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.
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.
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.
ID Source | ID |
---|---|
PubMed CID | 2520 |
CHEMBL ID | 6966 |
CHEBI ID | 77733 |
CHEBI ID | 9948 |
SCHEMBL ID | 16742 |
SCHEMBL ID | 13287282 |
MeSH ID | M0022608 |
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) |
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.
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.
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)
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.
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.
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)
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
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.
Excerpt | Relevance | Reference |
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"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 |
Class | Description |
---|---|
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
polyether | Any ether that contains more than one ether linkage. |
nitrile | A 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] |
Pathway | Proteins | Compounds |
---|---|---|
Verapamil Action Pathway | 47 | 8 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
glp-1 receptor, partial | Homo sapiens (human) | Potency | 14.1254 | 0.0184 | 6.8060 | 14.1254 | AID624172 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.3981 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
TDP1 protein | Homo sapiens (human) | Potency | 26.5101 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 1.5112 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 26.4193 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743054; AID743063 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 26.6032 | 0.0010 | 22.6508 | 76.6163 | AID1224838 |
progesterone receptor | Homo sapiens (human) | Potency | 33.4915 | 0.0004 | 17.9460 | 75.1148 | AID1346784 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 9.4662 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.6609 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.0054 | 0.0013 | 10.1577 | 42.8575 | AID1259256 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 26.8325 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 4.2163 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 31.2718 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743079; AID743091 |
G | Vesicular stomatitis virus | Potency | 37.9083 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
glucocerebrosidase | Homo sapiens (human) | Potency | 28.1838 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 21.3138 | 0.0010 | 19.4141 | 70.9645 | AID743094 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 39.8107 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 26.6032 | 0.0016 | 28.0151 | 77.1139 | AID1259385 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 0.3011 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 50.1187 | 0.0366 | 19.6376 | 50.1187 | AID2112 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 7.9433 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 28.2263 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.2202 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Interferon beta | Homo sapiens (human) | Potency | 37.9083 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 37.9083 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 19.9526 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 37.9083 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Ataxin-2 | Homo sapiens (human) | Potency | 17.7828 | 0.0119 | 12.2221 | 68.7989 | AID588378 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 37.9083 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Albumin | Homo sapiens (human) | Kd | 645.6540 | 0.0893 | 3.3135 | 8.0000 | AID327170 |
Muscarinic acetylcholine receptor M2 | Sus scrofa (pig) | EC50 (µMol) | 30.9742 | 0.0135 | 1.8625 | 6.3096 | AID142787 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | EC50 (µMol) | 6.4109 | 0.0160 | 0.6786 | 3.1000 | AID1062339; 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) | 10.8312 | 1.7000 | 4.3028 | 9.8000 | AID1168903; AID1414427; AID1565850; AID1595500 |
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | EC50 (µMol) | 19.1000 | 0.0054 | 0.4220 | 3.2000 | AID1168904; AID1565853 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
ATP-dependent translocase ABCB1 | Homo sapiens (human) | Activity | 1.6000 | 0.0200 | 1.6700 | 4.5000 | AID282999; AID310897 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | ED50 | 3.0000 | 0.0500 | 1.5250 | 3.0000 | AID399366 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | I0.5 | 1.6000 | 1.6000 | 1.6000 | 1.6000 | AID1565851 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | INH | 1.6000 | 1.6000 | 1.6000 | 1.6000 | AID464018 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 13.3433 | 0.0140 | 3.7172 | 10.0000 | AID239740; AID350526; AID681163; AID681164; AID682516; AID713773 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | MIC | 8.0000 | 8.0000 | 8.0000 | 8.0000 | AID714426 |
ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | Km | 10.0000 | 10.0000 | 10.0000 | 10.0000 | AID350523 |
Multidrug resistance-associated protein 1 | Homo sapiens (human) | Activity | 2.6000 | 2.6000 | 2.6000 | 2.6000 | AID427722 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1378879 | Effective permeability of the compound at 100 mg/ml after 16 hrs by UV based PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
AID1180228 | Inhibition of L-type calcium channel in Wistar rat aorta rings assessed as reduction in L-type Ba(2+) current at Vh of -50 mV | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID1576576 | Effective permeability of compound by PAMPA | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling. |
AID379509 | Reversal 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 vinblastine | 1999 | Journal of natural products, May, Volume: 62, Issue:5 | Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance. |
AID1673441 | Effect on P-gp expression in human K562/A02 cells overexpressing P-gp at 5 uM after 72 hrs by Western blot analysis | 2019 | Bioorganic & 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. |
AID1502892 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID351903 | Chemosensitizing 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 assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1239240 | Increase in rhodamine 123 accumulation in human MDA435/LCC6 cells at 2 uM after 2.5 hrs by spectrofluorometric analysis relative to control | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors. |
AID1764875 | Permeability of the compound at 50 uM measured after 4 hrs by PAMPA assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
AID1486983 | Inhibition of ABCB1 in human K562/A02 cells assessed as increase in doxorubicin accumulation after 90 mins by rhodamine123 staining based flow cytometric analysis | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID1761200 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID1633048 | Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method | |||
AID230566 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID406534 | Inhibition of NorA efflux pump in Staphylococcus aureus 1199 assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml | 2008 | Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13 | Citral derived amides as potent bacterial NorA efflux pump inhibitors. |
AID726493 | Inhibition 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 control | 2013 | Bioorganic & 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. |
AID1807362 | Metabolic stability in mouse liver microsomes assessed as intrinsic clearance in presence of NADPH regenerating system by UPLC-MS analysis | |||
AID167265 | Electrophysiological effect in isolated rabbit hearts in atrio-His bundle (A-H) interval | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives. |
AID331503 | Reversal 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 cytometry | 2008 | Bioorganic & 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. |
AID1900354 | Stability in pooled human liver microsomes assessed as intrinsic clearance at 8 uM in presence of NADPH measured upto 60 mins by HPLC-MS analysis | 2022 | Journal 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. |
AID1215169 | AUC (0 to 90 mins) in Sprague-Dawley rat portal vein plasma at 10 mg/kg, po | 2011 | Drug 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. |
AID1776729 | Inhibition of Multidrug resistance efflux pump in Mycobacterium tuberculosis FURG-2 assessed as relative final fluorescence at 128 ug/ml measured by ethidium bromide accumulation assay | 2021 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 42 | 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis. |
AID1322367 | Metabolic stability in human liver microsomes assessed as compound remaining after 30 mins | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents. |
AID1215181 | Drug 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 NADPH | 2011 | Drug 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. |
AID1207204 | Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID1739842 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID514303 | Protection 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 uM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID1429868 | Permeability of the compound at pH 2 at 50 mM after 4 hrs by PAMPA-GI assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
AID1288623 | Reversal 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 control | 2016 | Bioorganic & 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. |
AID472413 | Inhibition 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 assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells. |
AID143479 | Inhibitory activity when combined with 5-fluorouracil (uM) in NCI/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID94172 | Increase in adriamycin uptake in modulator-treated cells relative to untreated KB-A1 cells at a concentration of 5 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID1703749 | Half life in human liver microsomes at 0.1 uM in presence of NADPH by LC/MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections. |
AID1228904 | Cytotoxicity against mouse L929 cells after 3 days by MTS assay | 2015 | Journal 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. |
AID680054 | TP_TRANSPORTER: inhibition of Daunorubicin intracellular accumulation (DMN: 0.05 uM, Verapamil: 100 uM) in MDA435/LCC6 MDR1 cells | 2003 | The 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. |
AID1215134 | Decrease of CYP3A2 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat intestine by Western blot analysis | 2011 | Drug 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. |
AID288565 | Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-C2 cells at 5 uM after 68 hrs by MTT assay | 2007 | Journal of natural products, Jun, Volume: 70, Issue:6 | Reversal of P-glycoprotein-mediated multidrug resistance by sipholane triterpenoids. |
AID1502866 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1652316 | Half life in human hepatocytes | 2020 | Journal 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. |
AID656837 | Inhibition 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 = 5 | 2012 | Bioorganic & 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. |
AID1502792 | Inhibition 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 er | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1770544 | Metabolic 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 analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1514559 | Cytotoxicity against human KBV cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID1473741 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID681441 | TP_TRANSPORTER: inhibition of TEA uptake by Verapamil at 5mM in Octn1-HRPE cells | 2000 | Biochimica 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. |
AID1761208 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID1322434 | Inhibition 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) | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors. |
AID587815 | Metabolic stability of the compound in human liver microsome assessed as compound remaining | 2011 | Journal 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. |
AID1623663 | Half life in mouse microsomes | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1215347 | Time 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 | 2011 | Drug 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. |
AID1273467 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 32 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1352540 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1235737 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1813151 | Reversal 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1548950 | Unbound hepatic clearance in rat liver microsomes | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Discovery of |
AID1446267 | Metabolic 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 method | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Evaluation of Novel Prodrugs of Transition State Inhibitors of Norovirus 3CL Protease. |
AID1351583 | Tracheorelaxant activity in Wistar rat trachea tonus assessed as reduction in 30 mM KCl-induced contraction at 100 uM after 15 mins relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, 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. |
AID1286275 | Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal 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. |
AID639368 | Permeability of the compound by PAMPA assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease. |
AID1595503 | Ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells incubated for 120 mins by UV spectroscopy | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Modulation 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. |
AID1235780 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1371163 | Half life in human liver microsomes in absence of NADPH by LC-MS/MS analysis | 2017 | Journal 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). |
AID324577 | Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control | 2007 | Proceedings 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. |
AID430563 | Reversal 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 assay | 2009 | Journal of natural products, Jul, Volume: 72, Issue:7 | Sipholane triterpenoids: chemistry, reversal of ABCB1/P-glycoprotein-mediated multidrug resistance, and pharmacophore modeling. |
AID1062344 | Modulation 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 control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID653458 | Reversal 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 assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1604717 | Stability in human plasma assessed as parent compound remaining level at 5 uM at 37 degC measured at 240 mins by LC-MS analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID1210069 | Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method | 2013 | Drug 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. |
AID1649259 | Potentiation 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) | 2020 | Journal 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. |
AID1460712 | Cytotoxicity against human MCF7/DX cells incubated for 48 hrs by MTT assay | 2017 | Journal of natural products, 04-28, Volume: 80, Issue:4 | Isolation, Structure Elucidation, and Absolute Configuration of Syncarpic Acid-Conjugated Terpenoids from Rhodomyrtus tomentosa. |
AID389747 | Inhibition of NorA efflux pump in Staphylococcus aureus 1199B assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1215164 | Clearance in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Drug 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. |
AID1182022 | Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay | 2014 | Journal 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. |
AID1246309 | Half life in human microsomes | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID1357218 | Intrinsic clearance in rat liver microsomes in presence of NADPH regeneration system | 2018 | Journal 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. |
AID1769164 | Inhibition 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 analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
AID679920 | TP_TRANSPORTER: inhibition of Saquinavir transepithelial transport (basal to apical)(Saquinavir: 10 uM, Verapamil: 5 uM) in HCT-8 cells | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein. |
AID1733395 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1129446 | Half life in mouse microsomes at 1 uM in presence of NADPH | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1174620 | Potentiation of adriamycin-induced cytotoxicity against human K562/ADR cells at 10 uM after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities. |
AID475688 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 umol/L after 15 mins by LC/MS/MS analysis | 2010 | Journal 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. |
AID1429865 | Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
AID1221963 | Transporter 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 LY335979 | 2011 | Drug 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. |
AID1502712 | Antimycobacterial activity against Mycobacterium avium isolate MAV3 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1275774 | Cytotoxicity against CHO cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID406196 | Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of puromycin | 2008 | Journal of natural products, Jun, Volume: 71, Issue:6 | Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells. |
AID1215129 | Total 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 NADPH | 2011 | Drug 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. |
AID230565 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1235720 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1352548 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID755314 | Inhibition of p-gp in human KB/VCR cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs. |
AID326369 | Inhibition of Pgp by daunorubicin accumulation assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. |
AID1459758 | Potentiation of doxorubicin-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1352544 | Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID351893 | Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1524536 | Potentiation 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 | |||
AID1459773 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of paclitaxel-induced cytotoxicity at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID681618 | TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells | 2003 | Anti-cancer drugs, Feb, Volume: 14, Issue:2 | Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. |
AID762398 | Inhibition 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 method | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 7-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155. |
AID1336845 | Inhibition 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 control | 2017 | Bioorganic & 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. |
AID1530709 | Reversal 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) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents. |
AID697544 | Activation of human recombinant P-glycoprotein using unmetabolized ATP by luminescence based p-gp-glo assay | 2012 | Journal 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. |
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AID345309 | Intrinsic cytotoxicity against wild type mouse NIH/3T3 cells at 10 uM after 72 hrs by MTT assay | 2008 | Journal 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. |
AID624629 | Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID247665 | Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22 | Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. |
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AID1155075 | Inhibition 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 hr | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1429863 | Effective permeability of the compound at pH 5.5 at 200 uM after 4 hrs by PAMPA-GI assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
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AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current 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. |
AID624628 | Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID1358241 | Inhibition 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%) | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell. |
AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID679788 | TP_TRANSPORTER: serosal to mucosal transport in SD rat intestinal segment | 1995 | Pharmaceutical 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. |
AID678746 | TP_TRANSPORTER: inhibition of Cyclosporin A efflux (CsA: 0.005 uM, Verapamil: 10 uM) in P388/S and P388/ADR cells | 2000 | Clinical and experimental pharmacology & physiology, Aug, Volume: 27, Issue:8 | Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo. |
AID1210014 | Inhibition 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 control | 2012 | Drug 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. |
AID1502901 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1273403 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 4 ug/ml after 7 days by microdilution checkerboard | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1330773 | Effective permeability of the compound by PAMPA | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
AID1530097 | Cell 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%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID509769 | Inhibition of P-gp expression in human KB cells at 4 to 16 uM after 48 hrs by Western blotting | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity. |
AID330505 | Apparent permeability from apical to basolateral side of human Caco-2 cell membrane | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | 4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators. |
AID1565856 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers. |
AID1215177 | Total 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 NADPH | 2011 | Drug 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. |
AID1459770 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1429934 | Substrate activity at P-gp in human LoVo/DX cells assessed as ATP consumption at 10 uM after 2 hrs by ATPlite assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity. |
AID1273474 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 4 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1496418 | Intrinsic clearance in human liver microsomes at 3 uM | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11 | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. |
AID1833359 | Reversal 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) | |||
AID324585 | Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control | 2007 | Proceedings 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. |
AID1683967 | Inhibition 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 | |||
AID102856 | Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, fluorescence activity ratio at 5 ug/mL. | 2002 | Journal 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. |
AID1750944 | Potentiation 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%) | |||
AID429849 | Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as reversal fold after 48 hrs by SRB assay relative to control | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures. |
AID681385 | TP_TRANSPORTER: RT-PCR in HK-2 cell | 2002 | Toxicology 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. |
AID1386183 | Inhibition 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 analysis | 2018 | Journal of natural products, 09-28, Volume: 81, Issue:9 | Cytotoxic p-Terphenyls from the Endolichenic Fungus Floricola striata. |
AID1352552 | Stimulation of human Pgp ATPase activity expressed in cell membranes at 50 uM after 1 hr by P-gp Glo assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1414430 | Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay | 2018 | Journal 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". |
AID1502793 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID699541 | Inhibition 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 counting | 2012 | Journal 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. |
AID1603237 | Permeability of the compound assessed as ratio of Kin to Kout by PAMPA | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID1584806 | Permeability of the compound at pH 7.4 by PAMPA | 2018 | Journal 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. |
AID1740406 | Half life in human microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID154123 | In vitro relative vinblastin uptake into P388/s (murine leukemia) cells following 10 uM treatment. | 1995 | Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26 | Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes. |
AID1225500 | Inhibition 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 assay | 2015 | Journal 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. |
AID1168903 | Modulation 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 analysis | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators. |
AID681118 | TP_TRANSPORTER: transepithelial transport in Caco-2 cells | 2003 | International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2 | Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. |
AID1739812 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1740449 | Half life in human hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID1879914 | Permeability of compound incubated for 3 hrs by UV plate reader based PAMPA assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Design, synthesis and biological evaluations of niclosamide analogues against SARS-CoV-2. |
AID1517887 | Reversal 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 control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1217729 | Intrinsic 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 formation | 2011 | Drug 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. |
AID1502808 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID717463 | Potentiation 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 control | 2012 | Bioorganic & 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. |
AID1733372 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1235793 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID185649 | Compound 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. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors. |
AID1684000 | Inhibition 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 | |||
AID680389 | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 60 uM, Verapamil: 1000 uM) in Xenopus laevis oocytes | 1999 | The 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. |
AID1235799 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1739803 | Inhibition 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 co | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1903287 | Potentiation 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 ) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID75362 | Nagative chronotropic activity was expressed as percent changes in atrial rate on guinea pig spontaneously beating isolated right atrium at 10 e-5 M | 1993 | Journal 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. |
AID159425 | Tested for beta-2 adrenoceptor blocking activity in anesthetized pigs (n=2) challenged with intravenous injections of isoproterenol. | 1987 | Journal 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. |
AID1566030 | Reversal 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 control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance. |
AID399196 | Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 0.1 ug/mL after 2 hrs relative to control | 2004 | Journal of natural products, Jan, Volume: 67, Issue:1 | Production of biologically active taxoids by a callus culture of Taxus cuspidata. |
AID1211795 | Dissociation constant, pKa of the compound | 2012 | Drug 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. |
AID1418886 | Inhibition 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 doxorubicin | 2018 | Bioorganic & 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). |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1155074 | Response 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 in | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID53614 | Percent of cell viability remaining after incubating the cells with the modulator alone a concentration of 5 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID681337 | TP_TRANSPORTER: Western blot, HK-2 cells | 2002 | Toxicology 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. |
AID360079 | Cytotoxicity against human MRP1 expressing hamster BHK21 cells at 10 to 20 uM by MTT assay | 2007 | The Journal of biological chemistry, Oct-26, Volume: 282, Issue:43 | (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1. |
AID1502822 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1813140 | Inhibition 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current 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. |
AID1215185 | AUC (0 to 480 mins) in Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID1603225 | Permeability of the compound assessed as molar fraction in donor well at 0.5 mM measured after 16 hrs by PAMPA | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID568588 | Vasodilatory activity in Sprague-Dawley rat thoracic aorta smooth muscle assessed as inhibition of KCL-induced vasoconstriction | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Macrophyllionium and macrophyllines A and B, oxindole alkaloids from Uncaria macrophylla. |
AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1427528 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA | 2017 | Bioorganic & 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. |
AID1062336 | Modulation 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 control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID153401 | Inhibitory activity when combined with taxol (nM) in P388/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID683265 | Inhibition 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 control | 2012 | Journal 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. |
AID193258 | Antiarrhythmic activity against anesthetized rats after peroral administration | 1992 | Journal 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. |
AID1350749 | Inhibition 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 method | 2018 | Journal 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. |
AID1338194 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID307742 | Cytotoxicity against human A2780 cells assessed as cell viability at 0.2 uM | 2007 | Bioorganic & 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. |
AID209801 | Inhibitory activity when combined with 5-Fluorouracil (uM) in T24 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID681131 | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID1174969 | Resistance 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 washo | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1290697 | Drug metabolism in human liver microsomes assessed as cytochrome P450-mediated compound oxidation by measuring drug recovery after 1 hr by HPLC analysis | 2016 | Journal 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. |
AID53608 | In vitro activity in DC-3F/AD cell line Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 10 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID1761209 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID230393 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID230558 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID27587 | Partition coefficient (logP) | 2002 | Journal 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. |
AID681164 | TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells | 2001 | Pharmaceutical research, Dec, Volume: 18, Issue:12 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. |
AID1228903 | Cytotoxicity against human MDA435/LCC6MDR cells after 3 days by MTS assay | 2015 | Journal 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. |
AID429848 | Reversal of p-gp-mediated multidrug-resistance in human MCF7/ADM cells after 48 hrs by SRB assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures. |
AID153400 | Inhibitory activity when combined with doxorubicin (uM) in P388/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID696928 | Cytotoxicity against MDR1 expressing human HCT15 cells | 2011 | Journal 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. |
AID1283420 | Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 10 uM by MTT assay | 2016 | Journal 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. |
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AID1904172 | Effect on P-gp expression in human K562/A02 cells at 5 uM measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
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AID161281 | Inhibition of human Potassium channel HERG expressed in mammalian cells | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
AID1739808 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
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AID96002 | percentage of the dead cells of K-562 cells was determined for the concentration of 1 uM of the compound. | 1999 | Journal 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. |
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AID1733402 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
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AID1673426 | Reversal 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 l | 2019 | Bioorganic & 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. |
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AID1703887 | Permeability of the compound incubated for 165 mins by PAMPA-BBB assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery 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. |
AID230553 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
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AID331505 | Reversal 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 cytometry | 2008 | Bioorganic & 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. |
AID1352547 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID615732 | Reversal 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 assay | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides. |
AID699540 | Inhibition 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 counting | 2012 | Journal 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. |
AID1275776 | Antiplasmodial activity against multidrug resistant Plasmodium falciparum Dd2 by spectroscopic method | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID1481498 | Inhibition 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 4 | 2017 | Journal 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. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID653466 | Reversal 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 assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1352539 | Cytotoxicity against human MCF7 cells assessed as cell survival at 10 uM after 48 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID453203 | Lipophilicity, log D of the compound | 2010 | Bioorganic & 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. |
AID1391818 | Inhibition of P-gp in human K562 cells assessed as increase in Rh123 accumulation at 5 uM after 2.5 hrs by by flow cytometry method | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors. |
AID1307797 | Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
AID364884 | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
AID53616 | Percent of cell viability remaining after incubating with a 10 uM concentration | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID1903291 | Potentiation 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 ) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID1816741 | Metabolic stability in human liver microsomes assessed as intrinsic clearance in presence of NADPH at 1 uM by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID714413 | Inhibition 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 cells | 2012 | Journal 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. |
AID1358116 | Metabolic 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 | |||
AID146413 | The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Aminoalkynyldithianes. A new class of calcium channel blockers. |
AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
AID681122 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID1156489 | Inhibition 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 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | 4,5-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. |
AID1350739 | Inhibition of ABCB1 in human SW620/AD300 cells assessed as potentiation of paclitaxel-induced cytotoxicity after 72 hrs by MTT assay | 2018 | Journal 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. |
AID150759 | P-gp activity was measured by a direct transport assay, using polarized LLC-mdr1a epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID1365717 | Half life in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID1530100 | Reversal 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 = 71.1 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID1633078 | Cytotoxicity against human HepG2/ADM cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay relative to control | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells. |
AID1502800 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1517886 | Reversal 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 control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1502891 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1481497 | Inhibition 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 measu | 2017 | Journal 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. |
AID1502883 | Inhibition 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 ofloxa | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1785078 | Inhibition 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 | |||
AID103926 | Compound (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 Taxol | 2000 | Bioorganic & 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. |
AID29140 | Apparent value (pKa) calculated with ACD/pKa (experimental pKa value) | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID1091957 | Apparent permeability of the compound by PAMPA | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Importance of physicochemical properties for the design of new pesticides. |
AID464018 | Inhibition 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 spectrofluorimetry | 2010 | Journal 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. |
AID150364 | MDR-reversal property tested in vitro on P388/VCR-20 cells, resistance was induced by vincristine | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | New purines and purine analogs as modulators of multidrug resistance. |
AID1758185 | Antiproliferative activity against human MCF7/ADR cells assessed as inhibition rate at 10 uM incubated for 48 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell. |
AID1813133 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1533103 | Inhibition 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 b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID680136 | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells | 2000 | Drug 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 |
AID1235753 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1064671 | Induction of human recombinant p-glycoprotein ATPase activity using ATP as substrate at 0.5 mM after 40 mins by luciferase-mediated Pgp-Glo assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication. |
AID1739814 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID362950 | Inhibition 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 uM | 2008 | Journal 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. |
AID1174968 | Resistance 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 treatment | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID150618 | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID54923 | Inhibition of human cytochrome P450 3A4 | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID1502867 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID714427 | Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Lineweaver-Burk plot analysis | 2012 | Journal 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. |
AID289064 | Effect on calcein accumulation in MDR 2780AD cells at 0.25 ug/mL relative to control | 2007 | Journal of natural products, Jun, Volume: 70, Issue:6 | Bioactive polyketides from Peperomia duclouxii. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1465293 | Effective permeability of the compound at 100 ug/ml by PAMPA-BBB assay | 2017 | Bioorganic & 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. |
AID406191 | Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of vinblastine | 2008 | Journal of natural products, Jun, Volume: 71, Issue:6 | Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells. |
AID1603235 | Permeability of the compound assessed as rate constant for partitioning to the membrane by PAMPA | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
AID1211798 | Intrinsic clearance in human using well stirred liver model by LC-MS/MS method | 2012 | Drug 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. |
AID1365649 | Permeability of the compound at 100 mg/ml after 16 hrs by BBB-PAMPA method | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease. |
AID1502762 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1228918 | Modulation 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 cells | 2015 | Journal 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. |
AID722211 | Reversal 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 compound | 2013 | Bioorganic & 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). |
AID1209593 | Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis | 2011 | Drug 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. |
AID1210967 | Ratio 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 control | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Effects of chronic renal failure on brain drug transporters in rats. |
AID166816 | Compound was evaluated for the alpha-Adrenoceptor pA2 blocking activity in vitro in rabbit thoracic aorta | 1987 | Journal 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. |
AID158040 | Concentration required to reduce chloroquine IC50 by 50% | 2002 | Journal 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. |
AID306134 | Effect on calcein accumulation in multidrug-resistant human 2780AD cells at 2.5 ug/ml relative to control | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Structure-activity relationships of some taxoids as multidrug resistance modulator. |
AID653451 | Inhibition of p-glycoprotein-mediated rhodamine 123 efflux in human K562/A02 cells at 0.25 to 5 after 60 mins by fluorescence microscopic analysis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1459772 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1785069 | Inhibition 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 | |||
AID1851936 | Metabolic stability in mouse microsomes assessed as compound remaining measured after 30 mins | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
AID1595499 | Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Modulation 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. |
AID540211 | Fraction unbound in human after iv administration | 2008 | Drug 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. |
AID1813135 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1904176 | Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability at 50 uM after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID27572 | Partition coefficient (logD7.0) | 2002 | Journal 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. |
AID619536 | Inhibition 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 assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes. |
AID76313 | Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro Negative inotropic potency) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
AID1675373 | Stimulation of P-gp ATPase activity (unknown origin) assessed as increase in ATP consumption at 10 uM relative to control | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Ecdysteroid Derivatives that Reverse P-Glycoprotein-Mediated Drug Resistance. |
AID1313195 | Intrinsic clearance in human liver microsomes assessed per mg of protein at 3 uM in presence of NADPH by LC-MS/MS analysis | 2016 | Bioorganic & 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. |
AID318687 | Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of paclitaxel by MTS assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Synthesis of curcumin mimics with multidrug resistance reversal activities. |
AID1288621 | Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID1368307 | Inhibition of P-gp in human K562/Dox cells assessed as maximum increase in nuclear accumulation of pirarubicin by spectrofluorometric assay | 2018 | Bioorganic & 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). |
AID1198506 | Inhibition of Trypanosoma cruzi cruzaine at 100 uM using mMBz-Pro-Phe-Arg-pNA substrate incubated for for 5 mins by UV-vis spectrophotometry | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Computer-guided drug repurposing: identification of trypanocidal activity of clofazimine, benidipine and saquinavir. |
AID1673437 | Inhibition 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 analysis | 2019 | Bioorganic & 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. |
AID1733389 | Modulation 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 analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1530762 | Inhibition 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 method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | 1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1. |
AID1239239 | Inhibition 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 control | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors. |
AID1517908 | Inhibition 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 c | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1190830 | Cytotoxicity against human KB/VCR cells at 10 uM after 72 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Multidrug resistance-reversal effects of resin glycosides from Dichondra repens. |
AID230554 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1167634 | Blood brain permeability of the compound at donor and acceptor by PAMPA assay | 2014 | Bioorganic & 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. |
AID1215182 | 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 NADPH | 2011 | Drug 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. |
AID1351582 | Tracheorelaxant activity in Wistar rat trachea tonus assessed as reduction in 30 mM KCl-induced contraction after 15 mins | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, 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. |
AID681127 | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID332136 | Reversal 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 assay | 1997 | Journal of natural products, Nov, Volume: 60, Issue:11 | Multidrug-resistance modulators from Stephania japonica. |
AID653455 | Cytotoxicity against human K562/A02 cells expressing p-glycoprotein assessed as cell killing at 5 uM after 72 hrs by MTS assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1228919 | Modulation 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 cells | 2015 | Journal 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. |
AID1684008 | Reversal 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 | |||
AID1906055 | Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. |
AID1750903 | Reversal 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 | |||
AID681163 | TP_TRANSPORTER: ATP hydrolysis in reconstituted proteoliposomes | 1996 | The 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. |
AID103936 | Inhibitory activity when combined with 5-fluorouracil (uM) in MCF-7/VP cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1530092 | Reversal 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) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID105434 | Ability of compound to inhibit MDA-435/LCC6-MDR cell growth relative to progesterone. | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID1785072 | Inhibition 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 | |||
AID1576577 | Effective permeability of compound incubated for 8 hrs by PAMPA | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling. |
AID166558 | Fractional inhibitory concentration (FIC) tested against RCS cells, isolate from Brazil. | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum. |
AID1062341 | Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID1334753 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA assay | 2017 | Bioorganic & 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. |
AID1429867 | Effective permeability of the compound at pH 7.4 at 50 uM after 4 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
AID330503 | Activation of human P-gp ATPase in human Caco-2 cells at 100 uM | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | 4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators. |
AID340721 | Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Role of the ABC transporter PRP1 (ABCC7) in pentamidine resistance in Leishmania amastigotes. |
AID680675 | TP_TRANSPORTER: increase in saquinavir intracellular accumulation by Verapamil at 100uM in LLC-GA5-COL150 cells | 2004 | British journal of pharmacology, Dec, Volume: 143, Issue:7 | Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. |
AID492324 | Inhibition of Pgp expressed in mouse L5178Y cells at 10 uM relative to control | 2010 | Bioorganic & 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. |
AID1237324 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID230556 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1771040 | Half life in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
AID1683969 | Inhibition 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 | |||
AID1472782 | Inhibition 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 ass | 2018 | Journal 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. |
AID1207718 | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID1502729 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1210072 | Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method | 2013 | Drug 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. |
AID1502815 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1211794 | Fraction unbound in blood (not specified) | 2012 | Drug 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. |
AID1502872 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID103923 | Effective 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. | 1998 | Journal 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. |
AID681907 | TP_TRANSPORTER: inhibition of MTX uptake (MTX: 20 uM, Verapamil: 30 uM) in membrane vesicles from MRP4-expressing Sf9 cells | 2002 | Cancer 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. |
AID619537 | Inhibition 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 assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes. |
AID1413459 | Permeability of the compound at 50 ug/ml after 16 hrs by PAMPA | |||
AID1739824 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1589935 | Half life in rat liver microsomes | 2019 | Bioorganic & 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. |
AID179048 | Compound was evaluated for the slow action potential blockade in 4 spontaneously hypertensive rats (SHR) | 1987 | Journal 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. |
AID1427564 | Metabolic stability in rat liver microsomes assessed as parent compound remaining measured after 30 mins in presence of NADPH | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A |
AID1459767 | Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID368371 | Reversal 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 spectrofluorimetry | 2009 | Journal 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. |
AID1174628 | Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence microscopy | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities. |
AID313273 | Inhibition of P-glycoprotein in MDR human KBChR-8-5 cells assessed as retention of [3H]VLB after 2 hrs | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells. |
AID1235784 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID88420 | In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100 (uM) of infected host | 2000 | Journal 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. |
AID1617119 | Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Macroline-Sarpagine Bisindole Alkaloids with Antiproliferative Activity from |
AID1215162 | AUC (0 to infinity) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Drug 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. |
AID1210070 | Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method | 2013 | Drug 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. |
AID1362715 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria. |
AID229582 | Ratio of maximal driving frequency to atrial rate in isolated guinea pig atria | 1980 | Journal 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. |
AID77932 | Left ventricular pressure of isolated guinea pig heart at dose 0.5 (ug/heart) | 1985 | Journal 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. |
AID1525470 | Protein binding in rat plasma | 2019 | Journal 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. |
AID1565852 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers. |
AID1703921 | Permeability of the compound by PAMPA-BBB assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery 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. |
AID73909 | Potency expressed as EC50 for the negative inotropic activity. | 1999 | Journal 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. |
AID1833338 | Reversal 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 | |||
AID156089 | Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system | 2000 | Journal 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. |
AID175483 | Compound was evaluated for the concentration dependent negative ionotropic effect in rat right myocardial ventricular strips | 1986 | Journal 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. |
AID1517907 | Inhibition 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 | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID80297 | Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.03 mg/mL concentration | 1992 | Journal 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. |
AID194806 | Antihypertensive 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) | 1987 | Journal 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. |
AID1459761 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID88407 | In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 100 uM | 2000 | Journal 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. |
AID1235783 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID444052 | Hepatic clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1376831 | Modulation 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) | 2017 | Journal of natural products, 05-26, Volume: 80, Issue:5 | Exploring Jolkinol D Derivatives To Overcome Multidrug Resistance in Cancer. |
AID1771041 | Intrinsic clearance in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
AID76077 | Inhibition concentration of vasodilation was calculated from log concentration/response curves | 1993 | Journal 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. |
AID481936 | Inhibition of P-gp-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells by flow cytometry | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells. |
AID1459771 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of vincristine-induced cytotoxicity at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1245597 | Half life in human microsomes at 1 uM in absence of NADPH | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation. |
AID1702313 | Inhibition of P-gp in human MDR1-MDCKII cells | |||
AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug 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. |
AID310122 | Inhibition of P-glycoprotein by Hoechst assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1709005 | Permeability of compound at 100 uM at pH 7.4 by PAMPA assay | 2021 | Journal 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. |
AID1769163 | Inhibition 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 analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
AID331513 | Cytocidal activity against human MDR1 gene transfected mouse L5178Y cells after 48 hrs by MTT method | 2008 | Bioorganic & 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. |
AID1129441 | Intrinsic clearance in human microsomes at 1 uM in presence of NADPH | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1321568 | Inhibition 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 No | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance. |
AID1684011 | Reversal 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) | |||
AID1228905 | Modulation 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 | 2015 | Journal 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. |
AID1533104 | Inhibition 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 b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current 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. |
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AID1833374 | Reversal 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 | |||
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AID513628 | Induction 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 analysis | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID288184 | Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
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AID1264249 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Design, synthesis and biological evaluation of tricyclic diterpene derivatives as novel neuroprotective agents against ischemic brain injury. |
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AID1874535 | Metabolic stability in mouse liver microsomes assessed as half life at 5 uM measured for 60 mins by LC-MS/MS analysis | 2022 | Journal 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. |
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AID1353449 | Inhibition 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 a | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents. |
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AID1517901 | Reversal 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 analy | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
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AID1459757 | Potentiation of doxorubicin-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1273451 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 32 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
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AID695916 | Inhibition of Hoechst 33342 dye in norA-deficient Escherichia coli DH10B expressing pTrc99A at 2 ug/mL by spectrofluorometer analysis | 2012 | Bioorganic & 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. |
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AID251492 | Multi drug resistance reversal in HCT116/VM46 cell line treated with Vinblastine | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Multidrug resistance reversal activity of permethyl ningalin B amide derivatives. |
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AID159764 | Fractional inhibitory concentration (FIC) against Plasmodium falciparum W2 of equimolar (1:1) combination dose with chloroquine | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum. |
AID43526 | The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin | 1995 | Journal 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. |
AID1357216 | Intrinsic clearance in mouse liver microsomes in presence of NADPH regeneration system | 2018 | Journal 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. |
AID1564095 | Reversal 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) | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance. |
AID510387 | Inhibition of Staphylococcus aureus 1199 norA efflux pump assessed as potentiation of ciprofloxacin MIC by spectrophotometry | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus. |
AID1155076 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
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AID1336843 | Activity 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 control | 2017 | Bioorganic & 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. |
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AID368554 | Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID368382 | Intrinsic cytotoxicity against human doxorubicin-sensitive K562 cells at 1 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID1649243 | Reversal 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) | 2020 | Journal 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. |
AID1200540 | Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 50 uM relative to untreated control | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Xanthone analogues as potent modulators of intestinal P-glycoprotein. |
AID1762450 | Metabolic stability in human liver microsomes assessed as parent compound remaining after 120 mins in presence of NADPH regeneration system by UPLC/MS anlaysis | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
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AID96336 | Potency that causes a half maximal increase in nuclear concentration of pirarubicin. | 1999 | Journal 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. |
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AID1739433 | Metabolic stability in human liver microsomes assessed as half life at 100 uM measured upto 30 mins | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Substituted 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. |
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AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID464023 | Growth inhibition in doxorubicin-resistant human K562 cells overexpressing Pgp at 1 uM after 72 hrs by MTT assay | 2010 | Journal 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. |
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AID246154 | Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22 | Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. |
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AID1683996 | Inhibition 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 | |||
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AID1781218 | Anti-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 | |||
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AID1862044 | Effective permeability of the compound at pH 7.4 measured after 18 hrs by PAMPA-BBB assay | 2022 | Bioorganic & medicinal chemistry, 09-01, Volume: 69 | 2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors. |
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AID427742 | Reversal 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 uM | 2009 | Journal 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. |
AID1514562 | Potentiation 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) | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID1429862 | Effective permeability of the compound at pH 2 at 200 uM after 4 hrs by PAMPA-GI assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
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AID101595 | Inhibitory activity when combined with vinblastine (nM) in MCF-7 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
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AID324380 | Induction of light chain 3-GFP level in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings 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. |
AID514302 | Protection 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 uM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
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AID1514560 | Potentiation 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) | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
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AID389767 | Inhibition of MDR1 overexpressed in MDCK cells at 25 uM relative to LSN335984 | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells. |
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AID513626 | Induction 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 analysis | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
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AID1595500 | Inhibition of MRP1 (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Modulation 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. |
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AID230563 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1771037 | Intrinsic clearance in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
AID1772563 | Apparent permeability of the compound across apical side to basolateral side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID713774 | Binding 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 control | 2012 | Bioorganic & 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). |
AID1215166 | AUC (0 to 90 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat portal vein plasma at 10 mg/kg, po | 2011 | Drug 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. |
AID1502772 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1371162 | Intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis | 2017 | Journal 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). |
AID656823 | Inhibition 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 control | 2012 | Bioorganic & 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. |
AID265200 | Reversal of multi-drug resistance in L5178Y cells transfected with human MDR1 as relative fluorescent rhodamine123 activity at 10 ug/mL | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | New potent P-glycoprotein inhibitors carrying a polycyclic scaffold. |
AID1728591 | Inhibition 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 f | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Alkylated monoterpene indole alkaloid derivatives as potent P-glycoprotein inhibitors in resistant cancer cells. |
AID379508 | Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method | 1999 | Journal of natural products, May, Volume: 62, Issue:5 | Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance. |
AID379471 | Cytotoxicity against human KB31 cells after 48 hrs by SRB assay | 1999 | Journal of natural products, Apr, Volume: 62, Issue:4 | Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii. |
AID1273401 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 16 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1481490 | Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay | 2017 | Journal 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. |
AID321881 | Apparent permeability from basolateral to apical side of human Caco-2 cell membrane | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. |
AID159876 | Accumulation coefficient of chloroquine at 1 uM-10 uM of DEEA against Plasmodium falciparum W2 | 2002 | Journal 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. |
AID368401 | Reversal 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 uM | 2009 | Journal 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. |
AID1223490 | Apparent permeability across human differentiated Caco2 cells | 2012 | Drug 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. |
AID1904170 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID1358240 | Inhibition 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 alone | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell. |
AID1647654 | Reversal 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) | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, |
AID332133 | Reversal 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 assay | 1997 | Journal of natural products, Nov, Volume: 60, Issue:11 | Multidrug-resistance modulators from Stephania japonica. |
AID1502738 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1215184 | Tmax in Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID1904130 | Reversal 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 | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID317949 | Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells | 2008 | Journal 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. |
AID1769132 | Inhibition 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 analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
AID230392 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1771038 | Half life in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
AID1273438 | Modulation factor, ratio of refampin MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of refampin | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1273463 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 4 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID427402 | Reversal 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 test | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Tabernines A-C, beta-carbolines from the leaves of Tabernaemontana elegans. |
AID1603231 | Permeability of the compound assessed as molar fraction in membrane at 0.5 mM measured after 2 hrs by PAMPA | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1054122 | Inhibition of human ERG | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Polypharmacology - foe or friend? |
AID1817177 | Stability 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 control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of G Protein-Biased Ligands against 5-HT |
AID1502785 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID514301 | Protection of neurodegeneration in Drosophila Huntington's disease model assessed as induction autophagy at 2.5 mM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID1833362 | Reversal 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 | |||
AID1374514 | Activity 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 control | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | MF-8, a novel promising arylpiperazine-hydantoin based 5-HT |
AID350218 | Octanol-water partition coefficient, log PC of the compound | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
AID1225502 | Cytotoxicity against human MDR1 transfected mouse NIH/3T3 MDR1-G185 cells assessed as cell growth at 10 uM after 24 hrs by MTT assay | 2015 | Journal 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. |
AID1739828 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID193139 | inhibitory activity was tested against anesthetized rats at 10 mg/kg | 1992 | Journal 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. |
AID379773 | Reversal 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 method | 1999 | Journal of natural products, May, Volume: 62, Issue:5 | Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance. |
AID1174944 | Reversal 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 assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID693225 | Binding affinity to truncated human PrP 121-231 at 50 uM by surface plasmon resonance method | 2011 | European 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. |
AID1623668 | Permeability of compound at pH 7.4 by PAMPA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1502873 | Inhibition 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 alone | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502920 | Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1524535 | Potentiation 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) | |||
AID1604713 | Permeability at 200 uM incubated for 4 hrs by PAMPA method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID103939 | Inhibitory activity when combined with vinblastine (nM) in MCF-7/VP cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1849433 | Stability of the compound in simulated intestinal fluid at pH 6 to 8 assessed as compound remaining at 120 mins by LC-MS/MS analysis | |||
AID1215186 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID1273479 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 32 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1909448 | Permeability of the compound by PAMPA-BBB assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease. |
AID1888851 | Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of norfloxacin-induced antibacterial activity by measuring fractional inhibitory concentration | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID1514555 | Cytotoxicity against HUVEC assessed as survival at 10 uM after 48 hrs by MTT assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID1459762 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID399032 | Inhibition 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 control | 2005 | Journal of natural products, Nov, Volume: 68, Issue:11 | Bioactive tetrahydrofuran lignans from Peperomia dindygulensis. |
AID1283419 | Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 3 uM by MTT assay | 2016 | Journal 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. |
AID1215163 | Half life in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Drug 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. |
AID1733396 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1807361 | Metabolic stability in mouse liver microsomes assessed as half life in presence of NADPH regenerating system by UPLC-MS analysis | |||
AID1604133 | Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate | 2020 | Journal 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. |
AID714415 | Cytotoxicity against human LCC-6 cells after 72 hrs | 2012 | Journal 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. |
AID1234531 | Inhibition 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 cytometry | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Discovery of substituted 1,4-dihydroquinolines as novel class of ABCB1 modulators. |
AID1235719 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1330413 | Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing GFP assessed as growth inhibition at 1 ug/ml measured after 7 days by fluorescence analysis relative to control | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Discovery of novel N-phenyl 1,4-dihydropyridines with a dual mode of antimycobacterial activity. |
AID1502820 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1816740 | Metabolic stability in rat liver microsomes assessed as half life in presence of NADPH at 1 uM by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID1888852 | Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring ethidium bromide MIC at sub MIC | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID1502778 | Inhibition 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 erythromy | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1770542 | Metabolic 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 analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold. |
AID510384 | Inhibition of Staphylococcus aureus 1199B norA efflux pump assessed as potentiation of ciprofloxacin MIC by spectrophotometry | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus. |
AID29338 | Dissociation constant (pKa) | 2002 | Journal 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. |
AID1517905 | Reversal 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 analys | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1833353 | Reversal 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) | |||
AID1816742 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance in presence of NADPH at 1 uM by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
AID77643 | Antagonism of calcium-induced contractions of guinea pig ileal strips | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Aminoalkynyldithianes. A new class of calcium channel blockers. |
AID1322437 | Inhibition 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 cytometry | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors. |
AID1739840 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1822204 | Fold 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 | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore. |
AID1602170 | Metabolic stability in mouse liver microsomes at 1 uM in presence of NADPH incubated for 0 mins by LC-MS/MS analysis | 2019 | Journal 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. |
AID728948 | Myorelaxant activity in albino rat aorta rings assessed as relaxation of 30 mM KCl-induced contraction of aorta rings | 2013 | Journal 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. |
AID1167513 | Modulatory 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) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters. |
AID546592 | Inhibition 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 control | 2010 | Journal 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. |
AID1833365 | Reversal 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 | |||
AID158683 | In vitro inhibitory activity against multidrug-resistant Plasmodium falciparum W2 Indochina | 2002 | Journal 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. |
AID499784 | Activation of phospholipase A2/C in human OC2 cells assessed as increase in intracellular calcium level at 1 uM | 2010 | Journal 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). |
AID1180220 | Inhibition 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) | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID231934 | Ratio for antagonistic activity for Pgp/MRP1 was determined | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists. |
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AID1623673 | Protein binding in human plasma | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
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AID307748 | Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 10 uM | 2007 | Bioorganic & 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. |
AID331363 | Inhibition of Pgp-mediated multidrug resistance activity in rat RBMEC cells assessed as decrease in Rh123 efflux | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer. |
AID262090 | Antiarrhythmic activity in iv dosed rat | 2006 | Bioorganic & 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. |
AID1623690 | Permeability of compound at pH 7.4 assessed as drug retention by PAMPA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1200541 | Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 100 uM relative to untreated control | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Xanthone analogues as potent modulators of intestinal P-glycoprotein. |
AID1338180 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
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AID1374214 | Effective permeability of the compound in pH 7.4 buffer after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & 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. |
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AID1525471 | Stability in rat liver microsomes assessed as parent compound remaining level | 2019 | Journal 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. |
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AID80864 | Percent reversion in HCT116 cell line (IC50(-)/MDR IC50(+) X 100 | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10 | Multidrug resistance reversal activity of key ningalin analogues. |
AID268084 | Metabolic stability in rat liver microsomes | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors. |
AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1235765 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1481494 | Substrate 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 control | 2017 | Journal 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. |
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AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1079938 | Chronic 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] | |||
AID1446672 | Displacement 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 | |||
AID1502766 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1702159 | Clearance 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 analysis | 2018 | Journal 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. |
AID1235762 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID714416 | Cytotoxicity against mouse L929 cells after 72 hrs | 2012 | Journal 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. |
AID1168387 | Inhibition 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 cytometry | 2014 | Journal of natural products, Oct-24, Volume: 77, Issue:10 | Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition. |
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AID1739834 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1371164 | Aqueous solubility of the compound in PBS after 2 hrs by turbidimetric method | 2017 | Journal 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). |
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AID1357220 | Intrinsic clearance in human liver microsomes in presence of NADPH regeneration system | 2018 | Journal 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. |
AID319361 | Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells | 2008 | Bioorganic & 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. |
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AID1062340 | Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID562098 | Chemosensitization of amodiaquin against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid. |
AID1444095 | Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
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AID321384 | Apparent permeability from apical to basolateral side of human Caco-2 cell membrane at pH 7.4 after 21 days | 2008 | Bioorganic & 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. |
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AID1761222 | Reversal 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%) | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID502262 | Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay | 2010 | Bioorganic & 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. |
AID306135 | Effect on calcein accumulation in multidrug-resistant human 2780AD cells at 25 ug/ml relative to control | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Structure-activity relationships of some taxoids as multidrug resistance modulator. |
AID322362 | Inhibition of human multidrug resistant gene Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein. |
AID475689 | Metabolic stability in cryopreserved human hepatocytes assessed as compound remaining at 5 umol/L after 240 mins by LC/MS/MS analysis | 2010 | Journal 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. |
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AID1246312 | Intrinsic clearance in mouse microsomes | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
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AID722615 | Inhibition 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 analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Enhancing macrocyclic diterpenes as multidrug-resistance reversers: structure-activity studies on jolkinol D derivatives. |
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AID1525469 | Protein binding in human plasma | 2019 | Journal 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. |
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AID1738698 | Inhibition of P-gp-mediated doxorubicin efflux in human K562/4 cells assessed as increase in doxorubicin accumulation by flow cytometric analysis | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin. |
AID1649256 | Effect 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 assay | 2020 | Journal 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. |
AID1502803 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID345308 | Intrinsic cytotoxicity against mouse NIH/3T3 cells overexpressing MDR1 at 3 uM after 72 hrs by MTT assay | 2008 | Journal 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. |
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AID1783322 | Inhibition 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%) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis, computational docking and biological evaluation of celastrol derivatives as dual inhibitors of SERCA and P-glycoprotein in cancer therapy. |
AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID551246 | Half life in human microsome by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis. |
AID1702153 | Metabolic stability in mouse liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis | 2018 | Journal 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. |
AID153399 | Inhibitory activity when combined with cisplatin (uM) in P388/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
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AID1237325 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID1481913 | Inhibition 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 assay | 2017 | Journal 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. |
AID653307 | Inhibition of p-glycoprotein in human K562/A02 cells assessed as accumulation of rhodamine 123 by flow cytometry | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1764805 | Half 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 analysis | 2021 | Journal 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. |
AID317950 | Activation of human P-glycoprotein ATPase in Caco-2 cells assessed as ATP depletion at 100 uM | 2008 | Journal 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. |
AID427738 | Inhibition of MRP1 in human 2008/MRP1 cells by Lineweaver-Burke plot analysis | 2009 | Journal 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. |
AID1502859 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
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AID324536 | Increase 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 control | 2007 | Proceedings 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. |
AID1350734 | Inhibition 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 analysis | 2018 | Journal 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. |
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AID1305711 | Half life in mouse liver microsomes at 0.1 uM | 2016 | Bioorganic & 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. |
AID1310680 | Inhibition 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 control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Synthesis and bioevaluation of novel benzodipyranone derivatives as P-glycoprotein inhibitors for multidrug resistance reversal agents. |
AID1235701 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
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AID1351579 | Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 80 mM KCl-induced contraction after 15 mins | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, 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. |
AID1207266 | Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range) | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID1483833 | Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS analysis | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ. |
AID150758 | P-gp activity was measured by a direct transport assay, using polarized LLC-PK1 epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID1273476 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 16 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1502850 | Inhibition 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 t | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1225499 | Inhibition 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 assay | 2015 | Journal 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. |
AID1623665 | Half life in human microsomes | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1502763 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1418856 | Potentiation 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 alone | 2018 | Bioorganic & 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). |
AID1225501 | Inhibition 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 assay | 2015 | Journal 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. |
AID1200585 | Inhibition of human P-glycoprotein ATPase activity assessed as inorganic phosphorus measured as ATPase activity ratio at 20 uM relative to untreated control | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Xanthone analogues as potent modulators of intestinal P-glycoprotein. |
AID1235769 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1833329 | Reversal 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) | |||
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AID1378334 | Permeability of the compound by PAMPA | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, 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. |
AID1190546 | Cytotoxicity against taxol-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2015 | Bioorganic & 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. |
AID1849468 | Cytotoxicity 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 | |||
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AID1418883 | Inhibition 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 paclitaxel | 2018 | Bioorganic & 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). |
AID1502821 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID351890 | Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
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AID1635245 | Half life in human liver microsomes at 3 uM preincubated with compound followed by NADPH addition by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
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AID101594 | Inhibitory activity when combined with taxol (nM) in MCF-7 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
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AID243151 | Inhibitory concentration against potassium channel HERG | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. |
AID1502854 | Inhibition 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 t | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1739135 | Metabolic stability at phase 1 in mouse liver microsomes assessed as half life at 1 uM by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Chemical profiling of HIV-1 capsid-targeting antiviral PF74. |
AID636082 | Induction 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 counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID195351 | Inhibition of calcium activation was assessed against calcium-induced constriction of potassium-depolarized rat aorta (Negative logarithm of the molar concentration) | 1991 | Journal 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. |
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AID502840 | Cytotoxicity against human KB cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | Synthesis and structure-activity relationships of sinenxan A derivatives as multidrug resistance reversal agents. |
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AID1813139 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID544255 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as 50% revertant concentration required for chloroquine susceptibility | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vitro and in vivo properties of ellagic acid in malaria treatment. |
AID1215178 | Drug 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 NADPH | 2011 | Drug 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. |
AID455739 | Reversal of human MDR1-mediated multidrug resistance in mouse L5178Y cells expressing MDR1 mean fluorescence intensity of rhodamine-123 uptake after 10 mins by flow cytometry | 2009 | Bioorganic & 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. |
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AID1414432 | Inhibition of MRP1 in human 2008/MRP1 cells assessed as increase in doxorubicin accumulation at 2 uM after 120 mins by flow cytometry relative to control | 2018 | Journal 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". |
AID481446 | Effective permeability across human jejunum | 2010 | Journal 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? |
AID551245 | Intrinsic clearance in mouse microsome by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis. |
AID150617 | Concentration required for 50% inhibition (racemic) at binding site of human P-Glycoprotein (P-gp) in one-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID669852 | Inhibition 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 control | 2012 | Bioorganic & 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. |
AID1623078 | Effective permeability of the compound at 100 ug/ml after 10 hrs by BBB-PAMPA method | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease. |
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AID1279155 | Permeability of the compound at 25 ug/ml at pH 7.4 after 18 hrs by PAMPA | 2016 | Bioorganic & 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. |
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AID1585850 | Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA | 2018 | Bioorganic & 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. |
AID272487 | Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay | 2006 | Journal 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. |
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AID714418 | Reversal of P-gp-mediated vincristine-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
AID1739810 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID350523 | Induction of mouse cysteine-less MDR3 ATPase activity by apparent Michaelis-Menten constant | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity. |
AID105426 | Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells. | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID1739816 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID671173 | Inhibition of P-glycoprotein in rat primary hepatocytes assessed as increase in intracellular rhodamine 123 accumulation at 10 to 50 uM after 3 hrs | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Selective hydroboration of dieneamines. Formation of hydroxyalkylphenothiazines as MDR modulators. |
AID1481489 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2017 | Journal 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. |
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AID1683953 | Potentiation 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 | |||
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AID1569056 | Half-life in CD-1 mouse liver microsomes in presence of NADPH regenerating system measured up to 4 hrs by UPLC-MS analysis | |||
AID1623666 | Intrinsic clearance in human microsomes | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID43400 | Effective dose against CCRF-CEM vcr 100 cells by using MTT assay | 1996 | Journal 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. |
AID80743 | Evaluated for decrease in spontaneous frequency of atrial rate in isolated guinea pig atria | 1980 | Journal 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. |
AID1246310 | Half life in mouse microsomes | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID294090 | Antiviral activity against Sindbis virus replication in BHK cells after 12 hrs by XTT assay | 2007 | Bioorganic & 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. |
AID345310 | Intrinsic cytotoxicity against wild type mouse NIH/3T3 cells at 3 uM after 72 hrs by MTT assay | 2008 | Journal 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. |
AID103940 | Inhibitory activity when combined with vincristine (nM) in MCF-7/VP cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID680270 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Verapamil: 75 uM) in MDR1-expressing NIH-3T3 cells | 2004 | Biochemical 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. |
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AID345314 | Reversal 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 hrs | 2008 | Journal 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. |
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AID714428 | Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Dixon plot analysis | 2012 | Journal 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. |
AID1781217 | Anti-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) | |||
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AID106334 | Compound (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 doxorubicin | 2000 | Bioorganic & 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. |
AID1533100 | Inhibition 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 | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID240820 | Inhibitory concentration against IKr potassium channel | 2004 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18 | The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. |
AID615733 | Reversal 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 control | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides. |
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AID1502852 | Inhibition 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 t | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID310898 | Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing maximal increase in nuclear concentration of pirarubicin relative to control | 2007 | Journal 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. |
AID1683984 | Reversal 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) | |||
AID1351584 | Ratio of EC50 for Wistar rat trachea tonus to EC50 for Wistar rat endothelium-denuded thoracic aorta ring | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, 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. |
AID1585493 | Induction 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 method | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Optimization and preclinical evaluation of novel histamine H |
AID1502711 | Antimycobacterial activity against Mycobacterium avium isolate MAV2 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502902 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1429985 | Inhibition 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 0 | 2017 | Bioorganic & 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. |
AID1239236 | Selectivity index, ratio of IC50 for mouse L929 cells to EC50 for reversal of P-gp-mediated paclitaxel resistance in human MDA435/LCC6MDR cells | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors. |
AID18849 | Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology. | 2000 | Journal 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. |
AID1235696 | Inhibition 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 fluorometry | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID551248 | Intrinsic clearance in human microsome by LC-MS/MS analysis in presence of NADPH | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis. |
AID1321565 | Inhibition 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 cytometry | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance. |
AID1833356 | Reversal 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 | |||
AID165540 | Inhibition of contraction in rabbit pulmonary artery, K+. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID464024 | Growth inhibition in doxorubicin-resistant human K562 cells overexpressing Pgp at 3 uM after 72 hrs by MTT assay | 2010 | Journal 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. |
AID1155073 | Response 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 in | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1298979 | Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 26, Issue:12 | Identification of selenocompounds with promising properties to reverse cancer multidrug resistance. |
AID153402 | Inhibitory activity when combined with vinblastine (nM) in P388/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1211792 | Hepatic clearance in human | 2012 | Drug 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. |
AID427804 | Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as viability after 2 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis. |
AID1740405 | Half life in mouse microsomes at 1 uM up to 120 mins by HPLC/MS-MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID82675 | Effective 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. | 1998 | Journal 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. |
AID1548637 | Effective permeability of compound in PBS buffer at pH 7.4 at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay | 2020 | Journal 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. |
AID1533611 | Effective permeability of the compound by PAMPA | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
AID1273452 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 128 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1235704 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1174949 | Reversal 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 assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID1429866 | Effective permeability of the compound at pH 7.4 at 100 uM after 4 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
AID1374472 | Half life in dog liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID717465 | Potentiation 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 control | 2012 | Bioorganic & 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. |
AID1283414 | Intrinsic cytotoxicity against mouse NIH/3T3 cells transfected with human MDR1 by MTT assay | 2016 | Journal 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. |
AID1785083 | Inhibition of P-gp in paclitaxel-resistant human SW620/AD300 cells assessed as accumulation of paclitaxel incubated for 24 hrs by HPLC analysis | |||
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AID1194717 | Solubility in pH 7.4 buffer after 18 hrs by UV spectroscopy based microSol assay | 2015 | Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9 | Improving both aqueous solubility and anti-cancer activity by assessing progressive lead optimization libraries. |
AID1502833 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502777 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID264304 | Ratio of rhodamine123 uptake in MDR1 transfected cells vs parental L5178Y cells at 3 uM | 2006 | Journal 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. |
AID1350746 | Inhibition 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 fl | 2018 | Journal 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. |
AID1578508 | Stability in ICR/CD1 mouse hepatocytes assessed as half life at 1 uM measured upto 120 mins by LCMS analysis | 2020 | ACS 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. |
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AID252860 | Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (10 uM) and Vinblastine (VNB) | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13 | Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis. |
AID170812 | Effect (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. | 1992 | Journal 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. |
AID1210071 | Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method | 2013 | Drug 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. |
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AID472447 | Antioxidant 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 assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives. |
AID1596589 | Solubility of compound in PBS after 2 hrs by turbidity based absorbance analysis | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity. |
AID1750945 | Potentiation 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%) | |||
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AID1129443 | Intrinsic clearance in human microsomes at 1 uM | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID681334 | TP_TRANSPORTER: transepithelial transport in Caco 2 cell | 2004 | Pharmaceutical 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. |
AID1683991 | Inhibition 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 | |||
AID1312935 | Intrinsic clearance in human liver microsomes measured after 10 to 60 mins in absence of NADPH by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties. |
AID1419452 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy. |
AID1502708 | Antimycobacterial activity against Mycobacterium avium 104 mc'2 4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID150736 | Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID656820 | Inhibition 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 control | 2012 | Bioorganic & 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. |
AID1517889 | Reversal 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) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
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AID313271 | Lipophilicity, log P of the compound | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells. |
AID1348874 | Inhibition 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 | |||
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AID681847 | TP_TRANSPORTER: inhibition of Digoxin uptake (Digoxin: 0.05 uM, Verapamil: 1000 uM) in Oatp2-expressing LLC-PK1 cells | 2002 | Pharmaceutical research, Feb, Volume: 19, Issue:2 | Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. |
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AID407205 | Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13 | Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum. |
AID1397459 | Half life in rat liver microsomes | 2018 | Bioorganic & 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. |
AID1502838 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1565853 | Inhibition 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers. |
AID1772565 | Efflux ratio of apparent permeability in human Caco-2 cells | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID427713 | Increase in doxorubicin accumulation in doxorubicin-co-incubated human 2008/P cells at 3 uM after 120 mins by spectrofluorimetry | 2009 | Journal 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. |
AID536851 | Half life in human liver microsomes at 3 uM by LC-MS/MS analysis | 2010 | Journal 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. |
AID1502910 | Inhibition 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 relati | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID379510 | Reversal 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 method | 1999 | Journal of natural products, May, Volume: 62, Issue:5 | Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance. |
AID1309710 | Metabolic stability in mouse liver S9 fraction assessed as compound remaining after 30 mins | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery, Optimization, and Biological Evaluation of Sulfonamidoacetamides as an Inducer of Axon Regeneration. |
AID1476985 | Effective permeability of compound at 200 uM after 17 hrs by PAMPA-BBB assay | 2017 | Journal 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. |
AID283796 | Effect on calcein accumulation in human multidrug-resistant 2780AD cells at 25 ug/mL relative to control | 2007 | Journal of natural products, Apr, Volume: 70, Issue:4 | Bioactive lignans from Peperomia duclouxii. |
AID1155072 | Response 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 drug | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1215130 | Total 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 presence | 2011 | Drug 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. |
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AID1215187 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID76245 | Potency expressed as IC50 for the vasorelaxant activity. | 1999 | Journal 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. |
AID1683975 | Inhibition 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 | |||
AID205267 | Inhibition 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 | 1985 | Journal 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. |
AID389397 | Reversal 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 test | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Synergistic interaction between p-glycoprotein modulators and epirubicine on resistant cancer cells. |
AID1526015 | Half life in mouse liver microsomes | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases. |
AID1273402 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 8 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1183278 | Permeability of the compound by PAMPA | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies. |
AID350216 | Dissociation constant, pKa of the compound | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
AID1918143 | Inhibition 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 | |||
AID379725 | Reversal 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 control | 2006 | Journal of natural products, Feb, Volume: 69, Issue:2 | Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii. |
AID1215179 | Intrinsic 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 NADPH | 2011 | Drug 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. |
AID1530089 | Reversal 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%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID1750904 | Reversal 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 | |||
AID1129439 | Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM in presence of NADPH | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID562100 | Chemosensitization of desethylamodiaquin against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid. |
AID1299183 | Inhibition 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 control | 2016 | Bioorganic & 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. |
AID755311 | Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 0.5 uM after 2 hrs by microplate fluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs. |
AID1296093 | Inhibition 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 fluorimetri | 2016 | Journal 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 |
AID682516 | Induction of ATPase activity of human His10-tagged P-gp expressed in BHK cells assessed as inorganic phosphate release after 30 mins by Michaelis-Menten analysis | 2012 | Journal 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). |
AID1207717 | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID350525 | Induction of human histidine10-tagged MDR1 ATPase activity expressed in BHK cells relative to basal activity | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity. |
AID1155077 | Inhibition 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 control | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1704101 | Reversal 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) | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
AID1207722 | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID331354 | Antitumor activity against human K562/A02 cells xenografted in nude mouse at 8 mg/kg | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer. |
AID656826 | Growth inhibition of human K562 cells at 10 uM after 72 hrs by MTS assay | 2012 | Bioorganic & 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. |
AID1228911 | Selectivity 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 resistance | 2015 | Journal 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. |
AID1275770 | Inhibition 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 uM | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID1353450 | Inhibition 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 a | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents. |
AID81855 | Inhibitory concentration of vinblastine against the MDR resistant cell line HCT116/VM46 in the presence of 1 mM of the compound | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10 | Multidrug resistance reversal activity of key ningalin analogues. |
AID379772 | Reversal 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 method | 1999 | Journal of natural products, May, Volume: 62, Issue:5 | Sesquiterpene esters from Celastrus orbiculatus and their structure-activity relationship on the modulation of multidrug resistance. |
AID1225494 | Inhibition 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%) | 2015 | Journal 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. |
AID1502767 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1215174 | Drug metabolism in Sprague-Dawley rat intestinal microsomes assessed as CYP3A-mediated formation of norverapamil by HPLC analysis in presence of NADPH | 2011 | Drug 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. |
AID1215183 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID1565857 | Ratio 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 method | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers. |
AID1502824 | Inhibition 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 az | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1888878 | Inhibition 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 spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID1833350 | Reversal 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 | |||
AID1906056 | Reversal fold, ratio of ADR IC50 for reversal of multidrug resistance in human MCF7/ADR cells over IC50 of ADR in presence of test compound | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. |
AID1321569 | Inhibition 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 cytometry | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance. |
AID1878311 | Inhibition of P-gp mediated doxorubicin resistance in human SW620/AD300 cells overexpressing P-gp measured after 48 hrs by MTT assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2 | Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived |
AID1180211 | Inhibition of L-type calcium channel in endothelium-intact Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID1228906 | Modulation 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 cell | 2015 | Journal 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. |
AID1893724 | Metabolic 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 | |||
AID1603227 | Permeability of the compound assessed as molar fraction in acceptor well at 0.5 mM measured after 16 hrs by PAMPA | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID1163835 | Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | Polyoxypregnane steroids from the stems of Marsdenia tenacissima. |
AID368391 | Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID492328 | Inhibition of BCRP expressed in human EPG-257RNOV cells at 1 uM relative to control | 2010 | Bioorganic & 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. |
AID1502823 | Inhibition 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 az | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1878313 | Fold 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 IC50 | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2 | Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived |
AID1502791 | Inhibition 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 er | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID165537 | Inhibition of [Ca2+] uptake in rabbit aorta, K+. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID1190827 | Cytotoxicity against human KB/VCR cells assessed as vincristine IC50 at 25 uM after 72 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Multidrug resistance-reversal effects of resin glycosides from Dichondra repens. |
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AID714420 | Reversal of P-gp-mediated mitoxantrone-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
AID1502841 | Inhibition 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 ciprofl | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1426677 | Effect on rhodamine123 accumulation in human K562 cells at 0.33 to 10 uM measured after 1 hr by flow cytometry | 2017 | Journal 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. |
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AID193032 | Antihypertensive 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) | 1987 | Journal 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. |
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AID1174945 | Resistance 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 | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID313272 | Inhibition of P-glycoprotein in MDR human KBChR-8-5 cells assessed as uptake of vinblastin relative to control | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells. |
AID331368 | Toxicity in Sprague-Dawley rat assessed as ventricular sustained tachycardia by measuring aconitine nitrate level at 2 mg.kg, iv by echocardiography | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer. |
AID611696 | Inhibition 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 control | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6 | Jatrophane diterpenes from Euphorbia esula as antiproliferative agents and potent chemosensitizers to overcome multidrug resistance. |
AID669859 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID1758183 | Antiproliferative activity against human MCF7 cells assessed as inhibition rate at 10 uM incubated for 48 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell. |
AID1813141 | Inhibition 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID427724 | Reversal 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 control | 2009 | Journal 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. |
AID1502893 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1064667 | Inhibition 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 assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication. |
AID714425 | Increase in human P-gp ATPase activity at 200 uM by luciferase assay relative to basal level | 2012 | Journal 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. |
AID1283423 | Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in vinblastine IC50 at 10 uM by MTT assay | 2016 | Journal 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. |
AID717464 | Potentiation 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 control | 2012 | Bioorganic & 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. |
AID1368939 | Inhibition 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 control | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2 | Monoterpene indole alkaloid azine derivatives as MDR reversal agents. |
AID1502755 | Inhibition 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 relativ | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID368392 | Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID1273454 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 256 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1307806 | Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension at 10'-5 M | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
AID1568822 | Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
AID1235733 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1273457 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 64 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
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AID26362 | Ionization constant (pKa) | 2004 | Journal 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. |
AID351908 | Chemosensitizing 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 assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1673435 | Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2019 | Bioorganic & 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. |
AID1459764 | Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of vincristine-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID455727 | Reversal 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 cytometry | 2009 | Bioorganic & 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. |
AID47004 | Compound (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 vinblastine | 2000 | Bioorganic & 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. |
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AID469403 | Permeability across PAMPA membrane | 2009 | Journal 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. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID672543 | Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis | 2012 | Journal 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. |
AID683267 | Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as vincristine-induced cytotoxicity at 10 uM after 72 hrs by SRB assay | 2012 | Journal 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. |
AID664486 | Intrinsic clearance in human liver microsomes assessed per mg of protein | 2012 | Journal 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. |
AID1514557 | Cytotoxicity against human A2780/TAX cells assessed as survival at 10 uM after 48 hrs by MTT assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID154133 | Multidrug-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 vincristine | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents. |
AID1235768 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID76005 | Compound was tested in vitro for chronotropic activity on isolated atria preparations of guinea pig at 10E-6 M concentration | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Verapamil analogues with restricted molecular flexibility. |
AID1459774 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1708807 | Permeability of compound in PBS/EtOH buffer (70:30) at 25 ug/ml incubated for 16 hrs by UV plate reader based PAMPA-BBB | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors. |
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AID74046 | Negative chronotropic activity was calculated from log concentration/response curves | 1993 | Journal 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. |
AID656825 | Growth inhibition of human K562/A02 cells at 10 uM after 72 hrs by MTS assay | 2012 | Bioorganic & 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. |
AID395103 | Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6 | Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators. |
AID143482 | Inhibitory activity when combined with taxol (nM) in NCI/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1514561 | Potentiation 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) | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID1334754 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay | 2017 | Bioorganic & 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 papillary | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID1374473 | Half life in human liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID142787 | Ability to dissociate radioligand [3H]NMS from muscarinic acetylcholine receptor M2 of porcine heart | 2003 | Journal 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. |
AID1491366 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies. |
AID619532 | Inhibition 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 assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes. |
AID75204 | Percent inhibition of [Ca2+] induced contraction on K+ depolarized guinea pig aortic strips at 5-10e4 M concentration | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Verapamil analogues with restricted molecular flexibility. |
AID48348 | [Ca2+] antagonistic activity on [Ca2+] current in cat ventricular trabeculae | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID43874 | The percentage uptake of [3H]daunomycin in resistant CCRF-CEM vcr 100 cells to sensitive CCRF-CEM cells in presence of the compound. | 1995 | Journal 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. |
AID680500 | TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical)(Doxorubicin: 3 uM, Verapamil: 20 uM) in MDR1-expressing LLC-PK1 cells | 2000 | European 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. |
AID1168902 | Modulation 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 analysis | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators. |
AID1502754 | Inhibition 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 relativ | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1557184 | Permeability of the compound at 25 ug/ml by PAMPA-BBB assay | 2019 | Bioorganic & 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. |
AID762417 | Antimicrobial activity against Mycobacterium smegmatis MC2 155 ATCC 700084 after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 7-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155. |
AID94173 | Percent of cell viability remaining after incubating the cells with the modulator alone | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID1174964 | Reversal 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 assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID1833383 | Inhibition of human CYP3A4 at 3.3 uM preincubated with compound followed by substrate and NADP addition by fluorescence assay | |||
AID80295 | Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.003 mg/mL concentration | 1992 | Journal 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. |
AID1460714 | Reversal 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 assay | 2017 | Journal of natural products, 04-28, Volume: 80, Issue:4 | Isolation, Structure Elucidation, and Absolute Configuration of Syncarpic Acid-Conjugated Terpenoids from Rhodomyrtus tomentosa. |
AID1604716 | Stability in human plasma assessed as half life at 5 uM at 37 degC measured up to 250 mins by LC-MS analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID230143 | The 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. | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists. |
AID624626 | Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID1509218 | Otoprotective 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 control | 2019 | Journal 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. |
AID427814 | Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as inhibition of calcium uptake | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis. |
AID307746 | Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 0.2 uM | 2007 | Bioorganic & 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. |
AID368383 | Intrinsic cytotoxicity against human doxorubicin-sensitive K562 cells at 3 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID310120 | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
AID1418889 | Inhibition 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 cisplatin | 2018 | Bioorganic & 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). |
AID1324014 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB method | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease. |
AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug 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. |
AID1904131 | Reversal 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 assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID243043 | Ratio of maximum velocity to that of Km value was determined by P-glycoprotein | 2005 | Bioorganic & 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. |
AID1623664 | Intrinsic clearance in mouse microsomes | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID681144 | TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells | 2003 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 305, Issue:1 | Inhibition of P-glycoprotein by newer antidepressants. |
AID1435956 | Intrinsic clearance in human liver microsomes after 10 to 60 mins in absence of NADPH by LC/MS/MS analysis | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action. |
AID562107 | Chemosensitization of methotrexate against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid. |
AID606417 | Vasorelaxant activity in Sprague-Dawley rat langendorff perfused thoracic aorta assessed as inhibition of phenylephrine-induced vasoconstriction at 10'-6 M relative to control | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5 | Lathyrane diterpenoids from the roots of Euphorbia micractina and their biological activities. |
AID307747 | Cytotoxicity against multidrug-resistant human 2780AD cells assessed as cell viability at 2 uM | 2007 | Bioorganic & 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. |
AID340720 | Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Role of the ABC transporter PRP1 (ABCC7) in pentamidine resistance in Leishmania amastigotes. |
AID1336731 | Permeability of compound at 100 ug/ml after 18 hrs by PAMPA | 2017 | Bioorganic & 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. |
AID3216 | Relative activity on the cellular accumulation of vincristine in multidrug-resistant (MDR) human ovarian cancer 2780AD cells | 1999 | Bioorganic & 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. |
AID1459755 | Potentiation of paclitaxel-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1129361 | Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | A high-throughput cell-based method to predict the unbound drug fraction in the brain. |
AID681611 | TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells | 2003 | Pharmaceutical research, Feb, Volume: 20, Issue:2 | Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. |
AID60874 | Percent inhibition of calcium-dependent potassium-polarized smooth muscle contraction in canine trachea | 1988 | Journal 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. |
AID1704100 | Reversal 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 assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
AID80296 | Inhibitory activity on atrial rate in isolated Guinea pig right atrea at 0.01 mg/mL concentration | 1992 | Journal 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. |
AID154221 | Percent of cell viability of P388/VCR-20 murine leukemia cells remaining after inoculation with the modulator alone | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | New purines and purine analogs as modulators of multidrug resistance. |
AID1502898 | Inhibition 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/ml | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1878312 | Inhibition of P-gp mediated doxorubicin resistance in human SW620/AD300 cells overexpressing P-gp in presence of doxorubicin measured after 52 hrs by MTT assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2 | Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived |
AID313274 | Displacement of [3H]azidopine from human P-glycoprotein in KB-Vi cells | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells. |
AID486955 | Inhibition of ABCB1 efflux pump-mediated rhodamine 123 uptake expressed in mouse L5178Y cells assessed as fluorescence activity ratio at 1 uM | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators. |
AID664602 | Inhibition 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 control | 2012 | Bioorganic & 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. |
AID233362 | modulation factor: IC50 (uM) | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3 | Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships. |
AID1426678 | Effect 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) | 2017 | Journal 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. |
AID1486973 | Inhibition 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) | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID102844 | Ability to reverse the multidrug resistance (MDR) of mouse Lymphoma cells, FL-1at 5 ug/mL | 2002 | Journal 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. |
AID1215180 | Intrinsic 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 NADPH | 2011 | Drug 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. |
AID1338178 | Inhibition 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 alone | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID1750928 | Inhibition 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 | |||
AID1459747 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1481888 | Inhibition 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 assay | 2017 | Journal 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. |
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AID1235721 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID78278 | Effect on force of atrial contractions induced by PTX-B in guinea pig | 1985 | Journal 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 |
AID1365724 | Intrinsic clearance in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
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AID1215136 | Decrease of CYP3A2 level in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat duodenum by Western blot analysis relative to wild type rat | 2011 | Drug 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. |
AID1459769 | Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID714421 | Reversal of P-gp-mediated daunorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
AID1180201 | Inhibition 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 control | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID105424 | Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells. | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
AID1683988 | Inhibition 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 | |||
AID368399 | Intrinsic cytotoxicity against human doxorubicin-resistant K562 cells expressing Pgp at 1.6 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID609330 | Reversal 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 4 | 2011 | Bioorganic & 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. |
AID159174 | Percent reversal against Plasmodium falciparum W2 at 1 uM DEEA | 2002 | Journal 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. |
AID680499 | TP_TRANSPORTER: inhibition of Fluorescein-Colchicine transport (FL-Colchicin: 0.3 uM, Verapamil: 10 uM) in membranes from CEM/VLB100 cells | 1999 | Analytical 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. |
AID1174956 | Resistance 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 compound | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID1273419 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 8 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID682288 | TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, Verapamil: 500 uM) in OCTN2-expressing HEK293 cells | 1999 | The 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. |
AID1418880 | Potentiation 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 cisplatin | 2018 | Bioorganic & 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). |
AID1062337 | Induction of doxorubicin accumulation in human MDA435/LCC6 cells at 1 uM after 150 mins by spectrofluorometric analysis | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID492327 | Inhibition of BCRP expressed in human EPG-257RNOV cells at 0.1 uM relative to control | 2010 | Bioorganic & 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. |
AID1352065 | Inhibition 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 alone | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and biological evaluation of bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potential P-glycoprotein and tumor metastasis inhibitors. |
AID551807 | Inhibition 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 assay | 2011 | Bioorganic & 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. |
AID121700 | Ratio 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. | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | New purines and purine analogs as modulators of multidrug resistance. |
AID283000 | Reversal of P-gp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as increase in nuclear pirarubicin concentration | 2005 | Journal 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. |
AID318686 | Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of vincristine by MTS assay | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Synthesis of curcumin mimics with multidrug resistance reversal activities. |
AID1502710 | Antimycobacterial activity against Mycobacterium avium isolate MAV1 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID680007 | TP_TRANSPORTER: inhibition of Fexofenadine uptake (Fexofenadine: 2 uM, Verapamil: 100 uM) in Xenopus laevis oocytes | 1999 | Drug 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. |
AID1129448 | Half life in mouse microsomes at 1 uM | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1628220 | Inhibition of P-gp in human A549/CDDP cells assessed as accumulation of rhodamine 123 at 1.2 uM by flow cytometry | 2016 | Journal 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. |
AID354662 | Inhibition of p-glycoprotein expressing human MCF7 cells assessed as [3H]vinblastine accumulation | 1996 | Journal of natural products, Jun, Volume: 59, Issue:6 | Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A. |
AID679127 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells | 2000 | The 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. |
AID288564 | Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay | 2007 | Journal of natural products, Jun, Volume: 70, Issue:6 | Reversal of P-glycoprotein-mediated multidrug resistance by sipholane triterpenoids. |
AID1155066 | Inhibition 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 hrs | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1243598 | Inhibition 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) | 2015 | Journal 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. |
AID1458340 | Inhibition 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 time | 2017 | Journal 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. |
AID67781 | Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0 | 1999 | Bioorganic & medicinal chemistry letters, Feb-22, Volume: 9, Issue:4 | Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives. |
AID1888850 | Inhibition 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 alone | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1275769 | Inhibition 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 uM | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID1365650 | Permeability of the compound at pH 7.4 by BBB-PAMPA | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis, and evaluation of salicyladimine derivatives as multitarget-directed ligands against Alzheimer's disease. |
AID455723 | Reversal 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 test | 2009 | Bioorganic & 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. |
AID1418859 | Potentiation 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 alone | 2018 | Bioorganic & 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). |
AID1179311 | Inhibition of multidrug resistance efflux pump Rv1258c in Mycobacterium tuberculosis H37Rv assessed as potentiation of rifampicin-induced antimycobacterial activity by MABA method based Chequerboard synergy assay | 2014 | Bioorganic & 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. |
AID90145 | To 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 used | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID80742 | Evaluated for decrease in maximal driving frequency in isolated guinea pig atria | 1980 | Journal 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. |
AID1338181 | Inhibition 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 assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID1502836 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1785063 | Reversal 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 | |||
AID1533102 | Inhibition 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 b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID1446767 | Half life in human liver microsomes in absence of NADPH by LC-MS/MS method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus. |
AID1903293 | Potentiation 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 ) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID190398 | Antihypertensive 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) | 1987 | Journal 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. |
AID1218867 | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake | 2012 | Drug 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. |
AID578761 | Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP). |
AID695903 | Inhibition 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+ | 2012 | Bioorganic & 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. |
AID1514564 | Reversal 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 compound | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Seco-4-methyl-DCK derivatives as potent chemosensitizers. |
AID310121 | Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
AID237331 | cLogD was determined | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22 | Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. |
AID630754 | Reversal 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 line | 2011 | Bioorganic & 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. |
AID1235752 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1502907 | Inhibition 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 relati | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID408340 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Support vector machines classification of hERG liabilities based on atom types. |
AID1904127 | Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID1427562 | Metabolic stability in rat liver microsomes assessed as metabolic rate measured after 30 mins in presence of NADPH | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A |
AID1502906 | Inhibition 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 e | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID464026 | Growth inhibition in human K562 cells at 3 uM after 72 hrs by MTT assay | 2010 | Journal 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. |
AID1498593 | Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation at 10 uM after 2 hrs by flow cytometry | 2018 | Bioorganic & 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. |
AID666856 | Reversal 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 assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells. |
AID1809045 | Apparent permeability of the compound at 50 uM by PAMPA | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR. |
AID1785054 | Reversal 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 | |||
AID1673428 | Reversal 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 la | 2019 | Bioorganic & 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. |
AID562096 | Chemosensitization of chloroquine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid. |
AID656834 | Inhibition 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) | 2012 | Bioorganic & 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. |
AID726434 | Inhibition 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 control | 2013 | Bioorganic & 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. |
AID330502 | Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | 4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators. |
AID472446 | Antioxidant 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 assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives. |
AID1429864 | Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-GI assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal 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. |
AID696917 | Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 40 uM by fluorescence assay | 2011 | Journal 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. |
AID229315 | Ratio of IC50 of cytotoxicity to the IC50 of MDR- reversal for P388/VMDRC.04 cells | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents. |
AID1427527 | Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA | 2017 | Bioorganic & 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. |
AID1301015 | Inhibition 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 control | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
AID1702158 | Clearance 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 analysis | 2018 | Journal 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. |
AID1733383 | Reversal 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 control | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1169854 | Intrinsic clearance in human liver microsomes at 1 uM after 30 mins in presence of NADPH | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Structure-guided development of deoxycytidine kinase inhibitors with nanomolar affinity and improved metabolic stability. |
AID1168390 | Potentiation 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 control | 2014 | Journal of natural products, Oct-24, Volume: 77, Issue:10 | Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition. |
AID1386859 | Modulation 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_ | 2018 | Journal of natural products, 09-28, Volume: 81, Issue:9 | Terpenoids from Euphorbia pedroi as Multidrug-Resistance Reversers. |
AID1365718 | Half life in human liver S9 microsomes at 1 uM in absence of NADPH by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID379472 | Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay | 1999 | Journal of natural products, Apr, Volume: 62, Issue:4 | Pregnane glycoside multidrug-resistance modulators from Cynanchum wilfordii. |
AID1696657 | Inhibition 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 cells | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22 | N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H |
AID1439234 | Inhibition 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 cytometry | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Dregamine and tabernaemontanine derivatives as ABCB1 modulators on resistant cancer cells. |
AID1207724 | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID101593 | Inhibitory activity when combined with cisplatin (uM) in MCF-7 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1288624 | Reversal 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) | 2016 | Bioorganic & 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. |
AID1215161 | AUC (0 to 300 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Drug 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. |
AID576612 | Inhibition of human ERG | 2011 | European 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. |
AID401284 | Displacement of N-(p-azido-[3-125I]salicyl)-N'-beta-aminoethylvindesine from P-glycoprotein at 12.4 uM | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
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AID1315280 | Potentiation of vinblastin-induced cytotoxicity against human CEM cells at 5 uM after 72 hrs by Alamar blue assay relative to control | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis. |
AID1464385 | Resistance 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) | 2017 | Bioorganic & 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. |
AID25870 | Tested for the dissociation constant of the compound | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Accumulation of drugs by guinea pig isolated atria. Quantitative correlations. |
AID1221960 | Apparent 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 LY335979 | 2011 | Drug 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. |
AID728951 | Myorelaxant activity in albino rat aorta rings assessed as relaxation of 80 mM KCl-induced contraction of aorta rings | 2013 | Journal 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. |
AID464022 | Inhibition 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 | 2010 | Journal 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. |
AID1350735 | Inhibition 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 alone | 2018 | Journal 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. |
AID1374471 | Half life in rat liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID1180202 | Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 30 mM K+-induced contraction | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID1833379 | Inhibition 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 | |||
AID230387 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1517902 | Reversal 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 analysis | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1141747 | Myorelaxant 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 glibenclamide | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Influence 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? |
AID1603229 | n-Octanol/water partition coefficient, log P of the compound by UV-RP-HPLC analysis | 2019 | Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8 | Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycin A |
AID1181955 | Stability in human liver microsomes assessed as metabolite formation at 8 uM at 37 degC in presence of NADPH and glucose-6-phosphate | 2014 | Bioorganic & 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. |
AID1407666 | Substrate 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 control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
AID1197237 | Reversal 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 | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological profile of new inhibitors of multidrug resistance associated proteins carrying a polycyclic scaffold. |
AID368552 | Reversal 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 uM | 2009 | Journal 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. |
AID377772 | Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 1 ug/mL after 2 hrs relative to control | 2005 | Journal of natural products, Apr, Volume: 68, Issue:4 | Taxoids and abietanes from callus cultures of Taxus cuspidata. |
AID1055546 | Inhibition of side population in human HT-29 cells at 100 uM after 90 mins using vybrant dyecycle violet staining by FACS analysis | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis and anticancer potential of certain novel 2-oxo-N'-(2-oxoindolin-3-ylidene)-2H-chromene-3-carbohydrazides. |
AID1472781 | Potentiation 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 assay | 2018 | Journal 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. |
AID1228909 | Modulation 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 assay | 2015 | Journal 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. |
AID264309 | Ratio of rhodamine123 uptake in MDR1 transfected cells vs parental L5178Y cells at 11 uM | 2006 | Journal 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. |
AID1631492 | Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | Vobatensines A-F, Cytotoxic Iboga-Vobasine Bisindoles from Tabernaemontana corymbosa. |
AID449585 | Reversal index, Taxol IC50 to compound and taxol IC50 for inhibition of ABCB1 in human MES-SA/Dx5 cells at 5 uM | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives. |
AID1900353 | Stability in pooled human liver microsomes assessed as half life at 8 uM in presence of NADPH measured upto 60 mins by HPLC-MS analysis | 2022 | Journal 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. |
AID1443980 | Inhibition 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]-tauroch | 2010 | Toxicological 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. |
AID1853712 | Metabolic 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 analysis | 2021 | RSC 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. |
AID321880 | Activation of human Pgp ATPase in human Caco-2 cells at 100 uM | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. |
AID656835 | Inhibition 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 = 35 | 2012 | Bioorganic & 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. |
AID1813136 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1374215 | Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & 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. |
AID324484 | Increase 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 control | 2007 | Proceedings 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. |
AID1235692 | Inhibition 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 fluorometry | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1348613 | Metabolic stability in human liver microsomes at 5 uM after 120 mins in absence of NADPH by UPLC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation. |
AID1379031 | Effective permeability of compound at 50 ug/mL after 16 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
AID1502706 | Antimycobacterial activity against Mycobacterium avium 104 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1322435 | Inhibition 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 cytometry | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors. |
AID1502825 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1485936 | Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease. |
AID90140 | Ratio of effect of compound on DOX accumulation (antiPgp activity) to its intrinsic cellular toxicity; | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID1211294 | Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug 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. |
AID1530096 | Cell 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%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID1623672 | Protein binding in mouse plasma | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID209802 | Inhibitory activity when combined with cisplatin (uM) in T24 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID230561 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID455717 | Reversal 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 cytometry | 2009 | Bioorganic & 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. |
AID1079936 | Choleostatic 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] | |||
AID1391799 | Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors. |
AID1502741 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID436087 | Antioxidant activity against ferrous ion-induced lipid peroxidation in liver microsomes assessed as inhibition rate at 10 uM by TBA method in presence of cysteine | 2008 | Journal 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. |
AID1163834 | Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | Polyoxypregnane steroids from the stems of Marsdenia tenacissima. |
AID492326 | Inhibition of MRP2 expressed in human A2780 cells at 10 uM relative to control | 2010 | Bioorganic & 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. |
AID1483832 | Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ. |
AID1481894 | Substrate 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 control | 2017 | Journal 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. |
AID679063 | TP_TRANSPORTER: transepithelial transport of Verapamil at a concentration of 0.1 uM in Caco-2 cells | 2003 | Pharmaceutical 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. |
AID1739804 | Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1311930 | Permeability of the compound at 50 ug/ml in 70:30 PBS:EtOH by PAMPA-BBB assay | 2016 | Bioorganic & 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. |
AID1502918 | Inhibition 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 relati | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1352545 | Cytotoxicity against HEK293 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1530094 | Reversal 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 alone | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID185796 | Compound 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. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors. |
AID1647653 | Reversal 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 No | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, |
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AID209804 | Inhibitory activity when combined with vinblastine in T24 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID75200 | Coronary perfusion pressure of isolated guinea pig heart at dose 0.05 (ug/heart) | 1985 | Journal 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. |
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AID78281 | Effect on rate of atrial contractions induced by PTX-B in guinea pig (control value) | 1985 | Journal 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 |
AID326367 | Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. |
AID230391 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1362740 | Inhibition 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 analysis | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria. |
AID1315281 | Inhibition 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 control | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis. |
AID437142 | Reversal of P-gp-mediated multidrug resistance in human 2780AD cells assessed as vincristine accumulation | 2009 | European 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. |
AID444054 | Oral bioavailability in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1502810 | Inhibition 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 azithromy | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1275780 | Inhibition of voltage-gated calcium channel in Plasmodium flaciparum Dd2 cells assessed as reversal of of choloroquine resistance at 0.8 uM relative to control | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID1459753 | Potentiation of vincristine-induced cytotoxicity against human Flp-In-293 cells at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1502735 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID722217 | Cytotoxicity against human doxorubicin-resistant K562 cells at 1 uM after 72 hrs by MTT assay | 2013 | Bioorganic & 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). |
AID82355 | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | 2002 | Journal 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. |
AID1739836 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1769162 | Inhibition 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 analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
AID1502909 | Inhibition 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 relati | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1312953 | Aqueous solubility of the compound in PBS after 2 hrs by turbidity assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties. |
AID165790 | Inhibition of [Ca2+] influx in response to a stimulus of KCL (60 uM) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
AID1215350 | Time 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 s | 2011 | Drug 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. |
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AID1733375 | Reversal 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) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
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AID1439230 | Inhibition 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 (Rv | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Dregamine and tabernaemontanine derivatives as ABCB1 modulators on resistant cancer cells. |
AID1576578 | Fraction absorbed of the compound by PAMPA | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling. |
AID762408 | Antimicrobial activity against Mycobacterium smegmatis MC2 155 ATCC 700084 at 80 mg/L after 72 hrs by MTT assay in presence of EtBr | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 7-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155. |
AID1357219 | Half life in human liver microsomes in presence of NADPH regeneration system | 2018 | Journal 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. |
AID1459763 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1739846 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1336844 | Inhibition 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 control | 2017 | Bioorganic & 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. |
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AID1517912 | Stimulation of P-gp ATPase activity (unknown origin) at 10 uM incubated for 40 mins by P-gp-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1352674 | Effective permeability at 25 ug/ml after 16 hrs by PAMPA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
AID1604715 | Stability in human plasma assessed as elimination rate at 5 uM at 37 degC measured up to 250 mins by LC-MS analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
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AID1822203 | Inhibition 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 alone | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore. |
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AID1702156 | Inhibition of human ERG by fluorescence polarization assay | 2018 | Journal 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. |
AID1079931 | Moderate 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] | |||
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AID1740453 | Metabolic stability in human hepatocytes assessed as hepatic extraction ratio at 1 uM up to 120 mins by HPLC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID1739852 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1502905 | Inhibition 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 e | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
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AID762411 | Inhibition 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 control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 7-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155. |
AID1904188 | Inhibition 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 analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
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AID230562 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
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AID1305710 | Half life in human liver microsomes at 0.1 uM | 2016 | Bioorganic & 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. |
AID295524 | Growth inhibition of human CEM/VLB500 cells after 3 days by resazurin assay | 2007 | Bioorganic & 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). |
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AID1764399 | Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
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AID502259 | Inhibition of MRP1 expressed in hamster BHK21 cells assessed as reduction of GSH efflux at 5 uM after 20 mins | 2010 | Bioorganic & 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. |
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AID322363 | Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein. |
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AID1833347 | Reversal 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) | |||
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AID230551 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID48973 | Antagonistic activity against K+ induced responses in canine trachea. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID1215146 | AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv | 2011 | Drug 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. |
AID78280 | Effect on rate of atrial contractions induced by PTX-B in guinea pig | 1985 | Journal 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 |
AID1750926 | Inhibition 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 | |||
AID1079933 | Acute 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 | |||
AID310897 | Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing half maximal increase in nuclear concentration of pirarubicin | 2007 | Journal 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. |
AID1174978 | Inhibition 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 control | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID321879 | Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. |
AID1221982 | Fraction absorbed in human | 2011 | Drug 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. |
AID1520013 | Half life in rat liver microsomes up to 60 mins by HPLC-LC/MS analysis | |||
AID615734 | Reversal 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 assay | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides. |
AID331508 | Lipophilicity, log P of the compound | 2008 | Bioorganic & 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. |
AID1502765 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID354669 | Inhibition of MRP expressed in human MCF7/VP cells assessed as increase in vincristine-induced cytotoxicity at 20 uM after 48 hrs by SRB binding assay | 1996 | Journal of natural products, Jun, Volume: 59, Issue:6 | Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A. |
AID1569057 | Intrinsic clearance in CD-1 mouse liver microsomes in presence of NADPH regenerating system measured up to 4 hrs by UPLC-MS analysis | |||
AID1352559 | Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Lineweaver-Burk plot analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1738694 | Inhibition 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 f | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Novel curcumin derivatives as P-glycoprotein inhibitors: Molecular modeling, synthesis and sensitization of multidrug resistant cells to doxorubicin. |
AID202471 | In vitro concentration required to inhibit tumor activity on subclone of human colon carcinoma cells (S1-B1-20) resistant to bisantrene | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Novel multidrug resistance reversal agents. |
AID1533101 | Inhibition 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 b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID1602186 | Half life in mouse liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | 2019 | Journal 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. |
AID656821 | Induction 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 control | 2012 | Bioorganic & 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. |
AID53611 | Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 10 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1273396 | Cytotoxicity against human MDM assessed as cell viability after 3 days by Alamar blue dye-based fluorocytometric analysis relative to control | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID165539 | Inhibition of contraction in rabbit aorta, K+. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID1625122 | Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & 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. |
AID1903289 | Potentiation 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 ) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID701948 | Inhibition of human recombinant P-glycoprotein after 40 mins by Pgp-Glo assay | 2012 | Journal 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. |
AID1502843 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID165788 | In vitro inhibition of development of isometric tension, in response to norepinephrine (NE, 10 uM) in rabbit aorta | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
AID1211295 | Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug 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. |
AID1733393 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID714431 | Reversal of P-gp-mediated paclitaxel-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1739807 | Cytotoxicity against human KB-VIN cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1631736 | Reversal 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 control | 2016 | Journal 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. |
AID1235734 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID272485 | Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay | 2006 | Journal 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. |
AID70546 | In vitro hemolytic concentration on uninfected erythrocytes. | 2002 | Journal 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. |
AID1530090 | Reversal 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%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID358657 | Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL | 2001 | Journal of natural products, Dec, Volume: 64, Issue:12 | Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei. |
AID1903295 | Potentiation 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 assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID94171 | Compound 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 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID1286274 | Cytotoxicity against human vincristine-sensitive KB cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal 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. |
AID1246314 | Plasma protein binding in mouse | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID1275779 | Inhibition of voltage-gated calcium channel in Wistar rat synaptoneurosomes after 30 mins by fluorescent ratiometric indicator method | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
AID228176 | Inhibition of tetraethylammonium chloride(TEA)-induced acetylcholine hyperactivity in rat tracheal segments by the compound. | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | New N-(pyridin-4-yl)-(indol-3-yl)acetamides and propanamides as antiallergic agents. |
AID1173449 | Effective permeability of the compound by PAMPA assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23 | Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID252995 | Toxicity of compound (1 uM) is expressed as percentage of cell growth inhibition with respect to the control | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13 | Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis. |
AID1502896 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1459748 | Cytotoxicity against human Flp-In-293 cells assessed as reduction in cell viability by SRB assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1502768 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1464386 | Resistance 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) | 2017 | Bioorganic & 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. |
AID1739806 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID82676 | Inhibitory 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 drug | 1998 | Journal 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. |
AID1502726 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502831 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID604022 | Fraction 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 method | 2009 | Journal 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. |
AID1502916 | Inhibition 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 rela | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID80725 | Inhibitory concentration required to block Ca+2 induced contraction of K+ depolarized guinea pig aorta | 1990 | Journal 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. |
AID1496040 | Effective permeability of the compound in PBS/EtOH at 50 ug/mL after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11 | Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold. |
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AID1371140 | Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS analysis | 2017 | Journal 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). |
AID401285 | Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as increase in rhodamine 6G accumulation | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein. |
AID1704099 | Reversal 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) | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
AID1702161 | Drug 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 analysis | 2018 | Journal 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. |
AID1739826 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID1750897 | Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay | |||
AID1235736 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID537733 | Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u | 2010 | European 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. |
AID1400033 | Half life in Sprague-Dawley rat liver microsomes at 500 ng/ml preincubated for 5 mins followed by NADPH addition by C-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | An antimycobacterial pleuromutilin analogue effective against dormant bacilli. |
AID615730 | Reversal 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 control | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides. |
AID1733388 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1330750 | Effective permeability of the compound after 18 hrs by PAMPA | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
AID1776728 | Inhibition of Multidrug resistance efflux pump in Mycobacterium tuberculosis H37Rv assessed as measuring relative final fluorescence at 128 ug/ml measured by ethidium bromide accumulation assay | 2021 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 42 | 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis. |
AID76860 | Percent inhibition of calcium-induced contraction on K+ -depolarized guinea pig aortic strips at 10 e-4 M | 1993 | Journal 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. |
AID1683978 | Inhibition 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 | |||
AID1377031 | Inhibition 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 control | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6 | Terpenoids from Euphorbia soongarica and Their Multidrug Resistance Reversal Activity. |
AID1418877 | Potentiation 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 doxorubicin | 2018 | Bioorganic & 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). |
AID1338179 | Cytotoxicity against mouse L929 cells measured after 3 days by MTS assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID1336842 | Inhibition 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 control | 2017 | Bioorganic & 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. |
AID1383661 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
AID1480943 | Permeability of the compound at pH 7.4 at 5 mg/ml after 18 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Enzymatic 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. |
AID1239241 | Inhibition 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 control | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors. |
AID1683962 | Inhibition of CYP3A4 in in human liver microsomes at 30 uM incubated for 10 mins in presence of CYP3A4 substrate/NADP+ by fluorescence based assay | |||
AID26798 | Partition coefficient (logP) | 1996 | Journal 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. |
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AID681614 | TP_TRANSPORTER: inhibition of Saquinavir transepithelial transport (basal to apical) in Caco-2 cells | 1999 | British 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. |
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AID1907126 | Stability in mouse liver microsomes assessed as half life measured upto 60 mins in presence of NADPH by LC-MS/MS analysis | 2022 | Journal 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. |
AID1418874 | Potentiation 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 paclitaxel | 2018 | Bioorganic & 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). |
AID714200 | Inhibition 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 cells | 2012 | Journal 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. |
AID1254933 | Half life in human liver S9 microsomes in absence of NADPH by LC-MS/MS method | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents. |
AID1502895 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1851935 | Metabolic stability in human microsomes assessed as compound remaining measured after 30 mins | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
AID762412 | Inhibition 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 control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 7-Hydroxy-(E)-3-phenylmethylene-chroman-4-one analogues as efflux pump inhibitors against Mycobacterium smegmatis mc² 155. |
AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID350540 | Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity. |
AID1273468 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 64 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1502757 | Inhibition 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 relativ | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID683399 | Inhibition 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 control | 2012 | Journal 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. |
AID150753 | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID1595492 | Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as reduction of ATP consumption at 1 uM incubated for 2 hrs by luminescence assay | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Modulation 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. |
AID1352546 | Therapeutic 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 cytotoxicity | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID653302 | Cytotoxicity against human K562 cells assessed as cell killing at 5 uM after 72 hrs by MTS assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1478796 | Permeability of the compound by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
AID389758 | Octanol-water partition coefficient, log P after 5 hrs by shake flask method | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells. |
AID680084 | TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Azidopine: 0.2 uM, Verapamil: 1 uM) in membranes from KB/V20C cells | 1993 | Biochemical pharmacology, Jan-26, Volume: 45, Issue:2 | Terfenadine (Seldane): a new drug for restoring sensitivity to multidrug resistant cancer cells. |
AID509768 | Reversal 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 assay | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Bisbibenzyl derivatives sensitize vincristine-resistant KB/VCR cells to chemotherapeutic agents by retarding P-gp activity. |
AID406532 | Inhibition of NorA efflux pump in Staphylococcus aureus 1199B assessed as fold reduction of ciprofloxacin MIC at 50 ug/ml | 2008 | Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13 | Citral derived amides as potent bacterial NorA efflux pump inhibitors. |
AID233360 | modulation factor: IC50 (uM) | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3 | Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships. |
AID1502819 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1271449 | Vasodilator activity in Sprague-Dawley rat mesentric artery assessed as reduction in of K+-induced contraction | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and fluorescent study of 5-phenyl furocoumarin derivatives as vasodilatory agents. |
AID1352543 | Inhibition 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 control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1502865 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1683973 | Inhibition 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 | |||
AID540210 | Clearance in human after iv administration | 2008 | Drug 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. |
AID1062342 | Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID103927 | Inhibitory 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 drug | 1998 | Journal 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. |
AID1759974 | Apparent permeability across apical to basolateral in human Caco2 cells by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
AID551808 | Inhibition 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 assay | 2011 | Bioorganic & 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. |
AID679465 | TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells | 2001 | Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 29, Issue:8 | Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein. |
AID43402 | Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies. | 1996 | Journal 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. |
AID1211293 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method | 2011 | Drug 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. |
AID683264 | Inhibition 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 control | 2012 | Journal 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. |
AID1235747 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1530095 | Cell 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%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID1411807 | Selectivity 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 | 2017 | MedChemComm, Dec-01, Volume: 8, Issue:12 | N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry. |
AID1879297 | Permeability of compound by PAMPA-BBB assay | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | Design, 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. |
AID1459754 | Potentiation of vincristine-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID243188 | Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state | 2005 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6 | A two-state homology model of the hERG K+ channel: application to ligand binding. |
AID1502722 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1168389 | Potentiation 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 control | 2014 | Journal of natural products, Oct-24, Volume: 77, Issue:10 | Identification of key structural characteristics of Schisandra chinensis lignans involved in P-glycoprotein inhibition. |
AID1196792 | Metabolic stability in human microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in presence of NADPH | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents. |
AID681130 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID1336846 | Inhibition 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 control | 2017 | Bioorganic & 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. |
AID1312933 | Intrinsic clearance in human liver microsomes measured after 10 to 60 mins in presence of NADPH by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties. |
AID674363 | Inhibition 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 assay | 2012 | Journal of natural products, Jun-22, Volume: 75, Issue:6 | Isolation and structural elucidation of cyclic tetrapeptides from Onychocola sclerotica. |
AID1502911 | Inhibition 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 rela | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1180198 | Inhibition of L-type calcium channel in endothelium-denuded Wistar rat aorta rings assessed as relaxation of 60 mM K+-induced contraction | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID1235766 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID704793 | Inhibition 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 cells | 2012 | Journal 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. |
AID1739820 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID295523 | Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay | 2007 | Bioorganic & 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). |
AID1740451 | Intrinsic clearance in human hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID1813131 | Reversal 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 control | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1228916 | Modulation 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 control | 2015 | Journal 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. |
AID635079 | Permeability of the compound after 2.5 hrs by PAMPA-BBB assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model. |
AID1436078 | Permeability of compound at 100 ug/ml after 18 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
AID1418865 | Inhibition 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 paclitaxel | 2018 | Bioorganic & 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). |
AID1709007 | Substrate 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 assay | 2021 | Journal 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. |
AID679744 | TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.0175 uM, Verapamil: 100 uM) in CEM/VBL600 cells | 1999 | Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5 | P-glycoprotein inhibition by glibenclamide and related compounds. |
AID283910 | Inhibition of P-gp mediated efflux-pump activity in human MDR1 gene transfected mouse L5178 Y cells at 10 ug/mL by rhodamine 123 accumulation test | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Apoptosis induction and modulation of P-glycoprotein mediated multidrug resistance by new macrocyclic lathyrane-type diterpenoids. |
AID510382 | Inhibition of Staphylococcus aureus 1199B norA efflux pump by spectrophotometry | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus. |
AID1918144 | Inhibition 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 | |||
AID683262 | Inhibition 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 control | 2012 | Journal 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. |
AID1321554 | Inhibition 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 286 | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance. |
AID620606 | Reversal of P-gp-mediated multidrug-resistance in adriamycin-resistant human K562/A02 cells at 10 uM after 48 hrs by MTT assay relative to adriamycin | 2011 | Bioorganic & 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. |
AID427198 | Membrane permeability dissolved in PBS/EtOH (80:20) mixture by PAMPA-BBB assay | 2009 | Journal 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. |
AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1888853 | Inhibition 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 alone | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID1888849 | Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of norfloxacin-induced antibacterial activity by measuring Norfloxacin MIC at sub MIC | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID1647652 | Reversal 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) | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, |
AID365465 | Inhibition of P-gp in human A2780 cells | 2008 | Bioorganic & 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. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1273477 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 256 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID154132 | Evaluated 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 vincristine | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents. |
AID80192 | Inhibitory activity on atrial contractility in isolated Guinea pig right atrea at 0.03 mg/mL concentration | 1992 | Journal 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. |
AID562109 | Chemosensitization of sesquiterpene dihydroartemisinin pyronaridine against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid. |
AID681146 | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells | 1998 | The 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). |
AID1207720 | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID427197 | Membrane permeability dissolved in PBS/EtOH (70:30) mixture by PAMPA-BBB assay | 2009 | Journal 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. |
AID1382494 | Intrinsic 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 analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
AID1459766 | Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of paclitaxel-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID8002 | Observed volume of distribution | 2004 | Journal 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. |
AID1174979 | Inhibition 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 control | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis and evaluation of novel triazole core based P-glycoprotein-mediated multidrug resistance reversal agents. |
AID1292330 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2016 | Bioorganic & 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. |
AID1319024 | Substrate 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 control | 2016 | Journal 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. |
AID53612 | Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 5 uM | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | New triazine derivatives as potent modulators of multidrug resistance. |
AID455714 | Reversal 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 cytometry | 2009 | Bioorganic & 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. |
AID1350758 | Inhibition 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 assay | 2018 | Journal 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. |
AID1739134 | Metabolic stability at phase 1 in human liver microsomes assessed as half life at 1 uM by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Chemical profiling of HIV-1 capsid-targeting antiviral PF74. |
AID1502913 | Inhibition 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 rela | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID399366 | Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Two pimarane diterpenoids from Ephemerantha lonchophylla and their evaluation as modulators of the multidrug resistance phenotype. |
AID1813129 | Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID1215151 | AUC (0 to 480 mins) in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat at 10 mg/kg, po | 2011 | Drug 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. |
AID1740450 | Half life in mouse hepatocytes at 1 uM up to 120 mins by HPLC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID399197 | Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 1 ug/mL after 2 hrs relative to control | 2004 | Journal of natural products, Jan, Volume: 67, Issue:1 | Production of biologically active taxoids by a callus culture of Taxus cuspidata. |
AID1675374 | Stimulation of P-gp ATPase activity (unknown origin) assessed as increase in ATP consumption at 25 uM relative to control | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Ecdysteroid Derivatives that Reverse P-Glycoprotein-Mediated Drug Resistance. |
AID1502734 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID515780 | Intrinsic solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19 | QSAR-based solubility model for drug-like compounds. |
AID327170 | Binding affinity to human serum albumin by PAMPA method | 2008 | Journal 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. |
AID1283418 | Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in daunomycin IC50 at 1 uM by MTT assay | 2016 | Journal 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. |
AID1491367 | Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies. |
AID1683981 | Reversal 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 | |||
AID1180210 | Inhibition 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 control | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Vascular L-type Ca²⁺ channel blocking activity of sulfur-containing indole alkaloids from Glycosmis petelotii. |
AID103349 | Cytotoxicity against MCF-7 breast carcinoma cells at 10 ug/mL | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists. |
AID1319976 | Permeability of the compound at 25 ug/ml at 7.4 pH after 18 hrs by PAMPA | 2016 | Bioorganic & 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. |
AID1273412 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 64 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1769133 | Inhibition 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 analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
AID1235702 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1163825 | Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | Polyoxypregnane steroids from the stems of Marsdenia tenacissima. |
AID1585800 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 3 uM after 30 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
AID696926 | Induction of human MDR1 ATPase activity assessed as inorganic phosphate production in presence of MDR1 inhibitor cyclosporin A | 2011 | Journal 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. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1273478 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as amikacin MIC at 128 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID678840 | TP_TRANSPORTER: Western blot, LS-180V | 2000 | AIDS (London, England), Jun-16, Volume: 14, Issue:9 | Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. |
AID1283415 | Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay | 2016 | Journal 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. |
AID1283421 | Inhibition of human MDR1 expressed in mouse NIH/3T3 cells assessed as reduction in vinblastine IC50 at 1 uM by MTT assay | 2016 | Journal 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. |
AID351906 | Chemosensitizing 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 assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1785082 | Effect on intracellular Rhodamine 123 accumulation in human SW620 cells at 0.5 to 2 uM incubated for 24 hrs by flow cytometry | |||
AID1888854 | Inhibition of NorA in Staphylococcus aureus 1199B assessed as potentiation of ethidium bromide-induced antibacterial activity by measuring fractional inhibitory concentration | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID231788 | Ratio of contractility to atrial rate in isolated guinea pig atria | 1980 | Journal 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. |
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AID1129440 | Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1478786 | Permeability of the compound at 200 uL after 16 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug 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. |
AID1235732 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID331359 | Inhibition of Pgp-mediated multidrug resistance activity in human MCF7/ADM cells assessed as Rh123 accumulation at 10 umol/L after 30 mins | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer. |
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AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID264306 | Inhibition of P-glycoprotein | 2006 | Journal 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. |
AID1823835 | Inhibition of hERG at 1 uM by whole-cell electrophysiological assay relative to control | |||
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1683965 | Inhibition 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%) | |||
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AID351902 | Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76I mutant Plasmodium falciparum infected in human erythrocytes by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
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AID232670 | Selectivity ratio of IC50 for [Ca2+] antagonistic activity in aorta / IC50 for suppressive effect on contractile force | 1990 | Journal 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. |
AID1530761 | Inhibition 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 method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | 1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1. |
AID1486981 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID653467 | Reversal 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 assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID77841 | Heart rate of isolated guinea pig heart at dose 5 (ug/heart) | 1985 | Journal 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. |
AID1558702 | Intrinsic clearance in rat liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis | |||
AID360080 | Cytotoxicity against hamster BHK21 cells by MTT assay | 2007 | The Journal of biological chemistry, Oct-26, Volume: 282, Issue:43 | (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1. |
AID427741 | Reversal 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 uM | 2009 | Journal 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. |
AID1703888 | Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery 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. |
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AID91481 | Binding constant against human serum albumin (HSA) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | Cheminformatic models to predict binding affinities to human serum albumin. |
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AID1502802 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID80190 | Inhibitory activity on atrial contractility in isolated Guinea pig right atrea at 0.003 mg/mL concentration | 1992 | Journal 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. |
AID513665 | Induction 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 A1 | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID1496417 | Apparent half life in human liver microsomes at 3 uM | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11 | BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. |
AID157422 | Fractional inhibitory concentration (FIC) tested against Peruvian PC49 cells, isolate from South America | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum. |
AID1764807 | Half life in human pooled liver microsomes assessed as parent compound remaining measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | 2021 | Journal 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. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
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AID1595498 | Inhibition 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 cytometry | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Modulation 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. |
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AID1163827 | Potentiation of erlotinib-induced cytotoxicity against human H460/Vbl cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | Polyoxypregnane steroids from the stems of Marsdenia tenacissima. |
AID226029 | Tested 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) | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Classification of multidrug-resistance reversal agents using structure-based descriptors and linear discriminant analysis. |
AID755315 | Inhibition of p-gp in human KB/VCR cells assessed as potentiation of vincristine-induced cytotoxicity at 5 uM after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs. |
AID368553 | Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay | 2009 | Journal 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. |
AID1517891 | Reversal 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 control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance. |
AID1557178 | Permeability of the compound at 100 ug/ml measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay | 2019 | Bioorganic & 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. |
AID1273464 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ethidium bromide MIC at 8 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID167568 | Calcium channel-blocking activity by determined by ability to antagonize calcium-induced contractions of isolated rabbit aortic strips | 1991 | Journal 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. |
AID1192730 | Permeability of the compound by PAMPA | 2015 | Bioorganic & 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. |
AID1683993 | Inhibition 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 | |||
AID653465 | Reversal 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 assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID537735 | Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u | 2010 | European 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. |
AID399198 | Reversal of multidrug resistance in human 2780AD cells assessed as [3H]vincristine accumulation at 10 ug/mL after 2 hrs relative to control | 2004 | Journal of natural products, Jan, Volume: 67, Issue:1 | Production of biologically active taxoids by a callus culture of Taxus cuspidata. |
AID427739 | Inhibition of MRP1 in human 2008/MRP1 cells by dixon plot analysis | 2009 | Journal 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. |
AID1771039 | Intrinsic clearance in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
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AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1210013 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control | 2012 | Drug 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. |
AID1391814 | Inhibition 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 b | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors. |
AID680693 | TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in the presence of Verapamil at a concentration of 100uM in LLC-GA5-COL150 cells | 2004 | British journal of pharmacology, Dec, Volume: 143, Issue:7 | Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. |
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AID230559 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1196795 | Metabolic stability in mouse microsomes assessed as compound remaining at 1 uM after 60 mins by LC/MS/MS analysis in absence of NADPH | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents. |
AID1246313 | Plasma protein binding in human | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID1486974 | Inhibition 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 alone | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID681580 | TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID1459750 | Cytotoxicity against human HeLaS3 assessed as reduction in cell viability by SRB assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1502716 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1207235 | Inhibition of hERG K channel | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID481444 | Octanol-water partition coefficient, log P of the compound | 2010 | Journal 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? |
AID271726 | Inhibition of vinblastine-induced ATPase activation in Caco-2 cells | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. |
AID1459752 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1273426 | Modulation factor, ratio of isoniazid MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 27294T at 256 ug/ml in presence of isoniazid | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1486951 | Inhibition 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) | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID1062335 | Inhibition of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of doxorubicin drug resistance relative to control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID81850 | Effect on vinblastine IC50 against MDR human carcinoma HCT116/VM46 cell line at a dose of 1 uM concentration | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10 | Multidrug resistance reversal activity of key ningalin analogues. |
AID1273498 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as ofloxacin MIC at 256 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1502797 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1313189 | Half life in human liver microsomes at 3 uM in presence of NADPH by LC-MS/MS analysis | 2016 | Bioorganic & 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. |
AID193905 | Change in arterial blood pressure was measured at 0.3 mg/kg dose(iv) in anesthetized rats | 1992 | Journal 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. |
AID680493 | TP_TRANSPORTER: inhibition of IAAP photoaffinity labelling (IAAP: 0.02 uM, Verapamil: 100-fold molar excess) in plasma membranes from CEM/VLB1.0 cells | 1997 | Biochemical pharmacology, Jan-10, Volume: 53, Issue:1 | Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. |
AID1215165 | Cmax in streptozotocin-induced diabetes mellitus model of Sprague-Dawley rat portal vein plasma at 10 mg/kg, po | 2011 | Drug 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. |
AID1899078 | Inhibition of P-gp in human KB/VCR cells assessed as increase in Rho123 accumulation at 10 uM | |||
AID1534778 | Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease. |
AID1564939 | Inhibition of P-gp efflux in human KBtax cells at 100 uM after 1 hr by flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | 4(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin. |
AID1459756 | Potentiation of paclitaxel-induced cytotoxicity against human Flp-In-293 cells at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1225503 | Cytotoxicity against mouse NIH/3T3 cells assessed as cell growth at 10 uM after 24 hrs by MTT assay | 2015 | Journal 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. |
AID1129438 | Metabolic stability in human microsomes assessed as compound remaining at 1 uM | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1502769 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID514300 | Protection of neurodegeneration in Drosophila Huntington's disease model assessed as induction autophagy at 1.25 mM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID1362737 | Inhibition 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 analysis | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Efflux pump inhibition by 11H-pyrido[2,1-b]quinazolin-11-one analogues in mycobacteria. |
AID242908 | Maximum velocity against human P-glycoprotein expressed in Sf9 cells | 2005 | Bioorganic & 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. |
AID1273410 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as rifampin MIC at 128 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1702155 | n-Octanol/water distribution coefficient, logD of the compound at pH 7.4 | 2018 | Journal 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. |
AID1530729 | Stimulation 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 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents. |
AID389764 | Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells. |
AID1589936 | Half life in human liver microsomes | 2019 | Bioorganic & 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. |
AID90133 | Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50% | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID1785066 | Reversal 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 | |||
AID74439 | Percent inhibition of calcium-induced contraction on K+ depolarized guinea pig aortic strip. | 1999 | Journal 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. |
AID714422 | Therapeutic index, ratio of IC50 for L929 cells to EC50 for reversing paclitaxel resistance in human MDA435/LCC6MDR cells | 2012 | Journal 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. |
AID1179308 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by MABA method | 2014 | Bioorganic & 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. |
AID492323 | Inhibition of Pgp expressed in mouse L5178Y cells at 1 uM relative to control | 2010 | Bioorganic & 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. |
AID389766 | Inhibition of MDR1 overexpressed in MDCK cells at 5 uM relative to LSN335984 | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells. |
AID362951 | Inhibition 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 uM | 2008 | Journal 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. |
AID680309 | TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 50 mg/L, Verapamil: 10 uM) in Hs578T-Dox cells | 1999 | Biochemical pharmacology, Dec-01, Volume: 58, Issue:11 | Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. |
AID1683952 | Potentiation 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 | |||
AID1416320 | Inhibition 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 | |||
AID1502900 | Inhibition 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/ml | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1813132 | Selectivity 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 resistance | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. |
AID332135 | Reversal 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 assay | 1997 | Journal of natural products, Nov, Volume: 60, Issue:11 | Multidrug-resistance modulators from Stephania japonica. |
AID444050 | Fraction unbound in human plasma | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1502770 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1461763 | Inhibition of MDR1 in human MCF7/ADR cells assessed as potentiation of verapamil-induced cytotoxicity by measuring cell growth (Rvb = 78.2%) | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Recent synthetic and medicinal perspectives of tryptanthrin. |
AID514306 | Protection 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 uM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID1459760 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID143480 | Inhibitory activity when combined with cisplatin (uM) in NCI/ADR cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1502728 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1352565 | Inhibition 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 cells | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID406186 | Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of doxorubicin | 2008 | Journal of natural products, Jun, Volume: 71, Issue:6 | Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells. |
AID682079 | TP_TRANSPORTER: inhibition of Calcein-AM transport in HL60-MRP1 cells | 2006 | Chemico-biological interactions, Feb-25, Volume: 159, Issue:3 | Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). |
AID1338193 | Inhibition 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 control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID45736 | Reversal 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 doxorubicin | 1995 | Journal 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. |
AID101592 | Inhibitory activity when combined with 5-Fluorouracil (uM) in MCF-7 cell line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1391798 | Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors. |
AID1530109 | Stimulation 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 control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. |
AID1207719 | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID74169 | Decrease in developed tension of the right atrium of guinea pig expressed as the negative chronotropy. | 1999 | Journal 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. |
AID1552590 | Permeability of compound at 25 ug/ml at pH 7.4 incubated for 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & 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. |
AID288186 | Permeability coefficient through artificial membrane in presence of stirred water layer at 200 rpm stirring speed | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID1888846 | Antibacterial activity against Staphylococcus aureus 1199B measured after 24 hrs by Muller Hinton broth based MTT assay | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1631738 | Reversal 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 control | 2016 | Journal 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. |
AID1739434 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM measured per mg protein upto 30 mins | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Substituted 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. |
AID340929 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 1 mg/liter daptomycin | 2007 | Antimicrobial 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. |
AID1235693 | Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1155069 | Antiplasmodial 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 control | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 | Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT. |
AID1320724 | Inhibition 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Halogenated naphthochalcones and structurally related naphthopyrazolines with antitumor activity. |
AID210307 | Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity. |
AID1504335 | Inhibition 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 cytometry | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance. |
AID722220 | Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis | 2013 | Bioorganic & 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). |
AID1866897 | Permeability for across blood brain barrier by PAMPA | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
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AID1235764 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1307802 | Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as relaxation of calcium-induced contraction | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
AID1534777 | Effective permeability of the compound at 100 mg/ml incubated for 16 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease. |
AID368400 | Reversal 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 uM | 2009 | Journal 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. |
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AID88854 | Effect on cellular accumulation of Vincristine (VCR) in multidrug resistant human ovarian cancer 2780AD cells at 1 ug/mL | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12 | Modulation of multidrug resistance by taxuspine C and other taxoids from Japanese yew. |
AID1235703 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1486977 | Inhibition 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) | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID1504327 | Inhibition 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 hrs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance. |
AID1427565 | Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 30 mins in presence of NADPH | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A |
AID324432 | Increase 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 control | 2007 | Proceedings 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. |
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AID653471 | Induction of ATPase activity of p-glycoprotein at 200 uM by luminescence assay relative to control | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. |
AID1235717 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1502888 | Inhibition 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 ofloxaci | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1533105 | Inhibition 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 b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID1833371 | Reversal 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) | |||
AID1502756 | Inhibition 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 relativ | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
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AID1459775 | Inhibition of P-gp in human KBVIN cells assessed as potentiation of doxorubicin-induced cytotoxicity at 2.5 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
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AID1739848 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
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AID1761202 | Induction 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%) | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
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AID1765292 | Permeability of compound by PAMPA-BBB assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
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AID324583 | Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control | 2007 | Proceedings 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. |
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AID1444094 | Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
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AID604023 | Ratio 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 method | 2009 | Journal 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. |
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AID1761211 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID722218 | Cytotoxicity against human K562 cells at 1 uM after 72 hrs by MTT assay | 2013 | Bioorganic & 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). |
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AID1833385 | Inhibition of human CYP3A4 preincubated for 10 mins followed by substrate and NADP addition measured after 30 mins by fluorescence assay | |||
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AID1628201 | Inhibition of P-gp ATPase activity in human A549/CDDP cells at 200 uM by luminescence assay (Rvb = 706683 +/- 23554 RLU) | 2016 | Journal 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. |
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AID1533115 | Inhibition 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 cytometry | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors. |
AID230555 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1502862 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1273395 | Inhibition 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 control | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID1377751 | Effective permeability of the compound after 2.5 hrs at 25 degC by PAMPA assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents. |
AID351896 | Chemosensitizing activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes as IC50 ratio chloroquine +/- 500nM by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1459768 | Inhibition of P-gp in human HeLaS3 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 1 uM by SRB assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors. |
AID1764400 | Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID379729 | Reversal of multidrug resistance in human 2780AD cells assessed as accumulation of calcein at 25 ug/mL after 15 mins by fluorescence technique relative to control | 2006 | Journal of natural products, Feb, Volume: 69, Issue:2 | Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii. |
AID676757 | Inhibition 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 assay | 2012 | Journal of natural products, Jul-27, Volume: 75, Issue:7 | Putative mycobacterial efflux inhibitors from the seeds of Aframomum melegueta. |
AID1502776 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1348630 | Intrinsic clearance in human liver microsomes at 5 uM preincubated for 5 mins followed by NADPH addition measured after 45 mins by UPLC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation. |
AID1429933 | Inhibition 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 cytometry | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity. |
AID1502851 | Inhibition 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 t | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
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AID681880 | TP_TRANSPORTER: inhibition of bimane-GS efflux in the presence of Verapamil at a concentration of 25uM in MRP4-expressing HepG2 cells | 2004 | The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2 | Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione. |
AID1427563 | Metabolic stability in human liver microsomes assessed as metabolic rate measured after 30 mins in presence of NADPH | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A |
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AID205268 | Inhibition 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 uM | 1985 | Journal 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. |
AID1167504 | Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters. |
AID1558703 | Half life in mouse liver microsomes at 50 uM measured up to 45 mins by UPLC/MS analysis | |||
AID364887 | Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
AID1418868 | Inhibition 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 doxorubicin | 2018 | Bioorganic & 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). |
AID1770547 | Metabolic 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 analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold. |
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AID714414 | Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs | 2012 | Journal 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. |
AID90142 | Ratio of effect of compound on VBL accumulation (antiPgp activity) to its intrinsic cellular toxicity; | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. |
AID1169855 | Half life in human liver microsomes at 1 uM after 30 mins in presence of NADPH | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Structure-guided development of deoxycytidine kinase inhibitors with nanomolar affinity and improved metabolic stability. |
AID1235767 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1234530 | Inhibition 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 cytometry | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Discovery of substituted 1,4-dihydroquinolines as novel class of ABCB1 modulators. |
AID427811 | Antileishmanial 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 electrode | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis. |
AID427722 | Reversal of MRP1-mediated doxorubicin-resistance in human 2008/MRP1 cells assessed as reduction of doxorubicin IC50 percent by half | 2009 | Journal 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. |
AID389760 | Inhibition of verapamil-induced residual ATPase activity in lipid activated mouse P-glycoprotein mdr3 cys-less mutant assessed as ATP hydrolysis per ug of protein | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells. |
AID714419 | Reversal of P-gp-mediated doxorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
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AID1704095 | Cytotoxicity against human HUVEC cells assessed as reduction in cell viability at 10 uM incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
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AID656840 | Effect on P-gp ATPase activity assessed as relative light units at 200 uM by P-gp-GloTM assay (Rvb = 242328 +/- 1398 RLU) | 2012 | Bioorganic & 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. |
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AID1254927 | Half life in human liver S9 microsomes in presence of NADPH by LC-MS/MS method | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents. |
AID1502713 | Antimycobacterial activity against Mycobacterium avium isolate MAV4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502807 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1566022 | Reversal 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) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance. |
AID1338184 | Selectivity 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 half | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Extending the structure-activity relationship study of marine natural ningalin B analogues as P-glycoprotein inhibitors. |
AID1271450 | Vasodilator activity in Sprague-Dawley rat mesentric artery assessed as reduction in of K+-induced contraction relative to control | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and fluorescent study of 5-phenyl furocoumarin derivatives as vasodilatory agents. |
AID406201 | Reversal of P-glycoprotein-mediated multidrug resistance in human HepG2/Dox cells assessed as increase in sensitivity at 4 uM in presence of paclitaxel | 2008 | Journal of natural products, Jun, Volume: 71, Issue:6 | Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells. |
AID1062338 | Therapeutic 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 resistance | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers. |
AID1446766 | Intrinsic clearance in human liver microsomes in absence of NADPH by LC-MS/MS method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus. |
AID681582 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID1733394 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1785055 | Reversal 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 | |||
AID271725 | Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. |
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AID1481892 | Inhibition 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 analysis | 2017 | Journal 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. |
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AID1625123 | Permeability of the compound in pH 7.4 PBS at 200 uL after 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & 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. |
AID1873790 | Cytotoxicity 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 analysis | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Cytotoxicity of cinchona alkaloid organocatalysts against MES-SA and MES-SA/Dx5 multidrug-resistant uterine sarcoma cell lines. |
AID236918 | Apparent permeability of the compound was determined in MDCK (madin darby canine kidney) strain I; Activity = Papp 10e-6 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3 | In silico prediction of membrane permeability from calculated molecular parameters. |
AID1315282 | Inhibition 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 control | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Dihydro-β-agarofuran Sesquiterpenoids from the Australian Rainforest Plant Maytenus bilocularis. |
AID1696659 | Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22 | N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H |
AID150757 | P-gp activity was measured by a direct transport assay, using polarized LLC-MDR1 epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
AID502263 | Cytotoxicity against hamster BHK21 cells after 96 hrs by MTT assay | 2010 | Bioorganic & 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. |
AID1502801 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1381448 | Apparent permeability from basolateral to apical side in MDCK cells | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB. |
AID1502889 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID475690 | Clearance in human | 2010 | Journal 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. |
AID514304 | Protection 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 uM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID679222 | TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 1 uM, Verapamil: 100 uM) in membrane vesicles from MRP7-expressing HEK293 cells | 2003 | Molecular pharmacology, Feb, Volume: 63, Issue:2 | Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). |
AID1215170 | Tmax in Sprague-Dawley rat portal vein plasma at 10 mg/kg, po | 2011 | Drug 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. |
AID1502744 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID537734 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay | 2010 | European 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. |
AID1358239 | Inhibition of P-gp in human MCF7/ADR cells assessed as cell viability after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell. |
AID1750901 | Reversal 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 | |||
AID395037 | Inhibition 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 method | 2009 | Bioorganic & 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+. |
AID1352554 | Inhibition 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 d | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID252858 | Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (3 uM) and Vinblastine (VNB) | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13 | Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis. |
AID1321562 | Inhibition 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 t | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Triterpenoids from Momordica balsamina: Reversal of ABCB1-mediated multidrug resistance. |
AID677694 | Permeability of the compound at pH 7.4 by PAMPA | 2012 | Journal 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. |
AID1704104 | Reversal 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 assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
AID1481510 | Inhibition 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 control | 2017 | Journal 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. |
AID1454121 | Half life in human hepatic microsomes at 0.1 uM by HPLC-MS/MS method | 2017 | Bioorganic & 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. |
AID1502868 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502846 | Inhibition 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 | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1502897 | Inhibition 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/ml | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1893726 | Metabolic 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 | |||
AID245888 | Maximum intracellular vinblastine accumulation of the KB/MDR cells caused by the compound in 1 h | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22 | Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. |
AID487884 | Binding affinity to P-gp at 5 uM after 30 mins by spectrophotometry | 2010 | Bioorganic & 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. |
AID230560 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID1533612 | Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
AID1761214 | Reversal 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 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity. |
AID1633098 | Inhibition 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 control | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells. |
AID755309 | Inhibition of p-gp in human KB/VCR cells assessed as intracellular accumulation of rhodamine123 at 2 uM after 2 hrs by microplate fluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs. |
AID1704112 | Inhibition 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 microsocopy | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | New Seco-DSP derivatives as potent chemosensitizers. |
AID1164950 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for methicillin-resistant Staphylococcus aureus NRS 70 | 2014 | Journal 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. |
AID1502853 | Inhibition 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 t | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID345307 | Intrinsic cytotoxicity against mouse NIH/3T3 cells overexpressing MDR1 at 10 uM after 72 hrs by MTT assay | 2008 | Journal 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. |
AID714417 | Reversal of P-gp-mediated vinblastin-resistance in human LCC6MDR cells after 5 days by MTS assay | 2012 | Journal 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. |
AID1903284 | Cytotoxicity against human KBV cells assessed as decrease in cell survival rate at 10 uM measured after 72 hrs in presence of paclitaxel by MTT assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Design, synthesis, and tumor drug resistance reversal activity of novel hederagenin derivatives modified by nitrogen-containing heterocycles. |
AID1065213 | Permeability coefficient, log Pe of the compound at pH 7.4 by PAMPA | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Development of novel Vitamin D Receptor-Coactivator Inhibitors. |
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AID75927 | Potency expressed as EC30 for the negative chronotropic activity. | 1999 | Journal 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. |
AID513158 | Inhibition of heme crystallization after 16 hrs | 2006 | Nature chemical biology, Aug, Volume: 2, Issue:8 | A clinical drug library screen identifies astemizole as an antimalarial agent. |
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AID659472 | Effective permeability across porcine polar brain lipid after 4 hrs by PAMPA | 2012 | Journal 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. |
AID1381449 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side of MDCK cells | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB. |
AID671709 | Inhibition 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 analysis | 2012 | Bioorganic & 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. |
AID351897 | Chemosensitizing activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes as IC50 ratio chloroquine +/- 500 nM by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
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AID683266 | Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as paclitaxel-induced cytotoxicity at 10 uM after 72 hrs by SRB assay | 2012 | Journal 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. |
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AID1673433 | Reversal 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) | 2019 | Bioorganic & 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. |
AID351907 | Chemosensitizing 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 assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
AID1292332 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2016 | Bioorganic & 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. |
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AID1733379 | Reversal 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) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID1481514 | Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular Rh123 accumulation at 5 uM up to 90 mins by flow cytometry | 2017 | Journal 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. |
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AID1129447 | Intrinsic clearance in mouse microsomes at 1 uM | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1888882 | Inhibition 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 spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor. |
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AID1215348 | Time 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 | 2011 | Drug 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. |
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AID1352556 | Inhibition 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 d | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
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AID1602584 | Half life in ICR/CD1 mouse hepatocytes at 1 uM up to 120 mins by LC-MS/MS analysis | 2019 | Journal 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. |
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AID1684002 | Reversal 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 | |||
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AID1511118 | Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
AID331369 | Toxicity in Sprague-Dawley rat assessed as ventricular fibrillation by measuring aconitine nitrate level at 2 mg.kg, iv by echocardiography | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Design and synthesis of tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in cancer. |
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AID1352557 | Inhibition of P-gp in human MCF7/ADR cells assessed as increase in doxorubicin accumulation in cells after 150 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Jatrophane diterpenoids from Euphorbia sororia as potent modulators against P-glycoprotein-based multidrug resistance. |
AID1853713 | Metabolic 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 analysis | 2021 | RSC 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. |
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AID1502753 | Inhibition 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 relativ | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
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AID1167505 | Modulatory activity at P-gp in human K562/DOX cells assessed as maximum increase nuclear concentration of pirarubicin by spectrofluorometric assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters. |
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AID615812 | Reversal of MDR1-mediated paclitaxel resistance in multidrug resistant human NCI-H460 cells assessed as combination index at 5 uM after 72 hrs by SRB assay | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides. |
AID513649 | Induction 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 hrs | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. |
AID351891 | Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
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AID1129604 | Efflux 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 spectroscopy | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity. |
AID1235718 | Inhibition 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 assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy. |
AID1418862 | Potentiation 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 alone | 2018 | Bioorganic & 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). |
AID1758193 | Inhibition 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 analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell. |
AID1764806 | Stability in human pooled liver microsomes assessed as parent compound remaining measured at 60 mins in presence of NADPH by LC-MS/MS analysis | 2021 | Journal 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. |
AID678737 | TP_TRANSPORTER: inhibition of Vinblastine efflux (Vinblastine: 0.002 uM, Verapamil: 10 uM) in P388/S and P388/ADR cells | 2000 | Clinical and experimental pharmacology & physiology, Aug, Volume: 27, Issue:8 | Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo. |
AID1418871 | Inhibition 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 cisplatin | 2018 | Bioorganic & 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). |
AID1483831 | Intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ. |
AID95151 | Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3 | Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships. |
AID1486952 | Inhibition 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 alone | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID1733403 | Induction 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%) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID680712 | TP_TRANSPORTER: increase in Rhodamine 123 intracellular accumulation (R123: 150 uM, Verapamil: 2 ug/mL) in MDR1-expressing NIH3T3 cells | 2000 | The 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. |
AID1502806 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID1351575 | Vasorelaxing activity in Wistar rat endothelium-denuded thoracic aorta ring assessed as reduction in 30 mM KCl-induced contraction after 15 mins | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, 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. |
AID230390 | Reversal 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 line | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. |
AID288982 | Inhibition 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 cytometry | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Structure-activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors. |
AID271732 | Cytotoxicity against MCF7/Adr cells at 100 uM after 48 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. |
AID680527 | TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.01 uM, Verapamil: 500 uM) in OCTN2-expressing HEK293 cells | 2001 | Molecular pharmacology, Feb, Volume: 59, Issue:2 | Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. |
AID1161578 | Permeability of the compound by PAMPA-BBB assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
AID1566034 | Stimulation 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance. |
AID1739838 | Inhibition 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 IC50 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID487885 | Binding affinity to P-gp at 0.5 uM after 30 mins by spectrophotometry | 2010 | Bioorganic & 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. |
AID1631733 | Reversal 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 control | 2016 | Journal 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. |
AID1739818 | Inhibition 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) | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. |
AID540224 | Clearance in dog after iv administration | 2006 | Drug 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. |
AID1486972 | Inhibition 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 alone | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors. |
AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID252859 | Reversal index is defined as the ratio between the IC50 of cells without compound and IC50 with compound (10 uM) and Daunorubian (DNM) | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13 | Reversion of human Pgp-dependent multidrug resistance by new sesquiterpenes from Zinowiewia costaricensis. |
AID1273453 | Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294T assessed as isoniazid MIC at 256 ug/ml after 7 days by microdilution checkerboard assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis. |
AID681948 | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.85 uM, Verapamil: 5000 uM) in Xenopus laevis oocytes | 1997 | Molecular pharmacology, Jun, Volume: 51, Issue:6 | Cloning and functional expression of a human liver organic cation transporter. |
AID444057 | Fraction escaping hepatic elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1198140 | Permeability of the compound in PBS and EtOH by PAMPA method | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
AID1733405 | Reversal 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 analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance. |
AID637605 | Permeability of the compound by PAMPA | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation. |
AID1502739 | Inhibition 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) | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium. |
AID77931 | Left ventricular pressure of isolated guinea pig heart at dose 0.05 (ug/heart) | 1985 | Journal 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. |
AID654103 | Inhibition 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 control | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Dimeric 3,5-bis(benzylidene)-4-piperidones: a novel cluster of tumour-selective cytotoxins possessing multidrug-resistant properties. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The 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. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
AID1802796 | Fluorescence 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.\\ | 2017 | Biochemistry, 05-16, Volume: 56, Issue:19 | Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs. |
AID1802151 | Calcein-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.\\ | 2016 | Chemical 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. |
AID1346664 | Rat Cav1.2 (Voltage-gated calcium channels) | 1996 | Molecular 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. |
AID1346703 | Rat Kv3.2 (Voltage-gated potassium channels) | 2000 | Neuropharmacology, Jan-04, Volume: 39, Issue:2 | Sensitivity of native and cloned hippocampal delayed-rectifier potassium channels to verapamil. |
AID1346531 | Human TPC2 (CatSper and Two-Pore channels) | 2012 | Cell, Oct-12, Volume: 151, Issue:2 | TPC proteins are phosphoinositide- activated sodium-selective ion channels in endosomes and lysosomes. |
AID1346671 | Human Kv1.8 (Voltage-gated potassium channels) | 2000 | American 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. |
AID1346501 | Mouse Kir3.2 (Inwardly rectifying potassium channels) | 1996 | Neuron, May, Volume: 16, Issue:5 | Functional analysis of the weaver mutant GIRK2 K+ channel and rescue of weaver granule cells. |
AID1346493 | Human TPC1 (CatSper and Two-Pore channels) | 2014 | Nature chemical biology, Jun, Volume: 10, Issue:6 | The voltage-gated sodium channel TPC1 confers endolysosomal excitability. |
AID1345181 | Human Plasma membrane monoamine transporter (SLC29 family) | 2016 | Clinical pharmacology and therapeutics, Nov, Volume: 100, Issue:5 | The plasma membrane monoamine transporter (PMAT): Structure, function, and role in organic cation disposition. |
AID1346666 | Human Kv1.7 (Voltage-gated potassium channels) | 2002 | European 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). |
AID1345181 | Human Plasma membrane monoamine transporter (SLC29 family) | 2005 | Molecular pharmacology, Nov, Volume: 68, Issue:5 | Interaction of organic cations with a newly identified plasma membrane monoamine transporter. |
AID1345258 | Human CYP3A4 (CYP3 family) | 2001 | British journal of clinical pharmacology, May, Volume: 51, Issue:5 | Inhibitory effects of verapamil and diltiazem on simvastatin metabolism in human liver microsomes. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 6624 (40.13) | 18.7374 |
1990's | 4944 (29.95) | 18.2507 |
2000's | 2606 (15.79) | 29.6817 |
2010's | 1922 (11.64) | 24.3611 |
2020's | 411 (2.49) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (103.81) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1,527 (8.67%) | 5.53% |
Reviews | 834 (4.73%) | 6.00% |
Case Studies | 1,046 (5.94%) | 4.05% |
Observational | 4 (0.02%) | 0.25% |
Other | 14,210 (80.64%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Development and Clinical Application of [11C]Verapamil-PET, a Surrogate Marker on P-glycoprotein Expression [NCT02144792] | Phase 2 | 30 participants (Anticipated) | Interventional | 2013-05-31 | Recruiting | ||
Pharmacodynamics and Pharmacokinetics of Verapamil in Crohn's Disease Patients [NCT01261286] | Phase 1 | 0 participants | Interventional | Completed | |||
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 3 | 111 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
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 1 | 56 participants (Anticipated) | Interventional | 2023-09-01 | Recruiting | ||
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) | Interventional | 2022-01-31 | Not 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 2 | 32 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
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 1 | 82 participants (Actual) | Interventional | 2018-11-06 | Completed | ||
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 3 | 89 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
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 2 | 1 participants (Actual) | Interventional | 2013-11-30 | Terminated | ||
Pharmacokinetics and Safety of Commonly Used Drugs in Lactating Women and Breastfed Infants [NCT03511118] | 1,600 participants (Anticipated) | Observational | 2018-10-04 | Recruiting | |||
A Study of the Pharmacokinetic and Pharmacodynamic Responses in Healthy and Altered Human Cardiovascular Systems [NCT03098680] | Phase 1 | 18 participants (Actual) | Interventional | 2017-04-24 | Terminated(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 2 | 150 participants (Anticipated) | Interventional | 2022-05-17 | Recruiting | ||
Super-Selective Intra-Arterial Administration of Verapamil for Neuroprotection After Intra-Arterial Thrombolysis for Acute Ischemic Stroke Phase I Study [NCT02235558] | Phase 1 | 11 participants (Actual) | Interventional | 2013-02-01 | Completed | ||
Comparative Study Between the Efficacy of Verapamil and Bisoprolol on Reduction of Bleeding During Endoscopic Sinus Surgery Under General Anaesthesia. [NCT04356196] | Early Phase 1 | 135 participants (Anticipated) | Interventional | 2021-06-15 | Active, not recruiting | ||
Treatment of Hypoglycemia Following Gastric Bypass Surgery [NCT02527993] | Phase 4 | 11 participants (Actual) | Interventional | 2015-10-31 | Completed | ||
Effects of Atenolol, Perindopril and Verapamil on Haemodynamic and Vascular Function in Marfan Syndrome - A Randomised Double-Blind Crossover Trial [NCT01295047] | Phase 4 | 18 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
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 1 | 15 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
[NCT01126307] | 16 participants (Anticipated) | Interventional | 2010-06-30 | Not 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 1 | 45 participants (Actual) | Interventional | 2022-04-21 | Completed | ||
Use of Adenosine to Determine the Electrophysiological Mechanism of Premature Ventricular Contractions [NCT03218137] | Phase 4 | 100 participants (Anticipated) | Interventional | 2017-02-13 | Recruiting | ||
The Intra-arterial Vasospasm Trial(iVAST)- A Multi-center Randomized Study [NCT01996436] | Phase 4 | 330 participants (Anticipated) | Interventional | 2016-08-29 | Recruiting | ||
Blood Pressure and Weight Trajectory on a Dual Antihypertensive Combination Plus Sibutramine Versus Placebo in Obese Hypertensives [NCT00679653] | Phase 3 | 171 participants (Actual) | Interventional | 2002-02-28 | Completed | ||
A Double Blind Randomized Controlled Trial of Greater Occipital Nerve Infiltration in Cluster Headache [NCT00804895] | Phase 2/Phase 3 | 43 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
Efficacy of Adenosine Versus Verapamil for Management of Supraventricular Tachycardia Post- Coronary Artery Bypass Grafting: a Randomized Double Blinded Trial [NCT04203368] | 268 participants (Actual) | Interventional | 2020-02-01 | Completed | |||
The Effect of the Adipocyte-derived Hormone Leptin on Endothelial Function in Healthy Men and in Persons With Known Cardiovascular Disease [NCT04374500] | Early Phase 1 | 103 participants (Actual) | Interventional | 2006-01-01 | Completed | ||
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 1 | 24 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
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 1 | 40 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
The Effects of ATLAS (Arginine Tetrahydrobiopterin L-Ascorbate) Therapy on Nitric Oxide Bioavailability and Pain-free Walking in Patients With Intermittent Claudication [NCT04800692] | Phase 1 | 10 participants (Anticipated) | Interventional | 2021-06-15 | Recruiting | ||
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 2 | 138 participants (Anticipated) | Interventional | 2021-02-08 | Recruiting | ||
A Two-Phase Study for Primary and Secondary Prevention of Diabetic Nephropathy by Combined ACE Inhibition and Calcium Channel Blockade (BENEDICT) [NCT00235014] | Phase 4 | 1,204 participants (Actual) | Interventional | 1997-03-31 | Completed | ||
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 2 | 52 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
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) | Observational | 2020-01-19 | Completed | |||
Radiofrequency Ablation of Symptomatic Frequent Ventricular Premature Complexes as a First-line Therapy in Pediatric Population Without Structural Heart Disease [NCT02772354] | Phase 2/Phase 3 | 124 participants (Anticipated) | Interventional | 2016-04-30 | Recruiting | ||
Does Dilution of Verapamil With Normal Saline or Blood Reduce Discomfort Felt During Intraarterial Administration? [NCT05625503] | Early Phase 1 | 100 participants (Anticipated) | Interventional | 2022-12-13 | Recruiting | ||
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 1 | 24 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
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 1 | 79 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
A Phase 1, Open-Label, 4-Part, Drug-Drug Interaction Study With Omaveloxolone in Healthy Subjects [NCT04008186] | Phase 1 | 61 participants (Actual) | Interventional | 2019-06-14 | Completed | ||
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 1 | 18 participants (Anticipated) | Interventional | 2022-05-31 | Not yet recruiting | ||
Hybrid Closed Loop Therapy and Verapamil for Beta Cell Preservation in New Onset Type 1 Diabetes (CLVer) [NCT04233034] | Phase 3 | 113 participants (Actual) | Interventional | 2020-07-09 | Completed | ||
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 1 | 72 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
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 4 | 120 participants | Interventional | 2006-01-31 | Recruiting | ||
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 1 | 24 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
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 1 | 24 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
Drug Discrimination in Methadone-Maintained Humans Study 2 [NCT00733239] | Phase 1 | 15 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Elimination of Ventricular Premature Beats With CaTheter Ablation Versus OPtImal Anti-arrhythmic Drug Treatment [NCT03845010] | 22 participants (Actual) | Interventional | 2019-02-12 | Completed | |||
Drug Discrimination in Methadone-Maintained Humans Study 3 [NCT01068847] | Phase 1 | 9 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
[NCT00000556] | Phase 3 | 0 participants | Interventional | 1995-03-31 | Completed | ||
Pharmacotherapy of Treatment-Resistant Mania [NCT00518947] | Phase 3 | 45 participants (Actual) | Interventional | 1994-11-30 | Completed | ||
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 1 | 15 participants (Actual) | Interventional | 2016-01-22 | Completed | ||
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 2 | 190 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
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 4 | 102 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
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 3 | 45 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
A Phase 3, Multicenter, Open-Label Extension Study of Phenoptin in Subjects With Phenylketonuria Who Have Elevated Phenylalanine Levels [NCT00225615] | Phase 3 | 100 participants | Interventional | 2005-11-30 | Completed | ||
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 4 | 2,000 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
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 1 | 36 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
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 4 | 357 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
Superselective Citicoline And Verapamil for Ischemic Neuroprotection and Greater Effective Response (SCAVINGER) in the Kentucky Regional Population: A Clinical and Translational Study [NCT02823106] | Phase 1 | 0 participants (Actual) | Interventional | 2016-08-31 | Withdrawn(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 4 | 120 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
Drug Discrimination in Methadone-Maintained Humans Study 1 [NCT00593463] | Phase 1 | 40 participants (Anticipated) | Interventional | 2006-09-30 | Completed | ||
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 3 | 95 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
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 3 | 206 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
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 1 | 27 participants (Anticipated) | Interventional | 2008-07-31 | Completed | ||
Pacing and AV Node Ablation Compared to Drug Therapy in Symptomatic Elderly Patients With Atrial Fibrillation Clinical Trial (PACIFIC) - Pilot Study [NCT00589303] | Phase 3 | 27 participants (Actual) | Interventional | 2007-12-31 | Terminated(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 1 | 20 participants (Anticipated) | Interventional | 2023-02-06 | Recruiting | ||
Multimodal Neuroimaging and Neurocognitive Assessment of Biomarkers and Response to Sapropterin Dihydrochloride Treatment in Phenylketonuria [NCT01412437] | 0 participants (Actual) | Interventional | 2011-04-30 | Withdrawn(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) | Interventional | 2023-05-20 | Not 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 1 | 10 participants (Actual) | Interventional | 2017-10-11 | Completed | ||
The Surrogate Marker of Rate Control in Patients With Atrial Fibrillation [NCT04513509] | 50 participants (Anticipated) | Interventional | 2020-08-07 | Not yet recruiting | |||
Kuvan® (Sapropterin Dihydrochloride) for Improving Gastric Accommodation in Women With Diabetic Gastroparesis (KIGA-DG) [NCT01135186] | 9 participants (Actual) | Interventional | 2010-05-31 | Completed | |||
Study of Verapamil in Refractory Catamenial Epilepsy [NCT00559169] | 12 participants (Anticipated) | Interventional | 2009-02-28 | Withdrawn(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) | Interventional | 2020-12-30 | Active, not recruiting | |||
Intracavernosal Injection of Papaverine/Verapamil Versus Papaverine/Phentolamine in Erectile Dysfunction: A Pilot Study [NCT03033537] | 20 participants (Actual) | Observational [Patient Registry] | 2015-07-01 | Completed | |||
Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study) [NCT03070470] | Phase 1 | 60 participants (Actual) | Interventional | 2017-03-14 | Completed | ||
Assessment of Verapamil as an Adjunct for Prevention of Keloid Recurrence After Surgical Removal [NCT01720056] | Phase 4 | 14 participants (Actual) | Interventional | 2012-10-31 | Terminated(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 2 | 24 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
INternational VErapamil SR Trandolapril STudy [NCT00133692] | Phase 4 | 22,000 participants | Interventional | 1997-09-30 | Completed | ||
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 1 | 14 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
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 4 | 280 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
Treatment Effects of Bisoprolol and Verapamil in Symptomatic Patients With Non-obstructive Hypertrophic Cardiomyopathy [NCT05569382] | Phase 4 | 140 participants (Anticipated) | Interventional | 2022-08-10 | Recruiting | ||
Sapropterin Expanded Access Program [NCT00484991] | 0 participants | Expanded Access | Approved for marketing | ||||
Repurposing of Verapamil as a Beta Cell Survival Therapy in Type 1 Diabetes [NCT02372253] | Phase 2 | 32 participants (Actual) | Interventional | 2015-02-28 | Completed | ||
Targeting Beta Cell Dysfunction With Verapamil in Longstanding T1D [NCT05847413] | Early Phase 1 | 10 participants (Actual) | Interventional | 2020-05-30 | Completed | ||
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 2 | 700 participants | Interventional | 2004-12-31 | Completed | ||
RCVS: The Rational Approach to Diagnosis and Treatment [NCT03150524] | Phase 4 | 0 participants (Actual) | Interventional | 2017-07-01 | Withdrawn(stopped due to Failure to recruit patients meeting inclusion criteria.) | ||
Intraarterial Verapamil for Neuroprotection in Ischemic Stroke [NCT03347786] | Phase 1 | 20 participants (Anticipated) | Interventional | 2017-04-20 | Recruiting | ||
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 2 | 84 participants | Interventional | 2006-05-31 | Completed | ||
Rate Control in Atrial Fibrillation [NCT00313157] | Phase 3 | 80 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
Oral Propranolol, Diltiazem, Metoprolol and Verapamil in Atrial Fibrillation Rate Control in Patients With Stable Hemodynamic Status [NCT01655303] | Phase 4 | 90 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
[NCT01655316] | Phase 4 | 90 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
Pharmacologic Dissection of Vestibular Migraine and Chronic Subjective Dizziness: A Double-Blind Parallel Group Trial Comparing Response to Verapamil Versus Sertraline [NCT01669304] | Phase 1 | 32 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
A Phase I Trial of Brentuximab Vedotin Plus MDR1 Inhibitors in Relapsed/Refractory Hodgkin Lymphoma [NCT03013933] | Phase 1 | 29 participants (Actual) | Interventional | 2017-05-03 | Active, 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 4 | 100 participants | Interventional | 2006-01-31 | Recruiting | ||
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 1 | 58 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
Biomarkers of Central Nervous System Tetrahydrobiopterin Concentration and Response to Tetrahydrobiopterin Supplementation in Children With Idiopathic Cognitive Developmental Disorders [NCT01141595] | 10 participants (Actual) | Interventional | 2010-07-31 | Completed | |||
Phase Ib/II Clinical Trial of Topical Verapamil Hydrochloride for Chronic Rhinosinusitis With Nasal Polyps [NCT03102190] | Phase 1 | 6 participants (Actual) | Interventional | 2017-06-05 | Terminated(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 1 | 48 participants (Actual) | Interventional | 2017-09-27 | Completed | ||
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial [NCT04330300] | Phase 4 | 2,414 participants (Anticipated) | Interventional | 2020-04-30 | Suspended(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 1 | 45 participants (Actual) | Interventional | 2017-10-25 | Completed | ||
Randomized Double Blind Placebo Controlled Trial of Verapamil in Chronic Rhinosinusitis [NCT02454608] | 29 participants (Actual) | Interventional | 2015-05-31 | Terminated(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 2 | 81 participants (Actual) | Interventional | 2012-04-30 | Terminated(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 4 | 0 participants (Actual) | Interventional | 2019-07-31 | Withdrawn(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 4 | 418 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
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 1 | 135 participants (Anticipated) | Interventional | 2021-03-01 | Not yet recruiting | ||
Atrioventricular Block and Cluster Headache [NCT04406259] | Phase 4 | 60 participants (Anticipated) | Interventional | 2020-11-02 | Recruiting | ||
Treatment of Tinnitus With Migraine Medications: A Randomized Clinical Trial [NCT04404439] | Phase 4 | 150 participants (Anticipated) | Interventional | 2019-09-26 | Recruiting | ||
"Evaluation of Behavior, Executive Function, Neurotransmitter Function and Genomic Expression in PKU Nonresponders to Kuvan® (Sapropterin Dihydrochloride)" [NCT01274026] | 21 participants (Actual) | Observational | 2011-01-31 | Completed | |||
Combination of Hydroxyurea and Verapamil for Refractory Meningiomas [NCT00706810] | Phase 2 | 8 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
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 1 | 24 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
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 4 | 160 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
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 1 | 22 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
Acute Cardioversion Versus Wait And See-approach for Symptomatic Atrial Fibrillation in the Emergency Department (RACE 7 ACWAS-trial) [NCT02248753] | 437 participants (Actual) | Interventional | 2014-10-31 | Completed | |||
Amiodarone or Verapamil in COVID-19 Hospitalized Patients With Symptoms [NCT04351763] | Phase 2/Phase 3 | 804 participants (Actual) | Interventional | 2020-05-20 | Completed | ||
Relative Bioavailability of BI 10773 Given Alone and Together With Verapamil - an Open-label, Randomised, Crossover Trial in Healthy Subjects [NCT01276301] | Phase 1 | 16 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
Omission of Prophylactic Verapamil Use in Transradial Coronary Interventions [NCT01402427] | 591 participants (Actual) | Interventional | 2011-03-31 | Completed | |||
Quinidine Versus Verapamil in Short-coupled Idiopathic Ventricular Fibrillation: an Open-label, Randomized Crossover Pilot Trial [NCT05593757] | Phase 2 | 24 participants (Anticipated) | Interventional | 2022-10-01 | Enrolling 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 1 | 22 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
Assessment of Intravenous Rate Control Response in Atrial Fibrillation Trial Pilot Study (AIRCRAFT) [NCT04234477] | Phase 4 | 0 participants (Actual) | Interventional | 2021-12-31 | Withdrawn(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 2 | 170 participants (Anticipated) | Interventional | 2018-03-28 | Recruiting | ||
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 3 | 228 participants (Anticipated) | Interventional | 2023-07-31 | Recruiting | ||
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 1 | 36 participants (Anticipated) | Interventional | 2023-10-23 | Recruiting | ||
Verapamil as Adjunctive Seizure Therapy for Children and Young Adults With Dravet Syndrome [NCT01607073] | Phase 2 | 2 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |