93Xanthone analogues as potent modulators of intestinal P-glycoprotein.
AID1235769Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 2 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1833329Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
AID615731Reversal of MDR1-mediated paclitaxel resistance in human NCI-H460 cells assessed as ratio of compound IC50 to IC50 of paclitaxel at 5 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1378334Permeability of the compound by PAMPA2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.
AID1190546Cytotoxicity against taxol-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Structure-activity relationships of diverse ACGs against multidrug resistant human lung cancer cell line A549/Taxol.
AID1849468Cytotoxicity in human HepG2 cells assessed as number of live cells by measuring ATP metabolism incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID53606Compound was evaluated for in vitro activity in DC-3F/AD cell line (Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1418883Inhibition of ABCB1 (unknown origin) expressed in human HEK293T/ABCB1 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 4 uM after 72 hrs by MTT assay relative to paclitaxel2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1502821Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID351890Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1739832Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold change in vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to vincristine IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1635245Half life in human liver microsomes at 3 uM preincubated with compound followed by NADPH addition by LC-MS/MS analysis2016European journal of medicinal chemistry, Aug-08, Volume: 118Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID101594Inhibitory activity when combined with taxol (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID401289Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 2.20 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID1502854Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1739135Metabolic stability at phase 1 in mouse liver microsomes assessed as half life at 1 uM by LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Chemical profiling of HIV-1 capsid-targeting antiviral PF74.
AID636082Induction of [3H]-chloroquine accumulation in erythrocytes infected with chloroquine-resistant Plasmodium falciparum K1 trophozoites at 5 uM pre-incubated for 15 mins before exposure to [3H]-chloroquine measured after 1 hr by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents.
AID195351Inhibition of calcium activation was assessed against calcium-induced constriction of potassium-depolarized rat aorta (Negative logarithm of the molar concentration)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID1210017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1517893Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1392733Permeability of the compound at 100 ug/ml after 10 hrs by PAMPA
AID19419Partition coefficient (logD7.4)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID502840Cytotoxicity against human KB cells2010Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
Synthesis and structure-activity relationships of sinenxan A derivatives as multidrug resistance reversal agents.
AID1702152Metabolic stability in human liver pooled microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1813139Inhibition of P-glycoprotein in human LCC6MDR cells assessed as reversal fold by measuring reduction in paclitaxel by measuring paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID544255Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as 50% revertant concentration required for chloroquine susceptibility2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vitro and in vivo properties of ellagic acid in malaria treatment.
AID1215178Drug metabolism in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat hepatic microsomes assessed as CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID455739Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 mean fluorescence intensity of rhodamine-123 uptake after 10 mins by flow cytometry2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID1502773Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1414432Inhibition of MRP1 in human 2008/MRP1 cells assessed as increase in doxorubicin accumulation at 2 uM after 120 mins by flow cytometry relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
AID481446Effective permeability across human jejunum2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID551245Intrinsic clearance in mouse microsome by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis.
AID150617Concentration required for 50% inhibition (racemic) at binding site of human P-Glycoprotein (P-gp) in one-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID669852Inhibition of P-glycoprotein-mediated rhodamine 123 uptake expressed in multidrug-resistant human K562/A02 cells assessed as fluorescence activity ratio at 10 uM after 72 hrs by flow cytometry relative to untreated control2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents.
AID1623078Effective permeability of the compound at 100 ug/ml after 10 hrs by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1502828Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1279155Permeability of the compound at 25 ug/ml at pH 7.4 after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID1502863Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID509762Potentiation of vincristine-induced cytotoxicity against human KB cells at 16 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity.
AID1585850Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID272487Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID1426676Inhibition of P-gp in human K562/A02 cells assessed as increase in intracellular rhodamine123 accumulation at 0.33 to 10 uM measured after 1 hr by flow cytometry2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Potent Inhibition of Nitric Oxide-Releasing Bifendate Derivatives against Drug-Resistant K562/A02 Cells in Vitro and in Vivo.
AID714418Reversal of P-gp-mediated vincristine-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1739810Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 11.8 +/- 1.13 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID350523Induction of mouse cysteine-less MDR3 ATPase activity by apparent Michaelis-Menten constant2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
AID105426Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1739816Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 797 +/- 73 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID671173Inhibition of P-glycoprotein in rat primary hepatocytes assessed as increase in intracellular rhodamine 123 accumulation at 10 to 50 uM after 3 hrs2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Selective hydroboration of dieneamines. Formation of hydroxyalkylphenothiazines as MDR modulators.
AID1481489Cytotoxicity against human K562 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID1352541Cytotoxicity against human MCF7/ADR cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1683953Potentiation of PTX-induced antitumor activity against human SW620/Ad300 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 6 mg/kg/day, ig for 21 days relative to PTX alone
AID1514556Cytotoxicity against human T29 cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1569056Half-life in CD-1 mouse liver microsomes in presence of NADPH regenerating system measured up to 4 hrs by UPLC-MS analysis
AID1623666Intrinsic clearance in human microsomes2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID43400Effective dose against CCRF-CEM vcr 100 cells by using MTT assay1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID80743Evaluated for decrease in spontaneous frequency of atrial rate in isolated guinea pig atria1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID1246310Half life in mouse microsomes2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID294090Antiviral activity against Sindbis virus replication in BHK cells after 12 hrs by XTT assay2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Synthesis of dioxane-based antiviral agents and evaluation of their biological activities as inhibitors of Sindbis virus replication.
AID345310Intrinsic cytotoxicity against wild type mouse NIH/3T3 cells at 3 uM after 72 hrs by MTT assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
AID103940Inhibitory activity when combined with vincristine (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID680270TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Verapamil: 75 uM) in MDR1-expressing NIH-3T3 cells2004Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
AID656836Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 12 hrs post washout measured after 72 hrs by MTS assay (Rvb = 52012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID345314Reversal of human MDR1-mediated drug resistance assessed as ratio of daunorubicin IC50 for mouse NIH/3T3 cells expressing MDR1 to daunorubicin IC50 for wild type mouse NIH/3T3 cells at 10 uM after 72 hrs2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID230567Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vincristine (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID714428Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Dixon plot analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1781217Anti-MDR activity in human MCF7-DOX cells assessed as reversal of cell resistance to doxorubicin by measuring doxorubicin IC50 at 10 uM measured after 48 hrs by MTT assay (Rvb = 60.9 +/- 0.65 uM)
AID562102Chemosensitization of lumefantrine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID681120TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID106334Compound (1 uM) was evaluated for the inhibition of cell growth in MES-SA/DX5** cell line (over expresses Pgp and is for Doxorubicin resistant) in the presence of doxorubicin2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
AID1533100Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 25 uM preincubated for 1 hr followed by 2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID615733Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as Rho123 accumulation at 5 uM after 30 mins by FACScalibur flow cytometry relative to control2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1273408Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 16 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID230389Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with 5-fluorouracil (uM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1551047Effective permeability of compound at 25 mg/ml after 18 hrs by PAMPA-BBB assay
AID1357217Half life in rat liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID230550Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with cisplatin (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1903299Potentiation of vincristine-induced cytotoxicity against human KBV cells assessed as vincristine IC50 by measuring ratio IC50 as reversal fold at 5 uM for 72 hrs by MTT assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID1772564Apparent permeability of the compound across basolateral side to apical side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID95597Calcium antagonistic activity by measuring [3H]nitrendipine displacement at L-type [Ca2+] channel in rat cortex homogenate1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1386178Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring fold reduction in adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay relative to adriamycin alone2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID230557Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with taxol (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1056993Permeability of the compound at 100 mg/mL after 10 hrs by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
AID1168905Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
AID1485937Permeability of the compound in PBS/EtOH after 16 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1764402Unbound brain-to-plasma concentration ratio in P-gp knock out Sprague-Dawley rat2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID1631737Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1764401Ratio of drug concentration in brain to plasma of P-gp knock out Sprague-Dawley rat2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID105431Potency relative to progesterone in reversing of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1565849Inhibition of P-gp (unknown origin) expressed in MDCK-MDR1 cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID209805Inhibitory activity when combined with vincristine (nM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1215171Drug metabolism in Sprague-Dawley rat hepatic microsomes assessed as CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID389756Inhibition of NorA efflux pump in Staphylococcus aureus 1199 assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors.
AID1235705Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 2 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1833368Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/pcDNA3.1 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1602182Metabolic stability in mouse liver microsomes at 1 uM in presence of NADPH incubated for 15 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.
AID1168904Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
AID1704107Stimulation of human membrane P-gp ATPase activity at 0.5 mM using MgATP as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 120 mins by ADP-Glo luminescence assay relative to control2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1730211Permeability in PBS at pH 7.4 at 100 uM incubated for 5 hrs at room temperature by by UPLC/MS analysis based PAMPA method2021Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
Imidazopyridine-Based 5-HT
AID1589937Half life in rat hepatocytes2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
AID1566026Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as fold reduction in paclitaxel IC50 at 10 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID487886Binding affinity to P-gp at 0.05 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID1703908Permeability of the compound by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1129603Activation of ATPase activity of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction of reduction of ATP level at 100 uM after 2 hrs by luminescence/ATPlite assay2014European journal of medicinal chemistry, Apr-09, Volume: 76SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity.
AID379506Cytotoxicity against human KB31 cells after 48 hrs by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1273418Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 4 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1141748Myorelaxant activity in endothelium-free rat thoracic aorta assessed as inhibition of 30 mM of KCl-induced contraction in presence of 10 uM of KATP channel blocker glibenclamide2014European journal of medicinal chemistry, Jun-10, Volume: 80Influence of the alkylsulfonylamino substituent located at the 6-position of 2,2-dimethylchromans structurally related to cromakalim: from potassium channel openers to calcium entry blockers?
AID77934Left ventricular pressure of isolated guinea pig heart at dose 5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID513633Induction of autophagy in Atg deficient mouse MFF expressing EGFP-HDQ74 at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1411804Inhibition of Marburg virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-MarV-GP pseuotype virus infected HEK293 cells after 24 hrs post transfection by luciferase reporter gene assay2017MedChemComm, Dec-01, Volume: 8, Issue:12
N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.
AID1904191Inhibition of P-gp in human Caco-2 cells assessed as reduction in basal to apical transport of paclitaxel at 10 uM measured as apparent permeability after 180 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID664603Competitive inhibition of P-gp assessed as dose-dependent increase in P-gp-associated ATPase activity by Pgp-GloTM Assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Relationship between structure and P-glycoprotein inhibitory activity of dimeric peptides related to the Dmt-Tic pharmacophore.
AID1324013Permeability of the compound at 100 ug/ml after 16 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1298976Inhibition of human MDR1 transfected in multi-drug resistant mouse L5178Y cells assessed as fluorescence activity ratio at 20 uM incubated for 10 mins by rhodamine 123 accumulation assay2016Bioorganic & medicinal chemistry letters, Jun-15, Volume: 26, Issue:12
Identification of selenocompounds with promising properties to reverse cancer multidrug resistance.
AID1502912Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay rela2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1273480Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 64 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1228908Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vinblastine resistance measured as cell survival after 5 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1352558Inhibition of P-gp in human MCF7/ADR cells assessed as increase in doxorubicin accumulation in cells at 10 uM after 150 mins by fluorescence assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID401290Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 5.50 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1771036Half life in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID713773Binding affinity to human His10-tagged P-gp expressed in BHK cells assessed as induction of ATPase activity measured as inorganic phosphate release by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Thiorhodamines containing amide and thioamide functionality as inhibitors of the ATP-binding cassette drug transporter P-glycoprotein (ABCB1).
AID604024Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1530722Inhibition of P-gp-mediated Rhodamine-123 efflux in human KBV cells assessed as Rhodamine-123 accumulation preincubated for 2 hrs followed by Rhodamine-123 addition measured after 30 mins by flow cytometry2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID430564Reversal of ABCB1-mediated multidrug resistance assessed as ratio of colchicine IC50 for drug-resistant human KB-C2 cells to colchicine IC50 for human drug-sensitive KB-3-1 cells at 10 uM after 68 hrs by MTT assay2009Journal of natural products, Jul, Volume: 72, Issue:7
Sipholane triterpenoids: chemistry, reversal of ABCB1/P-glycoprotein-mediated multidrug resistance, and pharmacophore modeling.
AID1904189Inhibition of P-gp in human Caco-2 cells assessed as reduction in basal to apical transport of paclitaxel at 10 uM measured as apparent permeability after 90 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID371120Displacement of (-)-[3H]devapamil from L-type calcium channel in rabbit skeletal muscle cells2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile.
AID1517838Permeability of the compound in pH 7.4 PBS/EtOH at 25 ug/ml after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1239238Increase in doxorubicin accumulation in human MDA435/LCC6 cells at 2 uM after 2.5 hrs by spectrofluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID764760Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Design, synthesis and pharmacological evaluation of (E)-3,4-dihydroxy styryl sulfonamides derivatives as multifunctional neuroprotective agents against oxidative and inflammatory injury.
AID1486971Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1673440Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as inhibition of Rh123 efflux at 5 uM pretreated with Rh123 for 60 mins followed by incubation with compound for 90 mins by FACSCalibur flow cytometry anal2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID513627Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1129442Half life in human microsomes at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1504326Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition measured after 72 hrs2018European journal of medicinal chemistry, Jan-01, Volume: 143Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance.
AID368403Reversal of P-glycoprotein-mediated doxorubicin resistance in human doxorubicin-resistant K562 cells expressing Pgp assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of parent compound at 1 uM2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID695913Inhibition of norA in Staphylococcus aureus ATCC 29213 overexpressing norA assessed as fold reduction in ciprofloxacin MIC at 25 ug/mL by checkerboard assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID1733404Induction of cell cycle arrest in human KBV cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs in presence of 0.1 uM paclitaxel by PI/RNaseA staining based flow cytometric analysis (Rvb = 28.03 +/- 0.95%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID680522TP_TRANSPORTER: inhibition of Docetaxel transepithelial transport (basal to apical)(Docetaxel: 4 uM, Verapamil: 100 uM) in Caco-2 cells1994Biochemical pharmacology, Oct-07, Volume: 48, Issue:7
Polarized transport of docetaxel and vinblastine mediated by P-glycoprotein in human intestinal epithelial cell monolayers.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1386856Modulation of human ABCB1 expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 20 uM pretreated for 10 mins followed by rhodamine 123 addition and measured after 20 mins by flow cytometry (Rvb = 1.01 No_unit)2018Journal of natural products, 09-28, Volume: 81, Issue:9
Terpenoids from Euphorbia pedroi as Multidrug-Resistance Reversers.
AID127918Concentration causing local anesthetic activity in mice1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID1377587Inhibition of P-gp in human HCT116/VM46 cells assessed as potentiation of vinblastine-induced cytotoxicity at 1 uM by measuring fold reduction in vinblastine IC50 relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Natural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer.
AID562097Chemosensitization of primaquine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID377771Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 0.1 ug/mL after 2 hrs relative to control2005Journal of natural products, Apr, Volume: 68, Issue:4
Taxoids and abietanes from callus cultures of Taxus cuspidata.
AID1419460Inhibition of P-gp in human K562/DOX cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in doxorubicin IC50 at 3 uM incubated for 72 hrs by MTT assay relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy.
AID350522Induction of mouse cysteine-less MDR3 ATPase activity relative to basal activity2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
AID1739802Inhibition of human full-length ABCB1 expressed in Flp-In-293 cells assessed as reduction in calcein-AM uptake at 1.25 uM preincubated for 30 mins followed by calcein-AM addition and measured after 30 mins by fluorescence spectrometric assay relative to c2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1502789Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID537736Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1273445Modulation factor, ratio of amikacin MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of amikacin2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1464387Resistance index, ratio of mitoxantrone IC50 for human H460/MX20 cells to mitoxantrone IC50 for human H460 cells at 1 uM (Rvb = 28.66 No_unit)2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors.
AID1273394Anti-tubercular activity against Mycobacterium smegmatis MC2 155 ATCC 700084 after 3 days by microdilution method2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1352560Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Dixon plot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID289066Effect on calcein accumulation in MDR 2780AD cells at 25 ug/mL relative to control2007Journal of natural products, Jun, Volume: 70, Issue:6
Bioactive polyketides from Peperomia duclouxii.
AID1502725Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as increase in EtBr accumulation by measuring relative final fluorescence incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1382495Half life in human liver microsomes at 0.1 uM preincubated for 5 mins followed by NDAPH addition measured up to 60 mins by HPLC-MS/MS analysis2018European journal of medicinal chemistry, Mar-25, Volume: 148Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).
AID1502731Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1129444Half life in human microsomes at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1453097Effective permeability of the compound at 100 ug/ml incubated for 18 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
AID1350754Inhibition of recombinant human CYP3A4 in presence of NADPH generating system by fluorescence assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1526016Intrinsic clearance in mouse liver microsomes2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID1733385Reversal of Pgp-mediated multidrug resistance in human KBV cells assessed as fold change in vincristine IC50 at 10 uM after 72 hrs in presence of vincristine by MTT assay relative to control2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1504325Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring fold reduction in colchicine IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition measured after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance.
AID1502852Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID310898Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing maximal increase in nuclear concentration of pirarubicin relative to control2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors.
AID1683984Reversal of resistance to paclitaxel-induced cytotoxicity in HEK293 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb =1.93 +/- 0.06 nM)
AID1351584Ratio of EC50 for Wistar rat trachea tonus to EC50 for Wistar rat endothelium-denuded thoracic aorta ring2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID1585493Induction of phospholipidosis in human HepG2 cells assessed as increase in number of cellular lysosomes at 50 uM after 72 hrs by LYSO-ID Red and Hoechst 33342 staining based fluorescence microscopic method2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Optimization and preclinical evaluation of novel histamine H
AID1502711Antimycobacterial activity against Mycobacterium avium isolate MAV2 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502902Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 50 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1429985Inhibition of MDR1 in human COLO320/MDR-LRP cells assessed as rhodamine-123 accumulation measured as fluorescence activity ratio at 20 uM preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry (Rvb = 0.53 to 02017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line.
AID1239236Selectivity index, ratio of IC50 for mouse L929 cells to EC50 for reversal of P-gp-mediated paclitaxel resistance in human MDA435/LCC6MDR cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID18849Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1235696Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv using ethidium bromide as substrate assessed as relative final fluorescence at 1/2 MIC by real-time fluorometry2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID551248Intrinsic clearance in human microsome by LC-MS/MS analysis in presence of NADPH2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis.
AID1321565Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as fluorescence activity ratio at 22 uM preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID1833356Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID165540Inhibition of contraction in rabbit pulmonary artery, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID464024Growth inhibition in doxorubicin-resistant human K562 cells overexpressing Pgp at 3 uM after 72 hrs by MTT assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1155073Response modification index, ratio of IC50 for Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles in presence of drug to IC50 for Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles in2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1298979Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Jun-15, Volume: 26, Issue:12
Identification of selenocompounds with promising properties to reverse cancer multidrug resistance.
AID153402Inhibitory activity when combined with vinblastine (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID427804Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as viability after 2 hrs by MTT assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID1740405Half life in mouse microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID82675Effective concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which results in 50% of the cells being killed in the presence of particular cytotoxic drug.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin.
AID1548637Effective permeability of compound in PBS buffer at pH 7.4 at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.
AID1533611Effective permeability of the compound by PAMPA2019European journal of medicinal chemistry, Feb-01, Volume: 163Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory.
AID1273452Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 128 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1235704Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 4 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1174949Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1429866Effective permeability of the compound at pH 7.4 at 100 uM after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID1374472Half life in dog liver microsomes2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
AID717465Potentiation of paclitaxel-mediated cytotoxicity against human KBVIN cells assessed as reduction in paclitaxel IC50 at 10 uM after 72 hrs by SRB method relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity.
AID1283414Intrinsic cytotoxicity against mouse NIH/3T3 cells transfected with human MDR1 by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID1785083Inhibition of P-gp in paclitaxel-resistant human SW620/AD300 cells assessed as accumulation of paclitaxel incubated for 24 hrs by HPLC analysis
AID1750899Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay
AID1194717Solubility in pH 7.4 buffer after 18 hrs by UV spectroscopy based microSol assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Improving both aqueous solubility and anti-cancer activity by assessing progressive lead optimization libraries.
AID1502833Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502777Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 128 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID264304Ratio of rhodamine123 uptake in MDR1 transfected cells vs parental L5178Y cells at 3 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1,4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells.
AID1350746Inhibition of ABCB1 in human SW620/AD300 cells assessed as decrease in rhodamine 123 efflux up to 2 uM preincubated for 4 hrs followed by 30 mins incubation in Rho-123 containing medium and subsequent incubation in Rho-123 free medium up to 120 mins by fl2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1578508Stability in ICR/CD1 mouse hepatocytes assessed as half life at 1 uM measured upto 120 mins by LCMS analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1338186Selectivity index, ratio of IC50 for cytotoxicity against mouse L929 cells to EC50 for inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vinblastine cytotoxic IC50 by half2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID252860Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (10 uM) and Vinblastine (VNB)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID170812Effect (0.3 mg/kg, iv) on coronary reperfusion-induced arrhythmias was assessed in anesthetized rats.(Intervals of ventricular tachycardia (VT)+ventricular fibrillation (VF) within 600 s.1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1210071Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1371139Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA).
AID472447Antioxidant activity in HSMC assessed as protection from H2O2-induced toxicity at 50 uM pretreated for 2 hrs before H2O2 challenge measured after 1 hr by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
AID1596589Solubility of compound in PBS after 2 hrs by turbidity based absorbance analysis2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1750945Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as late apoptotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 17.9%)
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1129443Intrinsic clearance in human microsomes at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID681334TP_TRANSPORTER: transepithelial transport in Caco 2 cell2004Pharmaceutical research, May, Volume: 21, Issue:5
Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.
AID1683991Inhibition of ABCB1 in multidrug-resistant human KB-C2 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after
AID1312935Intrinsic clearance in human liver microsomes measured after 10 to 60 mins in absence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1419452Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by spectroflurometry2017European journal of medicinal chemistry, Feb-15, Volume: 127N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy.
AID1502708Antimycobacterial activity against Mycobacterium avium 104 mc'2 4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID150736Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID656820Inhibition of Pgp-mediated rhodamine 123 efflux in human K562/A02 cells assessed as intracellular rhodamine 123 accumulation preincubated for 1 hr prior rhodamine 123 addition measured after 30 mins by flow cytometry relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID1517889Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1215168Cmax in Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID313271Lipophilicity, log P of the compound2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells.
AID1348874Inhibition of MDR in human MCF7/ADR cells assessed as potentiation of adriamycin-induced antiproliferative activity by measuring fold reduction in adriamycin IC50 at 10 uM after 48 hrs by MTT assay
AID1502774Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID681847TP_TRANSPORTER: inhibition of Digoxin uptake (Digoxin: 0.05 uM, Verapamil: 1000 uM) in Oatp2-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID407205Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
AID1397459Half life in rat liver microsomes2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors.
AID1502838Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1565853Inhibition of BCRP (unknown origin) expressed in MDCK cells assessed as increase in Hoechst 33342 accumulation incubated for 30 mins by Hoechst 33342 dye based fluorescence assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID1772565Efflux ratio of apparent permeability in human Caco-2 cells2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID427713Increase in doxorubicin accumulation in doxorubicin-co-incubated human 2008/P cells at 3 uM after 120 mins by spectrofluorimetry2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID536851Half life in human liver microsomes at 3 uM by LC-MS/MS analysis2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.
AID1502910Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay relati2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID379510Reversal of P-glycoprotein-mediated multidrug resistance assessed as ratio of adriamycin IC50 for drug-resistant human KB-V1 cells to adriamycin IC50 for human drug-sensitive KB-3-1 cells at 10 uM after 48 hrs by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1309710Metabolic stability in mouse liver S9 fraction assessed as compound remaining after 30 mins2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Discovery, Optimization, and Biological Evaluation of Sulfonamidoacetamides as an Inducer of Axon Regeneration.
AID1476985Effective permeability of compound at 200 uM after 17 hrs by PAMPA-BBB assay2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.
AID283796Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 25 ug/mL relative to control2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID1155072Response modification index, ratio of IC50 for Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele in presence of drug to IC50 for Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele in absence of 800 nM of drug2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1215130Total intrinsic clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestinal microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil per gram of intestinal mucosa by HPLC analysis in presence2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID80191Inhibitory activity on atrial contractility in isolated Guinea pig right atrea at 0.01 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1180207Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of phenylephrine-induced contraction2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1164949Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
AID1174967Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs followed by adriamycin treatment 12 hrs post compound washout measured after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1673432Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as fold reduction in doxorubicin IC50 at 5 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID588999Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MDR32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1239237Solubility of the compound in phosphate buffer at pH 7.4 by capillary electrophoresis system2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID1566024Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of irinotecan-induced cytotoxicity by measuring irinotecan IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 49.2 +/- 0.46 nM)2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID1738697Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as increase in intracellular doxorubicin accumulation at 2.5 uM incubated for 1 hr in presence of 3 uM doxorubicin by flow cytometric analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID193029Antihypertensive activity as percent average (over 24 hr) decrease in blood pressure at 135 umol/kg po (~40-50 mg/kg) in 5 spontaneously hypertensive rats (SHR)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID376933Reversal of multidrug resistance in human AD10 cells assessed as increase in calcein accumulation at 0.25 ug/ml relative to control2006Journal of natural products, May, Volume: 69, Issue:5
Bioactive secolignans from Peperomia dindygulensis.
AID1381447Apparent permeability from apical to basolateral side in MDCK cells2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
AID1215187Half life in Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID76245Potency expressed as IC50 for the vasorelaxant activity.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID1683975Inhibition of ABCB1 (unknown origin) expressed in HEK293 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID389397Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected mouse L5178 cells assessed as fluorescence activity ratio at 10 ug/ml by rhodamine-123 exclusion test2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic interaction between p-glycoprotein modulators and epirubicine on resistant cancer cells.
AID1526015Half life in mouse liver microsomes2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases.
AID1273402Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 8 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1183278Permeability of the compound by PAMPA2014European journal of medicinal chemistry, Sep-12, Volume: 84Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1918143Inhibition of P-gp in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reversal fold ratio at 1 uM in presence of 10 nM to 30 uM doxorubicin incubated for 72 hrs by MTT assay
AID379725Reversal of multidrug resistance in human 2780AD cells assessed as accumulation of calcein at 0.25 ug/mL after 15 mins by fluorescence technique relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii.
AID1215179Intrinsic clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat hepatic microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1530089Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring cell survival at 10 uM after 72 hrs by MTT assay (Rvb = 104 +/- 8%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1750904Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 48 hrs by MTT assay relative to control
AID1129439Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID562100Chemosensitization of desethylamodiaquin against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1299183Inhibition of human MDR1 expressed in mouse L5178 cells assessed as rhodamine-123 accumulation measured as fluorescence activity ratio at 20 uM after 20 mins by flow cytometry relative to control2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies.
AID755311Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 0.5 uM after 2 hrs by microplate fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1296093Inhibition of multidrug resistance efflux pump in Mycobacterium aurum ATCC 23366 assessed as inhibition of ethidium bromide efflux by measuring relative fluorescence units for ethidium bromide accumulation at 125 ug/ml incubated for 60 mins by fluorimetri2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Design and Synthesis of 1-((1,5-Bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethylocta-2,6-dienyl)ethane-1,2-diamine (SQ109) Pyrrole Hybrid Derivatives: Discovery of Potent Antitubercul
AID682516Induction of ATPase activity of human His10-tagged P-gp expressed in BHK cells assessed as inorganic phosphate release after 30 mins by Michaelis-Menten analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Chalcogenopyrylium compounds as modulators of the ATP-binding cassette transporters P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1).
AID1207717Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID350525Induction of human histidine10-tagged MDR1 ATPase activity expressed in BHK cells relative to basal activity2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
AID1155077Inhibition of CTR in Plasmodium falciparum C67G8 expressing chloroquine-resistance-conferring pfcrt alleles assessed as increase of accumulation of [3H]-chloroquine level at 1 uM after 1 hr relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1704101Reversal of multidrug resistance activity in P-gp overexpressing human KB-VIN cells assessed as potentiation of VCR-induced cytotoxicity by measuring VCR IC50 at 10 uM incubated for 48 hrs in presence of VCR by MTT assay (Rvb = 666.3 nM)2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1207722Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID331354Antitumor activity against human K562/A02 cells xenografted in nude mouse at 8 mg/kg2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID656826Growth inhibition of human K562 cells at 10 uM after 72 hrs by MTS assay2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID1228911Selectivity index, ratio of IC50 for mouse L292 cells to EC50 for modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1275770Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as potentiation of choloroquine induced antimalarial activity by measuring ratio of chloroquine IC50 in presence to absence of compound at 0.5 uM2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID1353450Inhibition of P-gp in human K562/Dox cells assessed as reduction in Rh-123 efflux by measuring mean fluorescence intensity at 3 uM preincubated for 15 mins followed by Rh-123 addition for 30 mins and subsequent replacement in Rh-123 free medium measured a2018European journal of medicinal chemistry, Mar-10, Volume: 147Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents.
AID81855Inhibitory concentration of vinblastine against the MDR resistant cell line HCT116/VM46 in the presence of 1 mM of the compound2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID379772Reversal of P-glycoprotein-mediated multidrug resistance assessed as ratio of vinblastine IC50 for drug-resistant human KB-V1 cells to vinblastine IC50 for human drug-sensitive KB-3-1 cells at 10 uM after 48 hrs by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1225494Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as daunomycin accumulation at 10 uM after 30 mins by flow cytometry (Rvb = 13.2 +/- 1.1%)2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1502767Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1215174Drug metabolism in Sprague-Dawley rat intestinal microsomes assessed as CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1215183Cmax in Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1565857Ratio of apparent permeability across apical side to basolateral side over basolateral side to apical side in human Caco2 cells supplemented with fresh medium containing compound every 48 hrs for 21 days by UV spectroscopic method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
AID1502824Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to az2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1888878Inhibition of NorA in Staphylococcus aureus 1199B assessed as accumulation of norfloxacin at 50 ug/ml by measuring fluorescence intensity measured at 5 mins interval for 40 mins by fluorescence spectrophotometry2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1833350Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620 cells assessed as reversal fold at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to paclitaxel
AID1906056Reversal fold, ratio of ADR IC50 for reversal of multidrug resistance in human MCF7/ADR cells over IC50 of ADR in presence of test compound2022European journal of medicinal chemistry, May-05, Volume: 235Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells.
AID1321569Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as fluorescence activity ratio preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID1878311Inhibition of P-gp mediated doxorubicin resistance in human SW620/AD300 cells overexpressing P-gp measured after 48 hrs by MTT assay2022Journal of natural products, 02-25, Volume: 85, Issue:2
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived
AID1180211Inhibition of L-type calcium channel in endothelium-intact Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1228906Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay relative to PTX alone treated cell2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID1893724Metabolic stability in human liver S9 fraction assessed as half life at 1 micromol/L in presence of NADPH measured upto 24 hrs by LC-MS/MS analysis
AID1603227Permeability of the compound assessed as molar fraction in acceptor well at 0.5 mM measured after 16 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1163835Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID368391Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID492328Inhibition of BCRP expressed in human EPG-257RNOV cells at 1 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID1502823Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to az2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1878313Fold resistance, ratio of IC50 for human SW620/AD300 cells overexpressing P-gp by measuring doxorubicin IC50 to IC50 for doxorubicin sensitive human SW-620 cells by measuring doxorubicin IC502022Journal of natural products, 02-25, Volume: 85, Issue:2
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived
AID1502791Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to er2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID165537Inhibition of [Ca2+] uptake in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1190827Cytotoxicity against human KB/VCR cells assessed as vincristine IC50 at 25 uM after 72 hrs by SRB method2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Multidrug resistance-reversal effects of resin glycosides from Dichondra repens.
AID562108Chemosensitization of benzonaphthyridine pyronaridine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1449629Inhibition of BSEP in Sprague-Dawley rat canalicular membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID217926Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID714420Reversal of P-gp-mediated mitoxantrone-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1502841Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ciprofl2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1426677Effect on rhodamine123 accumulation in human K562 cells at 0.33 to 10 uM measured after 1 hr by flow cytometry2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Potent Inhibition of Nitric Oxide-Releasing Bifendate Derivatives against Drug-Resistant K562/A02 Cells in Vitro and in Vivo.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1493790Aqueous solubility in PBS after 2 hrs2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1904126Cytotoxicity against human K562 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID193032Antihypertensive activity as percent maximum (0-6 hr) decrease in blood pressure at 135 umol/kg po (~40-50 mg/kg) in 5 spontaneously hypertensive rats (SHR)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID194572Change in heart rate was measured at mg/kg dose(iv) in anesthetized rats1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1174945Resistance factor, ratio of adriamycin IC50 for human K562/A02 cells over-expressing Pgp to adriamycin IC50 for human K562/A02 cells over-expressing Pgp in presence of 5 uM compound2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID313272Inhibition of P-glycoprotein in MDR human KBChR-8-5 cells assessed as uptake of vinblastin relative to control2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells.
AID331368Toxicity in Sprague-Dawley rat assessed as ventricular sustained tachycardia by measuring aconitine nitrate level at 2 mg.kg, iv by echocardiography2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID611696Inhibition of MDR1-mediated rhodamine 123 uptake expressed in mouse L5178Y cells transfected with pHa MDR1/A assessed as fluorescence activity ratio at 10 ug/mL by flow cytometry relative to untreated control2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Jatrophane diterpenes from Euphorbia esula as antiproliferative agents and potent chemosensitizers to overcome multidrug resistance.
AID669859Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by fluorescence microscopic analysis2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents.
AID1758183Antiproliferative activity against human MCF7 cells assessed as inhibition rate at 10 uM incubated for 48 hrs by CCK-8 assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
AID1813141Inhibition of P-gp in human LCC6MDR cells assessed as fold increase in intracellular rhodamine 123 accumulation at 2 uM incubated for 150 mins in presence of rhodamine 123 by fluorescence microscopy relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID427724Reversal of MRP1-mediated doxorubicin resistance in doxorubicin co-incubated human 2008/MRP1 cells assessed as increase in doxorubicin accumulation after 120 mins by spectrofluorimetry relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1502893Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1064667Inhibition of p-glycoprotein (unknown origin) overexpressed in human KBV20C cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM incubated for 1 hr prior to vincristine challenge measured after 4 days by MTT assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication.
AID714425Increase in human P-gp ATPase activity at 200 uM by luciferase assay relative to basal level2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1283423Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in vinblastine IC50 at 10 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID717464Potentiation of vincristine-mediated cytotoxicity against human KBVIN cells assessed as reduction in vincristine IC50 at 10 uM after 72 hrs by SRB method relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity.
AID1368939Inhibition of MRP1 (unknown origin) expressed in HEK293FlpIN cells assessed as reduction in calcein-AM efflux at 35 uM incubated for 30 mins by flow cytometric analysis relative to control2018Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
Monoterpene indole alkaloid azine derivatives as MDR reversal agents.
AID1502755Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID368392Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1273454Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 256 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1307806Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension at 10'-5 M2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1568822Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1235733Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 32 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1273457Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 64 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1235699Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID351908Chemosensitizing activity as 500nM potentiation of quinine effect after 72 hrs against chloroquine-resistant transporter 106/1'76I mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1673435Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1459764Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID455727Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as mean fluorescence intensity of rhodamine-123 uptake after 10 mins by flow cytometry2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID47004Compound (1 uM) was evaluated for the inhibition of cell growth in MCF-7/ADR* cell line (over expresses Pgp and is for Doxorubicin resistant) in the presence of vinblastine2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
AID1235700Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID469403Permeability across PAMPA membrane 2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID672543Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.
AID683267Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as vincristine-induced cytotoxicity at 10 uM after 72 hrs by SRB assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID664486Intrinsic clearance in human liver microsomes assessed per mg of protein2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
AID1514557Cytotoxicity against human A2780/TAX cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID154133Multidrug-resistant reversal activity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the presence of 10 nM vincristine1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
AID1235768Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 4 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID76005Compound was tested in vitro for chronotropic activity on isolated atria preparations of guinea pig at 10E-6 M concentration1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Verapamil analogues with restricted molecular flexibility.
AID1459774Inhibition of P-gp in human KBVIN cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1708807Permeability of compound in PBS/EtOH buffer (70:30) at 25 ug/ml incubated for 16 hrs by UV plate reader based PAMPA-BBB2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1502864Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID74046Negative chronotropic activity was calculated from log concentration/response curves1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID656825Growth inhibition of human K562/A02 cells at 10 uM after 72 hrs by MTS assay2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID395103Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.
AID143482Inhibitory activity when combined with taxol (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1514561Potentiation of cisplatin-induced cytotoxicity against human A2780/CDDP cells assessed as cisplatin IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 43.11 nM)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID1334754Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID76670[Ca2+] antagonistic activity on contraction in guinea pig papillary1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1374473Half life in human liver microsomes2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
AID142787Ability to dissociate radioligand [3H]NMS from muscarinic acetylcholine receptor M2 of porcine heart2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.
AID1491366Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID619532Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for daunomycin-induced cytotoxicity in absence of drug to IC50 for daunomycin-induced cytotoxicity in presence of 1 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID75204Percent inhibition of [Ca2+] induced contraction on K+ depolarized guinea pig aortic strips at 5-10e4 M concentration1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Verapamil analogues with restricted molecular flexibility.
AID48348[Ca2+] antagonistic activity on [Ca2+] current in cat ventricular trabeculae1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID43874The percentage uptake of [3H]daunomycin in resistant CCRF-CEM vcr 100 cells to sensitive CCRF-CEM cells in presence of the compound.1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
AID680500TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical)(Doxorubicin: 3 uM, Verapamil: 20 uM) in MDR1-expressing LLC-PK1 cells2000European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Sep, Volume: 11, Issue:3
Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines.
AID1168902Modulation of P-gp mediated drug efflux in human MES-SA cells assessed as accumulation of rhodamine-123 incubated for 15 mins prior to rhodamine-123 addition measured after 1 hr by fluorescence analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
AID1502754Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1557184Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID762417Antimicrobial activity against Mycobacterium smegmatis MC2 155 ATCC 700084 after 72 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID94173Percent of cell viability remaining after incubating the cells with the modulator alone1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1174964Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs prior to adriamycin treatment measured after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1833383Inhibition of human CYP3A4 at 3.3 uM preincubated with compound followed by substrate and NADP addition by fluorescence assay
AID80295Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.003 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID1460714Reversal of multidrug resistance in human MCF7/DX cells assessed as potentiation doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 level at 5 uM incubated for 48 hrs by MTT assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
Isolation, Structure Elucidation, and Absolute Configuration of Syncarpic Acid-Conjugated Terpenoids from Rhodomyrtus tomentosa.
AID1604716Stability in human plasma assessed as half life at 5 uM at 37 degC measured up to 250 mins by LC-MS analysis2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
AID230143The MRP1 antagonism score is the percentage of MCF-7/VP cells surviving in the absence of vincristine to that of in the presence of vincristine.2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists.
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1509218Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 20 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID427814Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as inhibition of calcium uptake2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID307746Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 0.2 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID368383Intrinsic cytotoxicity against human doxorubicin-sensitive K562 cells at 3 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID310120Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID1418889Inhibition of ABCB1 (unknown origin) expressed in human HEK293T/ABCB1 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 4 uM after 72 hrs by MTT assay relative to cisplatin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1324014Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1904131Reversal of BCRP-mediated multidrug resistance in dog MDCK-II-BCRP cells assessed as potentiation of mitoxantrone-induced cytotoxicity at 5 uM by measuring mitoxantrone IC50 after 48 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID243043Ratio of maximum velocity to that of Km value was determined by P-glycoprotein2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.
AID1623664Intrinsic clearance in mouse microsomes2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID681144TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells2003The Journal of pharmacology and experimental therapeutics, Apr, Volume: 305, Issue:1
Inhibition of P-glycoprotein by newer antidepressants.
AID1435956Intrinsic clearance in human liver microsomes after 10 to 60 mins in absence of NADPH by LC/MS/MS analysis2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID562107Chemosensitization of methotrexate against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID606417Vasorelaxant activity in Sprague-Dawley rat langendorff perfused thoracic aorta assessed as inhibition of phenylephrine-induced vasoconstriction at 10'-6 M relative to control2011Journal of natural products, May-27, Volume: 74, Issue:5
Lathyrane diterpenoids from the roots of Euphorbia micractina and their biological activities.
AID307747Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 2 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID340720Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Role of the ABC transporter PRP1 (ABCC7) in pentamidine resistance in Leishmania amastigotes.
AID1336731Permeability of compound at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID3216Relative activity on the cellular accumulation of vincristine in multidrug-resistant (MDR) human ovarian cancer 2780AD cells1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
Highly increased cellular accumulation of vincristine, a useful hydrophobic antitumor-drug, in multidrug-resistant solid cancer cells induced by a simply reduced taxinine.
AID1459755Potentiation of paclitaxel-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID681611TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells2003Pharmaceutical research, Feb, Volume: 20, Issue:2
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.
AID60874Percent inhibition of calcium-dependent potassium-polarized smooth muscle contraction in canine trachea1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID1704100Reversal of multidrug resistance activity in P-gp overexpressing human A2780T cells assessed as potentiation of PTX-induced cytotoxicity by measuring reversal ratio at 10 uM incubated for 48 hrs in presence of paclitaxel by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID80296Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.01 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID154221Percent of cell viability of P388/VCR-20 murine leukemia cells remaining after inoculation with the modulator alone1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID1502898Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 12.5 ug/ml2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1878312Inhibition of P-gp mediated doxorubicin resistance in human SW620/AD300 cells overexpressing P-gp in presence of doxorubicin measured after 52 hrs by MTT assay2022Journal of natural products, 02-25, Volume: 85, Issue:2
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived
AID313274Displacement of [3H]azidopine from human P-glycoprotein in KB-Vi cells2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells.
AID486955Inhibition of ABCB1 efflux pump-mediated rhodamine 123 uptake expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 1 uM2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators.
AID664602Inhibition of P-gp-mediated rhodamine 123 efflux in doxorubicin-resistant human K652 cells at 100 uM treated for 1 hr measured after washout by FACS flow cytometry relative to control2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Relationship between structure and P-glycoprotein inhibitory activity of dimeric peptides related to the Dmt-Tic pharmacophore.
AID233362modulation factor: IC50 (uM)1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships.
AID1426678Effect on P-gp ATPase activity in human K562/A02 cell membranes assessed as remaining ATP level by measuring relative light units at 200 uM in presence of MgATP measured after 40 mins by luminescence based P-gp-Glo assay (Rvb = 216508 +/- 7426 RLU)2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Potent Inhibition of Nitric Oxide-Releasing Bifendate Derivatives against Drug-Resistant K562/A02 Cells in Vitro and in Vivo.
AID1486973Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID102844Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, FL-1at 5 ug/mL2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery and biological evaluation of a new family of potent modulators of multidrug resistance: reversal of multidrug resistance of mouse lymphoma cells by new natural jatrophane diterpenoids isolated from Euphorbia species.
AID1215180Intrinsic clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat hepatic microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil per gram of liver by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1338178Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay relative to paclitaxel alone2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1750928Inhibition of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as Adriamycin accumulation pretreated 1 hr followed by treated with adriamycin measured after 180 mins by flow cytometry
AID1459747Inhibition of ABCB1 (unknown origin) expressed in Flp-In-293 cells assessed as increase in calcein-AM uptake at 10 uM preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by fluorescence spectrometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1481888Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 5 uM preincubated for 24 hrs followed by compound washout for 6 hrs and subsequent doxorubicin addition measured after 48 hrs by MTT assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID1740452Intrinsic clearance in mouse hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID171866Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR), at 3-6h after 30 mg/kg oral administration1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID1235721Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 2 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID78278Effect on force of atrial contractions induced by PTX-B in guinea pig1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid A new class of A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid pu
AID1365724Intrinsic clearance in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID619540Intrinsic toxicity in wild type mouse NIH/3T3 cells assessed as cell growth at 10 uM relative to control2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID1215136Decrease of CYP3A2 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat duodenum by Western blot analysis relative to wild type rat2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1459769Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID714421Reversal of P-gp-mediated daunorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1180201Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 60 mM K+-induced contraction at 100 uM relative to untreated control2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID105424Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1683988Inhibition of ABCB1 in multidrug-resistant human KB-C2 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and me
AID368399Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 1.6 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID609330Reversal of chloroquine-resistance in Plasmodium chabaudi infected in mouse at 20 mg/kg, po coadministered with chloroquine 3 mg/kg, iv administered for 3 consecutive days measured on day 42011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi.
AID159174Percent reversal against Plasmodium falciparum W2 at 1 uM DEEA2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID680499TP_TRANSPORTER: inhibition of Fluorescein-Colchicine transport (FL-Colchicin: 0.3 uM, Verapamil: 10 uM) in membranes from CEM/VLB100 cells1999Analytical biochemistry, Mar-15, Volume: 268, Issue:2
A continuous fluorescence assay for the study of P-glycoprotein-mediated drug efflux using inside-out membrane vesicles.
AID1174956Resistance factor, ratio of adriamycin IC50 for human K562/A02 cells over-expressing Pgp to adriamycin IC50 for human K562/A02 cells over-expressing Pgp in presence of 2.5 uM compound2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1273419Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 8 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID682288TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, Verapamil: 500 uM) in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID1418880Potentiation of cisplatin-induced cytotoxicity in human HEK293T/NC cells assessed as fold reduction in cisplatin IC50 at 4 uM after 72 hrs by MTT assay relative to cisplatin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1062337Induction of doxorubicin accumulation in human MDA435/LCC6 cells at 1 uM after 150 mins by spectrofluorometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID492327Inhibition of BCRP expressed in human EPG-257RNOV cells at 0.1 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID1352065Inhibition of P-gp-mediated drug resistance in human K562/A02 cells assessed as reduction in adriamycin IC50 at 2 uM after 72 hrs by MTS assay relative to adriamycin alone2018European journal of medicinal chemistry, Feb-10, Volume: 145Synthesis and biological evaluation of bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potential P-glycoprotein and tumor metastasis inhibitors.
AID551807Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for 50% increase in nuclear concentration of pirarubicin by fluorescence assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Inhibition of P-glycoprotein-mediated Multidrug Resistance (MDR) by N,N-bis(cyclohexanol)amine aryl esters: further restriction of molecular flexibility maintains high potency and efficacy.
AID121700Ratio of survival time of mice treated with VCR (0.25 mg/kg ip)+modulator given at the optimal dose of 100 mg/kg po/survival time of mice treated with VCR alone.1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID283000Reversal of P-gp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as increase in nuclear pirarubicin concentration2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Exploratory chemistry toward the identification of a new class of multidrug resistance reverters inspired by pervilleine and verapamil models.
AID318686Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of vincristine by MTS assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis of curcumin mimics with multidrug resistance reversal activities.
AID1502710Antimycobacterial activity against Mycobacterium avium isolate MAV1 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID680007TP_TRANSPORTER: inhibition of Fexofenadine uptake (Fexofenadine: 2 uM, Verapamil: 100 uM) in Xenopus laevis oocytes1999Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 27, Issue:8
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
AID1129448Half life in mouse microsomes at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1628220Inhibition of P-gp in human A549/CDDP cells assessed as accumulation of rhodamine 123 at 1.2 uM by flow cytometry2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer.
AID354662Inhibition of p-glycoprotein expressing human MCF7 cells assessed as [3H]vinblastine accumulation1996Journal of natural products, Jun, Volume: 59, Issue:6
Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A.
AID679127TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells2000The Journal of pharmacology and experimental therapeutics, May, Volume: 293, Issue:2
Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.
AID288564Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay2007Journal of natural products, Jun, Volume: 70, Issue:6
Reversal of P-glycoprotein-mediated multidrug resistance by sipholane triterpenoids.
AID1155066Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation at 100 uM after 1 to 2 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1243598Inhibition of human ABCB1 expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 20 uM incubated for 10 mins by flow cytometry based rhodamine-123 accumulation assay (Rvb = 0.78 No_unit)2015Journal of natural products, Sep-25, Volume: 78, Issue:9
Epoxylathyrol Derivatives: Modulation of ABCB1-Mediated Multidrug Resistance in Human Colon Adenocarcinoma and Mouse T-Lymphoma Cells.
AID1458340Inhibition of efflux pump in wild type Mycobacterium tuberculosis H37Rv assessed as increase in accumulation of ethidium bromide by measuring relative final fluorescence index at 18.5 uM measured every second for 60 mins in absence of glucose by real time2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery.
AID67781Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.01999Bioorganic & medicinal chemistry letters, Feb-22, Volume: 9, Issue:4
Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives.
AID1888850Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of norfloxacin-induced antibacterial activity by measuring Norfloxacin MIC at sub MIC relative to norfloxacin MIC alone2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1275769Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as potentiation of choloroquine induced antimalarial activity by measuring ratio of chloroquine IC50 in presence to absence of compound at 0.8 uM2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID1365650Permeability of the compound at pH 7.4 by BBB-PAMPA2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease.
AID455723Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as fluorescence activity ratio at 22 uM after 10 mins by rhodamine-123 exclusion test2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID1418859Potentiation of doxorubicin-induced cytotoxicity in human SW620 cells assessed as fold reduction in doxorubicin IC50 at 4 uM after 72 hrs by MTT assay relative to doxorubicin alone2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1179311Inhibition of multidrug resistance efflux pump Rv1258c in Mycobacterium tuberculosis H37Rv assessed as potentiation of rifampicin-induced antimycobacterial activity by MABA method based Chequerboard synergy assay2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
AID90145To estimate the extent of resistance conferred by Pgp, the ratio of IC50 in MDA-435/LCC6-MDR1 and MDA-435/LCC6 cells (relative resistance of Pgp-positive cells) was used2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID80742Evaluated for decrease in maximal driving frequency in isolated guinea pig atria1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID1338181Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of doxorubicin cytotoxic IC50 by half after 5 days by Cell Titer 96 Aqueous assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1502836Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1785063Reversal of resistance to colchicine-induced cytotoxicity in human SW620/AD300 cells assessed as reduction in colchicine IC50 at 2 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay
AID1533102Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 6.25 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1446767Half life in human liver microsomes in absence of NADPH by LC-MS/MS method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1903293Potentiation of cisplatin-induced cytotoxicity against human KBV cells assessed as cisplatin IC50 at 5 uM for 72 hrs by MTT assay (Rvb = 6.28 +/- 1.23 nM )2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID190398Antihypertensive activity as percent average (0-24 hr) decrease in blood pressure at 45 umol/kg po (~22 mg/kg) in 4 spontaneously hypertensive rats (SHR)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1218867Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID578761Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).
AID695903Inhibition of Staphylococcus aureus SA-1199B NorA expressed in Escherichia coli DH10B assessed as inhibition of Hoechst 33342 dye efflux at 2 ug/ml by spectrofluorometric analysis in presence of 50 uM Mg2+2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID1514564Reversal ratio of IC50 for cisplatin-induced cytotoxicity against human A2780/CDDP cells in absence of compound to IC50 for cisplatin-induced cytotoxicity against human A2780/CDDP cells in presence of compound2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Seco-4-methyl-DCK derivatives as potent chemosensitizers.
AID310121Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID237331cLogD was determined2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
AID630754Reversal of human MDR1-mediated rhodamine 123 uptake in mouse L5178Y cells assessed as fluorescence activity ratio at 1 mM by flow cytometry relative to non p-gp expressing parental cell line2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Discovery of pyridine-2-ones as novel class of multidrug resistance (MDR) modulators: first structure-activity relationships.
AID1235752Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 4 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1502907Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay relati2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1904127Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID1427562Metabolic stability in rat liver microsomes assessed as metabolic rate measured after 30 mins in presence of NADPH2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID1502906Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay relative to e2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID464026Growth inhibition in human K562 cells at 3 uM after 72 hrs by MTT assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1498593Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation at 10 uM after 2 hrs by flow cytometry2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
The inhibitory effect of kokusaginine on the growth of human breast cancer cells and MDR-resistant cells is mediated by the inhibition of tubulin assembly.
AID666856Reversal of p-glycoprotein-mediated drug resistant in human LCC-6/MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM after 5 days by MTS assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells.
AID1809045Apparent permeability of the compound at 50 uM by PAMPA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.
AID1785054Reversal of resistance to paclitaxel-induced cytotoxicity in paclitaxel-resistant human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 2 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1673428Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 5 uM preincubated for 24 hrs followed by compound washout and 6 hrs la2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID562096Chemosensitization of chloroquine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID656834Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout before addition of adriamycin measured after 72 hrs by MTS assay (Rvb = 33.59 uM)2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID726434Inhibition of human MDR1 expressed in mouse L5178Y cells assessed as reduction of rhodamine-123 uptake by measuring fluorescence activity ratio at 10 uM preincubated for 10 mins measured after 40 mins relative to control2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Development of small-molecule P-gp inhibitors of the N-benzyl 1,4-dihydropyridine type: novel aspects in SAR and bioanalytical evaluation of multidrug resistance (MDR) reversal properties.
AID330502Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
AID472446Antioxidant activity in CHO cells assessed as protection from H2O2-induced toxicity at 50 uM pretreated for 2 hrs before H2O2 challenge measured after 1 hr by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
AID1429864Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-GI assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
AID696917Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 40 uM by fluorescence assay2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID229315Ratio of IC50 of cytotoxicity to the IC50 of MDR- reversal for P388/VMDRC.04 cells1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
AID1427527Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1301015Inhibition of human P-gp expressed in MDCK2-MDR1 cells assessed as reduction in calcien-AM efflux at 8 uM incubated for 20 mins by fluorimetry relative to control2016European journal of medicinal chemistry, Jul-19, Volume: 1172-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
AID1702158Clearance in human liver pooled microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1733383Reversal of Pgp-mediated multidrug resistance in human KBV cells assessed as fold change in paclitaxel IC50 at 10 uM after 72 hrs in presence of paclitaxel by MTT assay relative to control2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1169854Intrinsic clearance in human liver microsomes at 1 uM after 30 mins in presence of NADPH2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Structure-guided development of deoxycytidine kinase inhibitors with nanomolar affinity and improved metabolic stability.
AID1168390Potentiation of 0.6 uM doxorubicin-induced cytotoxicity in human HL60/MDR cells assessed as viable cells at 25 uM after 48 hrs by WST assay relative to control2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition.
AID1386859Modulation of ABCB1 (unknown origin) expressed in human COLO320 cells co-expressing LRP assessed as fluorescence activity ratio at 20 uM pretreated for 10 mins followed by rhodamine 123 addition and measured after 20 mins by flow cytometry (Rvb = 0.79 No_2018Journal of natural products, 09-28, Volume: 81, Issue:9
Terpenoids from Euphorbia pedroi as Multidrug-Resistance Reversers.
AID1365718Half life in human liver S9 microsomes at 1 uM in absence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID379472Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay1999Journal of natural products, Apr, Volume: 62, Issue:4
Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii.
AID1696657Inhibition of human ABCB1 in expressed in multidrug resistant mouse L5178Y cells assessed as fluorescence activity ratio at 20 uM by rhodamine 123 retention assay relative to parental L5178Y cells2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
AID1439234Inhibition of human ABCB1 expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 20 uM pretreated for 10 mins followed by rhodamine-123 addition after 20 mins by flow cytometry2017European journal of medicinal chemistry, Mar-10, Volume: 128Dregamine and tabernaemontanine derivatives as ABCB1 modulators on resistant cancer cells.
AID1207724Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID101593Inhibitory activity when combined with cisplatin (uM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1288624Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID1215161AUC (0 to 300 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID401284Displacement of N-(p-azido-[3-125I]salicyl)-N'-beta-aminoethylvindesine from P-glycoprotein at 12.4 uM1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID230564Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vincristine (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1315280Potentiation of vinblastin-induced cytotoxicity against human CEM cells at 5 uM after 72 hrs by Alamar blue assay relative to control2016Journal of natural products, 05-27, Volume: 79, Issue:5
Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis.
AID1464385Resistance index, ratio of mitoxantrone IC50 for human H460/MX20 cells to mitoxantrone IC50 for human H460 cells at 10 uM (Rvb = 28.66 No_unit)2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors.
AID25870Tested for the dissociation constant of the compound1980Journal of medicinal chemistry, May, Volume: 23, Issue:5
Accumulation of drugs by guinea pig isolated atria. Quantitative correlations.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID728951Myorelaxant activity in albino rat aorta rings assessed as relaxation of 80 mM KCl-induced contraction of aorta rings2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action.
AID464022Inhibition of P-glycoprotein-mediated in absence of test compound multidrug resistance in human doxorubicin-resistant K562 cells assessed as doxorubicin cytotoxic IC50 to doxorubicin cytotoxic IC50 in presence of test compound at 3 uM after 72 hrs by MTT 2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.
AID1350735Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 2 uM after 72 hrs by MTT assay relative to paclitaxel alone2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1374471Half life in rat liver microsomes2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
AID1180202Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1833379Inhibition of ABCB1-mediated 3H-[PTX] efflux in human SW-620/AD300 cells assessed as accumulation of intracellular 3H-[PTX] at 4 uM preincubated for 4 hrs followed by 3H-[PTX] addition and measured after 2 hrs by liquid scintillation analysis
AID230387Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with 5-Fluorouracil (uM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1517902Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1141747Myorelaxant activity in endothelium-free rat thoracic aorta assessed as inhibition of 30 mM of KCl-induced contraction in presence of 1 uM of KATP channel blocker glibenclamide2014European journal of medicinal chemistry, Jun-10, Volume: 80Influence of the alkylsulfonylamino substituent located at the 6-position of 2,2-dimethylchromans structurally related to cromakalim: from potassium channel openers to calcium entry blockers?
AID1603229n-Octanol/water partition coefficient, log P of the compound by UV-RP-HPLC analysis2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1181955Stability in human liver microsomes assessed as metabolite formation at 8 uM at 37 degC in presence of NADPH and glucose-6-phosphate2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Straightforward entry to pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones and their ADME properties.
AID1407666Substrate activity at recombinant human P-gp in membrane fraction assessed as increase in ATPase activity at 10 uM by luminescent P-gp-Glo assay relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.
AID1197237Reversal of human MDR1-mediated drug efflux in mouse L5178 cells using rhodamine 123 as substrate assessed as fluorescence activity ratio at 40 uM incubated for 10 mins prior to substrate addition measured after 20 mins by FACScan flow cytometry relative 2015European journal of medicinal chemistry, Mar-06, Volume: 92Design, synthesis and biological profile of new inhibitors of multidrug resistance associated proteins carrying a polycyclic scaffold.
AID368552Reversal of P-glycoprotein-mediated doxorubicin resistance in human doxorubicin-resistant K562 cells expressing Pgp assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of parent compound at 1.6 uM2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID377772Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 1 ug/mL after 2 hrs relative to control2005Journal of natural products, Apr, Volume: 68, Issue:4
Taxoids and abietanes from callus cultures of Taxus cuspidata.
AID1055546Inhibition of side population in human HT-29 cells at 100 uM after 90 mins using vybrant dyecycle violet staining by FACS analysis2013European journal of medicinal chemistry, , Volume: 70Synthesis and anticancer potential of certain novel 2-oxo-N'-(2-oxoindolin-3-ylidene)-2H-chromene-3-carbohydrazides.
AID1472781Potentiation of paclitaxel-induced cytotoxicity against parental HEK293-pcDNA 3.1 transfected cells assessed as fold reduction in paclitaxel IC50 at 10 uM pre-incubated for 1 hr before paclitaxel addition and measured after 72 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.
AID1228909Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vincristine resistance measured as cell survival after 5 days by MTS assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID264309Ratio of rhodamine123 uptake in MDR1 transfected cells vs parental L5178Y cells at 11 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1,4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells.
AID1631492Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Vobatensines A-F, Cytotoxic Iboga-Vobasine Bisindoles from Tabernaemontana corymbosa.
AID449585Reversal index, Taxol IC50 to compound and taxol IC50 for inhibition of ABCB1 in human MES-SA/Dx5 cells at 5 uM2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.
AID1900353Stability in pooled human liver microsomes assessed as half life at 8 uM in presence of NADPH measured upto 60 mins by HPLC-MS analysis2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Multitarget Hybrid Fasudil Derivatives as a New Approach to the Potential Treatment of Amyotrophic Lateral Sclerosis.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1853712Metabolic stability in human liver microsomes assessed as half-life at 1 uM measured upto 15 mins in the presence of NADPH as co-factor by LC-MS/MS analysis2021RSC medicinal chemistry, Dec-15, Volume: 12, Issue:12
Potency and metabolic stability: a molecular hybrid case in the design of novel PF74-like small molecules targeting HIV-1 capsid protein.
AID321880Activation of human Pgp ATPase in human Caco-2 cells at 100 uM2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID656835Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 6 hrs post washout measured after 72 hrs by MTS assay (Rvb = 352012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID1813136Reversal of P-glycoprotein mediated drug resistance in human LCC6MDR cells assessed as reversal of vincristine resistance measured after 5 days by Cell Titer-Glo luminescence assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1374215Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID324484Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1235692Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 using ethidium bromide as substrate assessed as relative final fluorescence at 1/2 MIC by real-time fluorometry2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1348613Metabolic stability in human liver microsomes at 5 uM after 120 mins in absence of NADPH by UPLC-MS/MS analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1379031Effective permeability of compound at 50 ug/mL after 16 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.
AID1502706Antimycobacterial activity against Mycobacterium avium 104 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1322435Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine influx by measuring ratio of rhodamine mean fluorescence intensity in presence and absence of compound at 10 uM incubated for 20 mins by flow cytometry2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
AID1502825Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1485936Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID90140Ratio of effect of compound on DOX accumulation (antiPgp activity) to its intrinsic cellular toxicity;2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1530096Cell cycle arrest in human KBV cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 70.35 +/- 0.79%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1623672Protein binding in mouse plasma2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID209802Inhibitory activity when combined with cisplatin (uM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID230561Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vinblastine (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID455717Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as side scatter count measured by cell size ratio at 22 uM after 10 mins by flow cytometry2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1391799Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID1502741Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID436087Antioxidant activity against ferrous ion-induced lipid peroxidation in liver microsomes assessed as inhibition rate at 10 uM by TBA method in presence of cysteine2008Journal of natural products, Nov, Volume: 71, Issue:11
Targeted isolation and structure elucidation of stilbene glycosides from the bark of Lysidice brevicalyx Wei guided by biological and chemical screening.
AID1163834Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID492326Inhibition of MRP2 expressed in human A2780 cells at 10 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID1483832Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of natural products, 02-24, Volume: 80, Issue:2
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
AID1481894Substrate activity at P-gp in human P-gp membrane fraction assessed as increase in ATPase activity at 50 uM in presence of ATP after 1 hr by luciferase reporter gene assay relative to control2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID679063TP_TRANSPORTER: transepithelial transport of Verapamil at a concentration of 0.1 uM in Caco-2 cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
AID1739804Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1311930Permeability of the compound at 50 ug/ml in 70:30 PBS:EtOH by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.
AID1502918Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay relati2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1352545Cytotoxicity against HEK293 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1530094Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring decrease in paclitaxel IC50 at 10 uM after 72 hrs by MTT assay relative to paclitaxel alone2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID185796Compound was tested for the % inhibition rate of infarct size (myoglobin depleted area) on iv administration 15 min prior to the ligation at a dose of 1.0 mg/kg.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.
AID1647653Reversal of P-gp mediated multidrug resistance in human SW620/AD300 cells assessed as gain in sensitivity by measuring [doxorubicin IC50 for SW620/AD300 cells alone to doxorubicin IC50 for SW620/AD300 cells at 2.5 uM] after 48 hrs by MTT assay (Rvb = 1 No2020Journal of natural products, 02-28, Volume: 83, Issue:2
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus,
AID680793TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical)(Verapamil: 50 uM) in MRP2-expressing MDCK cells2002Pharmaceutical research, Jun, Volume: 19, Issue:6
Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa?
AID695909Inhibition of norA in Staphylococcus aureus SA-1199B overexpressing norA assessed as fold reduction in ciprofloxacin MIC at 25 ug/mL by checkerboard assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID209804Inhibitory activity when combined with vinblastine in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID75200Coronary perfusion pressure of isolated guinea pig heart at dose 0.05 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID399031Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780 cells assessed as calcein accumulation at 2.5 ug/ml after 15 mins relative to control2005Journal of natural products, Nov, Volume: 68, Issue:11
Bioactive tetrahydrofuran lignans from Peperomia dindygulensis.
AID78281Effect on rate of atrial contractions induced by PTX-B in guinea pig (control value)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid A new class of A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid pu
AID326367Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.
AID230391Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with 5-fluorouracil (uM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1362740Inhibition of LfrA in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as increase in norfloxacin accumulation at 150 ug/ml measured every 5 mins for 35 mins by fluorometric analysis2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria.
AID1315281Inhibition of P-gp in human CCRF-CEM VCR/R cells assessed as potentiation of vinblastin-induced cytotoxicity at 5 uM after 72 hrs by Alamar blue assay relative to control2016Journal of natural products, 05-27, Volume: 79, Issue:5
Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis.
AID437142Reversal of P-gp-mediated multidrug resistance in human 2780AD cells assessed as vincristine accumulation2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1502810Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to azithromy2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1275780Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as reversal of of choloroquine resistance at 0.8 uM relative to control2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID1459753Potentiation of vincristine-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1502735Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID722217Cytotoxicity against human doxorubicin-resistant K562 cells at 1 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID82355K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID1739836Inhibition of ABCB1 in FLp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold change in doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to doxorubicin IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1769162Inhibition of CYP1A2 in human liver microsomes assessed as remaining activity at 1 to 10 uM using phenacetin as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID1502909Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay relati2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1312953Aqueous solubility of the compound in PBS after 2 hrs by turbidity assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID165790Inhibition of [Ca2+] influx in response to a stimulus of KCL (60 uM)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1215350Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by refined CYP450 IC50 s2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID1673430Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 5 uM preincubated for 24 hrs followed by compound washout and later in2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID1733375Reversal of Pgp-mediated multidrug resistance in human KBV cells assessed as paclitaxel IC50 at 10 uM after 72 hrs in presence of paclitaxel by MTT assay (Rvb = 807.56 +/- 51.21 nM)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1215172Intrinsic clearance in Sprague-Dawley rat hepatic microsomes assessed as ratio of Vmax to Km for CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1439230Inhibition of human ABCB1 expressed in mouse L5178Y cells assessed as increase in rhodamine-123 accumulation by measuring forward scatter count of cells at 20 uM pretreated for 10 mins followed by rhodamine-123 addition after 20 mins by flow cytometry (Rv2017European journal of medicinal chemistry, Mar-10, Volume: 128Dregamine and tabernaemontanine derivatives as ABCB1 modulators on resistant cancer cells.
AID1576578Fraction absorbed of the compound by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID762408Antimicrobial activity against Mycobacterium smegmatis MC2 155 ATCC 700084 at 80 mg/L after 72 hrs by MTT assay in presence of EtBr2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1357219Half life in human liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID1459763Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1739846Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold change in paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to paclitaxel IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1336844Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold reduction in doxorubicin EC50 at 5 uM after 72 hrs by MTT assay relative to untreated control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1190829Resistance factor, ratio of vincristine IC50 to vincristine IC50 in presence of compound for human KB/VCR cells2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Multidrug resistance-reversal effects of resin glycosides from Dichondra repens.
AID1517912Stimulation of P-gp ATPase activity (unknown origin) at 10 uM incubated for 40 mins by P-gp-Glo luminescence assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1352674Effective permeability at 25 ug/ml after 16 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1604715Stability in human plasma assessed as elimination rate at 5 uM at 37 degC measured up to 250 mins by LC-MS analysis2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
AID1414427Inhibition of MRP1 in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in cell survival after 5 days by MTS assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
AID1822203Inhibition of P-glycoprotein overexpressed in human SW620/AD300 cells assessed as gain of sensitivity ratio by measuring reversal of doxorubicin IC50 after 48 hrs by MTT assay relative to doxorubicin alone2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore.
AID1502737Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID288190Permeability coefficient through artificial membrane in presence of stirred water layer at 100 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1702156Inhibition of human ERG by fluorescence polarization assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1064673Binding affinity to p-glycoprotein (unknown origin) by intrinsic tryptophan fluorescence quenching assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication.
AID1740453Metabolic stability in human hepatocytes assessed as hepatic extraction ratio at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID1739852Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold change in paclitaxel IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to paclitaxel IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1502905Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay relative to e2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1273407Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 8 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1750902Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by after 48 hrs by MTT assay relative to control
AID1481495Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-mediated cytotoxicity by measuring reduction in ADR IC50 at 5 uM preincubated for 24 hrs followed by compound washout for 12 hrs and subsequent addition of adriamycin measu2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID96340The efficacy in reverting MDR was evaluated on erythroleukemia K-562 cell line.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID313270Dissociation constant, pKa of the compound2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells.
AID1211298Dissociation constant, pKa of the compound2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1350760Inhibition of ABCB1 (unknown origin) expressed in HEK293 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold reduction in vincristine IC50 at 3 uM preincubated for 4 hrs followed by vincristine addition measured after 72 h2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID75198Concentration needed to elicit a 75% increase beyond control in coronary flow in ''Langendorff'', guinea pig heart (in vitro)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID762411Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as reduction in EtBr MIC at 80 mg/L by MTT assay relative to control2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1904188Inhibition of P-gp in human Caco-2 cells assessed as reduction in basal to apical transport of paclitaxel at 10 uM measured as apparent permeability after 60 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID1201747Permeability of the compound by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
AID562101Chemosensitization of halofantrine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1155070Antiplasmodial activity against Plasmodium falciparum C4Dd2 expressing chloroquine-resistance-conferring pfcrt alleles assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1275771Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as potentiation of choloroquine induced antimalarial activity by measuring ratio of chloroquine IC50 in presence to absence of compound at 1 uM2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID230562Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vinblastine (nM) in P388/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID449584Intrinsic cytotoxicity against human MES-SA/Dx5 cells2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.
AID653309Inhibition of p-glycoprotein in human K562/A02 cells assessed as accumulation of adriamycin by flow cytometry2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1421885Effective permeability of the compound at 1 mg/ml after 4 hrs by BBB-PAMPA method2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID78315In vitro molar concentration required to block [Ca2+] -induced contraction of K+-depolarized taenia cecum of guinea pigs1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID1764398Substrate activity at P-gp (unknown origin) assessed as net efflux ratio2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID755308Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 3 uM after 2 hrs by microplate fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1305710Half life in human liver microsomes at 0.1 uM2016Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14
Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents.
AID295524Growth inhibition of human CEM/VLB500 cells after 3 days by resazurin assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).
AID1155068Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1353440Inhibition of P-gp in human K562/Dox cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring ratio of doxorubicin IC50 to doxorubicin IC50 in presence of test compound at 3 uM after 72 hrs by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents.
AID1404016Permeability of the compound by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID1764399Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID1739850Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold change in vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to vincristine IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID502259Inhibition of MRP1 expressed in hamster BHK21 cells assessed as reduction of GSH efflux at 5 uM after 20 mins2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
AID398094Reversal of P-glycoprotein-mediated multidrug resistance in human MDR1 gene transfected mouse L5178Y cells assessed as fluorescence activity ratio at 5.2 uM by rhodamine 123 accumulation assay2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: a novel cluster of tumor-specific cytotoxins which reverse multidrug resistance.
AID1684005Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
AID681353TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in F4-6RADR cells1992Biochemical pharmacology, Jun-23, Volume: 43, Issue:12
Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID283798Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 2.5 ug/mL relative to verapamil2007Journal of natural products, Apr, Volume: 70, Issue:4
Bioactive lignans from Peperomia duclouxii.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID683396Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as doxorubicin-induced cytotoxicity at 10 uM after 72 hrs by SRB assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID171865Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR),at 0.5-2h after 30 mg/kg oral administration1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID1211796Intrinsic clearance in cryopreserved human HepaRG cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1264455Permeability of the compound by high throughput PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID322363Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein.
AID620607Reversal of P-gp-mediated multidrug-resistance in human K562 cells at 10 uM after 48 hrs by MTT assay relative to adriamycin2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and evaluation of furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline as anticancer and multidrug resistance reversal agents.
AID1833347Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1207723Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1481871Cytotoxicity against human K562/A02 cells assessed as cell viability at 5.0 uM after 48 hrs by MTT assay (Rvb = >99%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID562103Chemosensitization of mefloquine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID74168Decrease in developed tension of the left atrium of guinea pig expressed as the negative inotropy.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID578762Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).
AID1235716Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1517892Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1439232Inhibition of human ABCB1 expressed in mouse L5178Y cells assessed as increase in rhodamine-123 accumulation by measuring side scatter count of cells at 20 uM pretreated for 10 mins followed by rhodamine-123 addition after 20 mins by flow cytometry (Rvb =2017European journal of medicinal chemistry, Mar-10, Volume: 128Dregamine and tabernaemontanine derivatives as ABCB1 modulators on resistant cancer cells.
AID1502887Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxaci2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1807360Metabolic stability in human liver microsomes assessed as intrinsic clearance in presence of NADPH regenerating system by UPLC-MS analysis
AID683075Inhibition of human ABCB1 pump expressed in mouse L5178 cells assessed as fluorescence activity ratio at 22 uM for 10 mins by flow cytometry2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Significant activity of ecdysteroids on the resistance to doxorubicin in mammalian cancer cells expressing the human ABCB1 transporter.
AID1903297Potentiation of mitoxantrone-induced cytotoxicity against human KBV cells assessed as mitoxantrone IC50 by measuring ratio IC50 as reversal fold at 5 uM for 72 hrs by MTT assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID680485TP_TRANSPORTER: inhibition of JC-1 uptake (JC-1: ca 0.1 uM, Verapamil: 5 uM) in K562 and K562/ADR cells, flow cytometry1997Leukemia, Jul, Volume: 11, Issue:7
Functional assay of multidrug resistant cells using JC-1, a carbocyanine fluorescent probe.
AID1411803Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by MTT assay2017MedChemComm, Dec-01, Volume: 8, Issue:12
N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.
AID1449543Clearance in human intestinal microsomes2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID717088Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate.
AID681383TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells2001Pharmaceutical research, Feb, Volume: 18, Issue:2
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.
AID1336851Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring compound concentration required for reduction of paclitaxel IC50 by half after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211793Lipophilicity, log P of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID230551Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with cisplatin (uM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID48973Antagonistic activity against K+ induced responses in canine trachea.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1215146AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID78280Effect on rate of atrial contractions induced by PTX-B in guinea pig1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid A new class of A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid pu
AID1750926Inhibition of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as Adriamycin accumulation at 1 to 10 uM pretreated 1 hr followed by treated with adriamycin measured after 180 mins by fluorescence microscopy
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID310897Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing half maximal increase in nuclear concentration of pirarubicin2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors.
AID1174978Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular adriamycin accumulation incubated for 60 mins prior to substrate addition measured after 90 mins by fluorescence microscopy relative to control2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID321879Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1520013Half life in rat liver microsomes up to 60 mins by HPLC-LC/MS analysis
AID615734Reversal of MDR1-mediated paclitaxel resistance in human NCI-H460 cells assessed as ratio of compound IC50 to IC50 of paclitaxel at 1 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID331508Lipophilicity, log P of the compound2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.
AID1502765Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID354669Inhibition of MRP expressed in human MCF7/VP cells assessed as increase in vincristine-induced cytotoxicity at 20 uM after 48 hrs by SRB binding assay1996Journal of natural products, Jun, Volume: 59, Issue:6
Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A.
AID1569057Intrinsic clearance in CD-1 mouse liver microsomes in presence of NADPH regenerating system measured up to 4 hrs by UPLC-MS analysis
AID1352559Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Lineweaver-Burk plot analysis2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1738694Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as doxorubicin accumulation by measuring increase in mean fluorescence channel at 1 uM pretreated with compound for 30 mins followed by incubation with doxorubicin for 1 hr by f2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID202471In vitro concentration required to inhibit tumor activity on subclone of human colon carcinoma cells (S1-B1-20) resistant to bisantrene1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Novel multidrug resistance reversal agents.
AID1533101Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 12.5 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1602186Half life in mouse liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.
AID656821Induction of rhodamine-123 accumulation in human K562 cells preincubated for 1 hr prior rhodamine 123 addition measured after 30 mins by flow cytometry relative to control2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID53611Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 10 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1273396Cytotoxicity against human MDM assessed as cell viability after 3 days by Alamar blue dye-based fluorocytometric analysis relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID165539Inhibition of contraction in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1625122Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1903289Potentiation of mitoxantrone-induced cytotoxicity against human KBV cells assessed as mitoxantrone IC50 at 5 uM for 72 hrs by MTT assay (Rvb = 695.15 +/- 57.54 nM )2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID701948Inhibition of human recombinant P-glycoprotein after 40 mins by Pgp-Glo assay2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity.
AID1502843Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID165788In vitro inhibition of development of isometric tension, in response to norepinephrine (NE, 10 uM) in rabbit aorta1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1733393Induction of cell cycle arrest in human KBV cells assessed as accumulation at sub-G1 phase at 10 uM after 24 hrs by PI/RNaseA staining based flow cytometric analysis (Rvb = 4.26 +/- 0.35%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID714431Reversal of P-gp-mediated paclitaxel-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1217709Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1739807Cytotoxicity against human KB-VIN cells assessed as reduction in cell viability measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1631736Reversal of P-gp-mediated resistance in adriamycin-resistant human HepG2 cells assessed as reduction in ADR IC50 at 500 nM after 48 hrs by MTT assay relative to control2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1235734Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 16 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID272485Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID70546In vitro hemolytic concentration on uninfected erythrocytes.2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives.
AID1530090Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring cell survival at 5 uM after 72 hrs by MTT assay (Rvb = 104 +/- 8%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID358657Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL2001Journal of natural products, Dec, Volume: 64, Issue:12
Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei.
AID1903295Potentiation of paclitaxel-induced cytotoxicity against human KBV cells assessed as paclitaxel IC50 by measuring ratio IC50 as reversal fold at 5 uM for 72 hrs by MTT assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID94171Compound was evaluated for the in vitro activity in KB-A1 cell line. Activity expressed as fold reversion (Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1286274Cytotoxicity against human vincristine-sensitive KB cells assessed as cell viability after 72 hrs by MTT assay2016Journal of natural products, Jan-22, Volume: 79, Issue:1
Aspidofractinine and Eburnane Alkaloids from a North Borneo Kopsia. Ring-Contracted, Additional Ring-Fused, and Paucidactine-Type Aspidofractinine Alkaloids from K. pauciflora.
AID1246314Plasma protein binding in mouse2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1275779Inhibition of voltage-gated calcium channel in Wistar rat synaptoneurosomes after 30 mins by fluorescent ratiometric indicator method2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID228176Inhibition of tetraethylammonium chloride(TEA)-induced acetylcholine hyperactivity in rat tracheal segments by the compound.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
New N-(pyridin-4-yl)-(indol-3-yl)acetamides and propanamides as antiallergic agents.
AID1173449Effective permeability of the compound by PAMPA assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID252995Toxicity of compound (1 uM) is expressed as percentage of cell growth inhibition with respect to the control2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID1502896Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1459748Cytotoxicity against human Flp-In-293 cells assessed as reduction in cell viability by SRB assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1502768Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1464386Resistance index, ratio of mitoxantrone IC50 for human H460/MX20 cells to mitoxantrone IC50 for human H460 cells at 3 uM (Rvb = 28.66 No_unit)2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors.
AID1739806Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID82676Inhibitory concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which inhibits cell proliferation by 20% in the absence of particular cytotoxic drug1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin.
AID1502726Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as increase in EtBr accumulation by measuring relative final fluorescence incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502831Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 2 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID604022Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1502916Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay rela2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID80725Inhibitory concentration required to block Ca+2 induced contraction of K+ depolarized guinea pig aorta1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID1496040Effective permeability of the compound in PBS/EtOH at 50 ug/mL after 18 hrs by PAMPA-BBB assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold.
AID1702160Clearance in rat liver microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1371140Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS analysis2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA).
AID401285Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as increase in rhodamine 6G accumulation1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1704099Reversal of multidrug resistance activity in P-gp overexpressing human A2780T cells assessed as potentiation of PTX-induced cytotoxicity by measuring PTX IC50 at 10 uM incubated for 48 hrs in presence of paclitaxel by MTT assay (Rvb = 3.972 uM)2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1702161Drug metabolism assessed as human recombinant CYP3A4-mediated clearance at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH by LC-MS analysis2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1739826Inhibition of ABCB1 in human KB-VIN cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 2867 +/- 142 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1750897Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay
AID1235736Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 4 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID537733Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1400033Half life in Sprague-Dawley rat liver microsomes at 500 ng/ml preincubated for 5 mins followed by NADPH addition by C-MS/MS analysis2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID615730Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as Rho123 accumulation at 20 uM after 30 mins by FACScalibur flow cytometry relative to control2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID1733388Reversal of BCRP-mediated multidrug resistance in human KBV cells assessed as fold change in mitoxantrone IC50 at 10 uM after 72 hrs in presence of mitoxantrone by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1330750Effective permeability of the compound after 18 hrs by PAMPA2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID1776728Inhibition of Multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as measuring relative final fluorescence at 128 ug/ml measured by ethidium bromide accumulation assay2021Bioorganic & medicinal chemistry letters, 06-15, Volume: 422,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis.
AID76860Percent inhibition of calcium-induced contraction on K+ -depolarized guinea pig aortic strips at 10 e-4 M1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.
AID1683978Inhibition of ABCB1 (unknown origin) expressed in HEK293 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured afte
AID1377031Inhibition of P-gp in human KBv200 cells assessed as potentiation of navelbine-induced cytotoxicity by measuring reduction in navelbine IC50 at 10 uM after 72 hrs by MTT assay relative to control2017Journal of natural products, 06-23, Volume: 80, Issue:6
Terpenoids from Euphorbia soongarica and Their Multidrug Resistance Reversal Activity.
AID1418877Potentiation of doxorubicin-induced cytotoxicity in human HEK293T/NC cells assessed as fold reduction in doxorubicin IC50 at 4 uM after 72 hrs by MTT assay relative to doxorubicin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1338179Cytotoxicity against mouse L929 cells measured after 3 days by MTS assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1336842Inhibition of P-gp in human MES-SA/Dx5 cells assessed as increase in doxorubicin accumulation at 5 uM after 30 mins by flow cytometry relative to control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1383661Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease.
AID1480943Permeability of the compound at pH 7.4 at 5 mg/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID1239241Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in rhodamine 123 accumulation at 2 uM after 2.5 hrs by spectrofluorometric analysis relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID1683962Inhibition of CYP3A4 in in human liver microsomes at 30 uM incubated for 10 mins in presence of CYP3A4 substrate/NADP+ by fluorescence based assay
AID26798Partition coefficient (logP)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID1566394Inhibition of rat P-gp ATPase in jejuna mucosa membrane assessed as remaining enzyme activity using ATP as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Green chemistry appended synthesis, metabolic stability and pharmacokinetic assessment of medicinally important chromene dihydropyrimidinones.
AID681614TP_TRANSPORTER: inhibition of Saquinavir transepithelial transport (basal to apical) in Caco-2 cells1999British journal of clinical pharmacology, Oct, Volume: 48, Issue:4
Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.
AID1201746Permeability of the compound after 16 hrs by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
AID1907126Stability in mouse liver microsomes assessed as half life measured upto 60 mins in presence of NADPH by LC-MS/MS analysis2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
4,5-Dihydroxypyrimidine Methyl Carboxylates, Carboxylic Acids, and Carboxamides as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease.
AID1418874Potentiation of paclitaxel-induced cytotoxicity in human HEK293T/NC cells assessed as fold reduction in paclitaxel IC50 at 4 uM after 72 hrs by MTT assay relative to paclitaxel2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID714200Inhibition of P-gp-mediated paclitaxel resistance in human LCC6MDR cells assessed as fold decrease in paclitaxel IC50 for cytotoxic activity at 1 uM after 5 days by MTS assay relative to parental cells2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1254933Half life in human liver S9 microsomes in absence of NADPH by LC-MS/MS method2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1502895Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1851935Metabolic stability in human microsomes assessed as compound remaining measured after 30 mins2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID762412Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as reduction in EtBr MIC at 40 mg/L by MTT assay relative to control2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID350540Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
AID1273468Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 64 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1502757Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID683399Inhibition of P-gp over expressed in human multidrug-resistant KBVIN cells assessed as intracellular accumulation of doxorubicin at 10uM after 3 hrs by fluorescence microplate reader analysis relative to control2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID150753Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1595492Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as reduction of ATP consumption at 1 uM incubated for 2 hrs by luminescence assay2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID1352546Therapeutic index, ratio of IC50 for HEK293 cells to EC50 for inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID653302Cytotoxicity against human K562 cells assessed as cell killing at 5 uM after 72 hrs by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1478796Permeability of the compound by PAMPA-BBB assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors.
AID389758Octanol-water partition coefficient, log P after 5 hrs by shake flask method2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID680084TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Azidopine: 0.2 uM, Verapamil: 1 uM) in membranes from KB/V20C cells1993Biochemical pharmacology, Jan-26, Volume: 45, Issue:2
Terfenadine (Seldane): a new drug for restoring sensitivity to multidrug resistant cancer cells.
AID509768Reversal of P-glycoprotein-mediated vincristine-resistance in human KB/VCR cells expressing Pgp assessed as ratio of adriamycin IC50 to adriamycin IC50 in presence of compound at 16 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity.
AID406532Inhibition of NorA efflux pump in Staphylococcus aureus 1199B assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Citral derived amides as potent bacterial NorA efflux pump inhibitors.
AID233360modulation factor: IC50 (uM)1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships.
AID1502819Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring reduction in azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1271449Vasodilator activity in Sprague-Dawley rat mesentric artery assessed as reduction in of K+-induced contraction2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and fluorescent study of 5-phenyl furocoumarin derivatives as vasodilatory agents.
AID1352543Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity at 10 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1502865Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 4 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1683973Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in intracellular concentration of PTX at 4 uM pre-incubated for 72 hrs followed by PTX addition and measured after 3 hrs by UPLC analysis
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1062342Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID103927Inhibitory concentration against MCF-7/ADR cells using P-gp-mediated MDR assay using 25 nM actinomycin D which inhibit cells proliferation by 20% in the absence of particular cytotoxic drug1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin.
AID1759974Apparent permeability across apical to basolateral in human Caco2 cells by LC-MS/MS analysis2021European journal of medicinal chemistry, Jul-05, Volume: 219Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.
AID551808Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for maximum increase in nuclear concentration of pirarubicin by fluorescence assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Inhibition of P-glycoprotein-mediated Multidrug Resistance (MDR) by N,N-bis(cyclohexanol)amine aryl esters: further restriction of molecular flexibility maintains high potency and efficacy.
AID679465TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells2001Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 29, Issue:8
Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein.
AID43402Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID683264Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as fold decrease in vincristine IC50 for cytotoxic activity at 10 uM after 72 hrs by SRB assay relative to control2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1235747Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1530095Cell cycle arrest in human KBV cells assessed as accumulation at sub-G1 phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2.21 +/- 1.02%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1411807Selectivity ratio of IC50 for Marburg virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-MarV-GP pseuotype virus infected HEK293 cells to IC50 for Vesicular stomatitis Indiana virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-G 2017MedChemComm, Dec-01, Volume: 8, Issue:12
N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.
AID1879297Permeability of compound by PAMPA-BBB assay2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.
AID1459754Potentiation of vincristine-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID1502722Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as increase in EtBr accumulation by measuring relative final fluorescence at 1/2 times MIC incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1168389Potentiation of 0.2 uM doxorubicin-induced cytotoxicity in human HL60/MDR cells assessed as viable cells at 25 uM after 48 hrs by WST assay relative to control2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition.
AID1196792Metabolic stability in human microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in presence of NADPH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID681130TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1336846Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of vinblastine-induced cytotoxicity by measuring fold reduction in vinblastine EC50 at 5 uM after 72 hrs by MTT assay relative to untreated control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1312933Intrinsic clearance in human liver microsomes measured after 10 to 60 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID674363Inhibition of human voltage-dependent L-type calcium channel subunit alpha1C/alpha2delta/beta2a expressed in C1-6-37-3 cells assessed as inhibition of K+-induced calcium influx incubated for 30 mins prior to K+-induction by Fluo-4-AM based FLIPR assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Isolation and structural elucidation of cyclic tetrapeptides from Onychocola sclerotica.
AID1502911Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay rela2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1180198Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 60 mM K+-induced contraction2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID1235766Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 16 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID704793Inhibition of MDR1-mediated rhodamine 123 uptake expressed in human COLO320 cells assessed as fluorescence activity ratio at 22 ug/mL after 10 mins by flow cytometry relative to parent cells2012Journal of natural products, Nov-26, Volume: 75, Issue:11
Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon adenocarcinoma cells.
AID1739820Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 4.55 +/- 0.28 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID295523Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).
AID1740451Intrinsic clearance in human hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID1813131Reversal of Pgp-mediated paclitaxel resistance in human LCC6MDR cells assessed as relative fold by measuring paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay relative to control2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1228916Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as induction of intracellular doxorubicin accumulation at 2 uM after 150 mins by spectrofluorometric analysis relative to control2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
AID635079Permeability of the compound after 2.5 hrs by PAMPA-BBB assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model.
AID1436078Permeability of compound at 100 ug/ml after 18 hrs by PAMPA2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID1418865Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel IC50 at 4 uM after 72 hrs by MTT assay relative to paclitaxel2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1709007Substrate activity at human P-glycoprotein assessed as stimulation of ATPase activity at 10 uM in presence of MgATP incubated for 1.5 hrs by luminescence-based Pgp-glo assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
AID679744TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.0175 uM, Verapamil: 100 uM) in CEM/VBL600 cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID283910Inhibition of P-gp mediated efflux-pump activity in human MDR1 gene transfected mouse L5178 Y cells at 10 ug/mL by rhodamine 123 accumulation test2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Apoptosis induction and modulation of P-glycoprotein mediated multidrug resistance by new macrocyclic lathyrane-type diterpenoids.
AID510382Inhibition of Staphylococcus aureus 1199B norA efflux pump by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus.
AID1918144Inhibition of P-gp in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reversal fold ratio at 3 uM in presence of 10 nM to 30 uM doxorubicin incubated for 72 hrs by MTT assay
AID683262Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as fold decrease in paclitaxel IC50 for cytotoxic activity at 10 uM after 72 hrs by SRB assay relative to control2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1321554Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as side scattered light at 22 uM preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry (Rvb = 194.6 to 2862016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID620606Reversal of P-gp-mediated multidrug-resistance in adriamycin-resistant human K562/A02 cells at 10 uM after 48 hrs by MTT assay relative to adriamycin2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and evaluation of furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline as anticancer and multidrug resistance reversal agents.
AID427198Membrane permeability dissolved in PBS/EtOH (80:20) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1888853Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at sub MIC relative to ethidium bromide MIC alone2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1888849Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of norfloxacin-induced antibacterial activity by measuring Norfloxacin MIC at sub MIC2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1647652Reversal of P-gp mediated multidrug resistance in human SW620/AD300 cells assessed as potentiation of doxorubicin-induced antiproliferative activity by measuring doxorubicin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 4.9 microM)2020Journal of natural products, 02-28, Volume: 83, Issue:2
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus,
AID365465Inhibition of P-gp in human A2780 cells2008Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1273477Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 256 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID154132Evaluated for cytotoxicity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the absence of 10 nM vincristine1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
AID80192Inhibitory activity on atrial contractility in isolated Guinea pig right atrea at 0.03 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID562109Chemosensitization of sesquiterpene dihydroartemisinin pyronaridine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID681146TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID1207720Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID427197Membrane permeability dissolved in PBS/EtOH (70:30) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID1382494Intrinsic clearance in human liver microsomes at 0.1 uM preincubated for 5 mins followed by NDAPH addition measured up to 60 mins by HPLC-MS/MS analysis2018European journal of medicinal chemistry, Mar-25, Volume: 148Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).
AID1459766Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1174979Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular rhodamine-123 accumulation incubated for 90 mins post substrate addition by flow cytometry relative to control2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents.
AID1292330Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1319024Substrate activity at P-gp (unknown origin) in P-gp enriched membranes assessed as increase in ATPase activity at 200 uM in presence of Mg2-ATP after 40 mins by luciferase reporter gen assay relative to control2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID53612Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID455714Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as forward scatter count measured by cell size ratio at 22 uM after 10 mins by flow cytometry2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
New potent P-glycoprotein modulators with the cucurbitane scaffold and their synergistic interaction with doxorubicin on resistant cancer cells.
AID1350758Inhibition of ABCB1 in human KB-C2 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold reduction in vincristine IC50 at 3 uM preincubated for 4 hrs followed by vincristine addition measured after 72 hrs by MTT assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
AID1739134Metabolic stability at phase 1 in human liver microsomes assessed as half life at 1 uM by LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Chemical profiling of HIV-1 capsid-targeting antiviral PF74.
AID1502913Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring reduction in ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay rela2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID399366Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry1998Journal of natural products, Jan, Volume: 61, Issue:1
Two pimarane diterpenoids from Ephemerantha lonchophylla and their evaluation as modulators of the multidrug resistance phenotype.
AID1813129Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID1215151AUC (0 to 480 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1740450Half life in mouse hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID399197Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 1 ug/mL after 2 hrs relative to control2004Journal of natural products, Jan, Volume: 67, Issue:1
Production of biologically active taxoids by a callus culture of Taxus cuspidata.
AID1675374Stimulation of P-gp ATPase activity (unknown origin) assessed as increase in ATP consumption at 25 uM relative to control2020Journal of natural products, 08-28, Volume: 83, Issue:8
Ecdysteroid Derivatives that Reverse P-Glycoprotein-Mediated Drug Resistance.
AID1502734Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID327170Binding affinity to human serum albumin by PAMPA method2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin.
AID1283418Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 1 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID1491367Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID1683981Reversal of resistance to paclitaxel-induced cytotoxicity in HEK293 cells assessed as reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1180210Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of phenylephrine-induced contraction at 100 uM relative to untreated control2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID103349Cytotoxicity against MCF-7 breast carcinoma cells at 10 ug/mL2001Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4
Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists.
AID1319976Permeability of the compound at 25 ug/ml at 7.4 pH after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID1273412Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 64 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1769133Inhibition of CYP2D6 in human liver microsomes assessed as remaining activity at 1 to 10 uM using dextromethorphan as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Discovery of G Protein-Biased Antagonists against 5-HT
AID1235702Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 16 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1163825Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID1585800Metabolic stability in human liver microsomes assessed as parent compound remaining at 3 uM after 30 mins by LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
AID696926Induction of human MDR1 ATPase activity assessed as inorganic phosphate production in presence of MDR1 inhibitor cyclosporin A2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1273478Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 128 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID678840TP_TRANSPORTER: Western blot, LS-180V2000AIDS (London, England), Jun-16, Volume: 14, Issue:9
Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture.
AID1283415Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID1283421Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in vinblastine IC50 at 1 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID351906Chemosensitizing activity as 500nM potentiation of quinine effect after 72 hrs against chloroquine-resistant transporter 106/1'76T mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1785082Effect on intracellular Rhodamine 123 accumulation in human SW620 cells at 0.5 to 2 uM incubated for 24 hrs by flow cytometry
AID1888854Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring fractional inhibitory concentration2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID231788Ratio of contractility to atrial rate in isolated guinea pig atria1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID1502794Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1129440Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1478786Permeability of the compound at 200 uL after 16 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1235732Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as amikacin MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID331359Inhibition of Pgp-mediated multidrug resistance activity in human MCF7/ADM cells assessed as Rh123 accumulation at 10 umol/L after 30 mins2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID288187Permeability coefficient through artificial membrane in presence of stirred water layer at 250 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID264306Inhibition of P-glycoprotein2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1,4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells.
AID1823835Inhibition of hERG at 1 uM by whole-cell electrophysiological assay relative to control
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1683965Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as [3H]PTX efflux loss at 4 uM pre-incubated for 4 hrs followed by PTX addition and measured after 2 hrs by liquid scintillation counting analysis (Rvb = 97%)
AID1502740Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID351902Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76I mutant Plasmodium falciparum infected in human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1168388Potentiation of 0.02 uM doxorubicin-induced cytotoxicity in human HL60/MDR cells assessed as viable cells at 25 uM after 48 hrs by WST assay relative to control2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition.
AID232670Selectivity ratio of IC50 for [Ca2+] antagonistic activity in aorta / IC50 for suppressive effect on contractile force1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID1530761Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method2019European journal of medicinal chemistry, Jan-01, Volume: 1611,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.
AID1486981Cytotoxicity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID653467Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated for 24 hrs followed by adriamycin treated 24 hrs after drug washout by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID77841Heart rate of isolated guinea pig heart at dose 5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID1558702Intrinsic clearance in rat liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis
AID360080Cytotoxicity against hamster BHK21 cells by MTT assay2007The Journal of biological chemistry, Oct-26, Volume: 282, Issue:43
(R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1.
AID427741Reversal of MRP1-mediated doxorubicin resistance in human 2008/MRP1 cells assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of compound at 10 uM2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1703888Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1414431Selectivity index, ratio of IC50 for mouse L929 cells to EC50 for MRP1 in human 2008/MRP1 cells2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
AID288193Flux ionization constant, pKa of the membrane permeability coefficient of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID427308Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 assessed as mean fluorescence intensity of rhodamine-123 uptake at 22.2 uM after 10 mins by flow cytometry2009Journal of natural products, Jun, Volume: 72, Issue:6
Tabernines A-C, beta-carbolines from the leaves of Tabernaemontana elegans.
AID1502802Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID80190Inhibitory activity on atrial contractility in isolated Guinea pig right atrea at 0.003 mg/mL concentration1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID513665Induction of autophagy in differentiated rat stable inducible PC12 cells assessed as increase in LC3-2 level cell pretreated at 1 uM in presence of 400 nM bafilomycin A12008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1496417Apparent half life in human liver microsomes at 3 uM2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
AID157422Fractional inhibitory concentration (FIC) tested against Peruvian PC49 cells, isolate from South America2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum.
AID1764807Half life in human pooled liver microsomes assessed as parent compound remaining measured up to 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1502870Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1595498Inhibition of P-glycoprotein-mediated Rhodamine-123 efflux in human K562/DOX cells assessed as fluorescence ratio of accumulation of Rhodamine-123 at 3 uM preincubated for 15 mins followed by Rhodamine-123 addition measured after 30 mins by flow cytometry2019European journal of medicinal chemistry, Jun-15, Volume: 172Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.
AID1517890Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as fold reduction in doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1163827Potentiation of erlotinib-induced cytotoxicity against human H460/Vbl cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID226029Tested for the multidrug resistance reversal activity against P388 murine leukemia cell line, activity is expressed as RF(ED50 with no adriamycin (ADR)/ED50 with 200 nM ADR)2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Classification of multidrug-resistance reversal agents using structure-based descriptors and linear discriminant analysis.
AID755315Inhibition of p-gp in human KB/VCR cells assessed as potentiation of vincristine-induced cytotoxicity at 5 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID368553Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID1517891Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as fold reduction in doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID1557178Permeability of the compound at 100 ug/ml measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1273464Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 8 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID167568Calcium channel-blocking activity by determined by ability to antagonize calcium-induced contractions of isolated rabbit aortic strips1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID1192730Permeability of the compound by PAMPA2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1683993Inhibition of ABCB1 in multidrug-resistant human SW620/Ad300 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition
AID653465Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated for 24 hrs followed by adriamycin treated 6 hrs after drug washout by MTS assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID537735Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID399198Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 10 ug/mL after 2 hrs relative to control2004Journal of natural products, Jan, Volume: 67, Issue:1
Production of biologically active taxoids by a callus culture of Taxus cuspidata.
AID427739Inhibition of MRP1 in human 2008/MRP1 cells by dixon plot analysis2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID1771039Intrinsic clearance in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID77840Heart rate of isolated guinea pig heart at dose 0.5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1391814Inhibition of P-gp in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring adriamycin IC50 at 5 uM preincubated for 24 hrs followed by compound wash out and subsequent addition of adriamycin measured after 48 hrs b2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID680693TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in the presence of Verapamil at a concentration of 100uM in LLC-GA5-COL150 cells2004British journal of pharmacology, Dec, Volume: 143, Issue:7
Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux.
AID1377028Inhibition of P-gp in human KBv200 cells assessed as increase in intracellular rhodamine123 accumulation by measuring fluorescence activity ratio at 10 uM incubated for 4 hrs followed by rhodamine123 addition measured after 1 hr by flow cytometry2017Journal of natural products, 06-23, Volume: 80, Issue:6
Terpenoids from Euphorbia soongarica and Their Multidrug Resistance Reversal Activity.
AID1369736Passive permeability of the compound at 500 uM after 5 hrs by PAMPA2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides.
AID230559Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vinblastine (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1196795Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in absence of NADPH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1246313Plasma protein binding in human2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1486974Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay relative to ADR alone2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID681580TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1459750Cytotoxicity against human HeLaS3 assessed as reduction in cell viability by SRB assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1502716Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as increase in EtBr accumulation by measuring relative final fluorescence at 1/2 times MIC incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1207235Inhibition of hERG K channel2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID481444Octanol-water partition coefficient, log P of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID271726Inhibition of vinblastine-induced ATPase activation in Caco-2 cells2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID1459752Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1273426Modulation factor, ratio of isoniazid MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of isoniazid2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1486951Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1062335Inhibition of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of doxorubicin drug resistance relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID81850Effect on vinblastine IC50 against MDR human carcinoma HCT116/VM46 cell line at a dose of 1 uM concentration2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Multidrug resistance reversal activity of key ningalin analogues.
AID1273498Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 256 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1502797Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1313189Half life in human liver microsomes at 3 uM in presence of NADPH by LC-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID193905Change in arterial blood pressure was measured at 0.3 mg/kg dose(iv) in anesthetized rats1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
AID680493TP_TRANSPORTER: inhibition of IAAP photoaffinity labelling (IAAP: 0.02 uM, Verapamil: 100-fold molar excess) in plasma membranes from CEM/VLB1.0 cells1997Biochemical pharmacology, Jan-10, Volume: 53, Issue:1
Reversal of P-glycoprotein-associated multidrug resistance by ivermectin.
AID1215165Cmax in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1899078Inhibition of P-gp in human KB/VCR cells assessed as increase in Rho123 accumulation at 10 uM
AID1534778Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID1564939Inhibition of P-gp efflux in human KBtax cells at 100 uM after 1 hr by flow cytometry2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1459756Potentiation of paclitaxel-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1225503Cytotoxicity against mouse NIH/3T3 cells assessed as cell growth at 10 uM after 24 hrs by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1129438Metabolic stability in human microsomes assessed as compound remaining at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1502769Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID514300Protection of neurodegeneration in Drosophila Huntington's disease model assessed as induction autophagy at 1.25 mM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1362737Inhibition of LfrA in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as increase in EtBr accumulation at 150 ug/ml measured every 5 mins for 35 mins by fluorometric analysis2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria.
AID242908Maximum velocity against human P-glycoprotein expressed in Sf9 cells2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.
AID1273410Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 128 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1702155n-Octanol/water distribution coefficient, logD of the compound at pH 7.42018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1530729Stimulation of P-gp ATPase activity (unknown origin) at 0.5 mM preincubated for 5 mins followed by Mg-ATP addition measured after 40 mins by ATP-Glo luminescence assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID389764Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID1589936Half life in human liver microsomes2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
AID90133Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1785066Reversal of resistance to colchicine -induced cytotoxicity in human SW620/AD300 cells assessed as colchicine IC50 by measuring reversal fold at 2 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay relative to
AID74439Percent inhibition of calcium-induced contraction on K+ depolarized guinea pig aortic strip.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID714422Therapeutic index, ratio of IC50 for L929 cells to EC50 for reversing paclitaxel resistance in human MDA435/LCC6MDR cells2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1179308Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by MABA method2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
AID492323Inhibition of Pgp expressed in mouse L5178Y cells at 1 uM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
AID389766Inhibition of MDR1 overexpressed in MDCK cells at 5 uM relative to LSN3359842008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID362951Inhibition of P-glycoprotein expressed in mouse L5178Y cells measured by rhodamine 123 uptake assessed as fluorescence activity ratio relative to wild type mouse L5178 cells at 10 uM2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes.
AID680309TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 50 mg/L, Verapamil: 10 uM) in Hs578T-Dox cells1999Biochemical pharmacology, Dec-01, Volume: 58, Issue:11
Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity.
AID1683952Potentiation of PTX-induced antitumor activity against human SW620/Ad300 cells xenografted in BALB/c mouse assessed as reduction in tumor weight at 6 mg/kg/day, ig for 21 days relative to PTX alone
AID1416320Inhibition of p-gp in human MES-SA/DX5 cells assessed as increase in rhodamine 123 accumulation by measuring ratio of fluorescence intensity of compound-treated cells to control cells at 25 uM preincubated for 20 mins followed by rhodamine 123 addition an
AID1502900Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 12.5 ug/ml2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1813132Selectivity index, ratio of IC50 for cytotoxicity against mouse L929 cells to EC50 for inhibition of P-gp in human LCC6MDR cells assessed as reversal of paclitaxel resistance2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
AID332135Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of doxorubicin ED50 without drug to doxorubicin ED50 with drug at 3 ug/ml after 6 days by BCA assay1997Journal of natural products, Nov, Volume: 60, Issue:11
Multidrug-resistance modulators from Stephania japonica.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1502770Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1461763Inhibition of MDR1 in human MCF7/ADR cells assessed as potentiation of verapamil-induced cytotoxicity by measuring cell growth (Rvb = 78.2%)2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Recent synthetic and medicinal perspectives of tryptanthrin.
AID514306Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as induction of rhodopsin expression at 3 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1459760Inhibition of ABCB1 (unknown origin) expressed in human Flp-In-293 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID143480Inhibitory activity when combined with cisplatin (uM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1502728Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as increase in EtBr accumulation by measuring relative final fluorescence incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1352565Inhibition of P-gp in human MCF7/ADR cells assessed as concentration required to restore doxorubicin accumulation in cells after 150 mins by fluorescence assay relative to MCF7 cells2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID406186Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of doxorubicin2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID682079TP_TRANSPORTER: inhibition of Calcein-AM transport in HL60-MRP1 cells2006Chemico-biological interactions, Feb-25, Volume: 159, Issue:3
Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3).
AID1338193Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in doxorubicin accumulation at 2 uM measured after 150 mins by fluorescence spectrophotometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID45736Reversal of sensitivity of multidrug resistant chinese hamster ovary cell line CHRC/5 expressed as concentration that restores 50% of cytotoxic activity of 5 ug/mL toward doxorubicin1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Synthesis and activity against multidrug resistance in Chinese hamster ovary cells of new acridone-4-carboxamides.
AID101592Inhibitory activity when combined with 5-Fluorouracil (uM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1391798Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID1530109Stimulation of P-gp ATPase activity (unknown origin) at 0.5 mM preincubated for 5 mins followed by Mg-ATP addition measured after 40 mins by ATP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1207719Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID74169Decrease in developed tension of the right atrium of guinea pig expressed as the negative chronotropy.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID1552590Permeability of compound at 25 ug/ml at pH 7.4 incubated for 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease.
AID288186Permeability coefficient through artificial membrane in presence of stirred water layer at 200 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1888846Antibacterial activity against Staphylococcus aureus 1199B measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1631738Reversal of P-gp-mediated resistance in human MCF7/ADR cells assessed as reduction in ADR IC50 at 200 nM after 48 hrs by MTT assay relative to control2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1739434Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM measured per mg protein upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID340929Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 1 mg/liter daptomycin2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Modulation of the cellular accumulation and intracellular activity of daptomycin towards phagocytized Staphylococcus aureus by the P-glycoprotein (MDR1) efflux transporter in human THP-1 macrophages and madin-darby canine kidney cells.
AID1235693Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1155069Antiplasmodial activity against Plasmodium falciparum C2GC03 expressing wild-type pfcrt allele assessed as parasite growth at 800 nM after 72 hrs by SYBR Green I-based fluorescence assay relative to control2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.
AID1320724Inhibition of P-gp in human KB-V1/Vbl cells assessed as calcein-AM accumulation preincubated for 15 mins followed by calcein-AM addition measured after 15 mins by fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Halogenated naphthochalcones and structurally related naphthopyrazolines with antitumor activity.
AID210307Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.
AID1504335Inhibition of ABCB1 in human SW620/AD300 cells assessed as reduction in Rh123 efflux at 2 uM treated followed by Rh123 addition in Rh123 free medium for 30 to 120 mins by flow cytometry2018European journal of medicinal chemistry, Jan-01, Volume: 143Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance.
AID722220Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID1866897Permeability for across blood brain barrier by PAMPA2022European journal of medicinal chemistry, Apr-15, Volume: 234Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1235764Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 64 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1307802Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as relaxation of calcium-induced contraction2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1534777Effective permeability of the compound at 100 mg/ml incubated for 16 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID368400Reversal of P-glycoprotein-mediated doxorubicin resistance in human doxorubicin-sensitive K562 cells assessed as ratio of doxorubicin IC50 to doxorubicin IC50 in presence of parent compound at 1 uM2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
N,N-bis(cyclohexanol)amine aryl esters: a new class of highly potent transporter-dependent multidrug resistance inhibitors.
AID695900Inhibition of Staphylococcus aureus SA-1199B NorA expressed in Escherichia coli DH10B assessed as inhibition of Hoechst 33342 dye efflux at 2 ug/ml after 150 to 160 secs by spectrofluorometric analysis in presence of 50 uM Mg2+2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles.
AID88854Effect on cellular accumulation of Vincristine (VCR) in multidrug resistant human ovarian cancer 2780AD cells at 1 ug/mL1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Modulation of multidrug resistance by taxuspine C and other taxoids from Japanese yew.
AID1235703Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as isoniazid MIC at 8 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1486977Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 12 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM)2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1504327Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as potentiation of colchicine-induced cytotoxicity by measuring fold reduction in colchicine IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition measured after 72 hrs2018European journal of medicinal chemistry, Jan-01, Volume: 143Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance.
AID1427565Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 30 mins in presence of NADPH2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID324432Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1784754Drug metabolism in mouse liver microsomes incubated for 2 hrs by UPLC-MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT
AID480944Inhibition of human MDR1 expressed in MDCK cells assessed as fluorescence activity at 30 uM after 1.5 hrs by rhodamine 123 efflux test2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
Identification of serotonin 5-HT1A receptor partial agonists in ginger.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID399030Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780 cells assessed as calcein accumulation at 0.25 ug/ml after 15 mins relative to control2005Journal of natural products, Nov, Volume: 68, Issue:11
Bioactive tetrahydrofuran lignans from Peperomia dindygulensis.
AID1215133Decrease of CYP3A1 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestine by Western blot analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1631742Half life in Sprague-Dawley rat liver microsomes at 100 uM by HPLC-UV analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1129456Solubility of the compound in PBS buffer after 45 mins2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1435955Half life in human liver microsomes after 10 to 60 mins in presence of NADPH by LC/MS/MS analysis2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID75201Coronary perfusion pressure of isolated guinea pig heart at dose 0.5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID653471Induction of ATPase activity of p-glycoprotein at 200 uM by luminescence assay relative to control2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID1235717Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 32 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1502888Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to ofloxaci2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1533105Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 0.78 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1833371Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/ABCB1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 91.40 +/- 23.32 nM)
AID1502756Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1481909Effect on plasma concentration of doxorubicin in Sprague-Dawley rat at 5 mg/kg, iv co-administered with doxorubicin measured after 8 hrs by LC-MS/MS analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID1459775Inhibition of P-gp in human KBVIN cells assessed as potentiation of doxorubicin-induced cytotoxicity at 2.5 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1336849Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of actinomycin D-induced cytotoxicity by measuring compound concentration required for reduction of actinomycin D IC50 by half after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID1603233Permeability of the compound assessed as molar fraction in donor well at 0.5 mM measured immediately by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1739848Inhibition of ABCB1 in human HeLa S3 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold change in doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to doxorubicin IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID1141749Myorelaxant activity in endothelium-free rat thoracic aorta assessed as inhibition of 80 mM of KCl-induced contraction2014European journal of medicinal chemistry, Jun-10, Volume: 80Influence of the alkylsulfonylamino substituent located at the 6-position of 2,2-dimethylchromans structurally related to cromakalim: from potassium channel openers to calcium entry blockers?
AID230568Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vincristine (nM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID379507Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs by SRB method1999Journal of natural products, May, Volume: 62, Issue:5
Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance.
AID1696660Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
AID1239169Inhibition of p-glycoprotein in human adriamycin-resistant MCF7 cells assessed as increase of adriamycin accumulation at 20 uM after 1 hr by by LC-MS/MS analysis relative to control2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Inhibitory Effects of Highly Oxygenated Lanostane Derivatives from the Fungus Ganoderma lucidum on P-Glycoprotein and α-Glucosidase.
AID1602180Metabolic stability in mouse liver microsomes at 1 uM in presence of NADPH incubated for 5 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1239235Modulation of P-gp in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.
AID1761202Induction of apoptosis in human KBV cells assessed as accumulation of cells in Sub-G1 phase at 10 uM measured by flowcytometry method (Rvb = 1.9%)2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID185794Compound was tested for the % inhibition rate of infarct size (myoglobin depleted area) on iv administration 15 min prior to the ligation at a dose of 0.3 mg/kg.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.
AID90144Potency relative to progesterone in reducing the difference in reversing of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1765292Permeability of compound by PAMPA-BBB assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.
AID1164948Solubility of the compound in DMEM/FBS medium2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID324583Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1739132Stability of the compound in human plasma assessed as half life incubated for 3 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Chemical profiling of HIV-1 capsid-targeting antiviral PF74.
AID1209974Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1273409Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 256 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1585801Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 3 uM after 30 mins by LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
AID1444094Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1517888Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID604023Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1210073Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1446764Intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1761211Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID722218Cytotoxicity against human K562 cells at 1 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).
AID1209973Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1631735Reversal of P-gp-mediated resistance in adriamycin-resistant human HepG2 cells assessed as reduction in ADR IC50 at 100 nM after 48 hrs by MTT assay relative to control2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1321557Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as forward scattered light at 22 uM preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry (Rvb = 455.7 to 2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID1129450Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM after 60 mins2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1192731Permeability of the compound in PBS/EtOH buffer at 100 ug/ml by PAMPA2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID679893TP_TRANSPORTER: inhibition of cyclosporin A transcellular transport by verapamil at a concentration of 100uM in MDR1-expressing MDCKII cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID1230204Permeability of the compound by PAMPA-BBB assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1386188Increase in adriamycin accumulation in human MCF7 cells at 10 ug/ml after 1 hr by flow cytometry2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID1391817Inhibition of P-gp in human K562/A02 cells assessed as increase in adriamycin accumulation at 5 uM after 2.5 hrs by flow cytometry method2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID20050Human absorption A (%)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID1180214Inhibition of L-type calcium channel in endothelium-intact Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction at 100 uM relative to untreated control2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1368306Inhibition of P-gp in human K562/Dox cells assessed as increase in nuclear accumulation of pirarubicin by spectrofluorometric assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Design and synthesis of aminoester heterodimers containing flavone or chromone moieties as modulators of P-glycoprotein-based multidrug resistance (MDR).
AID1833385Inhibition of human CYP3A4 preincubated for 10 mins followed by substrate and NADP addition measured after 30 mins by fluorescence assay
AID1235763Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID321882Apparent permeability from apical to basolateral side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
AID1196793Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in presence of NADPH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1481873Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold reduction in doxorubicin IC50 at 5.0 uM after 48 hrs by MTT assay relative to doxorubicin alone2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID1351577Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 30 mM KCl-induced contraction after 15 mins in presence of 1 uM glibenclamide2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID330506Ratio of permeability from apical to basolateral over basolateral to apical side of human Caco-2 cell membrane2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
AID1502840Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 32 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID682152TP_TRANSPORTER: drug resistance (paclitaxel) in HCT15/CL02 cells2003Anti-cancer drugs, Feb, Volume: 14, Issue:2
Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.
AID653450Induction of adriamycin accumulation in human K562 cells at 0.3 to 10 uM by flow cytometry2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
AID681460TP_TRANSPORTER: increase in Vinblastine intracellular accumulation (Vinblastine: 0.0125 uM, Verapamil: 25 uM) in RHC1 cells1995Biochemical pharmacology, May-11, Volume: 49, Issue:9
Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells.
AID250135Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID1502879Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring reduction in ofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative to ofloxa2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID762395Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as EtBr accumulation at 150 mg/L measured every 3 mins interval for 45 mins by spectrofluorometric method2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1273466Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 128 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID703732Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocyte assessed as inhibition of [3H]chloroquine uptake at 100 uM measured from 1 to 2 hrs2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling.
AID1628201Inhibition of P-gp ATPase activity in human A549/CDDP cells at 200 uM by luminescence assay (Rvb = 706683 +/- 23554 RLU)2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer.
AID1530099Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cell cycle arrest by measuring accumulation at sub-G1 phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2.22019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1357215Half life in mouse liver microsomes in presence of NADPH regeneration system2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities.
AID1603228Permeability of the compound assessed as molar fraction in acceptor well at 0.5 mM measured after 2 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1352675Effective permeability at 25 ug/ml after 18 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1491365Binding affinity to BACE1 (unknown origin) by SPR method2017European journal of medicinal chemistry, Sep-08, Volume: 1372-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
AID1816692Metabolic stability in human liver microsomes assessed as half life in presence of NADPH at 1 uM by LC-MS/MS analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
AID1275777Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 by spectroscopic method2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID101596Inhibitory activity when combined with vincristine (nM) in MCF-7 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID102850Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, by Granulation (SSC) at 5 ug/mL.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Discovery and biological evaluation of a new family of potent modulators of multidrug resistance: reversal of multidrug resistance of mouse lymphoma cells by new natural jatrophane diterpenoids isolated from Euphorbia species.
AID194923Percent Catecholamine-depletion in heart by administering a dose of 2 x 45 umol/kg, perorally to 4 spontaneously hypertensive rats (SHR).1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID1338183Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vincristine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID150755Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1283422Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in vinblastine IC50 at 3 uM by MTT assay2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Optimization by Molecular Fine Tuning of Dihydro-β-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.
AID1533115Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID230555Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with taxol (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1502862Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1273395Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as accumulation of EtBr at 0.25 ug/ml after 3 days by real time fluorometric analysis relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1377751Effective permeability of the compound after 2.5 hrs at 25 degC by PAMPA assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID351896Chemosensitizing activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes as IC50 ratio chloroquine +/- 500nM by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1459768Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM by SRB assay relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors.
AID1764400Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Development of an
AID379729Reversal of multidrug resistance in human 2780AD cells assessed as accumulation of calcein at 25 ug/mL after 15 mins by fluorescence technique relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii.
AID676757Inhibition of Multidrug resistance efflux pump in Mycobacterium smegmatis str. MC2 155 ATCC 700084 assessed as increase in normalized ethidium bromide fluorescence efflux at 0.5 MIC level by fluorimetric assay2012Journal of natural products, Jul-27, Volume: 75, Issue:7
Putative mycobacterial efflux inhibitors from the seeds of Aframomum melegueta.
AID1502776Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 128 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1348630Intrinsic clearance in human liver microsomes at 5 uM preincubated for 5 mins followed by NADPH addition measured after 45 mins by UPLC-MS/MS analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1429933Inhibition of P-gp in human LoVo/DX cells assessed as reduction in Rhodamine123 efflux at 2.5 to 10 uM preincubated for 15 mins followed by Rhodamine123 addition measured after 1 hr by flow cytometry2017European journal of medicinal chemistry, Feb-15, Volume: 127Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity.
AID1502851Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID472410Cytotoxicity against human multidrug-resistant KB-C2 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
AID681880TP_TRANSPORTER: inhibition of bimane-GS efflux in the presence of Verapamil at a concentration of 25uM in MRP4-expressing HepG2 cells2004The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.
AID1427563Metabolic stability in human liver microsomes assessed as metabolic rate measured after 30 mins in presence of NADPH2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID45790Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1167504Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.
AID1558703Half life in mouse liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis
AID364887Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID1418868Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold reduction in doxorubicin IC50 at 4 uM after 72 hrs by MTT assay relative to doxorubicin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1770547Metabolic stability of the compound in human liver microsomes assessed as clearance at 10 uM incubated for 10 mins in presence of NADPH by UPLC-MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.
AID1207176Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID714414Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID90142Ratio of effect of compound on VBL accumulation (antiPgp activity) to its intrinsic cellular toxicity;2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1169855Half life in human liver microsomes at 1 uM after 30 mins in presence of NADPH2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Structure-guided development of deoxycytidine kinase inhibitors with nanomolar affinity and improved metabolic stability.
AID1235767Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ethidium bromide MIC at 8 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1234530Inhibition of human ABCB1 expressed in mouse L5178Y cells using rhodamine 123 as substrate assessed as ratio of fluorescent intensity in ABCB1 expressing L5178Y cells to wild type L5178Y cells at 1 uM after 20 mins by flow cytometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Discovery of substituted 1,4-dihydroquinolines as novel class of ABCB1 modulators.
AID427811Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as inhibition of oxygen consumption at 30 ug/mL after 2 hrs by polarographically with Clark electrode2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID427722Reversal of MRP1-mediated doxorubicin-resistance in human 2008/MRP1 cells assessed as reduction of doxorubicin IC50 percent by half2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
AID389760Inhibition of verapamil-induced residual ATPase activity in lipid activated mouse P-glycoprotein mdr3 cys-less mutant assessed as ATP hydrolysis per ug of protein2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
AID714419Reversal of P-gp-mediated doxorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1639312Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay2019Journal of natural products, 04-26, Volume: 82, Issue:4
Conolodinines A-D, Aspidosperma- Aspidosperma Bisindole Alkaloids with Antiproliferative Activity from Tabernaemontana corymbosa.
AID150735High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1631484Growth inhibition of human KB/VJ300 cells after 72 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Vobatensines A-F, Cytotoxic Iboga-Vobasine Bisindoles from Tabernaemontana corymbosa.
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID1129602Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay2014European journal of medicinal chemistry, Apr-09, Volume: 76SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity.
AID1288622Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors.
AID165538Inhibition of [Ca2+] uptake in rabbit pulmonary artery, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1336847Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring fold reduction in paclitaxel EC50 at 5 uM after 72 hrs by MTT assay relative to untreated control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Quercetin-glutamic acid conjugate with a non-hydrolysable linker; a novel scaffold for multidrug resistance reversal agents through inhibition of P-glycoprotein.
AID209803Inhibitory activity when combined with taxol (nM) in T24 cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1502804Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID75202Coronary perfusion pressure of isolated guinea pig heart at dose 5 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID88421In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 50 (uM) of infected host2000Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18
A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID1235797Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in ofloxacin MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1368934Inhibition of MRP1 (unknown origin) expressed in BHK21 cells assessed as GSH efflux at 20 uM incubated for 3 hrs measured every 30 secs for 2 mins by GSH reductase enzyme based assay (Rvb = 100%)2018Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
Monoterpene indole alkaloid azine derivatives as MDR reversal agents.
AID1704095Cytotoxicity against human HUVEC cells assessed as reduction in cell viability at 10 uM incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1753998Permeability of the compound in PBS/EtOH buffer (7:3) incubated for 16 hrs by UV plate reader based PAMPA-BBB assay2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
AID509765Potentiation of adriamycin-induced cytotoxicity against human KB cells at 16 uM after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity.
AID1693561Effective permeability of compound in PBS/EtOH buffer (7:3) at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
AID167653Calcium channel blocking activity in vitro in rabbit thoracic aorta preparation (n=4) by using linear regression analysis1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects.
AID307743Cytotoxicity against human A2780 cells assessed as cell viability at 2 uM2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and structure-activity relationships of taxuyunnanine C derivatives as multidrug resistance modulator in MDR cancer cells.
AID1243600Inhibition of ABCB1 in multidrug resistant human COLO320 cells assessed as fluorescence activity ratio at 20 uM incubated for 10 mins by flow cytometry based rhodamine-123 accumulation assay (Rvb = 0.62 No_unit)2015Journal of natural products, Sep-25, Volume: 78, Issue:9
Epoxylathyrol Derivatives: Modulation of ABCB1-Mediated Multidrug Resistance in Human Colon Adenocarcinoma and Mouse T-Lymphoma Cells.
AID1530705Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID193717Hypotensive effect in Spontaneously hypertensive rats as maximum decrease in systolic blood pressure at 10 mg/kg, po dose1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID1603226Permeability of the compound assessed as molar fraction in donor well at 0.5 mM measured after 2 hrs by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID1649390Inhibition of human ERG
AID728952Myorelaxant activity in albino rat aorta rings assessed as relaxation of KCl-induced contraction of aorta rings2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action.
AID513646Induction of autophagy in pretreated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as calpain activation at 1 uM followed by doxycyline treatment measured after 24 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID288194Intrinsic artificial membrane permeability coefficient, log P0 of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1502764Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring erythromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1354580Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of 0.1 uM of vincristine by MTT assay2018Journal of natural products, 05-25, Volume: 81, Issue:5
Ajmaline, Oxindole, and Cytotoxic Macroline-Akuammiline Bisindole Alkaloids from Alstonia penangiana.
AID656840Effect on P-gp ATPase activity assessed as relative light units at 200 uM by P-gp-GloTM assay (Rvb = 242328 +/- 1398 RLU)2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors.
AID90143Potency relative to progesterone in reducing the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1530098Cell cycle arrest in human KBV cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.62 +/- 1.54%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1413458Permeability of the compound by PAMPA
AID681472TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.035 uM, Verapamil: 100 uM) in CC531mdr+ cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID1502826Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1758181Inhibition of P-glycoprotein in human MCF7/ADR cells assessed as reversal fold by measuring reduction in doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK-8 assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
AID1386181Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular accumulation of adriamycin by measuring increase in fluorescence intensity at 10 ug/ml after 24 hrs by fluorescence microscopic analysis2018Journal of natural products, 09-28, Volume: 81, Issue:9
Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata.
AID1603236Permeability of the compound assessed as rate constant for coming off the membrane by PAMPA2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A
AID551247Half life in mouse microsome by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis.
AID562106Chemosensitization of pyrimethamine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1235802Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as reduction in ethidium bromide MIC at 128 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1907125Stability in human liver microsomes assessed as half life measured upto 60 mins in presence of NADPH by LC-MS/MS analysis2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
4,5-Dihydroxypyrimidine Methyl Carboxylates, Carboxylic Acids, and Carboxamides as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease.
AID1243944Metabolic stability in human liver microsomes assessed as compound remaining incubated for 60 mins in absence of NADPH2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID377596Inhibition of human MDR1-mediated rhodamine efflux in mouse L5178 cells assessed as fluorescence activity ratio at 10 ug/mL by flow cytometry relative to untreated control2006Journal of natural products, Jun, Volume: 69, Issue:6
Euphoportlandols A and B, tetracylic diterpene polyesters from Euphorbia portlandica and their anti-MDR effects in cancer cells.
AID1769826Permeability of the compound across apical to basolateral membrane in human Caco-2 cells incubated for 2 hrs by LC-MS/MS analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
AID696927Inhibition of ABC transporter in human HCT15 cells assessed as calcein-AM efflux up to 100 uM2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID72888Increase in the accumulation of vincristine in multi-drug resistant GC3/Cl (human adenocarcinoma) cell line in vitro.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and chemical characterization of N-substituted phenoxazines directed toward reversing vinca alkaloid resistance in multidrug-resistant cancer cells.
AID248349inhibitory activity of compound against Multidrug resistant HCT116/VM46 cell line treated with Vinblastine2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
AID1273456Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 32 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1419453Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by spectroflurometry relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy.
AID1631483Growth inhibition of human KB/S cells after 72 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Vobatensines A-F, Cytotoxic Iboga-Vobasine Bisindoles from Tabernaemontana corymbosa.
AID1764870Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 30 mins2021European journal of medicinal chemistry, Jun-05, Volume: 218Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.
AID1738699Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as minimal concentration required for the effect by flow cytometric analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin.
AID1273450Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 64 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID401291Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 11.0 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID337344Inhibition of human MDR1 expressed in mouse L5178 cells assessed as fluorescence activity ratio at 23 uM by rhodamine 123 exclusion test relative to wild type mouse L5178 cells2003Journal of natural products, Jul, Volume: 66, Issue:7
Jatrophane diterpenoids from Euphorbia mongolica as modulators of the multidrug resistance of L5128 mouse lymphoma cells.
AID1254927Half life in human liver S9 microsomes in presence of NADPH by LC-MS/MS method2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1502713Antimycobacterial activity against Mycobacterium avium isolate MAV4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502807Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 64 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1566022Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 2.92 +/- 0.31 nM)2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID1338184Selectivity index, ratio of IC50 for cytotoxicity against mouse L929 cells to EC50 for inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of paclitaxel cytotoxic IC50 by half2017European journal of medicinal chemistry, Jan-05, Volume: 125Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors.
AID1271450Vasodilator activity in Sprague-Dawley rat mesentric artery assessed as reduction in of K+-induced contraction relative to control2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and fluorescent study of 5-phenyl furocoumarin derivatives as vasodilatory agents.
AID406201Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of paclitaxel2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID1062338Therapeutic index, ratio of IC50 for mouse L929 cells to EC50 for modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.
AID1446766Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID681582TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1733394Induction of cell cycle arrest in human KBV cells assessed as accumulation at G1/G0 phase at 10 uM after 24 hrs by PI/RNaseA staining based flow cytometric analysis (Rvb = 49.09 +/- 0.35%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1785055Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as paclitaxel IC50 by measuring reversal fold at 2 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay relative to
AID271725Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1481892Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular Rh123 accumulation at 5.0 uM measure up to 90 mins by flow cytometric analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID94487Increase in the accumulation of vinblastine in multi-drug resistant KB8-5 (HeLa variant) cell line in vitro.1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Synthesis and chemical characterization of N-substituted phenoxazines directed toward reversing vinca alkaloid resistance in multidrug-resistant cancer cells.
AID377773Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 10 ug/mL after 2 hrs relative to control2005Journal of natural products, Apr, Volume: 68, Issue:4
Taxoids and abietanes from callus cultures of Taxus cuspidata.
AID1625123Permeability of the compound in pH 7.4 PBS at 200 uL after 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1873790Cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as inhibition of calcein-AM efflux at 20 uM incubated for 15 mins by calcein-AM staining based flow cytometry analysis2022Bioorganic & medicinal chemistry, 08-01, Volume: 67Cytotoxicity of cinchona alkaloid organocatalysts against MES-SA and MES-SA/Dx5 multidrug-resistant uterine sarcoma cell lines.
AID236918Apparent permeability of the compound was determined in MDCK (madin darby canine kidney) strain I; Activity = Papp 10e-62005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
In silico prediction of membrane permeability from calculated molecular parameters.
AID1315282Inhibition of LAT3 in human LNCAP cells assessed as inhibition of [3H]L-leucine uptake at 10 uM after 15 mins by liquid scintillation counting method relative to control2016Journal of natural products, 05-27, Volume: 79, Issue:5
Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis.
AID1696659Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
AID150757P-gp activity was measured by a direct transport assay, using polarized LLC-MDR1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID502263Cytotoxicity against hamster BHK21 cells after 96 hrs by MTT assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1.
AID1502801Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = >512 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1381448Apparent permeability from basolateral to apical side in MDCK cells2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
AID1502889Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 25 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID475690Clearance in human2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
AID514304Protection of neurodegeneration in zebrafish Huntington's disease model expressing EGFP-tagged huntingtin exon with EGFP-HDQ71 in rod photoreceptor assessed as decrease in EGFP-HDQ74 aggregation at 3 uM2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID679222TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 1 uM, Verapamil: 100 uM) in membrane vesicles from MRP7-expressing HEK293 cells2003Molecular pharmacology, Feb, Volume: 63, Issue:2
Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10).
AID1215170Tmax in Sprague-Dawley rat portal vein plasma at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1502744Inhibition of multidrug resistance efflux pump in Mycobacterium avium ATCC 25291 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 8 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID537734Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1358239Inhibition of P-gp in human MCF7/ADR cells assessed as cell viability after 48 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell.
AID1750901Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay
AID395037Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID1352554Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM preincubated with cells followed by compound washout and subsequent incubation for 12 hrs prior to addition of d2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID252858Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (3 uM) and Vinblastine (VNB)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID1321562Inhibition of MDR1-mediated efflux-pump activity in mouse L5178Y cells expressing human MDR1 assessed as mean fluorescence intensity at 22 uM preincubated for 10 mins followed by rhodamine-123 addition measured after 20 mins by flow cytometry (Rvb = 7.1 t2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance.
AID677694Permeability of the compound at pH 7.4 by PAMPA2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators.
AID1704104Reversal of multidrug resistance activity in human A2780/CDDP cells assessed as potentiation of CDDP-induced cytotoxicity by measuring reversal ratio at 10 uM incubated for 48 hrs in presence of CDDP by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1481510Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-mediated cytotoxicity by measuring reduction in ADR IC50 at 5 uM after 48 hrs by MTT assay relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID1454121Half life in human hepatic microsomes at 0.1 uM by HPLC-MS/MS method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Structural development of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs) to improve metabolic stability, and investigation of metabolic fate.
AID1502868Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502846Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502897Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 12.5 ug/ml2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1893726Metabolic stability in CD-1 mouse liver S9 fraction assessed as half life at 1 micromol/L in presence of NADPH measured upto 24 hrs by LC-MS/MS analysis
AID245888Maximum intracellular vinblastine accumulation of the KB/MDR cells caused by the compound in 1 h2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
AID487884Binding affinity to P-gp at 5 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID230560Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with vinblastine (nM) in MCF-7/VP cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID1533612Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory.
AID1761214Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 5 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID1633098Inhibition of Pgp in human HepG2/ADM cells assessed as potentiation of ADM-induced cytotoxicity by measuring reduction in ADM IC50 at 20 uM incubated for 72 hrs by MTT assay relative to control2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID755309Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 2 uM after 2 hrs by microplate fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1704112Inhibition of P-gp mediated multidrug resistance activity in human A2780T cells assessed as increase in intracellular DOX accumulation at 10 uM incubated for 4 hrs in presence of doxorubicin by fluorescence microsocopy2020European journal of medicinal chemistry, Oct-15, Volume: 204New Seco-DSP derivatives as potent chemosensitizers.
AID1164950Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for methicillin-resistant Staphylococcus aureus NRS 702014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
AID1502853Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring reduction in ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay relative t2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID345307Intrinsic cytotoxicity against mouse NIH/3T3 cells overexpressing MDR1 at 10 uM after 72 hrs by MTT assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
AID714417Reversal of P-gp-mediated vinblastin-resistance in human LCC6MDR cells after 5 days by MTS assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.
AID1903284Cytotoxicity against human KBV cells assessed as decrease in cell survival rate at 10 uM measured after 72 hrs in presence of paclitaxel by MTT assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles.
AID1065213Permeability coefficient, log Pe of the compound at pH 7.4 by PAMPA2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Development of novel Vitamin D Receptor-Coactivator Inhibitors.
AID1502858Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 assessed as potentiation of ofloxacin-induced antibacterial activity by measuring ofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID105432Potency relative to progesterone in reversing of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID401292Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of adriamycin ED50 without drug to adriamycin ED50 with drug at 15.4 uM after 6 days by BCA assay1996Journal of natural products, Jan, Volume: 59, Issue:1
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
AID1481500Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular adriamycin accumulation at 5 uM after 2.5 hrs by spectrofluorimetric analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID75927Potency expressed as EC30 for the negative chronotropic activity.1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
AID513158Inhibition of heme crystallization after 16 hrs2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID1391815Inhibition of P-gp in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring adriamycin IC50 at 5 uM preincubated for 24 hrs followed by compound wash out and subsequent addition of adriamycin after 6 hrs measured af2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID659472Effective permeability across porcine polar brain lipid after 4 hrs by PAMPA2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
5-imino-1,2,4-thiadiazoles: first small molecules as substrate competitive inhibitors of glycogen synthase kinase 3.
AID1381449Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side of MDCK cells2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
AID671709Inhibition of P-glycoprotein overexpressed in human Caco2 cells assessed as increase in digoxin accumulation at 5 to 25 uM incubated for 1.5 hrs prior to digoxin treatment measured after 1.5 hrs by LC/MS/MS analysis2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells.
AID351897Chemosensitizing activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes as IC50 ratio chloroquine +/- 500 nM by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID683266Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as paclitaxel-induced cytotoxicity at 10 uM after 72 hrs by SRB assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
AID1207721Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1163836Potentiation of gefitinib-induced cytotoxicity against human H460/Vbl cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
AID1472790Cytotoxicity in P-gp tranfected HEK293 cells assessed as cell survival at 10 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1740454Metabolic stability in mouse hepatocytes assessed as hepatic extraction ratio at 1 uM up to 120 mins by HPLC-MS/MS analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase.
AID1502727Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as increase in EtBr accumulation by measuring relative final fluorescence incubated for 60 mins by real-time fluorometry relative to control2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID77838Heart rate of isolated guinea pig heart at dose 0.005 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID1673433Reversal of P-gp mediated multidrug resistance in human K562/A02 cells overexpressing P-gp assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 5 uM after 48 hrs by MTT assay (Rvb = 55.47 +/- 1.67 uM)2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID351907Chemosensitizing activity as 500nM potentiation of quinine effect after 72 hrs against chloroquine-resistant transporter 106/1'76N mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1292332Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1518033Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM preincubated for 5 mins followed by NADPH addition and measured after 30 mins by LC-MS/MS analysis relative to control2019European journal of medicinal chemistry, Dec-15, Volume: 184Identification of novel non-nucleoside vinyl-stilbene analogs as potent norovirus replication inhibitors with a potential host-targeting mechanism.
AID150752Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1275775Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine sensitive Plasmodium falciparum NF542016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
AID669854Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by flow cytometry analysis2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents.
AID1199782Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID105423Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
AID1733377Reversal of Pgp-mediated multidrug resistance in human KBV cells assessed as vincristine IC50 at 10 uM after 72 hrs in presence of vincristine by MTT assay (Rvb = 425.91 +/- 35.70 nM)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1733379Reversal of MRP2-mediated multidrug resistance in human KBV cells assessed as cisplatin IC50 at 10 uM after 72 hrs in presence of cisplatin by MTT assay (Rvb = 4902.89 +/- 130.33 nM)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID1481514Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular Rh123 accumulation at 5 uM up to 90 mins by flow cytometry2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID762402Inhibition of multidrug resistance efflux pump in Mycobacterium smegmatis MC2 155 ATCC 700084 assessed as EtBr accumulation at 150 mg/L measured every 3 mins interval for 45 mins by fluorometric method2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1728593Inhibition of ABCB1 in human resistant COLO 320 cells assessed as multidrug resistance reversing activity by measuring fluorescence activity ratio at 20 uM preincubated for 10 mins followed by rhodamine-123 addition and measured after 20 mins by flow cyto2021European journal of medicinal chemistry, Jan-15, Volume: 210Alkylated monoterpene indole alkaloid derivatives as potent P-glycoprotein inhibitors in resistant cancer cells.
AID327169Apparent permeability across parallel artificial membrane2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin.
AID1129447Intrinsic clearance in mouse microsomes at 1 uM2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1888882Inhibition of NorA in Staphylococcus aureus 1199B assessed as accumulation of ethidium bromide at 50 ug/ml by measuring fluorescence intensity measured at 5 mins interval for 40 mins by fluorescence spectrophotometry2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1502788Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of erythromycin-induced antibacterial activity by measuring reduction in erythromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relative to 2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1636268Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors.
AID1215348Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by LC-MS/MS analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID112426Effect on acute thrombic death induced by collagen in mice1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID331364Effect on membrane lipid fluidity in human K562 cells2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID666859Reversal of MRP1-mediated drug resistant in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM after 5 days by MTS assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells.
AID249672Effect of compound on multidrug resistance in murine L-5178 cells at 10 ug/ml concentration; expressed as fluorescence activity ratio (treated/untreated cells)2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
3-Arylidene-1-(4-nitrophenylmethylene)-3,4-dihydro-1H-naphthalen-2-ones and related compounds displaying selective toxicity and reversal of multidrug resistance in neoplastic cells.
AID1167514Modulatory activity at P-gp assessed as MDR-reversing activity by measuring potentiation of doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay relative to untreated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.
AID1246311Intrinsic clearance in human microsomes2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1352556Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM preincubated with cells followed by compound washout and subsequent incubation for 24 hrs prior to addition of d2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1502799Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1602584Half life in ICR/CD1 mouse hepatocytes at 1 uM up to 120 mins by LC-MS/MS analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer.
AID1319973Permeability of the compound by PAMPA assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID1684002Reversal of resistance to paclitaxel-induced cytotoxicity in human KB-3-1 cells assessed as reduction in paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay
AID1273420Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 16 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1511118Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID331369Toxicity in Sprague-Dawley rat assessed as ventricular fibrillation by measuring aconitine nitrate level at 2 mg.kg, iv by echocardiography2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID1404017Permeability of the compound at 500 uM after 8 hrs by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID1352557Inhibition of P-gp in human MCF7/ADR cells assessed as increase in doxorubicin accumulation in cells after 150 mins by fluorescence assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance.
AID1853713Metabolic stability in mouse liver microsomes assessed as half-life at 1 uM measured upto 15 mins in the presence of NADPH as co-factor by LC-MS/MS analysis2021RSC medicinal chemistry, Dec-15, Volume: 12, Issue:12
Potency and metabolic stability: a molecular hybrid case in the design of novel PF74-like small molecules targeting HIV-1 capsid protein.
AID1530101Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cell cycle arrest by measuring accumulation at S phase at 10 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.54 +/2019European journal of medicinal chemistry, Jan-01, Volume: 161Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
AID1502753Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring reduction in clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay relativ2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1502827Inhibition of multidrug resistance efflux pump in Mycobacterium avium 104 mc'2 3 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 16 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID360084Inhibition of human MRP1 mediated LTC4 transport in hamster BHK21 cells in presence of glutathione by rapid filtration technique2007The Journal of biological chemistry, Oct-26, Volume: 282, Issue:43
(R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1.
AID45614Displacement of [3H]nitrendipine binding to L-type calcium channel of Guinea pig cerebral cortex membranes1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID1673434Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as cell growth inhibition after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells.
AID482109Inhibition of P-gp-mediated paclitaxel-resistance in P-glycoprotein-expressing human LCC-6 cells assessed as fold decrease in paclitaxel IC50 for cytotoxic activity at 1 uM after 5 days by MTS assay relative to control2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Design and syntheses of permethyl ningalin B analogues: potent multidrug resistance (MDR) reversal agents of cancer cells.
AID1167505Modulatory activity at P-gp in human K562/DOX cells assessed as maximum increase nuclear concentration of pirarubicin by spectrofluorometric assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.
AID1449542Half life in human intestinal microsomes2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID150616Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID1481496Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-mediated cytotoxicity by measuring reduction in ADR IC50 at 5 uM preincubated for 24 hrs followed by compound washout for 6 hrs and subsequent addition of adriamycin measur2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
AID1391801Inhibition of P-gp in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring fold reduction in adriamycin IC50 at 5 uM after 48 hrs by MTT assay relative to adriamycin alone2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors.
AID1199781Inhibition of p-gp (unknown origin) in doxorubicin-resistant human K562/R7 cells assessed as increase in daunorubicin accumulation measured as fluorescence ratio at 10 uM incubated for 1 hr with 10 uM daunorubicin by flow cytometry relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Synthesis of new steroidal inhibitors of P-glycoprotein-mediated multidrug resistance and biological evaluation on K562/R7 erythroleukemia cells.
AID1129437Metabolic stability in human microsomes assessed as compound remaining at 1 uM in presence of NADPH2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1785075Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as reduction in colchicine IC50 at 2 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay
AID7779Oral bioavailability in human2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates.
AID681581TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID619539Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as ratio of IC50 for vinblastine-induced cytotoxicity in absence of drug to IC50 for vinblastine-induced cytotoxicity in presence of 10 uM of drug by MTT assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1461786Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM preincubated for 5 mins followed by NADPH addition measured after 30 mins relative to control2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis and biological evaluation of fluoro-substituted 3,4-dihydroquinazoline derivatives for cytotoxic and analgesic effects.
AID1900247Permeability of the compound at pH 7.4 PBS/EtOH buffer (70:30) by PAMPA-BBB assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.
AID762407Antimicrobial activity against Mycobacterium smegmatis MC2 155 ATCC 700084 at 40 mg/L after 72 hrs by MTT assay in presence of EtBr2013European journal of medicinal chemistry, Aug, Volume: 667-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155.
AID1517898Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as potentiation of doxorubicin-induced cell growth inhibition at 10 uM measured after 48 hrs by MTT assay (Rvb = 5%)2019European journal of medicinal chemistry, Dec-01, Volume: 183Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.
AID75199Coronary perfusion pressure of isolated guinea pig heart at dose 0.005 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID551249Intrinsic clearance in mouse microsome by LC-MS/MS analysis in presence of NADPH2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis.
AID615812Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as combination index at 5 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID513649Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74 assessed as inhibition of Bay K8644-induced EGFP-HDQ74 aggregation at 1 uM after 48 hrs2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID351891Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
AID1761210Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 5 uM measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
AID630755Reversal of human MDR1-mediated rhodamine 123 uptake in mouse L5178Y cells assessed as fluorescence activity ratio at 10 mM by flow cytometry relative to non p-gp expressing parental cell line2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Discovery of pyridine-2-ones as novel class of multidrug resistance (MDR) modulators: first structure-activity relationships.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID332134Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as ratio of doxorubicin ED50 without drug to doxorubicin ED50 with drug at 6 ug/ml after 6 days by BCA assay1997Journal of natural products, Nov, Volume: 60, Issue:11
Multidrug-resistance modulators from Stephania japonica.
AID681155TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID1215150Tmax in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Opposite effect of diabetes mellitus induced by streptozotocin on oral and intravenous pharmacokinetics of verapamil in rats.
AID1502899Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV3 assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at 1/2 MIC incubated for 3 days by MTT assay (Rvb = 12.5 ug/ml2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID492152Vasodilating activity in Langendorff-perfused Sprague-Dawley rat thoracic aorta assessed as relaxation of phenylephrine-induced vasoconstriction at 10 uM relative to untreated control2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Homo- and heptanor-sterols and tremulane sesquiterpenes from cultures of Phellinus igniarius.
AID1235750Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 16 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID562099Chemosensitization of piperaquine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1649242Reversal of Pgp-mediated DOX resistance in human SW620/AD300 cells assessed as potentiation of DOX-induced cytotoxicity by measuring inhibition of cell proliferation at 1 uM incubated for 48 hrs by SRB assay (Rvb = 5.3 +/- 3 %)2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
AID350526Induction of human histidine10-tagged MDR1 ATPase activity expressed in BHK cells by apparent Michaelis-Menten constant2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
AID1481870Cytotoxicity against human K562 cells assessed as cell viability at 5.0 uM after 48 hrs by MTT assay (Rvb = >99%)2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
AID45792Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID95583Inhibition of [3H]D-888 binding to L-type [Ca2+] channel of membranes from rat skeletal muscle1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID150754Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID143483Inhibitory activity when combined with vinblastine (nM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID679062TP_TRANSPORTER: transepithelial transport of Verapamil at a concentration of 0.1 uM in MDR1-expressing MDCK cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
AID1225498Inhibition of human MDR1 transfected in mouse NIH/3T3 MDR1-G185 cells assessed as reversion index by measuring ratio of daunomycin cytotoxic IC50 in absence of compound to daunomycin cytotoxic IC50 in presence of compound at 10 uM by MTT assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Restoration of Chemosensitivity in P-Glycoprotein-Dependent Multidrug-Resistant Cells by Dihydro-β-agarofuran Sesquiterpenes from Celastrus vulcanicola.
AID1502832Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV1 assessed as potentiation of ciprofloxacin-induced antibacterial activity by measuring ciprofloxacin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 2 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID615811Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as combination index at 2.5 uM after 72 hrs by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.
AID680470TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.1 uM, Verapamil: 1000 uM) in Oatp1-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID1235751Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as ofloxacin MIC at 8 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID331362Inhibition of Pgp-mediated multidrug resistance activity in rat RBMEC cells assessed as Rh123 accumulation at 10 umol/L after 90 mins2008Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12
Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer.
AID1502709Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1530706Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring cell survival at 5 uM after 72 hrs by MTT assay (Rvb = 98 +/- 19%)2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.
AID48971Antagonistic activity against ACh induced responses in canine trachea1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID1129604Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 100 uM after 30 mins by UV spectroscopy2014European journal of medicinal chemistry, Apr-09, Volume: 76SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity.
AID1235718Inhibition of multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as rifampin MIC at 16 ug/ml after 7 days by two-dimensional broth microdilution checkerboard assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy.
AID1418862Potentiation of cisplatin-induced cytotoxicity in human SW620 cells assessed as fold reduction in cisplatin IC50 at 4 uM after 72 hrs by MTT assay relative to cisplatin alone2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1758193Inhibition of P-glycoprotein in human MCF7/ADR cells assessed as rhodamine-123 accumulation by measuring fluorescence intensity at 20 uM measured after 30 mins by flow cytometry analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
AID1764806Stability in human pooled liver microsomes assessed as parent compound remaining measured at 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID678737TP_TRANSPORTER: inhibition of Vinblastine efflux (Vinblastine: 0.002 uM, Verapamil: 10 uM) in P388/S and P388/ADR cells2000Clinical and experimental pharmacology & physiology, Aug, Volume: 27, Issue:8
Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo.
AID1418871Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 4 uM after 72 hrs by MTT assay relative to cisplatin2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Discovery of a non-toxic [1,2,4]triazolo[1,5-a]pyrimidin-7-one (WS-10) that modulates ABCB1-mediated multidrug resistance (MDR).
AID1483831Intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis2017Journal of natural products, 02-24, Volume: 80, Issue:2
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
AID95151Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships.
AID1486952Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring reduction in ADR IC50 at 5 uM measured after 48 hrs by MTT assay relative to ADR alone2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1733403Induction of cell cycle arrest in human KBV cells assessed as accumulation at S phase at 10 uM after 24 hrs in presence of 0.1 uM paclitaxel by PI/RNaseA staining based flow cytometric analysis (Rvb = 13.06 +/- 0.39%)2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID680712TP_TRANSPORTER: increase in Rhodamine 123 intracellular accumulation (R123: 150 uM, Verapamil: 2 ug/mL) in MDR1-expressing NIH3T3 cells2000The Journal of pharmacology and experimental therapeutics, Dec, Volume: 295, Issue:3
Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation.
AID1502806Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV4 assessed as potentiation of azithromycin-induced antibacterial activity by measuring azithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = 256 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1351575Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 30 mM KCl-induced contraction after 15 mins2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
AID230390Reversal index is the ratio of IC50 in the absence of modulator to that of presence of modulator when combined with 5-fluorouracil (uM) in NCI/ADR cell line2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
AID288982Inhibition of P-glycoprotein in MDR mouse T lymphoma cells using rhodamine 123 assessed as ratio of fluorescent uptake relative to untreated control at 1 uM in MDR reversal assay by flow cytometry2007Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15
Structure-activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors.
AID271732Cytotoxicity against MCF7/Adr cells at 100 uM after 48 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID680527TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.01 uM, Verapamil: 500 uM) in OCTN2-expressing HEK293 cells2001Molecular pharmacology, Feb, Volume: 59, Issue:2
Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2.
AID1161578Permeability of the compound by PAMPA-BBB assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties.
AID1566034Stimulation of P-gp ATPase activity (unknown origin) assessed as increase in ATP consumption at 0.2 to 1 mM preincubated for 5 mins followed by Mg-ATP addition by P-gp-Glo luminescence assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
AID1739838Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring fold change in vincristine IC50 at 2.5 uM measured after 72 hrs by SRB assay relative to vincristine IC502020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID487885Binding affinity to P-gp at 0.5 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID1631733Reversal of P-gp-mediated resistance in adriamycin-resistant human HepG2 cells assessed as reduction in ADR IC50 at 200 nM after 48 hrs by MTT assay relative to control2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure-Activity Relationships and Discovery of Promising MDR Reversal Agents.
AID1739818Inhibition of human full-length ABCB1 expressed in FLp-In-293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 2.5 uM measured after 72 hrs by SRB assay (Rvb = 2264 +/- 196 nM)2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1486972Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring reduction in ADR IC50 measured after 48 hrs by MTT assay relative to ADR alone2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID252859Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (10 uM) and Daunorubian (DNM)2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis.
AID1273453Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 256 ug/ml after 7 days by microdilution checkerboard assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID681948TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.85 uM, Verapamil: 5000 uM) in Xenopus laevis oocytes1997Molecular pharmacology, Jun, Volume: 51, Issue:6
Cloning and functional expression of a human liver organic cation transporter.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1198140Permeability of the compound in PBS and EtOH by PAMPA method2015European journal of medicinal chemistry, Mar-26, Volume: 93Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
AID1733405Reversal of P-gp mediated drug efflux in human KBV cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 2 hrs followed by Rh123 addition measured after 0.5 hr by flow cytometry analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.
AID637605Permeability of the compound by PAMPA2012European journal of medicinal chemistry, Feb, Volume: 48A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.
AID1502739Inhibition of multidrug resistance efflux pump in Mycobacterium avium isolate MAV2 assessed as potentiation of clarithromycin -induced antibacterial activity by measuring clarithromycin MIC at 1/4 MIC incubated for 3 days by MTT assay (Rvb = >1024 ug/ml)2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID77931Left ventricular pressure of isolated guinea pig heart at dose 0.05 (ug/heart)1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
SAR studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds.
AID654103Inhibition of human MDR1-mediated multidrug resistant in mouse L5178Y cells at 5.2 uM treated 10 mins before rhodamine 123 challenge measured after 20 mins relative to control2012European journal of medicinal chemistry, May, Volume: 51Dimeric 3,5-bis(benzylidene)-4-piperidones: a novel cluster of tumour-selective cytotoxins possessing multidrug-resistant properties.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1802796Fluorescence Correlation Spectroscopy (FCS) from Article 10.1021/acs.biochem.6b01245: \\Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs.\\2017Biochemistry, 05-16, Volume: 56, Issue:19
Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs.
AID1802151Calcein-AM Assay from Article 10.1111/cbdd.12811: \\Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness.\\2016Chemical biology & drug design, Dec, Volume: 88, Issue:6
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness.
AID1346664Rat Cav1.2 (Voltage-gated calcium channels)1996Molecular pharmacology, Nov, Volume: 50, Issue:5
Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines.
AID1346703Rat Kv3.2 (Voltage-gated potassium channels)2000Neuropharmacology, Jan-04, Volume: 39, Issue:2
Sensitivity of native and cloned hippocampal delayed-rectifier potassium channels to verapamil.
AID1346531Human TPC2 (CatSper and Two-Pore channels)2012Cell, Oct-12, Volume: 151, Issue:2
TPC proteins are phosphoinositide- activated sodium-selective ion channels in endosomes and lysosomes.
AID1346671Human Kv1.8 (Voltage-gated potassium channels)2000American journal of physiology. Renal physiology, Jun, Volume: 278, Issue:6
KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
AID1346501Mouse Kir3.2 (Inwardly rectifying potassium channels)1996Neuron, May, Volume: 16, Issue:5
Functional analysis of the weaver mutant GIRK2 K+ channel and rescue of weaver granule cells.
AID1346493Human TPC1 (CatSper and Two-Pore channels)2014Nature chemical biology, Jun, Volume: 10, Issue:6
The voltage-gated sodium channel TPC1 confers endolysosomal excitability.
AID1345181Human Plasma membrane monoamine transporter (SLC29 family)2016Clinical pharmacology and therapeutics, Nov, Volume: 100, Issue:5
The plasma membrane monoamine transporter (PMAT): Structure, function, and role in organic cation disposition.
AID1346666Human Kv1.7 (Voltage-gated potassium channels)2002European journal of human genetics : EJHG, Jan, Volume: 10, Issue:1
Characterisation of the human voltage-gated potassium channel gene, KCNA7, a candidate gene for inherited cardiac disorders, and its exclusion as cause of progressive familial heart block I (PFHBI).
AID1345181Human Plasma membrane monoamine transporter (SLC29 family)2005Molecular pharmacology, Nov, Volume: 68, Issue:5
Interaction of organic cations with a newly identified plasma membrane monoamine transporter.
AID1345258Human CYP3A4 (CYP3 family)2001British journal of clinical pharmacology, May, Volume: 51, Issue:5
Inhibitory effects of verapamil and diltiazem on simvastatin metabolism in human liver microsomes.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16,507)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906624 (40.13)18.7374
1990's4944 (29.95)18.2507
2000's2606 (15.79)29.6817
2010's1922 (11.64)24.3611
2020's411 (2.49)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 103.81

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index103.81 (24.57)
Research Supply Index9.86 (2.92)
Research Growth Index4.35 (4.65)
Search Engine Demand Index201.01 (26.88)
Search Engine Supply Index2.03 (0.95)

This Compound (103.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,527 (8.67%)5.53%
Reviews834 (4.73%)6.00%
Case Studies1,046 (5.94%)4.05%
Observational4 (0.02%)0.25%
Other14,210 (80.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (121)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Development and Clinical Application of [11C]Verapamil-PET, a Surrogate Marker on P-glycoprotein Expression [NCT02144792]Phase 230 participants (Anticipated)Interventional2013-05-31Recruiting
Pharmacodynamics and Pharmacokinetics of Verapamil in Crohn's Disease Patients [NCT01261286]Phase 10 participants InterventionalCompleted
A Phase 3b, Multicenter, Open-Label Extension Study of Phenoptin in Subjects With Phenylketonuria Who Participated in Protocols PKU-004 or PKU-006 [NCT00332189]Phase 3111 participants (Actual)Interventional2006-07-31Completed
A Open-Label, Two-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of Leritrelvir With Midazolam, Omeprazole, Rosuvastatin, Verapamil, and Rifampin in Healthy Participants [NCT06031454]Phase 156 participants (Anticipated)Interventional2023-09-01Recruiting
Effect of Verapamil as an Adjuvant to Bupivacaine in Supraclavicular Brachial Plexus Block Guided by Ultrasound for Forearm and Hand Surgeries [NCT05183997]60 participants (Anticipated)Interventional2022-01-31Not yet recruiting
A Phase 2a, Multicenter, Open-label, Dose-escalation Study to Evaluate the Safety, Tolerability, and Efficacy of 6R-BH4 in Subjects With Sickle Cell Disease [NCT00445978]Phase 232 participants (Actual)Interventional2007-05-31Completed
An Adaptive, Part Open-label, Part Randomised Phase 1 Clinical Trial in Healthy Volunteers to Study Drug Interactions With RV521 Including Those Mediated by CYP3A4 and P-glycoprotein [NCT03782662]Phase 182 participants (Actual)Interventional2018-11-06Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of Phenoptin™ in Subjects With Phenylketonuria Who Have Elevated Phenylalanine Levels [NCT00104247]Phase 389 participants (Actual)Interventional2005-03-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Phase 2 Study to Evaluate the Safety and Efficacy of R-Verapamil in the Prophylaxis of Episodic Cluster Headache [NCT02209155]Phase 21 participants (Actual)Interventional2013-11-30Terminated
Pharmacokinetics and Safety of Commonly Used Drugs in Lactating Women and Breastfed Infants [NCT03511118]1,600 participants (Anticipated)Observational2018-10-04Recruiting
A Study of the Pharmacokinetic and Pharmacodynamic Responses in Healthy and Altered Human Cardiovascular Systems [NCT03098680]Phase 118 participants (Actual)Interventional2017-04-24Terminated(stopped due to Unable to recruit in time before end of PhD studentship)
The Preventive Effect of Combined Intracoronary of Nicorandil and Verapamil on Myocardial Injury in Preioperative Period of PCI [NCT05399576]Phase 2150 participants (Anticipated)Interventional2022-05-17Recruiting
Super-Selective Intra-Arterial Administration of Verapamil for Neuroprotection After Intra-Arterial Thrombolysis for Acute Ischemic Stroke Phase I Study [NCT02235558]Phase 111 participants (Actual)Interventional2013-02-01Completed
Comparative Study Between the Efficacy of Verapamil and Bisoprolol on Reduction of Bleeding During Endoscopic Sinus Surgery Under General Anaesthesia. [NCT04356196]Early Phase 1135 participants (Anticipated)Interventional2021-06-15Active, not recruiting
Treatment of Hypoglycemia Following Gastric Bypass Surgery [NCT02527993]Phase 411 participants (Actual)Interventional2015-10-31Completed
Effects of Atenolol, Perindopril and Verapamil on Haemodynamic and Vascular Function in Marfan Syndrome - A Randomised Double-Blind Crossover Trial [NCT01295047]Phase 418 participants (Actual)Interventional2006-07-31Completed
An Open-label, Single-Centre Study to Assess the Pharmacokinetics of R406 in Healthy Volunteers When Fostamatinib Disodium 150 mg is Administered Alone and in Combination With Verapamil [NCT01197781]Phase 115 participants (Actual)Interventional2010-09-30Completed
[NCT01126307]16 participants (Anticipated)Interventional2010-06-30Not yet recruiting
An Open-label, 3-Arm, Parallel Design Pharmacokinetic Interaction Study Between MYK-224 and Cytochrome P450 3A4 Inhibitors Itraconazole and Verapamil in Healthy Participants [NCT05304533]Phase 145 participants (Actual)Interventional2022-04-21Completed
Use of Adenosine to Determine the Electrophysiological Mechanism of Premature Ventricular Contractions [NCT03218137]Phase 4100 participants (Anticipated)Interventional2017-02-13Recruiting
The Intra-arterial Vasospasm Trial(iVAST)- A Multi-center Randomized Study [NCT01996436]Phase 4330 participants (Anticipated)Interventional2016-08-29Recruiting
Blood Pressure and Weight Trajectory on a Dual Antihypertensive Combination Plus Sibutramine Versus Placebo in Obese Hypertensives [NCT00679653]Phase 3171 participants (Actual)Interventional2002-02-28Completed
A Double Blind Randomized Controlled Trial of Greater Occipital Nerve Infiltration in Cluster Headache [NCT00804895]Phase 2/Phase 343 participants (Actual)Interventional2008-12-31Completed
Efficacy of Adenosine Versus Verapamil for Management of Supraventricular Tachycardia Post- Coronary Artery Bypass Grafting: a Randomized Double Blinded Trial [NCT04203368]268 participants (Actual)Interventional2020-02-01Completed
The Effect of the Adipocyte-derived Hormone Leptin on Endothelial Function in Healthy Men and in Persons With Known Cardiovascular Disease [NCT04374500]Early Phase 1103 participants (Actual)Interventional2006-01-01Completed
A Phase 1, Open-label, Single-Sequence, Crossover Drug Interaction Study to Evaluate the Effect of Verapamil on the Pharmacokinetics of ASP015K in Healthy Adult Subjects [NCT02111317]Phase 124 participants (Actual)Interventional2013-10-31Completed
Relative Bioavailability of Single Oral Doses of 150 mg Dabigatran Etexilate With or Without Oral Administration of Verapamil in Two Different Dosages (240 mg and 480 mg Daily) (Open-label, Fixed-sequence Design), and Relative Bioavailability of Single Or [NCT02171533]Phase 140 participants (Actual)Interventional2008-06-30Completed
The Effects of ATLAS (Arginine Tetrahydrobiopterin L-Ascorbate) Therapy on Nitric Oxide Bioavailability and Pain-free Walking in Patients With Intermittent Claudication [NCT04800692]Phase 110 participants (Anticipated)Interventional2021-06-15Recruiting
A Randomised, Double-blind, Placebo Controlled, Parallel Group, Multi-centre Trial in Adult Subjects With Newly Diagnosed Type 1 Diabetes Mellitus Investigating the Effect of Verapamil SR on Preservation of Beta-cell Function (Ver-A-T1D) [NCT04545151]Phase 2138 participants (Anticipated)Interventional2021-02-08Recruiting
A Two-Phase Study for Primary and Secondary Prevention of Diabetic Nephropathy by Combined ACE Inhibition and Calcium Channel Blockade (BENEDICT) [NCT00235014]Phase 41,204 participants (Actual)Interventional1997-03-31Completed
A Phase 2 Randomized Open-label 2-Treatment 2-Sequence 2-Period Crossover PK Study to Compare Plasma Concentrations of BH4 in Subjects With Endothelial Dysfunction Following 14 Days of Treatment by 2 Regimens: 6R-BH4 With Vitamin C and 6R-BH4 Alone [NCT00532844]Phase 252 participants (Actual)Interventional2007-09-30Completed
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Radiofrequency Ablation of Symptomatic Frequent Ventricular Premature Complexes as a First-line Therapy in Pediatric Population Without Structural Heart Disease [NCT02772354]Phase 2/Phase 3124 participants (Anticipated)Interventional2016-04-30Recruiting
Does Dilution of Verapamil With Normal Saline or Blood Reduce Discomfort Felt During Intraarterial Administration? [NCT05625503]Early Phase 1100 participants (Anticipated)Interventional2022-12-13Recruiting
Single-Dose Fasting Bioequivalence Study of Verapamil HCl Extended-Release Capsules (300 mg; Mylan) to Verelan® PM Extended-Release Capsules (300 mg; Schwarz) in Healthy Volunteers Dosed in the Evening [NCT00647673]Phase 124 participants (Actual)Interventional2006-01-31Completed
Bioequivalence Study Of Verapamil (Covera HS) 240 Mg Extended Release Tablets Produced By Alza Corporation, Vacaville And Pfizer Inc, Puerto Rico: A Two Sequence, Four-Way Crossover Design, Single Dose, Open-Label, Randomized Study In Healthy Volunteers [NCT00668967]Phase 179 participants (Actual)Interventional2008-02-29Completed
A Phase 1, Open-Label, 4-Part, Drug-Drug Interaction Study With Omaveloxolone in Healthy Subjects [NCT04008186]Phase 161 participants (Actual)Interventional2019-06-14Completed
Phase Ia/Ib Clinical Trial of Sapropterin Dihydrochloride Tablets in the Prevention and Treatment of Radiation-induced Skin Reactions in Intensity Modulated Radiotherapy for Head and Neck Squamous Cell Carcinoma (Including Nasopharyngeal Carcinoma) [NCT05299203]Phase 118 participants (Anticipated)Interventional2022-05-31Not yet recruiting
Hybrid Closed Loop Therapy and Verapamil for Beta Cell Preservation in New Onset Type 1 Diabetes (CLVer) [NCT04233034]Phase 3113 participants (Actual)Interventional2020-07-09Completed
Single-Dose Fasting Bioequivalence Study of Verapamil HCl Extended-Release Capsules (300 mg; Mylan) to Verelan® PM Extended-Release Capsules (300 mg; Schwarz) in Healthy Volunteers Dosed in the Evening [NCT00648050]Phase 172 participants (Actual)Interventional2006-03-31Completed
Prospective, Randomized Comparison of Therapy With Verapamil or Carvedilol on Long-Term Outcomes of Patients With Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy [NCT00348530]Phase 4120 participants Interventional2006-01-31Recruiting
Single-Dose Fed Bioequivalence Study of Verapamil HCl Extended-Release Capsules (300 mg; Mylan) and Verelan® PM Extended-Release Capsules (300 mg; Schwarz) in Healthy Volunteers [NCT00648401]Phase 124 participants (Actual)Interventional2006-01-31Completed
Single-Dose Fasting Bioequivalence Study of Verapamil HCl Extended-Release Capsules (300 mg;Mylan) and Verelan® PM Extended-Release Capsules (300 mg; Schwarz) Sprinkled on Applesauce in Healthy Volunteers [NCT00649805]Phase 124 participants (Actual)Interventional2006-01-31Completed
Drug Discrimination in Methadone-Maintained Humans Study 2 [NCT00733239]Phase 115 participants (Actual)Interventional2008-08-31Completed
Elimination of Ventricular Premature Beats With CaTheter Ablation Versus OPtImal Anti-arrhythmic Drug Treatment [NCT03845010]22 participants (Actual)Interventional2019-02-12Completed
Drug Discrimination in Methadone-Maintained Humans Study 3 [NCT01068847]Phase 19 participants (Actual)Interventional2010-02-28Completed
[NCT00000556]Phase 30 participants Interventional1995-03-31Completed
Pharmacotherapy of Treatment-Resistant Mania [NCT00518947]Phase 345 participants (Actual)Interventional1994-11-30Completed
An Open-label, Non-randomized, Fixed Sequence Study Assessing the Pharmacokinetics of AZD7986 When Administered Alone and With Multiple Doses of Verapamil and Itraconazole or Diltiazem in Healthy Subjects [NCT02653872]Phase 115 participants (Actual)Interventional2016-01-22Completed
A Phase 2, Multicenter, Multinational, Randomized, Double-blind, Placebo-controlled, Parallel Study of the Effects of Sapropterin Dihydrochloride on Symptomatic Peripheral Arterial Disease [NCT00403494]Phase 2190 participants (Actual)Interventional2006-12-31Completed
Reversal of No-reflow/Slow-flow During Percutaneous Coronary Intervention in Patients With Acute Myocardial Infarction--a Prospective Randomized Study Comparing Intracoronary Infusion of Diltiazem, Verapamil and Nitroglycerin [NCT00712894]Phase 4102 participants (Actual)Interventional2006-12-31Completed
A Phase 3, Double-blind, Placebo-controlled Study to Evaluate the Safety and Efficacy of Phenoptin to Increase Phenylalanine Tolerance in Phenylketonuric Children on a Phenylalanine-restricted Diet [NCT00272792]Phase 345 participants (Actual)Interventional2006-02-28Completed
A Phase 3, Multicenter, Open-Label Extension Study of Phenoptin in Subjects With Phenylketonuria Who Have Elevated Phenylalanine Levels [NCT00225615]Phase 3100 participants Interventional2005-11-30Completed
A Prospective, Open-Label Study to Evaluate the Effect of an Escalating Dose Regimen of Trandolapril on Blood Pressure in Treatment-Naïve and Concurrently Treated Hypertensive Patients (TRAIL) [NCT00233532]Phase 42,000 participants (Actual)Interventional2004-03-31Completed
A Phase 1, Open-label, One-sequence Study to Assess the Effect of Verapamil on the Steady State Pharmacokinetics of Solifenacin and Tamsulosin Administered as a Combination Tablet EC905 in Healthy Male Subjects. [NCT01943487]Phase 136 participants (Actual)Interventional2009-08-31Completed
A Phase IV, Randomized, Open-Label, Active Controlled Study to Compare the Effects of Tarka® and Lotrel® on Albuminuria in Hypertensive, Type 2 Diabetic Subjects With Diabetic Nephropathy [NCT00234871]Phase 4357 participants (Actual)Interventional2004-01-31Completed
Superselective Citicoline And Verapamil for Ischemic Neuroprotection and Greater Effective Response (SCAVINGER) in the Kentucky Regional Population: A Clinical and Translational Study [NCT02823106]Phase 10 participants (Actual)Interventional2016-08-31Withdrawn(stopped due to Study put on clinical hold by FDA. Sponsor decided to no pursue the study.)
A Multicenter, Open, Phase IV, 24-Hour Ambulatory Blood Pressure Monitoring Study of the Efficacy and Safety of Tarka in Patients With Arterial Hypertension [NCT00235001]Phase 4120 participants (Actual)Interventional2004-06-30Completed
Drug Discrimination in Methadone-Maintained Humans Study 1 [NCT00593463]Phase 140 participants (Anticipated)Interventional2006-09-30Completed
A Phase 3b Open-Label Study to Evaluate the Effect of Kuvan® on Neurocognitive Function, Maintenance of Blood Phenylalanine Concentrations, Safety, and Population Pharmacokinetics in Young Children With Phenylketonuria [NCT00838435]Phase 395 participants (Actual)Interventional2009-02-28Completed
A Double-blind, Placebo-controlled, Randomized Study to Evaluate the Safety and Therapeutic Effects of Sapropterin Dihydrochloride on Neuropsychiatric Symptoms in Subjects With Phenylketonuria [NCT01114737]Phase 3206 participants (Actual)Interventional2010-08-31Completed
A Phase I, Single-centre, Randomised, Open, Three-way Crossover Study to Evaluate the Effect of Ketoconazole and Verapamil, Respectively, on the Pharmacokinetics of AZD1305 After Repeated Oral Adm of Ketoconazole and Verapamil and Single Oral Dosing of AZ [NCT00707551]Phase 127 participants (Anticipated)Interventional2008-07-31Completed
Pacing and AV Node Ablation Compared to Drug Therapy in Symptomatic Elderly Patients With Atrial Fibrillation Clinical Trial (PACIFIC) - Pilot Study [NCT00589303]Phase 327 participants (Actual)Interventional2007-12-31Terminated(stopped due to Lack of funding)
Improving Outcomes in Atrial Fibrillation Patients Aided by Implantable Cardiac Monitor: Evaluation of Chronic Beta-blocker Use Versus As-needed Pharmacological Rate Control [NCT05745337]Phase 120 participants (Anticipated)Interventional2023-02-06Recruiting
Multimodal Neuroimaging and Neurocognitive Assessment of Biomarkers and Response to Sapropterin Dihydrochloride Treatment in Phenylketonuria [NCT01412437]0 participants (Actual)Interventional2011-04-30Withdrawn(stopped due to poor recruitment)
Intralesional Injection of Hyaluronic Acid Compared With Verapamil in Peyronie's Disease: A Prospective Randomized Clinical Trial [NCT05855070]42 participants (Anticipated)Interventional2023-05-20Not yet recruiting
Magnesium And Verapamil After Recanalization in Ischemia of the Cerebrum (MAVARIC) in the Kentucky Regional Population: a Clinical and Translational Study. [NCT02912663]Phase 110 participants (Actual)Interventional2017-10-11Completed
The Surrogate Marker of Rate Control in Patients With Atrial Fibrillation [NCT04513509]50 participants (Anticipated)Interventional2020-08-07Not yet recruiting
Kuvan® (Sapropterin Dihydrochloride) for Improving Gastric Accommodation in Women With Diabetic Gastroparesis (KIGA-DG) [NCT01135186]9 participants (Actual)Interventional2010-05-31Completed
Study of Verapamil in Refractory Catamenial Epilepsy [NCT00559169]12 participants (Anticipated)Interventional2009-02-28Withdrawn(stopped due to protocol changed and a new study using verapamil in epilepsy will be started in the near future)
Intracoronary Administration of Epinephrine and Verapamil in the Refractory No-reflow Phenomenon in Patients With Acute Myocardial Infarction: The EPIVER Randomized Controlled Trial [NCT04573751]104 participants (Actual)Interventional2020-12-30Active, not recruiting
Intracavernosal Injection of Papaverine/Verapamil Versus Papaverine/Phentolamine in Erectile Dysfunction: A Pilot Study [NCT03033537]20 participants (Actual)Observational [Patient Registry]2015-07-01Completed
Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study) [NCT03070470]Phase 160 participants (Actual)Interventional2017-03-14Completed
Assessment of Verapamil as an Adjunct for Prevention of Keloid Recurrence After Surgical Removal [NCT01720056]Phase 414 participants (Actual)Interventional2012-10-31Terminated(stopped due to Objective of study achieved after interim analysis.)
A Phase 1b, Drug-Drug Interaction Study Investigating the Pharmacokinetic Interaction Between INX-08189 and Verapamil HCL ER in Healthy Volunteers [NCT01471704]Phase 1/Phase 224 participants (Actual)Interventional2011-10-31Completed
INternational VErapamil SR Trandolapril STudy [NCT00133692]Phase 422,000 participants Interventional1997-09-30Completed
A Phase 1, Multicenter, Open-label, Dose-escalation Study to Evaluate the Safety and Efficacy of 6R-BH4 in Subjects With Pulmonary Arterial Hypertension [NCT00435331]Phase 114 participants (Actual)Interventional2008-03-31Completed
A Phase IV, Randomized, Open-Label, Active Controlled Study to Compare the Effects of Tarka® and Hyzaar® on Glucose Tolerance in Subjects With Metabolic Syndrome [NCT00234858]Phase 4280 participants (Actual)Interventional2004-03-31Completed
Treatment Effects of Bisoprolol and Verapamil in Symptomatic Patients With Non-obstructive Hypertrophic Cardiomyopathy [NCT05569382]Phase 4140 participants (Anticipated)Interventional2022-08-10Recruiting
Sapropterin Expanded Access Program [NCT00484991]0 participants Expanded AccessApproved for marketing
Repurposing of Verapamil as a Beta Cell Survival Therapy in Type 1 Diabetes [NCT02372253]Phase 232 participants (Actual)Interventional2015-02-28Completed
Targeting Beta Cell Dysfunction With Verapamil in Longstanding T1D [NCT05847413]Early Phase 110 participants (Actual)Interventional2020-05-30Completed
A Phase 2, Multicenter, Open-Label Study to Evaluate the Response to and Safety of an 8-Day Course of Phenoptin™ Treatment in Subjects With Phenylketonuria Who Have Elevated Phenylalanine Levels [NCT00104260]Phase 2700 participants Interventional2004-12-31Completed
RCVS: The Rational Approach to Diagnosis and Treatment [NCT03150524]Phase 40 participants (Actual)Interventional2017-07-01Withdrawn(stopped due to Failure to recruit patients meeting inclusion criteria.)
Intraarterial Verapamil for Neuroprotection in Ischemic Stroke [NCT03347786]Phase 120 participants (Anticipated)Interventional2017-04-20Recruiting
A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel Study of the Effects of 6R-BH4 on Blood Pressure in Subjects With Poorly Controlled Systemic Hypertension [NCT00325962]Phase 284 participants Interventional2006-05-31Completed
Rate Control in Atrial Fibrillation [NCT00313157]Phase 380 participants (Actual)Interventional2006-04-30Completed
Oral Propranolol, Diltiazem, Metoprolol and Verapamil in Atrial Fibrillation Rate Control in Patients With Stable Hemodynamic Status [NCT01655303]Phase 490 participants (Actual)Interventional2011-02-28Completed
[NCT01655316]Phase 490 participants (Actual)Interventional2010-10-31Completed
Pharmacologic Dissection of Vestibular Migraine and Chronic Subjective Dizziness: A Double-Blind Parallel Group Trial Comparing Response to Verapamil Versus Sertraline [NCT01669304]Phase 132 participants (Actual)Interventional2012-08-31Completed
A Phase I Trial of Brentuximab Vedotin Plus MDR1 Inhibitors in Relapsed/Refractory Hodgkin Lymphoma [NCT03013933]Phase 129 participants (Actual)Interventional2017-05-03Active, not recruiting
Prospective, Randomized Comparison of Therapy With Verapamil or Carvedilol on Long-Term Outcomes of Patients With Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy [NCT00374465]Phase 4100 participants Interventional2006-01-31Recruiting
Comparative, Randomized, Single-Dose, 2-way Crossover Bioavailability Study of Synerx Pharma and Verelan PM 300 mg Verapamil HCl Extended Release Capsules Controlled-Onset in Healthy Aduly Volunteers Under Fed Conditions [NCT01467687]Phase 158 participants (Actual)Interventional2007-07-31Completed
Biomarkers of Central Nervous System Tetrahydrobiopterin Concentration and Response to Tetrahydrobiopterin Supplementation in Children With Idiopathic Cognitive Developmental Disorders [NCT01141595]10 participants (Actual)Interventional2010-07-31Completed
Phase Ib/II Clinical Trial of Topical Verapamil Hydrochloride for Chronic Rhinosinusitis With Nasal Polyps [NCT03102190]Phase 16 participants (Actual)Interventional2017-06-05Terminated(stopped due to Phase II funding not available)
A Phase 1, Open-Label, Non-Randomized, Fixed-Sequence Composite Study to Evaluate the Effects of Probenecid, Rifampin, and Verapamil on the Pharmacokinetics and Pharmacodynamics of Bexagliflozin in Healthy Subjects [NCT03296800]Phase 148 participants (Actual)Interventional2017-09-27Completed
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial [NCT04330300]Phase 42,414 participants (Anticipated)Interventional2020-04-30Suspended(stopped due to Challenges with funding and very low incidence of COVID-19 at Irish study site)
The Effect of Potent Inhibitors of Drug Transporters (Verapamil, Rifampin, Cimetidine, Probenecid) on Pharmacokinetics of a Transporter Probe Drug Cocktail Consisting of Digoxin, Furosemide, Metformin and Rosuvastatin (an Open-label, Randomised, Crossover [NCT03307252]Phase 145 participants (Actual)Interventional2017-10-25Completed
Randomized Double Blind Placebo Controlled Trial of Verapamil in Chronic Rhinosinusitis [NCT02454608]29 participants (Actual)Interventional2015-05-31Terminated(stopped due to Evidence that the dose is insufficient.)
CS-201: A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Efficacy of Intra-Articular Verapamil in the Treatment of JoinT Pain in Subjects With Osteoarthritis of the Knee [NCT01645709]Phase 1/Phase 281 participants (Actual)Interventional2012-04-30Terminated(stopped due to Sponsor decision to terminate study)
Effects of Tetrahydrobiopterin (BH4) on Leg Blood Flow, Mitochondrial Function and Leg Performance in Patients With Peripheral Artery Disease [NCT03493412]Phase 40 participants (Actual)Interventional2019-07-31Withdrawn(stopped due to discontinued due to change in operating plans prior to study initiation and enrollment)
Comparison of VERapamil vs. Heparin Therapy on Procedural sUccess During Transradial Coronary Procedures (VERMUT Study) [NCT02454491]Phase 4418 participants (Actual)Interventional2015-05-31Completed
Comparative Study Between the Efficacy of Oral Verapamil and Oral Diltiazim on Reduction of Intraoperative Bleeding During Endoscopic Sinus Surgery Under General Anesthesia [NCT04790331]Early Phase 1135 participants (Anticipated)Interventional2021-03-01Not yet recruiting
Atrioventricular Block and Cluster Headache [NCT04406259]Phase 460 participants (Anticipated)Interventional2020-11-02Recruiting
Treatment of Tinnitus With Migraine Medications: A Randomized Clinical Trial [NCT04404439]Phase 4150 participants (Anticipated)Interventional2019-09-26Recruiting
"Evaluation of Behavior, Executive Function, Neurotransmitter Function and Genomic Expression in PKU Nonresponders to Kuvan® (Sapropterin Dihydrochloride)" [NCT01274026]21 participants (Actual)Observational2011-01-31Completed
Combination of Hydroxyurea and Verapamil for Refractory Meningiomas [NCT00706810]Phase 28 participants (Actual)Interventional2007-12-31Completed
A One-Directional, Open Label Drug Interaction Study to Investigate the Effects of Multiple Dose Verapamil HCl ER on Single Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983242]Phase 124 participants (Actual)Interventional2008-09-30Completed
A Randomized Controlled Trial for Evaluating Protective Effects of Antioxidants (Selenium and Vitamins A, C and E), Calcium Channel Blocker (Verapamil) and Angiotensin Receptor Blocker (Losartan) Against Extracorporeal Shockwaves Lithotripsy Induced Renal [NCT01675362]Phase 4160 participants (Actual)Interventional2012-08-31Completed
A Double-Blind, Randomized, Placebo-Controlled Single-Dose, Five Period Crossover Study of the Electrocardiographic Effects of Ranolazine, Dofetilide, Verapamil, and Quinidine in Healthy Subjects [NCT01873950]Phase 122 participants (Actual)Interventional2013-05-31Completed
Acute Cardioversion Versus Wait And See-approach for Symptomatic Atrial Fibrillation in the Emergency Department (RACE 7 ACWAS-trial) [NCT02248753]437 participants (Actual)Interventional2014-10-31Completed
Amiodarone or Verapamil in COVID-19 Hospitalized Patients With Symptoms [NCT04351763]Phase 2/Phase 3804 participants (Actual)Interventional2020-05-20Completed
Relative Bioavailability of BI 10773 Given Alone and Together With Verapamil - an Open-label, Randomised, Crossover Trial in Healthy Subjects [NCT01276301]Phase 116 participants (Actual)Interventional2011-01-31Completed
Omission of Prophylactic Verapamil Use in Transradial Coronary Interventions [NCT01402427]591 participants (Actual)Interventional2011-03-31Completed
Quinidine Versus Verapamil in Short-coupled Idiopathic Ventricular Fibrillation: an Open-label, Randomized Crossover Pilot Trial [NCT05593757]Phase 224 participants (Anticipated)Interventional2022-10-01Enrolling by invitation
A Phase 1, Randomized, Open-label, 3-sequence, 4-treatment, Incomplete Block Design To Estimate The Effect Of Steady State Cyp3a4 Inhibitors (Itraconazole, Diltiazem Or Verapamil) On The Pharmacokinetics Of Singe Dose Pf-00489791 In Healthy Volunteers [NCT02319148]Phase 122 participants (Actual)Interventional2014-07-31Completed
Assessment of Intravenous Rate Control Response in Atrial Fibrillation Trial Pilot Study (AIRCRAFT) [NCT04234477]Phase 40 participants (Actual)Interventional2021-12-31Withdrawn(stopped due to The study was not IRB approved and there were anticipated challenges in recruiting participants.)
A Series of Pilot Studies to Evaluate the Haemodynamic and Metabolic Effects of Apelin and Relaxin in Healthy Humans, Subjects With Increased Weight and Patients With Type 2 Diabetes Mellitus [NCT03449251]Phase 2170 participants (Anticipated)Interventional2018-03-28Recruiting
A Randomized, Double-blind, Multi-center, Therapeutic Confirmatory, Phase 3 Trial To Evaluate the Efficacy and Safety of D064 and D702 Combination Therapy Versus D064 or D702 Monotherapy in Essential Hypertension Patients [NCT06121518]Phase 3228 participants (Anticipated)Interventional2023-07-31Recruiting
An Open-label, Healthy Subject, Two-part Study to Assess the Effect of Verapamil on Systemic Exposure of EP395 (Part A), and to Assess the Effect of EP395 on Systemic Exposure of Midazolam and Digoxin (Part B) [NCT06118684]Phase 136 participants (Anticipated)Interventional2023-10-23Recruiting
Verapamil as Adjunctive Seizure Therapy for Children and Young Adults With Dravet Syndrome [NCT01607073]Phase 22 participants (Actual)Interventional2012-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00104247 (1) [back to overview]Change in Blood Phenylalanine Levels From Baseline to Week 6.
NCT00272792 (2) [back to overview]Amount of Dietary Supplemented Phenylalanine (Phe)Tolerated in Children With Phenylketonuria
NCT00272792 (2) [back to overview]Change in Phenylalanine Levels From Baseline to Week 3
NCT00332189 (2) [back to overview]Following Blood Phe Levels.
NCT00332189 (2) [back to overview]Tabulation of the Incidence and Frequency of All AEs and SAEs That Occur Throughout the Study.
NCT00403494 (4) [back to overview]Number of Subjects With Adverse Events (AEs)
NCT00403494 (4) [back to overview]Change in Peak Walking Time From Baseline With and Without Vitamin C
NCT00403494 (4) [back to overview]Change in Peak Walking Time (PWT) From Baseline
NCT00403494 (4) [back to overview]Change in Claudication Onset Time (COT) From Baseline
NCT00445978 (5) [back to overview]Change From Baseline in the Peripheral Arterial Tonometry (PAT) Scores
NCT00445978 (5) [back to overview]Change From Baseline in the Tricuspid Regurgitant Velocity (TRV)
NCT00445978 (5) [back to overview]Change From Baseline in the Urine 8-Isoprostane
NCT00445978 (5) [back to overview]Change From Baseline in the Urine Spot Albumin to Creatinine Ratio
NCT00445978 (5) [back to overview]Number of Subjects With Treatment Emergent Adverse Events (TEAEs)
NCT00532844 (12) [back to overview]Area Under the Curve (AUC0-12hours) for Calculated BH4 (From Total Biopterin)
NCT00532844 (12) [back to overview]Area Under the Curve (AUC0-12hrs) of Plasma BH4 Concentration
NCT00532844 (12) [back to overview]Area Under the Curve (AUC0-12hrs) of Plasma BH2 and B Concentration
NCT00532844 (12) [back to overview]Change From Baseline in Cyclic Guanosine Monophosphate (cGMP)
NCT00532844 (12) [back to overview]Change From Baseline in Diastolic Blood Pressure (DBP)
NCT00532844 (12) [back to overview]Change From Baseline in Peripheral Arterial Tonometry (PAT)
NCT00532844 (12) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP)
NCT00532844 (12) [back to overview]Change in Urinary Albumin to Creatinine Ratio (mg/g)
NCT00532844 (12) [back to overview]Number of Participants With Urinary Albumin to Creatinine Ratio <30 mg/g
NCT00532844 (12) [back to overview]Number of Subjects With Treatment Emergent Adverse Events (TEAEs)
NCT00532844 (12) [back to overview]Ratio of BH2, B and BH4 Calculated From Total Biopterin Area Under the Curve (0-12hours) for Subjects Administered Sapropterin Dihydrochloride With Vitamin C to Subjects Administered Sapropterin Alone.
NCT00532844 (12) [back to overview]Change From Baseline in Urinary 8-isoprostane/Creatinine
NCT00589303 (1) [back to overview]Cardiac Hospitalization Within Six Months of Enrollment
NCT00706810 (2) [back to overview]Number of Participants Experiencing Serious Adverse Events Including But Not Limited to Hospitalizations, Deaths Related to Treatment, or Other Incapacitating Conditions.
NCT00706810 (2) [back to overview]Median Progression-free Survival Rates of the Treatment Population.
NCT00838435 (10) [back to overview]Number of Subjects With Adverse Events (AEs)
NCT00838435 (10) [back to overview]Full-Scale Intelligence Quotient (FSIQ) Score
NCT00838435 (10) [back to overview]Change From Baseline in Growth Measurements - Weight Z-Scores
NCT00838435 (10) [back to overview]Change From Baseline in Growth Measurements - Height Z-Scores
NCT00838435 (10) [back to overview]Change From Baseline in Growth Measurements - Head Circumference Z-Scores
NCT00838435 (10) [back to overview]Apparent Volume of Distribution (V/F) of Kuvan
NCT00838435 (10) [back to overview]Baseline Concentration of Tetrahydrobiopterin (BH4)(C0)
NCT00838435 (10) [back to overview]Change From Baseline in Bayley-III Scores - Neurocognitive Testing Results
NCT00838435 (10) [back to overview]Absorption Rate Constant (Ka) of Kuvan
NCT00838435 (10) [back to overview]Apparent Clearance (CL/F) of Kuvan
NCT00983242 (3) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 to Time t [AUC(0-t)]
NCT00983242 (3) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]
NCT00983242 (3) [back to overview]Maximum Plasma Concentration (Cmax)
NCT01114737 (19) [back to overview]Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Week 13 to Week 26
NCT01114737 (19) [back to overview]Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Baseline to Week 26
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Baseline to Week 26
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Week 13 to Week 26
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Baseline to Week 26
NCT01114737 (19) [back to overview]Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Week 13 to Week 26
NCT01114737 (19) [back to overview]Change in Clinical Global Impression-Severity (CGI-S) From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Clinical Global Impression-Severity (CGI-S) From Baseline to Week 26
NCT01114737 (19) [back to overview]Change in Clinical Global Impression-Severity (CGI-S) From Week 13 to Week 26
NCT01114737 (19) [back to overview]Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Baseline to Week 26
NCT01114737 (19) [back to overview]Change in Hamilton Depression Rating Scale (HAM-D) Score From Baseline to Week 13
NCT01114737 (19) [back to overview]Change in Hamilton Depression Rating Scale (HAM-D) Score From Week 13 to Week 26
NCT01114737 (19) [back to overview]Change in Hamilton Rating Scale For Depression (HAM-D) Score From Baseline to Week 26
NCT01114737 (19) [back to overview]Number of Participants With a Score of 1 or 2 in Global Function Evaluation (CGI-I) From Baseline to Week 13.
NCT01114737 (19) [back to overview]Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Week 13 to Week 26
NCT01135186 (4) [back to overview]Gastric Accommodation
NCT01135186 (4) [back to overview]Secondary Outcome Measures Will Include Change in Quality of Life.
NCT01135186 (4) [back to overview]Secondary Outcome Measures Will Include Change in Symptom Severity as Measured by the Patient Assessment of Gastrointestinal Disorder-Symptom Severity Index Disorders Symptom Severity Index (PAGI-SYM)
NCT01135186 (4) [back to overview]Secondary Outcome Measures Will Include Change in Symptom Severity.
NCT01141595 (1) [back to overview]Preschool Language Scales
NCT01276301 (12) [back to overview]Area Under the Curve 0 to Infinity (AUC0-∞)
NCT01276301 (12) [back to overview]Area Under the Curve 0 to Time of Last Quantifiable Data Point (AUC0-tz)
NCT01276301 (12) [back to overview]Clinically Relevant Abnormalities for Physical Examination, Vital Signs, Blood Chemistry and Electrocardiogram (ECG).
NCT01276301 (12) [back to overview]Terminal Elimination Rate Constant (λz)
NCT01276301 (12) [back to overview]Maximum Measured Concentration (Cmax)
NCT01276301 (12) [back to overview]Mean Residence Time in the Body After Administration (MRTpo)
NCT01276301 (12) [back to overview]Apparent Volume of Distribution Following an Extravascular Dose (Vz/F)
NCT01276301 (12) [back to overview]Assessment of Tolerability by Investigator
NCT01276301 (12) [back to overview]Apparent Clearance in Plasma After Extravascular Administration (CL/F)
NCT01276301 (12) [back to overview]Terminal Half-life in Plasma (t1/2)
NCT01276301 (12) [back to overview]Time From 0 to Maximum Plasma Concentration (Tmax)
NCT01276301 (12) [back to overview]Verapamil Plasma Concentration
NCT01402427 (7) [back to overview]Fluoroscopic Time
NCT01402427 (7) [back to overview]Contrast Volume
NCT01402427 (7) [back to overview]Procedural Time
NCT01402427 (7) [back to overview]Rate of Access Site Conversions
NCT01402427 (7) [back to overview]Rate of Code Breaks
NCT01402427 (7) [back to overview]Rate of Vasodilator Use
NCT01402427 (7) [back to overview]Subjective Pain
NCT01607073 (3) [back to overview]Change in Number of Myoclonic Seizures From Week 8 (Baseline) to Week 12
NCT01607073 (3) [back to overview]Change in Number of Absence Seizures From Week 8 (Baseline) to Week 12
NCT01607073 (3) [back to overview]Change in Number of General Tonic-clonic Seizures From Week 8 (Baseline) Visit to Week 12 Visit
NCT01873950 (10) [back to overview]Change in PR, QRS, J-Tpeak, Tpeak-Tend and QTc Using Exposure/Response (Ranolazine and Quinidine Arms)
NCT01873950 (10) [back to overview]Placebo, and Baseline-adjusted Changes in PR, QRS, J-Tpeak, Tpeak-Tend and QTc
NCT01873950 (10) [back to overview]Change in Ventricular Gradient Using Exposure/Response (Dofetilide and Verapamil Arms)
NCT01873950 (10) [back to overview]Change in Spatial QRS-T Angle Using Exposure/Response (Dofetilide and Verapamil Arms)
NCT01873950 (10) [back to overview]Change in Relationship (Ratio) Between Heart Rate and QT
NCT01873950 (10) [back to overview]Change in Spatial QRS-T Angle Using Exposure/Response (Ranolazine and Quinidine Arms)
NCT01873950 (10) [back to overview]Change in PR, QRS, J-Tpeak, Tpeak-Tend and QTc Using Exposure/Response (Dofetilide and Verapamil Arms)
NCT01873950 (10) [back to overview]Change in Ventricular Gradient Using Exposure/Response (Ranolazine and Quinidine Arms)
NCT01873950 (10) [back to overview]Placebo, and Baseline-adjusted Changes in Spatial QRS-T Angle
NCT01873950 (10) [back to overview]Placebo, and Baseline-adjusted Changes in Ventricular Gradient
NCT02319148 (12) [back to overview]Number of Participants With Potentially Clinically Significant Vital Signs Findings
NCT02319148 (12) [back to overview]Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Findings
NCT02319148 (12) [back to overview]Number of Participants Who Used at Least 1 Concomitant Medication
NCT02319148 (12) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-00489791
NCT02319148 (12) [back to overview]Terminal Elimination Half-Life (t1/2) of PF-00489791
NCT02319148 (12) [back to overview]Maximum Observed Plasma Concentration (Cmax) of PF-00489791
NCT02319148 (12) [back to overview]Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-00489791
NCT02319148 (12) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-00489791
NCT02319148 (12) [back to overview]Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern
NCT02319148 (12) [back to overview]Apparent Volume of Distribution (Vz/F) of PF-00489791
NCT02319148 (12) [back to overview]Apparent Oral Clearance (CL/F) of PF-00489791
NCT02319148 (12) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
NCT02372253 (6) [back to overview]Percent Change From Baseline in Exogenous Insulin Requirements
NCT02372253 (6) [back to overview]HbA1c
NCT02372253 (6) [back to overview]Percent Change From Baseline in Exogenous Insulin Requirements
NCT02372253 (6) [back to overview]HbA1C
NCT02372253 (6) [back to overview]Functional Beta Cell Mass
NCT02372253 (6) [back to overview]Hypoglycemic Events
NCT02454608 (9) [back to overview]Heart Rate
NCT02454608 (9) [back to overview]Diastolic Blood Pressure
NCT02454608 (9) [back to overview]Subjective Sinonasal Symptoms on Sinonasal Outcomes Test-22(SNOT-22)
NCT02454608 (9) [back to overview]Subjective Sinonasal Symptoms on Sinonasal Outcomes Test-22(SNOT-22)
NCT02454608 (9) [back to overview]Systolic Blood Pressure
NCT02454608 (9) [back to overview]Subjective Sinonasal Symptoms on 10cm Visual Analogue Scale(VAS)
NCT02454608 (9) [back to overview]Objective Sinonasal Symptoms on Lund-McKay Score(LMS)
NCT02454608 (9) [back to overview]Objective Sinonasal Symptoms on Lund-Kennedy Score(LKS)
NCT02454608 (9) [back to overview]Subjective Sinonasal Symptoms on 10cm Visual Analogue Scale(VAS)
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-t]).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Vz/F).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Total Body Clearance After Extravascular Administration Estimated as Dose Divided by AUC (CL/F).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration-time Curve (t½λz).
NCT02653872 (9) [back to overview]Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Observed Maximum Plasma Concentration (Cmax).
NCT02653872 (9) [back to overview]Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC).
NCT02653872 (9) [back to overview]Assessment of the Tmax of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Time to Reach Maximum Plasma Concentration (Tmax)
NCT02653872 (9) [back to overview]Assessment of the Area Under the Plasma Concentration-curve Over the Dosing Interval (AUC [0 - τ]) of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.
NCT03070470 (3) [back to overview]QTc Shortening From Calcium Block (Diltiazem) in the Presence of hERG Block (Dofetilide)
NCT03070470 (3) [back to overview]"Change From Baseline QTc With Predominant hERG Blocking Drug (Chloroquine)"
NCT03070470 (3) [back to overview]"Change From Baseline J-Tpeakc With Balanced Ion Channel Drugs (Ranolazine, Verapamil, Lopinavir / Ritonavir)"
NCT03102190 (1) [back to overview]Number of Participants With Dose Limiting Toxicity
NCT03296800 (5) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT03296800 (5) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT03296800 (5) [back to overview]Urinary Glucose Excretion 0-48 hr
NCT03296800 (5) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT03296800 (5) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)
NCT04374500 (5) [back to overview]Systolic Blood Pressure
NCT04374500 (5) [back to overview]Release of Fibrinolytic Variables (Tissue Plasminogen Activator [tPA] and Plasminogen Activator Inhibitor-1 [PAI-1])
NCT04374500 (5) [back to overview]Leptin
NCT04374500 (5) [back to overview]Heart Rate
NCT04374500 (5) [back to overview]Forearm Blood-flow (FBF)

Change in Blood Phenylalanine Levels From Baseline to Week 6.

(NCT00104247)
Timeframe: baseline to week 6

,
Interventionmicromole per liter (Mean)
Baseline Blood Phe LevelWeek 6 Blood Phe LevelMean Change in Blood Phe from Baseline to Week 6
Placebo8888916
Sapropterin Dihydrochloride843607-239

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Amount of Dietary Supplemented Phenylalanine (Phe)Tolerated in Children With Phenylketonuria

(NCT00272792)
Timeframe: at Week 10

Interventionmg/kg/day (Mean)
Sapropterin Dihydrochloride20.9
Placebo2.9

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Change in Phenylalanine Levels From Baseline to Week 3

(NCT00272792)
Timeframe: Baseline to Week 3

Interventionumol/L (Mean)
Sapropterin Dihydrochloride-147.4
Placebo-90.3

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Following Blood Phe Levels.

There were no pre-specified efficacy analysis, blood Phe samples were taken at each visit. Blood Phe concentrations remained within levels consistent with local clinical site recommendations for blood Phe control. (NCT00332189)
Timeframe: Baseline through Final Visit (a Maximum of 30 months) with blood phe samples taken at months 3 and 6 then at 6 month intervals

Interventionmicromoles per liter (Mean)
Baseline Blood Phe Level (N=111)Month 3 Blood Phe Level (N=109)Month 3 Change from Baseline (N=109)Month 6 Blood Phe Level (N=104)Month 6 Change from Baseline (N=104)Month 12 Blood Phe Level (N=97)Month 12 Change from Baseline (N=97)Month 18 Blood Phe Level (N=58)Month 18 Change from Baseline (N=58)Month 24 Blood Phe Level (N=45)Month 24 Change from Baseline (N=45)Month 30 Blood Phe Level (N=1)Month 30 Change from Baseline (N=1)
Total Patient Population607.4504.6-105.7529.9-68.0494.4-95.7526.9-92.8482.0-122.2808.0542.0

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Tabulation of the Incidence and Frequency of All AEs and SAEs That Occur Throughout the Study.

Safety was assessed with regards to the rate and type of AEs, clinically significant changes to vital signs and/or physical examination findings, and clinically significant changes in laboratory test results. (NCT00332189)
Timeframe: Baseline through Final Visit (a Maximum of 30 months) with AEs collected at month 3 and 6 then at 6 month intervals

Interventionpercentage of subjects reporting events (Number)
% of Subjects Reporting Any Adverse Event% of Subjects Reporting Related Adverse Events% of Subjects Reporting Serious Adverse Events% of Subjects Reporting Related Serious AEs
Total Patient Population83.833.36.30.9

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Number of Subjects With Adverse Events (AEs)

Adverse events were described and summarized with focus on treatment- emergent events (TEAEs). A TEAE was defined as any AE that presented , increased in frequency or worsened in severity following initiation of study drug administration. If the onset of an AE was missing then the AE was considered treatment emergent. Drug-related AEs are AEs classified by the investigator as possibly or probably related to study drug. (NCT00403494)
Timeframe: Up to 24-weeks

,
InterventionParticipants (Count of Participants)
Any AEsStudy Drug-related AEsAny SAEsStudy-Drug-related SAEsAny AEs leading to Study WithdrawalStudy Drug-related AEs leading to Study WIthdrawalAny SAEs Leading to Study WithdrawalStudy Drug-related SAEs Leading to Study WithdrawalDeaths
Placebo663011175110
Sapropterin Dihydrochloride8429140114401

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Change in Peak Walking Time From Baseline With and Without Vitamin C

The first 50% of subjects enrolled in the study were randomized to receive sapropterin dihydrochloride at 400 mg BID or oral placebo BID alone (without vitamin C). When approximately 50% enrollment was met, 1000 mg/day vitamin C was added to the dose regimen of newly enrolled subjects in both sapropterin dihydrochloride and placebo treatment groups given orally in two divided doses of 500 mg with study drug. (NCT00403494)
Timeframe: Baseline up to 24 weeks

,
Interventionminutes (Mean)
Baseline without vitamin CChange from Baseline week 24; without vitamin CBaseline with vitamin CChange from Baseline week 24; with vitamin C
Placebo5.2010.6076.1642.255
Sapropterin Dihydrochloride4.7760.2645.9441.826

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Change in Peak Walking Time (PWT) From Baseline

This is to assess the effect of oral sapropterin dihydrochloride versus placebo on peak walking time (PWT) in subjects with intermittent claudication (IC) caused by peripheral arterial disease (PAD). (NCT00403494)
Timeframe: Baseline and up to Week 24

,
Interventionminutes (Mean)
BaselineChange from Baseline to Week 24
Placebo5.7121.493
Sapropterin Dihydrochloride5.3941.121

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Change in Claudication Onset Time (COT) From Baseline

Time, in minutes, when the subject first begins to experience claudication symptoms, regardless of whether this is manifested as muscle pain, ache, cramp, numbness or fatigue. (NCT00403494)
Timeframe: Baseline and up to Week 24

,
Interventionminutes (Mean)
BaselineChange from Baseline to Week 24
Placebo2.3131.015
Sapropterin Dihydrochloride2.1590.903

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Change From Baseline in the Peripheral Arterial Tonometry (PAT) Scores

The PAT score was calculated using the ratio between the arterial pulse wave amplitude following a 5-minute arterial occlusion in the forearm to the pre-occlusion value (Reactive Hyperemia Index). A value of NCT00445978)
Timeframe: At Baseline, Week 4, 8, 12 and 16.

InterventionRatio (Mean)
BaselineChange from Baseline to Week 4Change from Baseline to Week 8Change from Baseline to Week 12Change from Baseline to Week 16
Sapropterin Dihydrochloride1.58150.13170.28520.36560.3604

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Change From Baseline in the Tricuspid Regurgitant Velocity (TRV)

Change in tricuspid regurgitant velocity (TRV) from Baseline to post-treatment visit is calculated by subtracting the Baseline measurement from the post-treatment measurement. (NCT00445978)
Timeframe: At Baseline, Week 4, 8, 12 and 16.

Interventionm/sec (Mean)
BaselineChange from Baseline to Week 4Change from Baseline to Week 8Change from Baseline to Week 12Change from Baseline to Week 16
Sapropterin Dihydrochloride2.090.090.030.010.16

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Change From Baseline in the Urine 8-Isoprostane

Change in urine 8-isoprostane from Baseline to post-treatment visit is calculated by subtracting the Baseline measurement from the post-treatment measurement. This outcome was used to assess change in oxidative stress. (NCT00445978)
Timeframe: At Baseline, Week 4, 8, 12 and 16.

Interventionpg/mg creatinine (Mean)
BaselineChange from Baseline to Week 4Change from Baseline to Week 8Change from Baseline to Week 12Change from Baseline to Week 16
Sapropterin Dihydrochloride1019.68-27.58-69.7524.71-275.19

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Change From Baseline in the Urine Spot Albumin to Creatinine Ratio

Change in Urine Albumin to Creatinine Ratio from Baseline to post-treatment visit is calculated by subtracting the Baseline measurement from the post-treatment measurement. This outcome was used to assess change in renal function. (NCT00445978)
Timeframe: At Baseline, Week 4, 8, 12 and 16.

Interventionmg/mmol (Mean)
BaselineChange from Baseline to Week 4Change from Baseline to Week 8Change from Baseline to Week 12Change from Baseline to Week 16
Sapropterin Dihydrochloride17.881.66-5.51-10.76-9.32

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Number of Subjects With Treatment Emergent Adverse Events (TEAEs)

A treatment-emergent adverse events (TEAE) is any adverse events that newly appeared, increased in frequency or worsened in severity following initiation of study drug administration. (NCT00445978)
Timeframe: Up to 16 weeks

,,,
InterventionParticipants (Count of Participants)
Subjects with any adverse eventSubjects with any serious adverse eventsSubjects with any treatment-related adverse eventAny subject with a treatment-related serious adverse eventAny subject with an AE causing study discontinuationAny subject with an SAE causing study discontinuationDeath
Sapropterin Dihydrochloride 10.0 mg/kg/Day20662000
Sapropterin Dihydrochloride 2.5 mg/kg/Day27390110
Sapropterin Dihydrochloride 20.0 mg/kg/Day15330100
Sapropterin Dihydrochloride 5.0 mg/kg/Day18241110

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Area Under the Curve (AUC0-12hours) for Calculated BH4 (From Total Biopterin)

Total biopterin concentration area under the curve (AUC0-12hours) at the end of each regimen in subjects with endothelial dysfunction is theoretically the sum of BH4, BH2 and B. Biopterin is the metabolite of BH4 after oxidative conversion of BH4 and BH2 to biopterin. Total biopterin concentrations represent the summation of drug and metabolites: BH4, BH2 and B. The total biopterin concentrations can be converted to BH4 concentration using the conversion factor 2.150. (NCT00532844)
Timeframe: At 30 minutes prior to dosing, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 5.0, 6.0, 8.0, 10.0, and 12.0 hours after dosing.

InterventionnM*hr (Mean)
Sapropterin Dihydrochloride440
Sapropterin Dihydrochloride+Vitamin C440

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Area Under the Curve (AUC0-12hrs) of Plasma BH4 Concentration

Plasma BH4 concentration area under the curve (AUC0-12 hrs) at the end of each regimen in subjects with endothelial dysfunction. (NCT00532844)
Timeframe: At 30 minutes prior to dosing, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 5.0, 6.0, 8.0, 10.0, and 12.0 hours after dosing.

InterventionnM*hr (Mean)
Sapropterin Dihydrochloride 10 mg/kg633
Sapropterin Dihydrochloride+Vitamin C 10 mg/kg993

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Area Under the Curve (AUC0-12hrs) of Plasma BH2 and B Concentration

Plasma BH2 and B concentration area under the curve (AUC0-12hrs) at the end of each regimen in subjects with endothelial dysfunction. (NCT00532844)
Timeframe: At 30 minutes prior to dosing, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 5.0, 6.0, 8.0, 10.0, and 12.0 hours after dosing.

,
InterventionnM*hr (Mean)
BH2B
Sapropterin Dihydrochloride875231
Sapropterin Dihydrochloride+Vitamin C772185

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Change From Baseline in Cyclic Guanosine Monophosphate (cGMP)

Biomarkers of endothelial function, oxidative stress, and inflammation as measured by cyclic guanosine monophosphate (cGMP). (NCT00532844)
Timeframe: At Baseline, Day 14 and Day 28.

,
Interventionpmol/mL (Mean)
BaselineChange from Baseline to Day 14Change from Day 14 to Day 28
Sapropterin Dihydrochloride 10mg/kg Vitamin C3.79410.6278-0.0507
Sapropterin dihydrochloride10mg/kg and Vitamin C3.85330.2088-0.0078

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Change From Baseline in Diastolic Blood Pressure (DBP)

"Change is calculated as follows: end time measurement - starting time measurement.~Mean daytime diastolic blood pressure measured by ambulatory blood pressure monitoring (ABPM)" (NCT00532844)
Timeframe: At Baseline, Day 13 and Day 27

,
Interventionmm Hg (Mean)
BaselineChange from Baseline to Day 13Change from Day 13 to Day 27
Sapropterin Dihydrochloride 10mg/kg and Vitamin C80.150.451.23
Sapropterin dihydrochloride10mg/kg77.32-2.31-2.01

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Change From Baseline in Peripheral Arterial Tonometry (PAT)

PAT measures pulse wave amplitude of the small arteries of the finger as a surrogate to assess endothelial function and arterial stiffness using a finger plethysmographic probe and 5-minute occlusion of the brachial artery. Endothelial dysfunction, a protocol inclusion criteria, is defined by an abnormal PAT of < or = 1.70. Change is calculated as follows: end time measurement - starting time measurement. (NCT00532844)
Timeframe: At Baseline, Day 13 and Day 27

,
InterventionRatio (Mean)
BaselineDay 13Change from Baseline to Day 13Day 27Change from Day 13 to Day 27
Sapropterin Dihydrochloride 10mg/kg1.51131.85090.34671.90470.1293
Sapropterin Dihydrochloride 10mg/kg and Vitamin C1.48591.77540.29021.6482-0.1641

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Change From Baseline in Systolic Blood Pressure (SBP)

"Change is calculated as follows: end time measurement - starting time measurement.~Mean daytime systolic blood pressure measured by ambulatory blood pressure monitoring (ABPM)" (NCT00532844)
Timeframe: At Baseline, Day 13 and Day 27

,
Interventionmm Hg (Mean)
BaselineChange from Baseline to Day 13Change from Day 13 to Day 27
Sapropterin Dihydrochloride 10mg/kg and Vitamin C131.29-0.103.31
Sapropterin dihydrochloride10mg/kg125.14-3.24-1.67

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Change in Urinary Albumin to Creatinine Ratio (mg/g)

Change in Urinary Albumin to Creatinine Ratio (mg/g) from Baseline to Day 14, Baseline to Day 28, and from Day 14 to Day 28 (NCT00532844)
Timeframe: Baseline, Day 14 and Day 28

,
Interventionmg/g (Mean)
BaselineChange from Baseline to Day 14Change from Day 14 to Day 28
Sapropterin Dihydrochloride 10mg/kg13.3-1.2-2.2
Sapropterin Dihydrochloride 10mg/kg and Vitamin C12.32.74.9

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Number of Participants With Urinary Albumin to Creatinine Ratio <30 mg/g

Summary of Urinary Albumin to Creatinine Ratio (mg/g) by subjects with ratio <30 mg/g and subjects with ratios >=30 mg/g at Baseline, Day 14 and Day 28 (NCT00532844)
Timeframe: Baseline, Day 14 and Day 28

,
InterventionParticipants (Count of Participants)
Baseline < 30 mg/gBaseline >=30 mg/gDay 14 < 30 mg/gDay 14 >=30 mg/gDay 28 < 30 mg/gDay 28 >=30 mg/g
Sapropterin Dihydrochloride 10mg/kg131102121
Sapropterin Dihydrochloride 10mg/kg and Vitamin C162131102

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Number of Subjects With Treatment Emergent Adverse Events (TEAEs)

A treatment-emergent Adverse Events (TEAE) is any Adverse Events that newly appeared, increased in frequency or worsened in severity following initiation of study drug administration. (NCT00532844)
Timeframe: Up to 56 ± 3 Days.

,
InterventionParticipants (Count of Participants)
Subjects with any Adverse EventSubjects with any Serious Adverse EventSubjects with any treatment-related Adverse EventAny treatment-related Serious Adverse EventDeathAny AEs Leading to Study Discontinuation
Sapropterin Dihydrochloride19016001
Sapropterin Dihydrochloride+Vitamin C16013000

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Ratio of BH2, B and BH4 Calculated From Total Biopterin Area Under the Curve (0-12hours) for Subjects Administered Sapropterin Dihydrochloride With Vitamin C to Subjects Administered Sapropterin Alone.

Ratio of Mean AUC (0-12 hours) for subjects receiving (Sapropterin dihydrochloride + Vitamin C)/ Mean AUC (0-12 hours) for subjects receiving Sapropterin dihydrochloride alone) for BH4, BH2, B, BH4/BH2 Ratio, and BH4 Calculated from Total Biopterin. (NCT00532844)
Timeframe: At 30 minutes prior to dosing, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 5.0, 6.0, 8.0, 10.0, and 12.0 hours after dosing.

Interventionratio (Mean)
BH2BCalculated BH4 (from Total Biopterin)
(Sapropterin Dihydrochloride+Vitamin C)/(Sapropterin Dihydrochloride)0.9981.041.03

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Change From Baseline in Urinary 8-isoprostane/Creatinine

Biomarkers of endothelial function, oxidative stress, and inflammation as measured by 8-isoprostane. (NCT00532844)
Timeframe: At Baseline, Day 14 and Day 28

,
Interventionpg/mg (Mean)
BaselineChange from Baseline to Day 14Change from Day 14 to Day 28
Sapropterin Dihydrochloride 10mg/kg898.01-192.13-117.61
Sapropterin dihydrochloride10mg/kg and Vitamin C992.38-31.7532.44

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Cardiac Hospitalization Within Six Months of Enrollment

Number of patients who were hospitalized for cardiovascular problems within 6 months of enrollment. (NCT00589303)
Timeframe: Six months after enrollment

Interventionparticipants (Number)
Drug Therapy3
Atrioventricular Node (AVN) Ablation / Pacing4

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Median Progression-free Survival Rates of the Treatment Population.

Response and progression will be evaluated in this study using measurements from the MRI/CT scans. Measurements will be made of the image slice with the largest cross sectional area. Two orthogonal measures will be made to determine maximal AP and lateral dimensions. Progression of disease will be defined as a greater than 25% increase of largest cross sectional area by two orthogonal measurements, taking as reference the smallest sum recorded since the treatment started or the appearance of one or more new lesions. (NCT00706810)
Timeframe: 31 months

Interventionmonths (Median)
All Participants8.0

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Number of Subjects With Adverse Events (AEs)

"Adverse Event is any untoward medical occurrence in a patient or clinical investigation subject administered a pharmaceutical product, and that does not necessarily have a causal relationship with this treatment.~Drug Related Adverse all noxious and unintended responses to a medical product related to any dose. This means that a causal relationship between a medicinal product and an AE is at least a reasonable possibility, ie, the relationship cannot be ruled out.~A serious adverse event (SAE) is an AE that resulted in any of the following outcomes: death; life threatening; persistent/significant disability/incapacity; initial or prolonged inpatient hospitalization; congenital anomaly/birth defect." (NCT00838435)
Timeframe: Up to 7 years

InterventionParticipants (Count of Participants)
Any Adverse Events (AEs)Drug-Related Adverse EventsAny Serious Adverse EventsDrug-Related Serious Adverse EventsAny AEs causing study discontinuationDrug-related AEs causing study discontinuationDeath
Part 26535112220

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Full-Scale Intelligence Quotient (FSIQ) Score

"Full Scale Intelligence Quotient (FSIQ) is a score derived through administration of selected subtests from age appropriate Wechsler Intelligence assessments. Weschler Preschool and Primary Scale of Intelligence (WPPSI)-III is used for children >30 months and ≤6 years; and Weschler Intelligence Scale for Children (WISC)-IV is used for children >6 years old. The outcome variable will be the FSIQ score from WPPSI-III and/or WISC-IV tests.~FSIQ results can range from 40 being the lowest and 160 being the highest. Higher scores are associated with higher intelligence quotient." (NCT00838435)
Timeframe: Assessments through 84 months.

Interventionscore on a scale (Mean)
FSIQ BaselineFSIQ Month 12FSIQ Month 24FSIQ Month 36FSIQ Month 48FSIQ Month 60FSIQ Month 72FSIQ Month 84
Kuvan 20 mg/kg Once Daily101.06103.64104.69103.78104.25100.76104.57104.22

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Change From Baseline in Growth Measurements - Weight Z-Scores

"Z-scores of Weight determined using World Health Organization(WHO) growth charts for children <24 months and Centers for Disease Control and Prevention(CDC) clinical growth charts for children 24 months or older.~A weight z-score is a standardized weight measure after considering important factors like age and gender, in which higher z-scores are associated with heavier children. Z-scores (or standard deviation scores) describe how far a measurement is from the median (mean). A z-score of 0 is the same as a 50th percentile; a positive value is a factor of SD unit above the 50%; and a negative value is a factor of SD unit below 50%." (NCT00838435)
Timeframe: Baseline and up to 84 months

InterventionZ-score change from baseline (Mean)
BaselineChange from Baseline Week 4Change from Baseline Month 3Change from Baseline Month 6Change from Baseline Month 12Change from Baseline Month 18Change from Baseline Month 24Change from Baseline Month 30Change from Baseline Month 36Change from Baseline Month 42Change from Baseline Month 48Change from Baseline Month 54Change from Baseline Month 60Change from Baseline Month 66Change from Baseline Month 72Change from Baseline Month 78Change from Baseline Month 84
Sapropterin Dihydrochloride0.40.00.00.00.10.10.10.10.10.00.00.00.00.00.00.00.0

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Change From Baseline in Growth Measurements - Height Z-Scores

"Z-scores of Height determined using World Health Organization(WHO) growth charts for children <24 months and Centers for Disease Control and Prevention(CDC) clinical growth charts for children 24 months and older.~A height z-score is a standardized height measure after considering important factors like age and gender, in which higher z-scores are associated with taller children. Z-scores (or standard deviation scores) describe how far a measurement is from the median (mean). A z-score of 0 is the same as a 50th percentile; a positive value is a factor of standard deviation (SD) unit above the 50%; and a negative value is a factor of SD unit below 50%." (NCT00838435)
Timeframe: Baseline and up to 84 months

InterventionZ-score change from baseline (Mean)
BaselineChange from Baseline Week 4Change from Baseline Month 3Change from Baseline Month 6Change from Baseline Month 12Change from Baseline Month 18Change from Baseline Month 24Change from Baseline Month 30Change from Baseline Month 36Change from Baseline Month 42Change from Baseline Month 48Change from Baseline Month 54Change from Baseline Month 60Change from Baseline Month 66Change from Baseline Month 72Change from Baseline Month 78Change from Baseline Month 84
Sapropterin Dihydrochloride0.40.00.10.1-0.10.00.0-0.1-0.1-0.1-0.2-0.2-0.2-0.2-0.3-0.2-0.2

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Change From Baseline in Growth Measurements - Head Circumference Z-Scores

"Z-scores of Head Circumference determined using World Health Organization(WHO) growth charts for children <24 months and Centers for Disease Control and Prevention(CDC) clinical growth charts for children 24 months and older.~A head circumference z-score is a standardized head circumference measure after considering important factors like age and gender, in which higher z-scores are associated with children with larger heads. Z-scores (or standard deviation scores) describe how far a measurement is from the median (mean). A z-score of 0 is the same as a 50th percentile; a positive value is a factor of SD unit above the 50%; and a negative value is a factor of SD unit below 50%." (NCT00838435)
Timeframe: Baseline and up to 84 months

InterventionZ-score change from baseline (Mean)
BaselineChange from Baseline Week 4Change from Baseline Month 3Change from Baseline Month 6Change from Baseline Month 12Change from Baseline Month 18Change from Baseline Month 24Change from Baseline Month 30
Sapropterin Dihydrochloride0.20.10.00.10.1-0.10.20.8

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Apparent Volume of Distribution (V/F) of Kuvan

Population pharmacokinetic parameter apparent volume of distribution (V/F) (NCT00838435)
Timeframe: At predose and postdose - 0.22, 3.2 and 7 hours

InterventionL (Mean)
Sapropterin Dihydrochloride1209

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Baseline Concentration of Tetrahydrobiopterin (BH4)(C0)

Baseline concentration of BH4(C0) with associated inter-individual variability. (NCT00838435)
Timeframe: At predose and postdose - 0.22, 3.2 and 7 hours

Interventionµg/L (Least Squares Mean)
Sapropterin Dihydrochloride16.6

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Change From Baseline in Bayley-III Scores - Neurocognitive Testing Results

The Bayley-III is a tool for assessing all facets of development in infants within an age range of 12 to 30 months, with normative data available for infants as young as 16 days. Composite scores are derived for cognitive, language, and motor development and scaled to a metric, with a range of 40 to 160. Higher scores are a better outcome. (NCT00838435)
Timeframe: At Month 6, 12, 18 and 24

Interventionscore on a scale (Mean)
Cognitive: BaselineCognitive: Change from Baseline Month 6Cognitive: Change from Baseline Month 12Cognitive: Change from Baseline Month 18Cognitive: Change from Baseline Month 24Language: BaselineLanguage: Change from Baseline Month 6Language: Change from BaselineMonth 12Language: Change from Baseline Month 18Language: Change from Baseline Month 24Motor: BaselineMotor: Change from Baseline Month 6Motor: Change from Baseline Month 12Motor: Change from Baseline Month 18Motor: Change from Baseline Month 24
Sapropterin Dihydrochloride102.315.682.112.270.83100.732.591.374.82-3.00104.961.322.110.187.50

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Absorption Rate Constant (Ka) of Kuvan

Population pharmacokinetic parameter, Absorption Rate Constant (Ka) (NCT00838435)
Timeframe: At predose and postdose - 0.22, 3.2 and 7 hours

Interventionl/hour (Least Squares Mean)
Sapropterin Dihydrochloride0.235

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Apparent Clearance (CL/F) of Kuvan

Population pharmacokinetic parameter apparent clearance (CL/F) (NCT00838435)
Timeframe: At predose and postdose - 0.22, 3.2 and 7 hours

InterventionL/hour (Mean)
Sapropterin Dihydrochloride815

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Area Under the Concentration Versus Time Curve From Time 0 to Time t [AUC(0-t)]

The area under the plasma concentration versus time curve beginning from the first dose (time 0) to the last measurable colchicine concentration (time t), as calculated by the linear trapezoidal method. (NCT00983242)
Timeframe: On Days 1 and 19 - serial pharmacokinetic blood samples were collected pre-dose and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose.

Interventionpg-hr/mL (Mean)
Colchicine Alone13,085.26
Colchicine With Verapamil HCl ER24,637.91

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Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]

The area under the plasma concentration versus time curve from time 0 to infinity. AUC(0-∞) was calculated as the sum of AUC(0-t) plus the ratio of the last measurable colchicine plasma concentration to the elimination rate constant. (NCT00983242)
Timeframe: On Days 1 and 19 - serial pharmacokinetic blood samples were collected pre-dose and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose.

Interventionpg-hr/mL (Mean)
Colchicine Alone15,371.17
Colchicine With Verapamil HCl ER30,586.33

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Maximum Plasma Concentration (Cmax)

The maximum or peak concentration that colchicine reaches in the plasma. (NCT00983242)
Timeframe: On Days 1 and 19 - serial pharmacokinetic blood samples were collected pre-dose and at 0.5, 1.0, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose.

Interventionpg/mL (Mean)
Colchicine Alone2,968.42
Colchicine With Verapamil HCl ER3,850.63

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Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on ADHD through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The total ADHD-RS score and the corrected total ARS score range from 0 to 54, with higher scores corresponding to worse severity of ADHD symptoms." (NCT01114737)
Timeframe: Week 13 to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm With ADHD Symptoms-4.0
Responders in 6R-BH4 20 mg/kg/Day Arm With ADHD Symptoms-1.4

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Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Baseline to Week 13

"Effects of 6R-BH4 on symptoms of ADHD in PKU subjects who had symptoms of ADHD at screening in the subjects that had a blood Phe level reduction after treatment with 6R-BH4.~The total ADHD-RS score and the corrected total ARS score range from 0 to 54, with higher scores corresponding to worse severity of ADHD symptoms." (NCT01114737)
Timeframe: Baseline to Week 13

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm With ADHD Symptoms-4.9
Responders in 6R-BH4 20 mg/kg/Day Arm With ADHD Symptoms-9.1

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Change in Attention-Deficit Hyperactivity Disorder Rating Scale-IV (ADHD-RS) / Adult ADHD Self-Report Scale (ASRS) Total Score From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on ADHD through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The total ADHD-RS score and the corrected total ARS score range from 0 to 54, with higher scores corresponding to worse severity of ADHD symptoms." (NCT01114737)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm With ADHD Symptoms-9.5
Responders in 6R-BH4 20 mg/kg/Day Arm With ADHD Symptoms-9.3

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Baseline to Week 13

"Effects of 6R-BH4 on executive function in PKU subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Baseline to Week 13

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-8.1
Responders in 6R-BH4 20 mg/kg/Day Arm-9.1

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on executive function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Baseline to Week 26

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-7.1
Responders in 6R-BH4 20 mg/kg/Day Arm-7.7

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Adult-Global Executive Composite (GEC) T Score From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on executive function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Week 13 to Week 26

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-0.7
Responders in 6R-BH4 20 mg/kg/Day Arm0.9

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Baseline to Week 13

"Effects of 6R-BH4 on executive function in PKU subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Baseline to Week 13

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-0.7
Responders in 6R-BH4 20 mg/kg/Day Arm-4.8

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on executive function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Baseline to Week 26

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-2.6
Responders in 6R-BH4 20 mg/kg/Day Arm-4.8

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Change in Behavior Rating Inventory of Executive Function (BRIEF) Parent-Global Executive Composite (GEC) T Score From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on executive function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~The scoring for the GEC T Score is complex and is achieved using proprietary software designed to generate scores based on raw data collected. Higher scores suggest a higher level of dysfunction." (NCT01114737)
Timeframe: Week 13 to Week 26

InterventionT score (Least Squares Mean)
Responders in Placebo Arm-1.3
Responders in 6R-BH4 20 mg/kg/Day Arm0.0

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Change in Clinical Global Impression-Severity (CGI-S) From Baseline to Week 13

"Effects of 6R-BH4 on global function in PKU subjects who had a blood Phe level reduction after treatment with 6R-BH4.~CGI-S is a 7-point scale that requires the clinician to rate the severity of the subject's mental illness at the time of assessment, relative to clinician's past experience with subjects who have the same diagnosis. Considering total clinical experience, a subject is assessed on the severity of mental illness at the time of rating as: 1, normal, not at all ill; 2, borderline ill; 3, mildly ill; 4, moderately ill; 6, severely ill; or 7, among the most extremely ill." (NCT01114737)
Timeframe: Baseline to Week 13

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-0.5
Responders in 6R-BH4 20 mg/kg/Day Arm-0.6

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Change in Clinical Global Impression-Severity (CGI-S) From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on global function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~CGI-S is a 7-point scale that requires the clinician to rate the severity of the subject's mental illness at the time of assessment, relative to clinician's past experience with subjects who have the same diagnosis. Considering total clinical experience, a subject is assessed on the severity of mental illness at the time of rating as: 1, normal, not at all ill; 2, borderline ill; 3, mildly ill; 4, moderately ill; 6, severely ill; or 7, among the most extremely ill." (NCT01114737)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Mean)
Responders in Placebo Arm-0.6
Responders in 6R-BH4 20 mg/kg/Day Arm-0.5

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Change in Clinical Global Impression-Severity (CGI-S) From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on global function through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~CGI-S is a 7-point scale that requires the clinician to rate the severity of the subject's mental illness at the time of assessment, relative to clinician's past experience with subjects who have the same diagnosis. Considering total clinical experience, a subject is assessed on the severity of mental illness at the time of rating as: 1, normal, not at all ill; 2, borderline ill; 3, mildly ill; 4, moderately ill; 6, severely ill; or 7, among the most extremely ill." (NCT01114737)
Timeframe: Week 13 to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-0.0
Responders in 6R-BH4 20 mg/kg/Day Arm0.1

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Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Baseline to Week 13

"Effects of 6R-BH4 on symptoms of anxiety in PKU subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-A Score is a total score ranging from 0 to 56 with higher scores corresponding to worse severity of anxiety symptoms. The HAM-A has 14 items, each measuring specific anxiety symptom clusters. Each item is given a 5-point-score as: 0, absent; 1, mild; 2, moderate; 3, severe; or 4, incapacitating." (NCT01114737)
Timeframe: Baseline to Week 13

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-3.6
Responders in 6R-BH4 20 mg/kg/Day Arm-3.2

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Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on anxiety through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-A Score is a total score ranging from 0 to 56 with higher scores corresponding to worse severity of anxiety symptoms. The HAM-A has 14 items, each measuring specific anxiety symptom clusters. Each item is given a 5-point-score as: 0, absent; 1, mild; 2, moderate; 3, severe; or 4, incapacitating." (NCT01114737)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-3.9
Responders in 6R-BH4 20 mg/kg/Day Arm-4.2

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Change in Hamilton Depression Rating Scale (HAM-D) Score From Baseline to Week 13

"Effects of 6R-BH4 on symptoms of depression in PKU subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-D Score is a total score ranging from 0 to 48 with higher scores corresponding to worse severity of depression. The HAM-D is a 17-item depression rating scale. Nine of the items are scored on a 5-point scale as: 0, absence of depressive symptom being measured; 1, doubt concerning the presence of the symptom; 2, mild symptoms; 3, moderate symptoms; or 4, severe symptoms. The remaining 8 items are scored on a 3-point scale as: 0, absence; 1, doubt on the presence of the symptom; or 2, clear presence of symptoms." (NCT01114737)
Timeframe: Baseline to Week 13

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-2.5
Responders in 6R-BH4 20 mg/kg/Day Arm-2.1

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Change in Hamilton Depression Rating Scale (HAM-D) Score From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on depression through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-D Score is a total score ranging from 0 to 48 with higher scores corresponding to worse severity of depression. The HAM-D is a 17-item depression rating scale. Nine of the items are scored on a 5-point scale as: 0, absence of depressive symptom being measured; 1, doubt concerning the presence of the symptom; 2, mild symptoms; 3, moderate symptoms; or 4, severe symptoms. The remaining 8 items are scored on a 3-point scale as: 0, absence; 1, doubt on the presence of the symptom; or 2, clear presence of symptoms." (NCT01114737)
Timeframe: Week 13 to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm0.1
Responders in 6R-BH4 20 mg/kg/Day Arm0.5

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Change in Hamilton Rating Scale For Depression (HAM-D) Score From Baseline to Week 26

"Durability of the therapeutic effect of 6R-BH4 on depression through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-D Score is a total score ranging from 0 to 48 with higher scores corresponding to worse severity of depression. The HAM-D is a 17-item depression rating scale. Nine of the items are scored on a 5-point scale as: 0, absence of depressive symptom being measured; 1, doubt concerning the presence of the symptom; 2, mild symptoms; 3, moderate symptoms; or 4, severe symptoms. The remaining 8 items are scored on a 3-point scale as: 0, absence; 1, doubt on the presence of the symptom; or 2, clear presence of symptoms." (NCT01114737)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm-2.6
Responders in 6R-BH4 20 mg/kg/Day Arm-2.0

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Number of Participants With a Score of 1 or 2 in Global Function Evaluation (CGI-I) From Baseline to Week 13.

"Effects of 6R-BH4 on global function in PKU subjects in subjects that had a blood Phe level reduction after treatment with 6R-BH4 at screening.~The CGI-I is a 7-point scale that requires the clinician to assess how much the participant's illness has improved or worsened relative to a baseline state at the beginning of the intervention and rated as: 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse." (NCT01114737)
Timeframe: 13 weeks

InterventionNumber of participants with scale 1 or 2 (Number)
Responders in Placebo Arm15
Responders in 6R-BH4 20 mg/kg/Day Arm13

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Change in Hamilton Anxiety Rating Scale (HAM-A) Score From Week 13 to Week 26

"Durability of the therapeutic effect of 6R-BH4 on anxiety through 26 weeks in subjects who had a blood Phe level reduction after treatment with 6R-BH4.~HAM-A Score is a total score ranging from 0 to 56 with higher scores corresponding to worse severity of anxiety symptoms. The HAM-A has 14 items, each measuring specific anxiety symptom clusters. Each item is given a 5-point-score as: 0, absent; 1, mild; 2, moderate; 3, severe; or 4, incapacitating." (NCT01114737)
Timeframe: Week 13 to Week 26

Interventionunits on a scale (Least Squares Mean)
Responders in Placebo Arm0.1
Responders in 6R-BH4 20 mg/kg/Day Arm-0.5

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Gastric Accommodation

"Gastric Accommodation refers to the reflexive relaxation of the upper stomach after swallowing as measured by the Satiety Test at baseline, 4 weeks, and 8 weeks.~Increased gastric accommodation is considered a positive outcome." (NCT01135186)
Timeframe: Baseline, 4 Weeks, 8 Weeks

Interventionml (Mean)
Baseline4 Weeks8 Weeks
Open Label Study322.22402.78450.63

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Secondary Outcome Measures Will Include Change in Quality of Life.

"Quality of life as impacted by patients with upper gastrointestinal disorders (PAGI-QOL)~The PAGI-QOl is composed of 30 questions.~Each question asks about the degree to which a patient's quality of life is impacted by upper gastrointestinal disorders.~Questions measure quality of life impact on a scale of 1-5 listed below.~0=none of the time, 1=a little of the time, 2=some of the time, 3=a good bit of the time, 4= most of the time, 5= all of time~The 30 items are summed together for a cumulative PAGI-QOL score. The minimum cumulative score is 0 and the maximum score is 150.~Once we calculated the cumulative score for each participant, we took the average of all participants cumulative scores giving us the sample mean. This was done at baseline, week 4, and week 8.~Lower scores indicate an improved overall quality of life. Higher scores indicate a diminished overall quality of life." (NCT01135186)
Timeframe: Baseline, 4 Weeks, 8 Weeks

Interventionunits on a scale (Mean)
Baseline4 Weeks8 Weeks
Open Label Study91.2261.2960.50

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Secondary Outcome Measures Will Include Change in Symptom Severity as Measured by the Patient Assessment of Gastrointestinal Disorder-Symptom Severity Index Disorders Symptom Severity Index (PAGI-SYM)

"Symptom severity as measured by the Patient Assessment of Upper Gastrointestinal Disorder- Symptom Severity Index. (PAGI-SYM)~The PAGI-SYM is compose of 20 questions.~Each question can be answered on a scale of 1-5 (below)~0 = none, 1=very mild, 2=mild, 3=moderate, 4=severe, 5=very severe~Cumulative scores were calculated by summing all 20 questions.~The minimum cumulative scores would be 0 while the maximum cumulative score would be 100~Once we calculated the cumulative score for each participant, we took the average of all the cumulative scores giving us the sample mean. This was done at baseline, week 4, and week 8.~Lower score indicates decreased symptom severity. Higher score indicates increased symptom severity." (NCT01135186)
Timeframe: Baseline, 4 Weeks, 8 Weeks

Interventionunits on a scale (Mean)
Baseline4 Weeks8 Weeks
Open Label Study54.8941.5034.50

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Secondary Outcome Measures Will Include Change in Symptom Severity.

"Change in symptom severity over the past 2 weeks as measured by the patient reported Gastroparesis Cardinal Symptom Index (GCSI)~The GCSI is composed of 9 questions.~Each question asks about symptom severity on a scale of 1-5 listed below.~0=None 1= Very mild 2= Mild 3=Moderate 4=Severe 5= Very severe~The 9 scores are summed together for cumulative GCSI score. The minimum cumulative score is '0 and the maximum cumulative score is 45.~Once we calculated the cumulative score for each participant, we took the average of all participants cumulative scores giving us the sample mean. This was done at baseline, week 4, and week 8.~Higher total scores indicate higher symptom severity. Lower total scores indicate lower symptom severity." (NCT01135186)
Timeframe: Baseline, 4 Weeks, 8 Weeks

Interventionunits on a scale (Mean)
Baseline4 Weeks8 Weeks
Open Label Study32.0023.2523.67

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Preschool Language Scales

Change in the raw score from baseline of the Preschool Language Scales over the 16 week period. The raw score was measured at baseline, 8 weeks and 16 weeks after starting treatment and the change over the 16 week period from baseline to the end of the study was calculated. There was no imputed data and the analysis was as treated. The raw score ranged from 0 to 130. Higher scores indicate better performance. (NCT01141595)
Timeframe: 16 weeks

InterventionRaw score units / 16 weeks (Mean)
Kuvan®7.6

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Area Under the Curve 0 to Infinity (AUC0-∞)

Area under the concentration-time curve of empagliflozin in plasma over the time interval from 0 extrapolated to infinity. (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionnmol*h/L (Geometric Mean)
Empa5190
Empa Plus Verapamil5340

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Area Under the Curve 0 to Time of Last Quantifiable Data Point (AUC0-tz)

Area under the concentration-time curve of empagliflozin (empa) in plasma over the time interval from 0 to time of last quantifiable data point. (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionnmol*h/L (Geometric Mean)
Empa5140
Empa Plus Verapamil5280

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Clinically Relevant Abnormalities for Physical Examination, Vital Signs, Blood Chemistry and Electrocardiogram (ECG).

Clinically relevant abnormalities for physical examination, vital signs , blood chemistry and Electrocardiogram (ECG). New or abnormal findings were reported as adverse events. (NCT01276301)
Timeframe: Day1 to Day 11

Interventionparticipants (Number)
Empa0
Empa Plus Verapamil0

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Terminal Elimination Rate Constant (λz)

"Terminal elimination rate constant in plasma.~Note: The numbers provide below for standard deviation are of Coefficient of Variation." (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Intervention1/h (Geometric Mean)
Empa0.0573
Empa Plus Verapamil0.0531

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Maximum Measured Concentration (Cmax)

Maximum measured concentration of empagliflozin (empa) in plasma. (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionnmol (Geometric Mean)
Empa785
Empa Plus Verapamil725

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Mean Residence Time in the Body After Administration (MRTpo)

"Mean residence time of empagliflozin (empa) in the body after oral administration.~Note: The numbers provide below for standard deviation are of Coefficient of Variation." (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionh (Geometric Mean)
Empa9.47
Empa Plus Verapamil9.95

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Apparent Volume of Distribution Following an Extravascular Dose (Vz/F)

"Apparent volume of distribution during the terminal phase following an extravascular dose.~Note: The numbers provide below for standard deviation are of Coefficient of Variation." (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

InterventionL (Geometric Mean)
Empa186
Empa Plus Verapamil195

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Assessment of Tolerability by Investigator

Tolerability will be assessed by the investigator according to the categories good, satisfactory, not satisfactory , bad and not assessable. (NCT01276301)
Timeframe: Within Day 15 to Day 25

,
Interventionpercentage of participants (Number)
GoodSatisfactoryNot SatisfactoryBadNot assessable
Empa100.00.00.00.00.0
Empa Plus Verapamil87.56.36.30.00.0

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Apparent Clearance in Plasma After Extravascular Administration (CL/F)

"Apparent clearance of empagliflozin (empa) in plasma after extravascular administration.~Note: The numbers provide below for standard deviation are of Coefficient of Variation." (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

InterventionmL/min (Geometric Mean)
Empa178
Empa Plus Verapamil173

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Terminal Half-life in Plasma (t1/2)

"Terminal half-life of empagliflozin in plasma.~Note: The numbers provide below for standard deviation are of Coefficient of Variation." (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionh (Geometric Mean)
Empa12.1
Empa Plus Verapamil13.1

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Time From 0 to Maximum Plasma Concentration (Tmax)

Time from last dosing to the maximum plasma concentration (NCT01276301)
Timeframe: 0 hours (h), 20 minutes (min), 40min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after drug administration

Interventionh (Median)
Empa1.50
Empa Plus Verapamil1.75

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Verapamil Plasma Concentration

"Verapamil plasma concentration were measured in order to confirm exposure.~Note: No descriptive statistics was calculated for predose, 49.0 (h) and 73.0 (h), as most of the values were below the limit of quantification (BLQ)." (NCT01276301)
Timeframe: Predose and 1 hour (h), 25h, 49h and 73h after verapamil administration

Interventionng/mL (Geometric Mean)
Planned time: 1.0 (h)Planned time: 25.0(h) (included 11 participants)
Empa Plus Verapamil94.52.69

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Fluoroscopic Time

(NCT01402427)
Timeframe: Fluoroscopic time will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionminutes (Median)
Verapamil4.8
Placebo4.4

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Contrast Volume

(NCT01402427)
Timeframe: The amount of contrast medium will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionmilliliter (Median)
Verapamil75.0
Placebo72.5

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Procedural Time

(NCT01402427)
Timeframe: Procedural time will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionminutes (Median)
Verapamil17.0
Placebo16.0

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Rate of Access Site Conversions

(NCT01402427)
Timeframe: Occurrence of access site conversion will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionparticipants (Number)
Verapamil2
Placebo5

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Rate of Code Breaks

Code break: a composite of access site conversion and unplanned use of vasodilators. (NCT01402427)
Timeframe: Occurrence of code breaking will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionparticipants (Number)
Verapamil4
Placebo10

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Rate of Vasodilator Use

(NCT01402427)
Timeframe: Vasodilator use will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionparticipants (Number)
Verapamil297
Placebo6

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Subjective Pain

Analysis of the rates of significant pain defined as pain score ≥4 on a semiquantitative scale ranging from 1 to 6. (NCT01402427)
Timeframe: Subjective pain will be assessed within 1 minute after completion of coronary angiography or intervention.

Interventionparticipants (Number)
Verapamil26
Placebo21

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Change in Number of Myoclonic Seizures From Week 8 (Baseline) to Week 12

The secondary outcome is the change in number of myoclonic seizures between baseline Week 8 visit and Week 12 visit. (NCT01607073)
Timeframe: Week 8 (baseline) to Week 12

InterventionMyoclonic seizures (Number)
Week 8 Baseline116
Week 12 Verapamil 4mg/kg/Day175

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Change in Number of Absence Seizures From Week 8 (Baseline) to Week 12

The secondary outcome measure is the change in number of absence seizures from Week 8 (Baseline) to Week 12 (NCT01607073)
Timeframe: Week 8 to Week 12

InterventionAbscence seizures (Number)
Week 8 Baseline165
Week 12 Verapamil 4mg/kg/Day101

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Change in Number of General Tonic-clonic Seizures From Week 8 (Baseline) Visit to Week 12 Visit

The primary study endpoint is the change in number of seizures from baseline. Since we only had one participant finish the study, the endpoint was changed to Week 12 visit. Participants were on verapamil for 4 weeks at Week 12. (NCT01607073)
Timeframe: Week 8 (baseline) to Week 12

InterventionGeneral tonic-clonic seizures (Number)
Week 8 Baseline39
Week 12 Verapamil 4mg/kg/Day14

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Change in PR, QRS, J-Tpeak, Tpeak-Tend and QTc Using Exposure/Response (Ranolazine and Quinidine Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in QTc for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

,
Interventionms per mcg/ml (Mean)
Change in PRChange in QTcChange in QRSChange in J-TpeakcChange in Tpeak-Tend
Quinidine Sulfate 400mg3.078.90.426.151.2
Ranolazine 1500mg4.212.00.80.710.0

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Placebo, and Baseline-adjusted Changes in PR, QRS, J-Tpeak, Tpeak-Tend and QTc

Compute maximum mean placebo, and baseline-adjusted change for: PR (ms), QRS (ms), J-Tpeak (ms), Tpeak-Tend (ms) and QTc (ms) (NCT01873950)
Timeframe: 24 hours

,,,
Interventionms (Least Squares Mean)
Change in PR intervalChange in QRS durationChange in J-TpeakcChange in Tpeak-TendChange in QTc
Dofetilide 500mcg2.31.139.540.079.3
Quinidine Sulfate 400mg5.12.129.149.878.1
Ranolazine 1500mg6.52.73.38.812.6
Verapamil HCl 120 mg32.12.6-2.44.85.2

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Change in Ventricular Gradient Using Exposure/Response (Dofetilide and Verapamil Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in ventricular gradient for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

InterventionmV.ns per ng/ml (Mean)
Dofetilide 500mcg4.0
Verapamil HCl 120 mg1.2

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Change in Spatial QRS-T Angle Using Exposure/Response (Dofetilide and Verapamil Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in spatial QRS-T angle for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

Interventiondegrees per ng/ml (Mean)
Dofetilide 500mcg-3.9
Verapamil HCl 120 mg0.4

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Change in Relationship (Ratio) Between Heart Rate and QT

Different post-dose time-points employ different techniques for altering heart rate (leg raises and postural maneuvers). Using the measurements from all the time-points of postural maneuvers, the QT/RR relationship was modeled as a linear relationship between the square root of RR in seconds and QT in seconds and computed on a by subject, treatment and time-point basis. The change in the QT and heart rate relationship was assessed as the difference (mean and 95% CI) between the slopes from the models for each drug vs. placebo. (NCT01873950)
Timeframe: 24 hours

Interventionratio (Mean)
Ranolazine 1500mg0.01
Dofetilide 500mcg0.06
Verapamil HCl 120 mg0.02
Quinidine Sulfate 400mg0.11

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Change in Spatial QRS-T Angle Using Exposure/Response (Ranolazine and Quinidine Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in spatial QRS-T angle for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

Interventiondegrees per mcg/ml (Mean)
Ranolazine 1500mg-1.0
Quinidine Sulfate 400mg2.7

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Change in PR, QRS, J-Tpeak, Tpeak-Tend and QTc Using Exposure/Response (Dofetilide and Verapamil Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in QTc for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

,
Interventionms per ng/ml (Mean)
Change in PRChange in QTcChange in QRSChange in J-TpeakcChange in Tpeak-Tend
Dofetilide 500mcg-0.573.60.239.134.4
Verapamil HCl 120 mg28.73.90.3-0.73.6

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Change in Ventricular Gradient Using Exposure/Response (Ranolazine and Quinidine Arms)

"The exposure response analysis will be performed for each treatment and will use a linear or nonlinear model (as determined by visual inspection) to quantify the relationship between exposure and Baseline and placebo adjusted change from Baseline for each ECG parameter (same as for primary analysis).~The magnitude of change (mean and 95% CI) in ventricular gradient for the observed mean Cmax for each drug may be calculated." (NCT01873950)
Timeframe: 24 hours

InterventionmV.ns per mcg/ml (Mean)
Ranolazine 1500mg-0.7
Quinidine Sulfate 400mg1.6

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Placebo, and Baseline-adjusted Changes in Spatial QRS-T Angle

Compute maximum mean placebo, and baseline-adjusted change for: spatial QRS-T angle (degrees) (NCT01873950)
Timeframe: 24 hours

Interventiondegrees (Least Squares Mean)
Ranolazine 1500mg-2.2
Dofetilide 500mcg-4.9
Verapamil HCl 120 mg-2.4
Quinidine Sulfate 400mg3.9

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Placebo, and Baseline-adjusted Changes in Ventricular Gradient

Compute maximum mean placebo, and baseline-adjusted change for: ventricular gradient (mV*ms). (NCT01873950)
Timeframe: 24 hours

InterventionmV*ms (Least Squares Mean)
Ranolazine 1500mg2.5
Dofetilide 500mcg4.8
Verapamil HCl 120 mg4.2
Quinidine Sulfate 400mg6.0

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Number of Participants With Potentially Clinically Significant Vital Signs Findings

Vital signs assessment included pulse rate and blood pressure. Criteria for vital sign values meeting potential clinical concern included: supine/sitting pulse rate <40 or >120 beats per minute (bpm), standing pulse rate <40 or >140 bpm; systolic blood pressure (SBP) of >=30 millimeters of mercury (mm Hg) change from baseline in same posture or SBP <90 mm Hg, diastolic blood pressure (DBP) >=20 mmHg change from baseline in same posture or DBP <50 mm Hg. (NCT02319148)
Timeframe: Baseline up to Day 9

,,,
Interventionparticipants (Number)
Supine SBP <90 mm Hg (n=22,7,7,8)Standing SBP <90 mm Hg (n=22,7,6,8)Supine DBP <50 mm Hg (n=22,7,7,8)Standing DBP <50 mm Hg (n=22,7,6,8)Supine Pulse Rate <40 or >120 bpm (n=22,7,7,8)Standing Pulse Rate <40 or >120 bpm (n=22,7,6,8)Supine SBP >=30 mm Hg IFB (n=22,6,6,7)Standing SBP >=30 mm Hg IFB (n=22,6,6,7)Supine DBP >=20 mm Hg IFB (n=22,6,6,7)Standing DBP >=20 mm Hg IFB (n=22,6,6,7)Supine SBP >=30 mm Hg DFB (n=22,6,6,7)Standing SBP >=30 mm Hg DFB (n=22,6,6,7)Supine DBP >=20 mm Hg DFB (n=22,6,6,7)Standing DBP >=20 mm Hg DFB (n=22,6,6,7)
PF-00489791 20 mg00000000000001
PF-00489791 20 mg + Diltiazem 240 mg00000000000101
PF-00489791 20 mg + Itraconazole 200 mg00000000000000
PF-00489791 20 mg + Verapamil 240 mg11010000000101

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Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Findings

ECG parameters included PR interval, QRS interval, and corrected QT interval using Fridericia's formula (QTcF). Criteria for ECG changes meeting potential clinical concern included: PR interval greater than or equal to (>=)300 milliseconds (msec) or >=25% increase when baseline is greater than (>)200 msec and >=50% increase when baseline is less than or equal to (≤)200 msec; QRS interval >=140 msec or >=50% increase from baseline (IFB); and QTcF >=450 msec or >=30 msec increase. The number of participants with potentially clinically significant ECG findings at any visit were reported. (NCT02319148)
Timeframe: Pre-dose (Periods 1 and 2), 4, 72 and 96 hours post-dose in Period 2

,,,
Interventionparticipants (Number)
PR Interval >=300 msec (n=22,7,7,8)QRS Complex >=140 msec (n=22,7,7,8)QTcF Interval 450-<480 msec (n=22,7,7,8)QTcF Interval 480-<500 msec (n=22,7,7,8)QTcF Interval >=500 msec (n=22,7,7,8)PR Interval >=25/50% IFB (n=22,6,6,7)QRS Interval >=50% IFB (n=22,6,6,7)QTcF Interval 30-<60 msec IFB (n=22,6,6,7)QTcF Interval >=60 msec IFB (n=22,6,6,7)
PF-00489791 20 mg000000000
PF-00489791 20 mg + Diltiazem 240 mg000000000
PF-00489791 20 mg + Itraconazole 200 mg000000010
PF-00489791 20 mg + Verapamil 240 mg000000000

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Number of Participants Who Used at Least 1 Concomitant Medication

Participants were to abstain from all concomitant treatments, except for the treatment of AEs. Treatments taken after the first dose of study treatment were documented as concomitant treatments. (NCT02319148)
Timeframe: Baseline up to Day 15 (final study evaluation)

,,,
Interventionparticipants (Number)
Drug TreatmentsNon-Drug Treatments
PF-00489791 20 mg100
PF-00489791 20 mg + Diltiazem 240 mg40
PF-00489791 20 mg + Itraconazole 200 mg20
PF-00489791 20 mg + Verapamil 240 mg20

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Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-00489791

(NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionhour (Median)
PF-00489791 20 mg4.00
PF-00489791 20 mg + Itraconazole 200 mg3.50
PF-00489791 20 mg + Diltiazem 240 mg4.00
PF-00489791 20 mg + Verapamil 240 mg4.00

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Terminal Elimination Half-Life (t1/2) of PF-00489791

t1/2 is the time measured for the plasma concentration to decrease by one half. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionhour (Mean)
PF-00489791 20 mg11.39
PF-00489791 20 mg + Itraconazole 200 mg13.85
PF-00489791 20 mg + Diltiazem 240 mg11.75
PF-00489791 20 mg + Verapamil 240 mg13.29

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Maximum Observed Plasma Concentration (Cmax) of PF-00489791

(NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
PF-00489791 20 mg1140
PF-00489791 20 mg + Itraconazole 200 mg1238
PF-00489791 20 mg + Diltiazem 240 mg1198
PF-00489791 20 mg + Verapamil 240 mg1186

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Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-00489791

AUC is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
PF-00489791 20 mg17880
PF-00489791 20 mg + Itraconazole 200 mg18140
PF-00489791 20 mg + Diltiazem 240 mg16840
PF-00489791 20 mg + Verapamil 240 mg19560

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-00489791

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast). (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionng.hr/mL (Geometric Mean)
PF-00489791 20 mg17580
PF-00489791 20 mg + Itraconazole 200 mg17980
PF-00489791 20 mg + Diltiazem 240 mg16760
PF-00489791 20 mg + Verapamil 240 mg19400

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Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern

The following laboratory parameters were analyzed: hematology (hemoglobin, hematocrit, red blood cell [RBC] count, RBC morphology, platelet count, white blood cell [WBC] count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes); blood chemistry (blood urea nitrogen [BUN], creatinine, glucose, calcium, sodium, potassium, chloride, total bicarbonate, aspartate aminotransferase [AST], alanine aminotransferase [ALT], total bilirubin, alkaline phosphatase, uric acid, albumin, and total protein; urinalysis (pH, glucose, protein, blood, ketones, nitrites, leukocyte esterase, microscopy [if urine dipstick was positive for blood, protein, nitrites or leukocyte esterase]); others (coagulation panel, circulating immune complex, and complement activation). (NCT02319148)
Timeframe: Baseline up to 28 days after last study drug administration

Interventionparticipants (Number)
PF-00489791 20 mg3
PF-00489791 20 mg + Itraconazole 200 mg0
PF-00489791 20 mg + Diltiazem 240 mg0
PF-00489791 20 mg + Verapamil 240 mg2

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Apparent Volume of Distribution (Vz/F) of PF-00489791

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionliter (Geometric Mean)
PF-00489791 20 mg18.06
PF-00489791 20 mg + Itraconazole 200 mg21.65
PF-00489791 20 mg + Diltiazem 240 mg19.98
PF-00489791 20 mg + Verapamil 240 mg19.23

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Apparent Oral Clearance (CL/F) of PF-00489791

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionmilliliter per minute (mL/min) (Geometric Mean)
PF-00489791 20 mg18.64
PF-00489791 20 mg + Itraconazole 200 mg18.37
PF-00489791 20 mg + Diltiazem 240 mg19.81
PF-00489791 20 mg + Verapamil 240 mg17.02

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Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pre-treatment state. AEs included both SAEs and non-SAEs. (NCT02319148)
Timeframe: Baseline up to 28 days after last study drug administration

,,,,,,
Interventionparticipants (Number)
AEsSAEs
Diltiazem 240 mg40
Itraconazole 200 mg60
PF-00489791 20 mg180
PF-00489791 20 mg + Diltiazem 240 mg40
PF-00489791 20 mg + Itraconazole 200 mg60
PF-00489791 20 mg + Verapamil 240 mg50
Verapamil 240 mg30

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Percent Change From Baseline in Exogenous Insulin Requirements

Percent change in exogenous insulin requirements over the last 7-14 consecutive days at 12 months. This will be assessed as a surrogate inverse marker of residual beta cell function. (NCT02372253)
Timeframe: 12 months

InterventionPercent Change (Mean)
Verapamil27.0
Placebo69.8

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HbA1c

Glycemic control, as measured by HbA1c. In addition to being an important determinant of residual beta cell function/survival, it also helps reveal a more complete picture of beta cell function. (NCT02372253)
Timeframe: 12 weeks

InterventionPercent (Mean)
Verapamil6.0
Placebo6.6

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Percent Change From Baseline in Exogenous Insulin Requirements

Percent change in exogenous insulin requirements over the last 7-14 consecutive days at 12 weeks. This will be assessed as a surrogate inverse marker of residual beta cell function. (NCT02372253)
Timeframe: 12 weeks

InterventionPercent Change (Mean)
Verapamil5.9
Placebo26.0

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HbA1C

Glycemic control, as measured by HbA1c. In addition to being an important determinant of residual beta cell function/survival, it also helps reveal a more complete picture of beta cell function. (NCT02372253)
Timeframe: 12 months

InterventionPercent (Mean)
Verapamil6.4
Placebo6.9

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Functional Beta Cell Mass

Functional Beta Cell Mass as determined by the area under the curve (AUC) from a 2-hour Mixed Meal-Stimulated C-peptide after daily verapamil for 12 months. A greater improvement in insulin production (as an indirect measure of beta cell mass) in subjects receiving verapamil as compared to those receiving placebo would provide an indication of the efficacy of this intervention. The C-peptide AUC (0-120 min) was calculated by using the trapezoidal rule and was divided by the time of the test to obtain the mean AUC (in nmol/L). (NCT02372253)
Timeframe: 12 months

Interventionnmol/L (Mean)
Verapamil0.74
Placebo0.46

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Hypoglycemic Events

Glycemic control, as measured by hypoglycemic events. (NCT02372253)
Timeframe: 12 months

Interventionevents per month (Mean)
Verapamil0.55
Placebo2.72

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Heart Rate

(NCT02454608)
Timeframe: Mean change between baseline and week 8 measurements.

Interventionbeats per minute (Mean)
Treatment-1.4
Control4

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Diastolic Blood Pressure

(NCT02454608)
Timeframe: Mean change between baseline and week 8 measurements

InterventionmmHg (Mean)
Treatment-0.6
Control1

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Subjective Sinonasal Symptoms on Sinonasal Outcomes Test-22(SNOT-22)

Minimum Score: 0 Maximum Score: 110 A higher score indicates a worse outcome (NCT02454608)
Timeframe: baseline to week 56

Interventionunits on a scale (Mean)
Medicine Completers, baselineMedicine Completers, week 56Surgical Completers, baselineSurgical Completers, week 12
Open Label31.824.1472.008.00

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Subjective Sinonasal Symptoms on Sinonasal Outcomes Test-22(SNOT-22)

Minimum Score: 0 Maximum Score: 110 A higher score indicates a worse outcome (NCT02454608)
Timeframe: baseline to week 8

Interventionunits on a scale (Least Squares Mean)
Treatment-27.3
Control0.4

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Systolic Blood Pressure

(NCT02454608)
Timeframe: Mean change between baseline and week 8 measurements

InterventionmmHg (Mean)
Treatment-4.5
Control-6.6

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Subjective Sinonasal Symptoms on 10cm Visual Analogue Scale(VAS)

Minimum Score: 0 Maximum Score: 100 A higher score indicates a worse outcome. (NCT02454608)
Timeframe: baseline to week 56

Interventionunits on a scale (Mean)
Medicine Completers, baselineMedicine Completers, week 56Surgical Completers, baselineSurgical Completers, week 12
Open Label64.335.090.016.7

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Objective Sinonasal Symptoms on Lund-McKay Score(LMS)

Minimum Score: 0 Maximum Score: 24 Higher value represents worse outcome. (NCT02454608)
Timeframe: Week 8

Interventionunits on a scale (Mean)
Treatment12.5
Control17.7

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Objective Sinonasal Symptoms on Lund-Kennedy Score(LKS)

Minimum Score: 0 Maximum Score: 12 Higher value represents worse outcome. (NCT02454608)
Timeframe: baseline to week 8

Interventionunits on a scale (Least Squares Mean)
Treatment-1.3
Control-0.25

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Subjective Sinonasal Symptoms on 10cm Visual Analogue Scale(VAS)

Minimum Score: 0 Maximum Score: 100 A higher score indicates a worse outcome. (NCT02454608)
Timeframe: baseline to week 8

Interventionunits on a scale (Least Squares Mean)
Treatment-44.03
Control-6.07

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Pharmacokinetics (PK) of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-t]).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
AZD79866545
AZD7986 + Verapamil8739
AZD7986 + Itraconazole7361

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Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Vz/F).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

InterventionLitres (Mean)
AZD7986297.1
AZD7986 + Verapamil194.6
AZD7986 + Itraconazole317.8

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Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Total Body Clearance After Extravascular Administration Estimated as Dose Divided by AUC (CL/F).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

InterventionL/h (Mean)
AZD79869.807
AZD7986 + Verapamil7.359
AZD7986 + Itraconazole8.308

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Pharmacokinetics (PK) of AZD7986 by Assessment of Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration-time Curve (t½λz).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Mean)
AZD798623.35
AZD7986 + Verapamil20.36
AZD7986 + Itraconazole27.89

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Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Observed Maximum Plasma Concentration (Cmax).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionnmol/L (Geometric Mean)
AZD7986385.8
AZD7986 + Verapamil591.9
AZD7986 + Itraconazole234.1

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Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC).

To assess the effect of verapamil and itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
AZD79866697
AZD7986 + Verapamil8857
AZD7986 + Itraconazole7615

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Assessment of the Tmax of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.

To assess the time to reach maximum observed concentration of Verapamil, Itraconazole and OH-itraconazole (a metabolite of itraconazole) following co-administration of AZD7986 with Verapamil or Itraconazole. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Median)
Verapamil4.00
Itraconazole1.50
OH-itraconazole (a Metabolite of Itraconazole)5.00

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Pharmacokinetics (PK) of AZD7986 by Assessment of the Time to Reach Maximum Plasma Concentration (Tmax)

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Median)
AZD79860.75
AZD7986 + Verapamil1.50
AZD7986 + Itraconazole1.50

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Assessment of the Area Under the Plasma Concentration-curve Over the Dosing Interval (AUC [0 - τ]) of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.

To assess the area under the plasma concentration-time curve from time over the dosing interval tau (24 hours) of Verapamil, itraconazole and OH-itraconazole (a metabolite of Itraconazole) following co-administration of AZD7986 with Verapamil or Itraconazole. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
Verapamil2178
Itraconazole18090
OH-itraconazole (a Metabolite of Itraconazole)31390

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QTc Shortening From Calcium Block (Diltiazem) in the Presence of hERG Block (Dofetilide)

"It will be assessed whether the projected QTc effect of dofetilide alone is significantly greater (i.e., p<0.05) than the projected QTc effect of the combination of dofetilide + diltiazem. This will be assessed at the dofetilide peak plasma level on Day 3 (computed from the combination of dofetilide + diltiazem) on the pooled dofetilide alone, diltiazem alone, and dofetilide + diltiazem data using a linear mixed effects model.~Subsequently, and if the test is significant for QTc, the same test will be performed to assess calcium block (diltiazem) effects on J-Tpeakc." (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Dofetilide2.2
Diltiazem+Dofetilide-1.7

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"Change From Baseline QTc With Predominant hERG Blocking Drug (Chloroquine)"

"The primary outcome measure for the predominant hERG drug (chloroquine) is for the upper bound of the 2-sided 90% CI to be ≥10 msec for the projected placebo-corrected change from baseline QTc effect at the peak plasma level on Day 1 using a linear mixed-effects exposure response model" (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Chloroquine17.7
Placebo-9.3

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"Change From Baseline J-Tpeakc With Balanced Ion Channel Drugs (Ranolazine, Verapamil, Lopinavir / Ritonavir)"

"The primary outcome measure for the balanced ion channel drugs (ranolazine, verapamil, lopinavir / ritonavir) is for the upper bound of the 2-sided 90% confidence interval (CI) to be <10 msec for the projected placebo-corrected change from baseline J-Tpeakc effect at the peak plasma level on Day 3 using a linear mixed-effects exposure response model. Placebo drug concentration was set to 0 (see SAP)." (NCT03070470)
Timeframe: 3 days

Interventionms (Median)
Ranolazine-8.3
Verapamil-7.8
Lopinavir / Ritonavir-11.5
Placebo-10.9

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Number of Participants With Dose Limiting Toxicity

Dose Limiting Toxicity will be defined as a development of 2nd or 3rd degree heart block as measured by an EKG. (Phase Ib primary outcome) (NCT03102190)
Timeframe: 1-8 weeks

InterventionParticipants (Count of Participants)
Phase Ib0

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

Interventionhr*ng/mL (Geometric Mean)
Study 1: Bexagliflozin Alone1118.741
Study 1: Bexagliflozin/Probenecid1583.188
Study 2: Bexagliflozin Alone698.254
Study 2: Bexagliflozin/Rifampin601.334
Study 3: Bexagliflozin Alone1025.101
Study 3: Bexagliflozin/Verapamil1003.931

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

,,
Interventionhours (Median)
Bexagliflozin aloneBexagliflozin + additional drug
Bexagliflozin/Probenecid2.0003.000
Bexagliflozin/Rifampin2.0002.000
Bexagliflozin/Verapamil3.03.000

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Urinary Glucose Excretion 0-48 hr

Pre-dose urine samples were collected from -12 to 0 h for baseline measurement of pharmacodynamic parameters. Post-dose urine samples were collected without preservative in four batches: 0 to 12 h, 12 to 24 h, 24 to 36h, and 36 to 48 h after dosing. Urine aliquots were prepared from well mixed collections for the assessment of pharmacodynamics. (NCT03296800)
Timeframe: 0 to 48 hours

,,,,,
Interventiong (Mean)
Pre-dose (-12 - 0 hours)0 - 12 hours post-dose12 - 24 hours post-dose24 - 36 hours post-dose36 - 48 hours post-dose0 - 24 hours post-dose0 - 48 hours post-dose
Bexagliflozin/Probenecid0.4725.9020.9222.109.5346.8278.44
Bexagliflozin/Rifampin0.1231.4015.7216.323.4147.1266.86
Bexagliflozin/Verapamil1.3731.4620.5120.944.7851.9777.69
Study 1: Bexagliflozin Alone0.0225.0421.2822.0411.1547.7381.67
Study 2: Bexagliflozin Alone0.0231.5019.4321.516.9950.9379.43
Study 3: Bexagliflozin Alone0.0231.1422.3024.5411.3153.4489.29

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

Interventionng/mL (Geometric Mean)
Study 1: Bexagliflozin Alone161.675
Study 1: Bexagliflozin and Probenecid193.366
Study 2: Bexagliflozin Alone97.811
Study 2: Bexagliflozin and Rifampin117.001
Study 3: Bexagliflozin Alone159.355
Study 3: Bexagliflozin and Verapamil169.000

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

,,
Interventionhours (Geometric Mean)
Bexagliflozin aloneBexagliflozin + additional drug
Bexagliflozin/Probenecid12.09013.894
Bexagliflozin/Rifampin12.1905.318
Bexagliflozin/Verapamil10.70911.675

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. Geometric mean (gMean) presented here is an adjusted gMean and standard error (SE) presented is a geometric SE (gSE). (NCT03307252)
Timeframe: Samples were taken within 0:20 hour:minutes (hh:mm) prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Verapamil + R1 (T1)13.71165.801126.2298.98

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.3090.00243.4910.11
Probenecid + R1 (T4)1.13110.64246.7843.29

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)1.6597.69316.8313.21
Cocktail (R1)1.3593.23258.3311.30

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Rifampin + R1 (T2)2.55119.66251.3277.00

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Verapamil + R1 (T1)1.4284.32179.457.90

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Rifampin + R1 (T2)17.89211.821473.38303.81

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.52177.961321.20106.69
Probenecid + R1 (T4)14.44483.381331.83238.16

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)19.03196.392006.60139.54
Cocktail (R1)15.15194.051532.41129.90

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)188.111330.47113.78
Probenecid + R1 (T4)489.281346.62244.94

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)202.172023.33148.32
Cocktail (R1)200.611540.21139.21

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Rifampin + R1 (T2)215.631482.76320.72

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Verapamil + R1 (T1)176.441147.23116.80

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Systolic Blood Pressure

In all protocols, blood pressure (mmHg) was measured concomitantly using a semi-automated non-invasive sphygmomanometer. Systolic blood pressure is reported here after leptin or saline infusion, when applicable. (NCT04374500)
Timeframe: 18 minutes in protocol 1, 3 hours in protocol 2, NA in protocol 3

,,
InterventionmmHg (Mean)
Leptin infusedSaline infused
Leptin Infusion in Healthy Men140NA
Leptin or Saline Infusion Plus Vasodilators in Healthy Men134136
Vasodilators in CAD PatientsNANA

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Release of Fibrinolytic Variables (Tissue Plasminogen Activator [tPA] and Plasminogen Activator Inhibitor-1 [PAI-1])

"In all protocols, fibrinolytic variables were measured. In protocol 2 and 3, in the infused forearm after vasodilatation with bradykinin or substance P, respectively.~The fibrinolytic variable measured in all protocols was tPA activity (IU/mL) and is reported here after the leptin infusion, when applicable." (NCT04374500)
Timeframe: 18 minutes in protocol 1, 3 hours in protocol 2, NA in protocol 3

,,
InterventionIU/mL (Mean)
Leptin infusedSaline infused
Leptin Infusion0.56NA
Leptin Plus Vasodilators0.910.73
Vasodilators in CAD PatientsNANA

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Leptin

Plasma leptin concentration (ng/mL) was measured in all protocols, and in protocol 1 and 2, specifically in both infused and in non-infused arms. Data given are leptin concentrations in the infused arm at the end of the infusion. (NCT04374500)
Timeframe: 18 minutes in protocol 1, 3 hours in protocol 2, NA in protocol 3

,,
Interventionng/mL (Mean)
Leptin infusedSaline infused
Leptin Infusion186.2NA
Leptin Plus Vasodilators13.13.4
Vasodilators in CAD PatientsNANA

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Heart Rate

In all protocols, heart rate (beats per minute) was measured concomitantly. Heart rate is reported here after leptin or saline infusion, when applicable. (NCT04374500)
Timeframe: 18 minutes in protocol 1, 3 hours in protocol 2, NA in protocol 3

,,
InterventionBeats per minute (Mean)
Leptin infusedSaline infused
Leptin Infusion in Healthy Men59NA
Leptin or Saline Infusion Plus Vasodilators in Healthy Men6666
Vasodilators in CAD PatientsNANA

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Forearm Blood-flow (FBF)

The primary outcome in all protocols were local blood-flow in the forearm (FBF). This was measured by venous occlusion plethysmography using mercury-in-silastic strain gauges and the unit is mL/100mL of tissue/min. In protocol 1, the FBF response to increasing levels of leptin was evaluated, In protocol 2, the FBF response to vasodilators on top of leptin or saline infusion was evaluated, and in protocol 3, FBF was measured after infusion of vasodilators and no leptin was given. (NCT04374500)
Timeframe: 18 minutes in protocol 1, 3 hours in protocol 2, non-applicable (NA) in protocol 3

,,
Interventionml/100 mg tissue/min (Mean)
Leptin infusedSaline infused
Leptin Infusion, no Saline Given1.75NA
Leptin Plus Vasodilators3.13.4
Vasodilators in CAD PatientsNANA

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