Nifedipine is a calcium channel blocker used to treat high blood pressure, chest pain (angina), and certain types of heart conditions. It works by relaxing the blood vessels, which lowers blood pressure and makes it easier for the heart to pump blood. Nifedipine is typically taken by mouth. It is available as a tablet, capsule, and extended-release tablet. Nifedipine is also available as a topical ointment that is applied to the skin. Common side effects of nifedipine include headache, dizziness, swelling in the ankles or feet, and flushing. More serious side effects can include constipation, dry mouth, slow heartbeat, and a decrease in blood pressure. Nifedipine is not recommended for people who are pregnant or breastfeeding. It is also not recommended for people who have had a heart attack or have certain types of heart problems.'
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
hemanthamine: crinine-like alkaloid from AMARYLLIDACEAE; RN given for (3beta,5alpha,11R,13beta,19alpha)-isomer; structure in first source
ID Source | ID |
---|---|
PubMed CID | 4485 |
CHEMBL ID | 193 |
CHEBI ID | 7565 |
SCHEMBL ID | 3968 |
MeSH ID | M0014847 |
PubMed CID | 118701185 |
MeSH ID | M0014847 |
Synonym |
---|
BIDD:GT0442 |
BIDD:PXR0034 |
CBIOL_001826 |
MLS001148146 |
3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
HMS3393O03 |
HMS3267G06 |
AB00052051-05 |
afeditab cr |
CHEBI:7565 , |
coracten |
nifedipinum |
adapine |
nifedipres |
nifedipino |
nifecard |
adalat |
4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsaeuredimethylester |
procardia |
nifecor |
dimethyl 4-(2-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate |
adalat cc |
oxcord |
dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
citilat |
cordipin |
1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester |
corinfar |
procardia xl |
fenihidin |
fenihidine |
DIVK1C_000313 |
KBIO1_000313 |
fortipine la |
bay-a-1040 |
nificard |
tensipine mr |
kb-1712p |
adalate lp |
slofedipine xl |
emaberin |
adalat xl |
adipine xl |
aprical long |
EU-0100819 |
nifedipine, >=98% (hplc), powder |
SPECTRUM_000979 |
IDI1_033861 |
OPREA1_788617 |
PRESTWICK_357 |
lopac-n-7634 |
NCGC00015748-01 |
NCGC00015748-02 |
BIO1_000112 |
BIO2_000111 |
NCGC00024983-01 |
cas-21829-25-4 |
BIO2_000591 |
BIO1_001090 |
BIO1_000601 |
tocris-1075 |
PRESTWICK2_000063 |
BSPBIO_002071 |
IDI1_000313 |
SPECTRUM5_001278 |
LOPAC0_000819 |
CMAP_000042 |
PRESTWICK3_000063 |
BSPBIO_000245 |
BSPBIO_001391 |
BCBCMAP01_000046 |
fedcor |
fenamon |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, dimethyl ester |
adalat oros |
cordilan |
cardilat |
adalat pa |
alpha-nifedipine retard |
glopir |
megalat |
ecodipi |
corotrend |
4-(2-nitrophenyl)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridine |
chronadalate |
adapress |
hexadilat |
sepamit |
chronadalate lp |
dilcor |
dimethyl 1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-3,5-pyridinedicarboxylate |
4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridine |
adalat la |
ccris 6074 |
ecodipin e |
duranifin |
adalat 10 |
adalat gits |
fenamon sr |
macorel |
dilafed |
cardionorm |
dipinkor |
zenusin |
tibricol |
ecodipin |
alonix s |
bay-a 1040 |
cardifen |
cordafen |
adalat 5 |
alfadal |
adalate |
kordafen |
fedcor retard |
adalat ft |
calcilat |
cordalat |
apo-nifed |
calcigard |
adalat gits 30 |
dimethyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate |
adalat 20 |
adalat lp |
aldipin |
adalat retard |
pidilat |
adalat cr |
2,6-dimethyl-3,5-dicarbomethoxy-4-(2-nitrophenyl)-1,4-dihydropyridine |
depin |
camont |
cordicant |
corynphar |
bay 1040 |
bonacid |
alonix |
cordaflex |
myogard |
introcar |
bay a 1040 |
calcibloc |
aprical |
orix |
alat |
adalat crono |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-, dimethyl ester (8ci) |
angipec |
dignokonstant |
anpine |
anifed |
hadipin |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, dimethyl ester (9ci) |
NCGC00091707-01 |
BIM-0050796.0001 |
einecs 244-598-3 |
nifedipino [inn-spanish] |
nifediac |
brn 0497773 |
nifedipinum [inn-latin] |
afeditab |
4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsaeuredimethylester [german] |
nifedipine |
C07266 |
21829-25-4 |
MLS000758222 |
DB01115 |
afeditab cr (tn) |
D00437 |
nifedipine (jp17/usp/inn) |
adalat (tn) |
procardia (tn) |
NCGC00024983-06 |
NCGC00024983-03 |
NCGC00024983-04 |
NCGC00024983-07 |
MLS000028521 , |
smr000058291 |
KBIO2_005247 |
KBIO3_000222 |
KBIO2_002400 |
KBIOGR_002400 |
KBIO2_001459 |
KBIO2_002679 |
KBIOGR_000111 |
KBIO3_000221 |
KBIO2_000111 |
KBIO2_004027 |
KBIOSS_000111 |
KBIO2_006595 |
KBIOGR_000627 |
KBIO2_007536 |
KBIOSS_001459 |
KBIO2_004968 |
KBIO3_001571 |
KBIOSS_002405 |
KBIO3_002879 |
SPBIO_002166 |
PRESTWICK0_000063 |
PRESTWICK1_000063 |
SPECTRUM3_000516 |
SPECTRUM4_000074 |
SPECTRUM2_001058 |
SPBIO_001016 |
NINDS_000313 |
SPECTRUM1500431 |
BPBIO1_000271 |
NCGC00024983-05 |
NCGC00015748-03 |
NCGC00024983-08 |
NCGC00024983-02 |
gtpl2514 |
baya1040 |
MLS001401371 |
NCGC00015748-06 |
HMS2089H11 |
HMS1989F13 |
HMS2091H20 |
HMS2051O03 |
N 7634 , |
NCGC00015748-13 |
nsc-757242 |
nifedipine slow release |
AKOS002942507 |
L001054 |
HMS1791F13 |
HMS500P15 |
HMS1361F13 |
FT-0653833 |
N0528 |
HMS1568M07 |
HMS1920P19 |
bdbm50000778 |
cid_4485 |
CHEMBL193 , |
STK735567 |
NCGC00015748-11 |
NCGC00021710-02 |
NCGC00091707-02 |
NCGC00091707-03 |
HMS2095M07 |
HMS3262D19 |
dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate |
tox21_200304 |
NCGC00257858-01 |
pharmakon1600-01500431 |
nsc757242 |
tox21_110212 |
dtxsid2025715 , |
dtxcid205715 |
HMS2233B22 |
CCG-100758 |
CCG-40115 |
NCGC00015748-04 |
NCGC00015748-15 |
NCGC00015748-09 |
NCGC00015748-07 |
NCGC00015748-14 |
NCGC00015748-08 |
NCGC00015748-10 |
NCGC00015748-12 |
NCGC00015748-05 |
nsc 757242 |
unii-i9zf7l6g2l |
nifedical |
hsdb 7775 |
nifedipine [usan:usp:inn:ban:jan] |
i9zf7l6g2l , |
dimethyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate |
5-22-04-00268 (beilstein handbook reference) |
nifedical xl |
nifelan |
niphedipine |
nifelat |
nifedin |
nifedicor |
nifensar xl |
FT-0630478 |
LP00819 |
nifedipine [inci] |
nifedipinum [who-ip latin] |
nifedipine [inn] |
nifedipine [jan] |
nifedipine [ep monograph] |
nifedipine [mart.] |
nifedipine [hsdb] |
nifedipine [usp monograph] |
nifedipine [usp impurity] |
nifedipine [orange book] |
nifedipine [vandf] |
nifedipine [who-dd] |
nifedipine [mi] |
nifedipine [usp-rs] |
nifedipine [who-ip] |
nifedipine [usan] |
S1808 |
BBL023163 |
BRD-K96354014-001-01-3 |
HY-B0284 |
NC00008 |
SCHEMBL3968 |
tox21_110212_1 |
NCGC00015748-17 |
4-(2'-nitrophenyl)-2,6 dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine |
4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine |
2,6-dimethyl-4-(2nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-dimethyl ester |
tox21_500819 |
NCGC00261504-01 |
Q-201471 |
nifedipine, british pharmacopoeia (bp) reference standard |
1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylicaciddimethylester |
HB1228 |
dimethyl (4-(2-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate) |
dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate # |
AB00052051_06 |
AB00052051_07 |
OPERA_ID_1816 |
mfcd00057326 |
bdbm50101817 |
F2173-0802 |
AC-8061 |
sr-01000075332 |
SR-01000075332-1 |
nifedipine, united states pharmacopeia (usp) reference standard |
KS-1456 |
HMS3651M19 |
EN300-120627 |
nifedipine, pharmaceutical secondary standard; certified reference material |
nifedipine, european pharmacopoeia (ep) reference standard |
SR-01000075332-3 |
SR-01000075332-6 |
SR-01000075332-4 |
SBI-0050796.P004 |
cpd000058291 |
HMS3712M07 |
Z90350374 |
SW219724-1 |
BCP21147 |
bay-1040;bay 1040;bay1040 |
nifedipine - cas 21829-25-4 |
nifedipine (adalat) |
HMS3676E17 |
nifedipine,(s) |
101539-70-2 |
HMS3412E17 |
Q39111 |
BRD-K96354014-001-10-4 |
SDCCGSBI-0050796.P005 |
NCGC00015748-33 |
HMS3748O21 |
FT-0672727 |
nsc786036 |
nsc-786036 |
SY074220 |
l-type calcium channel blocker iii |
AKOS037515769 |
dimethyl2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
A899873 |
193689-82-6 |
BN166183 |
PD003075 |
nifedipine (usp monograph) |
nifedicalxl |
nifedipineer |
nifedipina |
afeditabcr |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-, dimethyl ester |
nifedicalxlxl |
procardiaxl |
dimethyl 4-(o-nitrophenyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylate |
nifedipine (usp-rs) |
nifedipine (usp impurity) |
2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester |
4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsauredimethylester |
nifedipineextended release |
nifedipino (inn-spanish) |
nifediac cc |
nifedipinum (inn-latin) |
tn 873r |
nifedipine (mart.) |
c08ca05 |
nifedipine (ep monograph) |
nifedipine (usan:usp:inn:ban:jan) |
PD033039 |
natalensin |
hemanthamine |
Nifedipine (NIF) is a Class II drug of the Biopharmaceutical Classification System (BCS) with low oral bioavailability, low dissolution rate and significant hepatic drug metabolism. It is a calcium channel blocker in widespread clinical use for preterm labour.
Nifedipine has a high incidence of neurologic adverse reactions as compared with other dihydropyridine Cav1 (L-type) channel blockers. It has an inhibitory effect on morphine-induced corticosterone secretion and a greater blood pressure-lowering effect the higher the initial blood pressure.
Nifedipine (NFD) has been used for the treatment of cutaneous lesions caused by peripheral vascular disease and diabetic ulcers. NifedIPine possibly has potential to be used for host modulation of periodontal disease.
Nifedipine plays a role in increase of hydrophobic property, swelling degree and regular surface as well as decrease of surface rough of the nanoparticles. Nifesipine did not increase the odds of developing pulmonary edema.
Treatment with nifedipine resulted in a significant inhibition of the progression of AAA such as aneurismal dilation. Treatment with SOD mimetic decreased blood pressure and reduced left ventricular wall thickness without changes in the systolic function.
Excerpt | Reference | Relevance |
---|---|---|
"Nifedipine treatment reduced blood pressure (BP) in SHRSP, however, did not prevent salt-induced reduction in urinary UMOD excretion." | ( Salt loading decreases urinary excretion and increases intracellular accumulation of uromodulin in stroke-prone spontaneously hypertensive rats. Boder, P; Delles, C; Flynn, A; Graham, D; Graham, L; Kipgen, D; Mary, S; Rossitto, G; Scott, K, 2021) | 1.34 |
"Nifedipine treatment seems not to affect systolic or diastolic functions." | ( Fetal echocardiographic evaluation before and after nifedipine treatment in preterm labor. Goncu Ayhan, S; Menekse Beser, D; Oluklu, D; Sahin, D; Tugrul Ersak, D; Uyan Hendem, D; Yildirim, M, 2022) | 1.69 |
"Nifedipine treatment did not reduce gene expression or protein secretion of pro-inflammatory cytokines in either cultured myometrial cells or ex vivo tissues." | ( Assessment of the tocolytic nifedipine in preclinical primary models of preterm birth. Arman, BM; Beard, S; Binder, NK; de Alwis, N; Debruin, DA; Hannan, NJ; Hayes, A; Kaitu'u-Lino, TJ; Tong, S, 2023) | 1.93 |
"Nifedipine treatment (1, 5 μmol/l) dose-dependently increased the activity and intracellular expression of PPAR-β/-γ by inhibiting the release of PPAR-β/-γ from activated platelets." | ( Mechanisms of antiplatelet activity of nifedipine: role of peroxisome proliferator-activated receptor-β-γ-dependent processes. Chen, FC; Chou, TC; Fan, HC; Lin, MH; Shih, CY, 2014) | 1.39 |
"Nifedipine achieved treatment success in most women, similar to hydralazine (84% with nifedipine; relative risk [RR] 1.07, 95% confidence interval [95% CI] 0.98-1.17) or labetalol (100% with nifedipine; RR 1.02, 95% CI 0.95-1.09)." | ( Oral antihypertensive therapy for severe hypertension in pregnancy and postpartum: a systematic review. Firoz, T; Gordon, R; MacDonell, K; Magee, LA; Payne, BA; Vidler, M; von Dadelszen, P, 2014) | 1.12 |
"Nifedipine treatment substantially reduced lipid accumulation and the expression of CD36, SR-A, and protein kinase C (PKC)-θ in human macrophages treated with ox-LDL." | ( Nifedipine inhibits ox-LDL-induced lipid accumulation in human blood-derived macrophages. Sha Ma, AZ; Song, ZY; Tang, WQ; Wang, C; Zhang, Q, 2015) | 2.58 |
"Nifedipine pretreatment (10mg/kg, s.c.) also suppressed 2-Me-5-HT-evoked interaction of 5-HT3 receptors with CaM as well as phosphorylation of CaMKIIα and ERK1/2 in the least shrew brainstem, and 5-HT3 receptors -CaM colocalization in jejunum of the small intestine." | ( L-type calcium channels contribute to 5-HT3-receptor-evoked CaMKIIα and ERK activation and induction of emesis in the least shrew (Cryptotis parva). Chebolu, S; Darmani, NA; Hutchinson, TE; Wilson, SM; Zhong, W, 2015) | 1.14 |
"The nifedipine and heparin treated groups (B & C) did not show higher patency rate compared to the control group (A)." | ( The effect of nifedipine on the patency of microvascular anastomosis in rats. Antonopoulos, D; Kepenekidis, A; Koutsouris, M; Panagiotopoulos, E; Panagiotopoulos, KE; Panagiotopoulos, V; Papalois, A, 2008) | 1.19 |
"Nifedipine-treated animals displayed hemodynamics, LV dilatation, hypertrophy, and loss of function similar to those of the untreated group." | ( Comparative study of vasodilators in an animal model of chronic volume overload caused by severe aortic regurgitation. Arsenault, M; Beaudoin, J; Champetier, S; Couet, J; Lachance, D; Plante, E; Roussel, E, 2009) | 1.07 |
"Nifedipine treatment significantly improved acetylcholine-induced relaxation by 27% compared with the vehicle SHRSP group, but it was still significantly impaired by 20% compared with the WKY group." | ( Nifedipine activates PPARgamma and exerts antioxidative action through Cu/ZnSOD independent of blood-pressure lowering in SHRSP. Guo, F; Hashimoto, R; Itoh, S; Kishi, H; Kobayashi, S; Matsuzaki, M; Umeji, K; Umemoto, S, 2010) | 2.52 |
"Nifedipine treatment significantly reduced ischemic lesion volume (116.5 ± 10.8 vs." | ( Nifedipine treatment reduces brain damage after transient focal ischemia, possibly through its antioxidative effects. Honda, Y; Ide, T; Shiba, T; Tsutsui, H; Yamada, K; Yamato, M, 2011) | 2.53 |
"Nifedipine treatment increased expression of ferroportin 1 in the spleen, whereas splenic levels of the iron storage protein ferritin and serum iron concentrations were reduced." | ( Nifedipine affects the course of Salmonella enterica serovar Typhimurium infection by modulating macrophage iron homeostasis. Bellmann-Weiler, R; Fang, FC; Mair, SM; Moser, PL; Muehlbacher, T; Nairz, M; Schroll, A; Talasz, H; Theurl, I; Weiss, G, 2011) | 2.53 |
"Nifedipine treatment ameliorated the oxidative status and increased the number of EPCs in the DIO mice." | ( Nifedipine ameliorates ischemia-induced revascularization in diet-induced obese mice. Ishii, M; Kito, T; Kondo, M; Murohara, T; Shibata, R; Suzuki, H; Yamamoto, T, 2012) | 2.54 |
"Nifedipine (1-1.5 hr pretreatment), a blocker of L-type calcium channel, reduces the inhibitory effect of insulin in autumn and winter animals, and on the contrary intensifies it in summer animals." | ( [Possible reasons for the variability of the inotropic insulin effect in papillary muscles of ground squirrel myocardium]. Andreeva, LA; Anufriev, AI; Chumaeva, LA; Kukushkin, NI; Nakipova, OV, ) | 0.85 |
"Nifedipine treatment produced significant reduction in plasma DD and FM levels along with the increase in tPA level [DD: (40.7+/-23.5) mg/dl vs (23.8+/-16.5) mg/dl; FM: (7.0+/-1.6) ng/microliter vs (4.8+/-1.5) ng/microliter tPA: (0.31+/-0.14) ng/ml vs(0.41+/-0.05) ng/ml, P<0.001]." | ( [Coagulative and fibrinolytic changes in patients with essential hypertension and the effect of sustained-release nifedipine]. Chi, DS; Ge, B; Hong, XS; Jin, FX; Su, YW; Wu, BM; Yang, SG; Yu, RS, 2002) | 1.25 |
"In nifedipine treated patients blood flow through grafts to posterior interventricular, anterior interventricular, anterior interventricular and diagonal branches rose by 61.2, 37.4, and 102.9%, respectively. " | ( [Postoperative spasm of mammary-coronary grafts and possibilities of its correction by dihydropyridine calcium antagonists nifedipine and amlodipine]. Dzhavadova, GK; Mamchur, SE; Nemik, BM; Tepliakov, AT; Vecherskiĭ, IuIu, 2002) | 1.14 |
"Nifedipine-treated patients were also less likely to have diabetes or have secondary events (a composite of all-cause mortality, death from a vascular cause, and death from a nonvascular cause) than co-amilozide recipients." | ( Outcomes with nifedipine GITS or Co-amilozide in hypertensive diabetics and nondiabetics in Intervention as a Goal in Hypertension (INSIGHT). Brown, M; Castaigne, A; de Leeuw, P; Mancia, G; Palmer, CR; Rosenthal, T; Ruilope, LM; Wagener, G, 2003) | 1.4 |
"Nifedipine-untreated and dimethylsulfoxide (DMSO)-treated animals served as control groups." | ( Effect of nifedipine on the expression of bcl-2 protein in rat gingiva. Handajani, J; Haniastuti, T; Santoso, AL; Sosroseno, W; Utoro, T, 2003) | 1.44 |
"Nifedipine treatment led to a significant decrease in concentrations of sVCAM-1, carbonyl residues, and AOPP but did not affect concentrations of VEGF and sVEGFR-1." | ( Nifedipine decreases sVCAM-1 concentrations and oxidative stress in systemic sclerosis but does not affect the concentrations of vascular endothelial growth factor or its soluble receptor 1. Allanore, Y; Borderie, D; Ekindjian, OG; Kahan, A; Lemaréchal, H, 2004) | 2.49 |
"Nifedipine treatment or removal of external calcium (Cao2+) reduced the norepinephrine-induced peak response." | ( Enhanced response to AVP in the interlobular artery from the spontaneously hypertensive rat. Hansen, FH; Iversen, BM; Vågnes, ØB, 2005) | 1.05 |
"Nifedipine treatment decreased the brain nNOS activity, induced by multiple administration of morphine." | ( Effects of nifedipine on behavioral and biochemical parameters in rats after multiple morphine administration. Mitcheva, M; Vitcheva, V, 2004) | 1.43 |
"Nifedipine treatment considerably decreased O2*- production by PMA-stimulated monocytes." | ( Nifedipine protects against overproduction of superoxide anion by monocytes from patients with systemic sclerosis. Allanore, Y; Borderie, D; Ekindjian, OG; Kahan, A; Lemaréchal, H; Périanin, A, 2005) | 2.49 |
"Nifedipine treatment led to a significant increase in the MRI perfusion index (mean (SD) 0.26 (0.07) v 0.19 (0.05) at baseline, p = 0.0003) and in systolic and diastolic strain rate (2.3 (0.6) v 1.5 (0.4) s(-1) at baseline, p = 0.0002, and 4.2 (1.6) v 3.0 (1.2) at baseline, p = 0.0003, respectively)." | ( Evaluation of the effect of nifedipine upon myocardial perfusion and contractility using cardiac magnetic resonance imaging and tissue Doppler echocardiography in systemic sclerosis. Allanore, Y; Duboc, D; Kahan, A; Legmann, P; Meune, C; Pascal, O; Vignaux, O; Weber, S, 2005) | 2.07 |
"Does nifedipine treatment reduce the development and progression of diabetic vascular complications? If the answer is yes, is this beneficial effect of nifedipine superior than that of other DHPs with equihypotensive properties? Does nifedipine treatment decrease the incidence of melanoma and/or prolong the survival of patients with this devastating disorder? These prospective studies will provide further valuable information whether blockade by nifedipine of the AGE-RAGE signaling could be clinically relevant." | ( Potential therapeutic implication of nifedipine, a dihydropyridine-based calcium antagonist, in advanced glycation end product (AGE)-related disorders. Nakamura, K; Takeuchi, M; Yamagishi, S, 2005) | 1.06 |
"Nifedipine-treated obese males showed a mild but significant decrease in weight gain that was due to a decrease in fat deposition in both subcutaneous and abdominal depots and systolic blood pressure was significantly reduced after one month of treatment." | ( Treatment of obese female and male SHHF/Mcc-fa(cp) rats with antihypertensive drugs, nifedipine and enalapril: effects on body weight, fat distribution, insulin resistance and systolic pressure. Chu, YY; Hoepf, TM; McCune, SA; Radin, MJ, 1993) | 1.23 |
"Nifedipine-treated cells also showed a decrease in cytosolic cytochrome c release and a decrease in caspase 3 activation, compared to cells treated only with Rec-1 antibody." | ( Anti-recoverin antibodies induce an increase in intracellular calcium, leading to apoptosis in retinal cells. Adamus, G; Duvoisin, RM; Shiraga, S; Webb, S, 2006) | 1.06 |
"Nifedipine treatment significantly changed the PI and S/D ratio (mean +/- SEM) of the uterine (PI from 0.66 +/- 0.01 to 0.51 + 0.01; SID ratio: from 2.00 +/- 0.09 to 1.79 + 0.05) and umbilical (PI: from 1.55 +/- 0.04 to 1.40 +/- 0.02; S/D ratio: from 2.45 +/- 0.09 to 2.31+/- 0.09) arteries and the middle cerebral PI (from 1.45 +/- 0.03 to 1.61 +/- 0.01) artery only in PIH, but not in PE patients." | ( Mid-trimester fetal-placental velocimetry response to nifedipine may predict early the onset of pre-eclampsia. Cobellis, G; Cobellis, L; Colacurci, N; De Luca, A; Di Pietto, L; Fornaro, F; Iannella, I; Mastrogiacomo, A; Pecori, E; Scaffa, C, ) | 1.1 |
"nifedipine-treated) but was still higher than in normal, ramipril-, or losartan-treated rats." | ( Role of angiotensin II in retinal leukostasis in the diabetic rat. Chen, P; Dahl, D; Edwards, PA; Fenstermacher, JD; Guo, M; Scicli, AG; Scicli, GM, 2006) | 1.06 |
"Does nifedipine treatment alone decrease the progression of renal disease with overt proteinuria? If these answers are yes, are these beneficial effects of nifedipine superior to that of other DHPs with equihypotensive properties? Does nifedipine treatment also reduce oxidative stress markers? Are these unique effects of nifedipine correlated with its anti-oxidative properties? These prospective studies will provide further valuable information whether nifedipine may be a preferred DHP to achieve BP goals in hypertensive patients with systolic dysfunction or overt proteinuria." | ( Revival of nifedipine, a dihydropyridine-based calcium blocker. Nakamura, K; Yamagishi, S, 2007) | 1.18 |
"Does nifedipine treatment slow down the progression of coronary calcification in diabetic patients? If the answer is yes, is this beneficial effect of nifedipine superior to that of other DHPs with equihypotensive properties? Does nifedipine treatment decrease expression levels of AGEs and RAGE in diabetic atherosclerosis? Is the unique effect of nifedipine on vascular calcification correlated with its AGE or RAGE-suppressing properties? These prospective studies will provide further valuable information whether nifedipine could prevent vascular calcification in diabetic atherosclerosis by blockade the AGE-RAGE signaling in vascular wall cells." | ( Prevention of diabetic vascular calcification by nifedipine, a dihydropyridine-based calcium channel blocker. Matsui, T; Nakamura, K; Yamagishi, S, 2007) | 1.05 |
"Nifedipine treatment also led to a lack of Ca(2+) increase in response to ACh stimulation, while ryanodine treatment led to a weak Ca(2+)-increase response." | ( Mechanism of Ca2+ increase in myoblasts derived from chicken embryos. Ikeda, M; Ikeuchi, Y; Iwamoto, H; Kobayashi, M; Nishimura, S; Sato, Y; Tabata, S; Takemura, Y; Tatsumi, R, 2006) | 1.06 |
"Nifedipine treatment decreased serum insulin level to one fifth of that in KK-A(y) mice without nifedipine." | ( Diabetes-associated cognitive impairment is improved by a calcium channel blocker, nifedipine. Fujita, T; Horiuchi, M; Iwai, M; Iwanami, J; Li, JM; Min, LJ; Mogi, M; Sakata, A; Tsukuda, K, 2008) | 1.29 |
"In nifedipine-treated rats, the pressor actions of guanabenz and clonidine were virtually abolished, while the onset of the depressor responses were significantly accelerated." | ( Effects of nifedipine on the hypotensive actions of alpha 2-agonists in conscious spontaneously hypertensive rats. Lappe, RW; Saslow, BA; Wendt, RL, 1984) | 1.17 |
"Nifedipine treatment lowered PLV from 170 to 136 mm Hg and Tsyst from 222 to 194 10(3) dyn/cm2." | ( Influence of nifedipine on ventricular function and myocardial hypertrophy in spontaneously hypertensive rats. Garthoff, B; Goeldel, N; Kazda, S; Motz, W; Ploeger, M; Ringsgwandl, G; Strauer, BE, ) | 1.22 |
"Nifedipine treatment failed to prevent progression of threatened infarction to AMI or to reduce infarct size in patients with AMI." | ( Nifedipine in acute myocardial infarction. Pearle, DL, 1984) | 2.43 |
"Nifedipine pretreatment inhibited the cessation of coronary flow." | ( Nifedipine on cardiovascular leukotriene D4 actions in the anaesthetized dog. Abram, TS; Fiedler, VB; Mardin, M, 1984) | 2.43 |
"Nifedipine treatment increased cardiac output (mean +/- SD, 3.6 +/- 1.7 to 5.3 +/- 2.8 L/min, p less than 0.001) and decreased mean aortic pressure (99 +/- 19 to 85 +/- 12 mm Hg, p less than 0.001) and total pulmonary and total systemic resistances (1605 +/- 787 to 1025 +/- 540 dyn X s X cm-5 and 2761 +/- 1557 to 1591 +/- 823 dyn X s X cm-5, respectively; p less than 0.005)." | ( Treatment of primary pulmonary hypertension with nifedipine. A hemodynamic and scintigraphic evaluation. Firth, BG; Hillis, LD; Nicod, P; Rubin, LJ, 1983) | 1.24 |
"The nifedipine treatment gave excellent or good results in a large majority of patients of both groups." | ( Clinical and manometric effects of nifedipine in patients with esophageal achalasia. Bortolotti, M; Labò, G, 1981) | 1.02 |
"Nifedipine treatment prior to APAP exposure, partially prevented LDH release, the plasma membrane blebbing, and thereby the loss of viability." | ( Protective effect of nifedipine against cytotoxicity and intracellular calcium alterations induced by acetaminophen in rat hepatocyte cultures. Claude, JR; Dutertre-Catella, H; Ellouk-Achard, S; Mawet, E; Thevenin, M; Thibault, N, ) | 1.17 |
"Nifedipine treatment significantly prevented STZ-induced increase in cholesterol and triglyceride levels." | ( Effects of chronic nifedipine treatment on streptozotocin-induced diabetic rats. Bangaru, RA; Gandhi, TP; Goyal, RK; Satia, MC; Shah, TS, 1995) | 1.34 |
"The Nifedipine-treated hypoplastic lungs showed a normal branching pattern, suggesting that airway contractions and calcium channel function are not necessary for cleft formation directly." | ( Effects of calcium channel blockade on mammalian lung branching morphogenesis. Roman, J, ) | 0.61 |
"2. Nifedipine pretreatment (1 nM-0.1 microM) reduced both types of phasic contractions in a concentration-dependent manner." | ( Pharmacological reactivity of human epicardial coronary arteries: phasic and tonic responses to vasoconstrictor agents differentiated by nifedipine. Cocks, TM; Stork, AP, 1994) | 1.01 |
"Nifedipine treatment did not modify the locomotion ratio (with a mean +/- SEM ratio of 0.66 +/- 0.12 for control and 0.45 +/- 0.08 for nifedipine-treated group) nor the rearing ratio (with a mean +/- SEM ratio of 0.51 +/- 0.12 for control and 0.62 +/- 0.18 for nifedipine-treated group)." | ( Effect of withdrawal from long-term nifedipine administration on open-field habituation in the rat. Chang, YH; Conceição, IM; Frussa-Filho, R; Maioline Júnior, M; Mattia, NF; Smaili, S, 1994) | 1.28 |
"Nifedipine treatment per se significantly increased circulating noradrenaline in both the primary Raynaud's phenomenon patient group and in the control group (from 0.29 +/- 0.15 to 0.49 +/- 0.13 and 0.21 +/- 0.14 to 0.43 +/- 0.21 ng/ml, respectively, p < 0.001)." | ( Sympathetic activation after two weeks of nifedipine treatment in primary Raynaud's patients and controls. Edvinsson, L; Hedner, T; Leppert, J; Myrdal, U; Nilsson, H; Ringqvist, I, 1993) | 1.27 |
"Nifedipine treatment caused a significant reduction of UAER after 6 and 12 months (median, Q1/Q3 in mg/24 h): baseline 84 (65/163); 6 months 35 (23/90), P < 0.02; 12 months 39 (15/79), P < 0.05)." | ( Long-term treatment with nifedipine reduces urinary albumin excretion and glomerular filtration rate in normotensive type 1 diabetic patients with microalbuminuria. Banyai, M; Capek, M; Kautzky-Willer, A; Prager, R; Schernthaner, G; Schnack, C, 1994) | 1.31 |
"Nifedipine treatment did not affect resting state free calcium levels in these cells." | ( Effect of nifedipine on calcium status and chemiluminescence response of phagocytes during Plasmodium berghei infection in mice. Dubey, ML; Ganguly, NK; Kalra, A; Mahajan, RC, 1993) | 1.41 |
"The nifedipine-treated artery displayed neither EDRC upon phenylephrine stimulation nor EIRC by the addition of ryanodine or CPA: however, these agents relaxed the arteries." | ( The role of sarcoplasmic reticulum in endothelium-dependent and endothelium-independent rhythmic contractions in the rabbit mesenteric artery. Mizusawa, H; Omote, M, 1993) | 0.77 |
"The nifedipine-treated rats (experimental group) were fed a caries-inducing diet containing nifedipine either with or without infection, while the nifedipine-untreated rats (control group) were fed the same diet, similarly with or without the infection." | ( Nifedipine-induced gingival overgrowth in the presence or absence of gingival inflammation in rats. Ishida, H; Kato, K; Loyola-Rodriguez, JP; Morisaki, I; Nagata, T, 1993) | 2.21 |
"3. Nifedipine-treatment and Ca(2+)-deprivation inhibited the high K(+)-induced inositol polyphosphate accumulation but failed to inhibit the Ang II-induced inositol polyphosphate accumulation." | ( Characteristics of inositol polyphosphate metabolism in cultured adrenal chromaffin cells. Kato, R; Nakaki, T; Sasakawa, N, 1993) | 0.8 |
"Nifedipine treatment was started at 48 weeks and concluded at 60 weeks." | ( Alterations in cardiac myosin isozymes associated with aging and chronic hypertension: their modulation with nifedipine. Blomquist, TM; Minser, R; Pathak, D; Raizada, V; Woodfin, B, 1993) | 1.22 |
"Nifedipine-treated groups also had a significant fall in blood pressure which was controlled by rehydration." | ( Enhancement of the epidural morphine-induced analgesia by systemic nifedipine. Dos Reis, MP; Pereira, IT; Prado, WA, 1993) | 1.24 |
"Nifedipine treatment did not alter these parameters of controls, but decreased the heart weight and heart weight-to-body weight ratio of diabetic rats without affecting the body weight." | ( Impaired mechanical response to calcium of diabetic rat hearts: reversal by nifedipine treatment. Higa, S; Murakami, K; Nagamine, F; Shimabukuro, M; Shinzato, T; Takasu, N, 1995) | 1.24 |
"Nifedipine treatment completely reversed diabetes-induced prolongation in both time-to-peak tension and time-to-90% relaxation." | ( Influence of calcium channel blocker treatment on the mechanical properties of diabetic rat myocardium. Brown, RA; Lee, MM; Savage, AO; Sundareson, AM; Woodbury, DJ, 1996) | 1.02 |
"In nifedipine-treated non-pregnant controls, only EC80 for adrenaline-induced aggregation decreased." | ( Nifedipine reduces thromboxane A2 production by platelets without changing aggregation in hypertensive pregnancy. Manninen, A, 1996) | 2.25 |
"Nifedipine treatment diminished the number of severe clinical outcomes in elderly hypertensives significantly." | ( Shanghai trial of nifedipine in the elderly (STONE). Ghadirian, P; Gong, L; Hamet, P; Kong, D; LeLorier, J; Pagé, V; Zhang, W; Zhu, J; Zhu, Y, 1996) | 2.07 |
"Nifedipine treatment resulted in an 18% decrease in fat pad weights (P<0.007) and a 74% decrease in adipose FAS activity (P=0.03), normalized circulating insulin levels and insulin sensitivity (P<0.05), and transiently elevated core temperature in the transgenic mice, but was without effect in the control mice." | ( The effects of calcium channel blockade on agouti-induced obesity. Kim, JH; Moore, JW; Moustaid, N; Mynatt, RL; Woychik, RP; Zemel, MB, 1996) | 1.02 |
"Nifedipine treatment (1 microM) both reduced intracellular calcium and decreased delta subunit mRNA expression by 79 +/- 4%." | ( Expression of the GABAA receptor delta subunit is selectively modulated by depolarization in cultured rat cerebellar granule neurons. Gault, LM; Siegel, RE, 1997) | 1.02 |
"Nifedipine pretreatment attenuated the ET-1-induced fall in renal blood flow (from 1088+/-93 to 907+/-68 mL/min) and increase in renal vascular resistance (from 105+/-9 to 133+/-10 mm Hg x min/L)." | ( Endothelin-1-induced vasopressor responses in essential hypertension. Kaasjager, KA; Koomans, HA; Rabelink, TJ, 1997) | 1.02 |
"Nifedipine and enalapril treatment produced increase in insulin sensitivity in these animals." | ( Effect of nifedipine and enalapril on insulin-induced glucose disposal in spontaneous hypertensive and diabetic rats. Goyal, RK; Mehta, AA; Patel, S; Santani, DD, ) | 1.26 |
"Nifedipine treatment has a favourable effect on the clinical course of patients with mild hyperinsulinism. " | ( Treatment of hyperinsulinaemic hypoglycaemia with nifedipine. Eichmann, D; Hufnagel, M; Quick, P; Santer, R, 1999) | 2 |
"Both nifedipine treatments did neither greatly modify the circadian blood pressure pattern nor reflexly increase heart rate." | ( Ambulatory blood pressure profiles in essential hypertensives after treatment with a new once daily nifedipine formulation. Herholz, C; Hopf, R; Lemmer, B; Nold, G; Sturm, M, 1999) | 0.97 |
"Nifedipine treatment for 5 days significantly reduced the blood pressure in cadmium-hypertensive and normotensive rats." | ( The effects of short-term nifedipine treatment on responsiveness of aortic rings of cadmium-hypertensive rats. Oğütman, C; Ozdem, SS, 1999) | 1.32 |
"Nifedipine treatment attenuated pulmonary hypertension in chronically hypoxic newborn piglets despite the persistence of blunted responses to acetylcholine and reduced lung eNOS amounts." | ( Nifedipine inhibits pulmonary hypertension but does not prevent decreased lung eNOS in hypoxic newborn pigs. Fike, CD; Kaplowitz, MR, 1999) | 2.47 |
"Nifedipine treatment in both young and adult hypertensive rats prevented the V3 rise due to hypertension and to the aging process." | ( Age-related difference in cardiac adaptation to chronic hypertension in rats, with and without nifedipine treatment. Malhotra, A; Nakouzi, A; Pathak, D; Raizada, V; Skipper, B, 1999) | 1.24 |
"Nifedipine treated mice behaved as controls." | ( GM1 ganglioside induced myocardial restoration and survival of mice with experimental Chagas' disease. Bronia, DH; Cossy Isasi, S; Fernandez, AR; Paglini, P, 1999) | 1.02 |
"Nifedipine for treatment of preterm labor was associated with a lower incidence of neonatal morbidity than ritodrine. " | ( Neonatal effects of nifedipine and ritodrine for preterm labor. Adèr, HJ; Bleker, OP; Dekker, GA; Kok, JH; Papatsonis, DN; van Geijn, HP, 2000) | 2.07 |
"Nifedipine pretreatment or coadministration with L-NAME limited P(A) resetting or suppressed autoregulation at higher doses." | ( Effects of Ca(2+) channel activity on renal hemodynamics during acute attenuation of NO synthesis in the rat. Caron, N; El Hajjam, A; Fourmanoir, P; Gerbaux, C; Joly, E; Kramp, RA; Ladrière, L, 2000) | 1.03 |
"Nifedipine-treated participants showed a 66% reduction in verified attacks compared with placebo recipients (P<.001); temperature biofeedback training did not reduce attacks significantly compared with control biofeedback (P = .37). " | ( Comparison of sustained-release nifedipine and temperature biofeedback for treatment of primary Raynaud phenomenon. Results from a randomized clinical trial with 1-year follow-up. , 2000) | 2.03 |
"Nifedipine treatment decreased circulating plasma lipoperoxides and isoprostanes and increased plasma antioxidant capacity." | ( Restoration of nitric oxide availability after calcium antagonist treatment in essential hypertension. Favilla, S; Ghiadoni, L; Magagna, A; Pompella, A; Salvetti, A; Taddei, S; Virdis, A, 2001) | 1.03 |
"Nifedipine treatment was also associated with increased urinary sodium excretion." | ( Altered expression of renal aquaporins and Na(+) transporters in rats treated with L-type calcium blocker. Flyvbjerg, A; Frøkiaer, J; Knepper, MA; Kwon, TH; Li, C; Nielsen, S; Wang, W, 2001) | 1.03 |
"Nifedipine treatment reduced mPer1 induction, suggesting that mPer1 mRNA expression depends on intracellular calcium concentration regulated through a voltage-dependent Ca2+ channel." | ( Calcium and pituitary adenylate cyclase-activating polypeptide induced expression of circadian clock gene mPer1 in the mouse cerebellar granule cell culture. Akiyama, M; Minami, Y; Moriya, T; Nakajima, T; Shibata, S, 2001) | 1.03 |
"Nifedipine and CGP 28392 treatment of nonpregnant and pregnant animals, respectively, did not modify the response of aortic rings to KCl." | ( Calcium channels contribute to the decrease in blood pressure of pregnant rats. Brochu, M; Cadorette, C; Poterek, M; Simaan, M; St-Louis, J, 2002) | 1.04 |
"Nifedipine pretreatment had no influence on oxygen delivery in placenta and fetal cerebrum during and after ischemia." | ( Short therapeutic window for nifedipine in transient intrauterine ischemia in fetal rat brain. Araki, T; Koshino, T; Nagano, R; Nakai, A; Oya, A; Shibazaki, Y; Taniuchi, Y, 2002) | 1.33 |
"Nifedipine treatment reduced the weekly number of anginal attacks as well as the weekly number of nitroglycerin tablets consumed by the pts, increased maximum workload tolerated and reduced the S-T segment depression for the same workload, meanwhile heart rate and blood pressure did not change significantly either at rest or during exercise." | ( [Effects of nifedipine in the treatment of effort stable angina: a double blind study (author's transl)]. Bonaduce, D; Carlomagno, A; Condorelli, M; De Caprio, L; Petretta, M; Rengo, F; Scarafile, P, 1978) | 1.36 |
"Nifedipine treatment had no significant effect on conduction velocity in non-diabetic rats." | ( The effect of the calcium antagonist nifedipine on peripheral nerve function in streptozotocin-diabetic rats. Cameron, NE; Cotter, MA; Robertson, S, 1992) | 1.28 |
"Nifedipine treatment did not alter basal, pulsatile, or TRH-stimulated PRL secretion." | ( Hypothalamic regulation of pulsatile thyrotopin secretion. Brabant, G; Hesch, RD; Hoang-Vu, C; Prank, K; von zur Mühlen, A, 1991) | 1 |
"Nifedipine pretreatment attenuated some subjective effects of cocaine." | ( Effects of nifedipine pretreatment on subjective and cardiovascular responses to intravenous cocaine in humans. Jaffe, JH; Kumor, KM; Muntaner, C; Nagoshi, C, 1991) | 1.39 |
"Nifedipine treatment did not modify plasma ANP values, whereas it increased PRA and PA circulating levels and urinary catecholamine excretion." | ( Short-term effects of atenolol and nifedipine on atrial natriuretic peptide, plasma renin activity, and plasma aldosterone in patients with essential hypertension. Bucci, V; Casale, R; Colantonio, D; Desiati, P; Giandomenico, G; Pasqualetti, P, 1991) | 1.28 |
"Nifedipine pretreatment prevented the early cocaine-induced decrease in coronary blood flow and improved left ventricular dP/dt compared with untreated control animals." | ( Nifedipine protects the heart from the acute deleterious effects of cocaine if administered before but not after cocaine. Alker, KJ; Eisenhauer, AC; Hale, SL; Kloner, RA; Rezkalla, SH, 1991) | 2.45 |
"Oral nifedipine retard treatment to suppress preterm labour was administered to 8 patients using a new scheme. " | ( Long term treatment with nifedipine retard to suppress preterm labour. Ghirardini, G, 1991) | 1.1 |
"Nifedipine treatment abolished the signs of abstinence and normalized the hot-plate latencies in morphine-dependent, naloxone-treated rats." | ( Cortical dihydropyridine binding sites and a behavioral syndrome in morphine-abstinent rats. Antkiewicz-Michaluk, L; Michaluk, J; Romańska, I; Vetulani, J, 1990) | 1 |
"Nifedipine treatment results in uniform or irregular CTC fluorescence." | ( Nifedipine-sensitive calcium channels are involved in polar growth of lily pollen tubes. Herth, W; Reiss, HD, 1985) | 2.43 |
"With nifedipine treatment, LAD flow (flow probe) was increased 44% as compared with the initial occluded value, with most of this increase going to the subepicardium (microspheres)." | ( Effect of nifedipine on regional O2 consumption in ischemic myocardial tissue. Grover, GJ; Mackenzie, JW; Scholz, P; Weiss, HR, 1988) | 1.13 |
"Nifedipine pretreatment markedly prevented this change induced by the abstinence syndrome." | ( Nifedipine reversal of decreased serotonin metabolite levels during morphine withdrawal. Colado, MI; Lorenzo, P; Martín, MI, ) | 2.3 |
"The nifedipine-treated animals maintained a high CO and low SVR." | ( Effects of nifedipine on the hemodynamic response to clamping and declamping of the abdominal aorta in dogs. Baele, H; Bastulli, JA; Dauchot, PJ; Derrer, SA; Rhodes, RS, 1989) | 1.15 |
"Nifedipine treatment resulted in variable improvement in tardive dyskinesia in eight geriatric psychiatric patients. " | ( Calcium channel blockers for tardive dyskinesia in geriatric psychiatric patients. Kushnir, SL; Ratner, JT, 1989) | 1.72 |
"With nifedipine treatment, diastolic function improved, with a decrease in the time to peak filling rate (PFR) at rest (from 174 +/- 34 to 152 +/- 31 ms, p less than 0.005) and an increase in PFR with exercise (from 2.5 +/- 0.6 to 3.4 +/- 0.7 end-diastolic volume/s, p less than 0.0005)." | ( Addition of nifedipine to maximal nitrate and beta-adrenoreceptor blocker therapy in coronary artery disease. Antman, EM; Holman, BL; Nesto, RW; Polak, JF; White, HD; Wynne, J, 1985) | 1.1 |
"Six nifedipine-treated patients reached target blood pressure, compared with one patient with ketanserin (P less than 0.02)." | ( Comparison of ketanserin and slow-release nifedipine added to the treatment of hypertensive patients uncontrolled by a thiazide diuretic plus beta-adrenoceptor blocker. Ramsay, LE; Solomon, SA; Waller, PC, 1987) | 1.02 |
"Nifedipine pretreatment delayed the development of cardiovascular derangement and reduced the severity of the intestinal but not the gastric mucosal injury." | ( Effects of a calcium antagonist (nifedipine) on cats in live E. coli bacteriemic shock. Bosson, S; Fält, K; Haglund, U, 1988) | 1.28 |
"Nifedipine treatment as an independent therapy is primarily indicated to patients showing spastic rheoencephalographic changes." | ( [Effect of an acute pharmacological test and a course of treatment with nifedipine on cerebral hemodynamic indices and information processing efficiency in hypertension patients]. Liventseva, MM; Nechesova, TA; Pavlova, AI; Sidorenko, GI, 1988) | 1.23 |
"Nifedipine treatment reduced mean total theophylline clearance by 9%, due to decreased clearances via 1- and 3-demethylation." | ( Selective inhibitory effects of nifedipine and verapamil on oxidative metabolism: effects on theophylline. Birkett, DJ; Miners, JO; Robson, RA, 1988) | 1.28 |
"Nifedipine pretreatment also increased the rates of excretion of various electrolytes and water followed by significantly lower plasma sodium, potassium, phosphate, and normal glucose values." | ( Effect of nifedipine on carbohydrate metabolism in the rat. Haag, M; Heidland, A; Hörl, WH; Riegel, W, 1987) | 1.4 |
"Treatment with Nifedipine (Ca" | ( Cocaine-induced ischemia in prefrontal cortex is associated with escalation of cocaine intake in rodents. Allen, CP; Du, C; Koob, GF; Pan, Y; Park, K; Volkow, ND; You, J, 2020) | 0.9 |
"Treatment with nifedipine in women with threatened preterm birth results in lower costs when compared with treatment with atosiban. " | ( Cost effectiveness of nifedipine compared with atosiban in the treatment of threatened preterm birth (APOSTEL III trial). Bloemenkamp, K; de Boer, MA; Franx, A; Gyselaers, W; Kok, M; Mol, B; Nijman, T; Oudijk, MA; Porath, MM; Sueters, M; van Baaren, GJ; van Vliet, E; Woiski, M, 2019) | 1.18 |
"Treatment with nifedipine reduced collagen-induced NF-κB events, including the phosphorylation of IκB kinase-β, IκBα and p65NF-κB, which were markedly attenuated by GSK0660, a PPAR-β antagonist, or GW9662, a PPAR-γ antagonist." | ( Antiplatelet activity of nifedipine is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity. Chen, FC; Chou, TC; Ding, JC; Lin, IH; Shih, CY, 2014) | 1.05 |
"Pre-treatment with nifedipine (1µM) did not affect responses to low concentrations of endothelin-1 but decreased Emax, while NNC 55-0396 (1µM) and SK&F 96365 (30-100µM) generally attenuated the endothelin-1-induced contraction." | ( The role of voltage-operated and non-voltage-operated calcium channels in endothelin-induced vasoconstriction of rat cerebral arteries. Angus, JA; Mamo, YA; Soeding, PF; Wright, CE; Ziogas, J, 2014) | 0.72 |
"Pretreatment with nifedipine not only significantly blocked the enhancing effects of DOB on LPS-induced elevation in cytosolic Ca(2+) concentration and CaMKII phosphorylation in cardiomyocytes, but also partly reversed the effects of DOB on caspase-9 and caspase-3/7 activities in LPS-treated cardiomyocytes." | ( β₁-adrenoceptor stimulation promotes LPS-induced cardiomyocyte apoptosis through activating PKA and enhancing CaMKII and IκBα phosphorylation. Li, H; Lu, D; Lv, X; Wang, H; Wang, Y; Yang, D; Yu, X, 2015) | 0.74 |
"Pre-treatment with nifedipine (10(-8) M), tetraethylammonium (10(-3) M), and theophylline (10(-5) M) attenuated the contracting effect of d- and l-limonene, while in the presence of paxilline (10(-5) M) d- and l-limonene were ineffective. " | ( Effects of d- and l-limonene on the pregnant rat myometrium in vitro. Gáspár, R; Hajagos-Tóth, J; Hódi, Á; Seres, AB, 2015) | 0.75 |
"Treatment with nifedipine exerted a strong influence on the activation and inactivation rate of Kv currents as well as an obvious leftward shift in the inactivation curve. " | ( The inhibitory effects of nifedipine on outward voltage-gated potassium currents in mouse neuroblastoma N2A cells. Li, K; Li, XQ; Li, XT; Qiu, XY, 2016) | 1.09 |
"Treatment with nifedipine, an inhibitor of L-type Ca(2+) channels, abrogated GDF-15-induced increases in [Ca(2+)]i and ICa The GDF-15-induced increase in ICa was mediated via up-regulation of the Cav1.3 α subunit, which was attenuated by inhibiting Akt/mTOR and ERK (extracellular-signal-regulated kinase) pathways and by pharmacological inhibition of Src-mediated TβRII phosphorylation." | ( GDF-15 enhances intracellular Ca2+ by increasing Cav1.3 expression in rat cerebellar granule neurons. Fang, YJ; Hu, C; Lu, JM; Mei, YA; Wang, CY, 2016) | 0.77 |
"Pretreatment with nifedipine attenuated anemoside A(3)-induced relaxation." | ( Anemoside A3-induced relaxation in rat renal arteries: role of endothelium and Ca2+ channel inhibition. Fan, CL; Huang, Y; Lau, CW; Li, Y; Lin, SM; Wang, J; Ye, WC; Yiu, A; Zhang, DM, 2010) | 0.68 |
"Treatment with nifedipine or removal of extracellular Ca(2+) reduced the thrombin-mediated increase of [Ca(2+)](i) in wild-type SMCs, whereas the response in Nox1 null SMCs was unchanged." | ( Activation of NADPH oxidase 1 increases intracellular calcium and migration of smooth muscle cells. Banfi, B; Bhalla, RC; Jagadeesha, DK; Miller, FJ; Stanic, B; Takapoo, M; Zimmerman, MC, 2011) | 0.71 |
"Treatment with nifedipine could improve the apomorphine-induced rotation behavior in 6-OHDA-lesioned rats." | ( L-type Cav1.2 calcium channel is involved in 6-hydroxydopamine-induced neurotoxicity in rats. Ma, Z; Wang, J; Wang, R; Xie, J, 2012) | 0.72 |
"Treatment with nifedipine accelerated angiogenic repair in the DIO mice to a level equal to that seen in the control mice." | ( Nifedipine ameliorates ischemia-induced revascularization in diet-induced obese mice. Ishii, M; Kito, T; Kondo, M; Murohara, T; Shibata, R; Suzuki, H; Yamamoto, T, 2012) | 2.16 |
"Treatment with nifedipine." | ( Syncope and Raynaud's disease. Angus-Leppan, H; Guiloff, RJ; Rajakulendran, S, 2012) | 0.73 |
"Treatment with nifedipine stopped recurrent syncope in all patients." | ( Syncope and Raynaud's disease. Angus-Leppan, H; Guiloff, RJ; Rajakulendran, S, 2012) | 0.72 |
"Treatment with nifedipine-telmisartan significantly decreased mean systolic and diastolic ambulatory blood pressure and resulted in a significant increase in sRAGE plasma concentrations after 24 weeks of therapy." | ( Microalbuminuria and sRAGE in high-risk hypertensive patients treated with nifedipine/telmisartan combination treatment: a substudy of TALENT. Boiocchi, C; Bozzini, S; Buzzi, MP; Choi, J; D'Angelo, A; Esposito, C; Falcone, C; Mancia, G; Ochan Kilama, M; Schirinzi, S; Torreggiani, M, 2012) | 0.95 |
"Treatment with nifedipine in rats led to the inducement of gingival hyperplasia and increase in the numbers of p53-positive gingival epithelial cells by a dose and frequency dependent mechanism, suggesting that p53 protein may play a crucial role in the regulation of nifedipine-induced gingival hyperplasia." | ( Effect of nifedipine on the expression of p53 protein in rat gingiva. Agustina, D; Agustiono, P; Haniastuti, T; Santoso, AS; Sosroseno, W, 2002) | 1.06 |
"Treatment with nifedipine was associated with decrease of graft systolic-diastolic index by 20.2, 20.7, 19.9%, respectively, treatment with amlodipine--by 27.3, 20.6, 32.9%, respectively." | ( [Postoperative spasm of mammary-coronary grafts and possibilities of its correction by dihydropyridine calcium antagonists nifedipine and amlodipine]. Dzhavadova, GK; Mamchur, SE; Nemik, BM; Tepliakov, AT; Vecherskiĭ, IuIu, 2002) | 0.86 |
"Treatment of nifedipine or culture in Ca2+-free media suppressed contraction of cardiomyocytes and inhibited skeletal muscle cells to express cardiac-specific proteins." | ( Beating is necessary for transdifferentiation of skeletal muscle-derived cells into cardiomyocytes. Akazawa, H; Iijima, Y; Komuro, I; Matsuura, K; Mizukami, M; Nagai, T; Nakaya, H; Ogura, T; Takano, H; Toko, H; Wada, H, 2003) | 0.67 |
"Treatment with nifedipine altered the mRNA expression of the transcription factor Gata4, which was absent in the developing ventricles, and the sarcomeric protein Mylpc (myosin light chain 2V), which was decreased distal to the left ventricle and was absent at the site of the developing right ventricle." | ( Intracellular calcium plays an essential role in cardiac development. Makuck, RF; Porter, GA; Rivkees, SA, 2003) | 0.66 |
"Treatment with nifedipine, ticlopidine or cilostazol had no significant effects on any of the parameters measured in this model." | ( Effects of OP-1206 alpha-CD on walking dysfunction in the rat neuropathic intermittent claudication model: comparison with nifedipine, ticlopidine and cilostazol. Akimaru, S; Ito, H; Katsube, N; Maegawa, H; Marsala, M; Nakai, K; Takenobu, Y; Takimizu, H, 2003) | 0.87 |
"Treatment with nifedipine and SKF-96365 increased intracellular calcium under normoglycemic conditions, instead of blocking calcium influx, and was protective against hypoxia-induced BBB disruption under normoglycemia." | ( Protection against hypoxia-induced blood-brain barrier disruption: changes in intracellular calcium. Brown, RC; Davis, TP; Egleton, RD; Mark, KS, 2004) | 0.66 |
"Pretreatment with nifedipine (10 microM), an L-type Ca2+ channel blocker, reduced PACAP-evoked pancreastatin secretion by 50-60%, gastrin-evoked secretion by approximately 80% and abolished the response to Bay K 8644." | ( Somatostatin, misoprostol and galanin inhibit gastrin- and PACAP-stimulated secretion of histamine and pancreastatin from ECL cells by blocking specific Ca2+ channels. Bernsand, M; Björkqvist, M; Eliasson, L; Håkanson, R; Lindström, E, 2005) | 0.65 |
"Treatment with nifedipine (10, 20 mg/kg) significantly improved the renal dysfunction, tissue and urine total nitric oxide levels, and renal oxidative stress and prevented the alterations in renal morphology." | ( Nifedipine attenuates changes in nitric oxide levels, renal oxidative stress, and nephrotoxicity induced by cyclosporine. Chander, V; Chopra, K, 2005) | 2.11 |
"Treatment with nifedipine significantly lowered both the 24-h mean systolic and diastolic BP (143+/-14/89 +/-12 to 124+/-16/80+/-8 mmHg, p<0.001/p=0.001), as well as the casual BP (167+/-11/101 +/-8 to 140+/-13/86+/-10 mmHg, p<0.001/p<0.01)." | ( Chronobiological analysis by ambulatory blood pressure monitoring of the hyperbaric and hypobaric indexes for evaluation of the antihypertensive effect of long-acting nifedipine. Imamoto, S; Ito, T; Iwano, K; Kanae, K; Koga, A; Kunoh, M; Miyazaki, H; Mochizuki, S; Ohsawa, S; Satoh, C; Seki, S; Takeda, S; Taniguchi, M, 2005) | 0.86 |
"Treatment with nifedipine also blocked changes in the anti-apoptotic protein bcl-xL and in expressions of the pro-apoptotic protein bax." | ( Anti-recoverin antibodies induce an increase in intracellular calcium, leading to apoptosis in retinal cells. Adamus, G; Duvoisin, RM; Shiraga, S; Webb, S, 2006) | 0.67 |
"Pretreatment with nifedipine also inhibited the functional maturation of neurons, which responded to membrane depolarization with weak Ca(2+) signals." | ( Role of L-type Ca2+ channels in neural stem/progenitor cell differentiation. Azzena, GB; Budoni, M; Casalbore, P; D'Ascenzo, M; Grassi, C; Pallini, R; Piacentini, R, 2006) | 0.66 |
"The treatment with nifedipine prevented the reduction of sexual behavior and the increase of plasma PRL, but did not alter the reduction of plasma testosterone and FSH and spermatogenesis of 2K/1C rats." | ( Effects of renovascular hypertension on reproductive function in male rats. Breigeiron, MK; Lucion, AB; Sanvitto, GL, 2007) | 0.66 |
"Treatment with nifedipine resulted in a significant inhibition of the progression of AAA such as aneurismal dilation at 14 and 28 days compared to the control (week 2: control, 2.98+/-0.71 mm; nifedipine, 2.37+/-0.64 mm; p<0.05 and week 4: control, 3.28+/-0.98 mm; nifedipine, 2.41+/-0.17 mm; p<0.05)." | ( Inhibition of experimental abdominal aortic aneurysm progression by nifedipine. Izawa, K; Kunugiza, Y; Morishita, R; Ogihara, T; Osako, MK; Tomita, N; Yamasaki, K, 2008) | 0.92 |
"The treatment with nifedipine in the CIH group attenuated blood pressure (159+/-2 mm Hg; P<0.001) and normalized left ventricular wall thickness and systolic function, whereas the treatment with SOD mimetic decreased blood pressure (165+/-2 mm Hg; P<0.001) and reduced left ventricular wall thickness without changes in the systolic function." | ( Postnatal intermittent hypoxia and developmental programming of hypertension in spontaneously hypertensive rats: the role of reactive oxygen species and L-Ca2+ channels. Gozal, D; Gu, Y; Nozdrachev, AD; Ortines, RV; Prabhu, SD; Soukhova-O'Hare, GK, 2008) | 0.66 |
"Treatment with nifedipine can safely be combined with administration of a beta receptor blocking agent." | ( Comparative pharmacology of calcium antagonists: nifedipine, verapamil and diltiazem. Henry, PD, 1980) | 0.86 |
"Treatment with nifedipine continued for 18 days." | ( A study of the antihypertensive effect and some pharmacodynamic aspects of nifedipine in medium-term treatment. Castellani, S; Galanti, G; Masotti, G; Morettini, A; Poggesi, L; Scarti, L, 1984) | 0.84 |
"Treatment with nifedipine and labetalol lowered the blood pressure to 150/100 mm Hg." | ( Severe hypertension in childhood due to prolonged skin application of a mineralocorticoid ointment. Bartorelli, A; Rimondini, A, ) | 0.47 |
"Treatment with nifedipine alone (80 mg/day) lowered MAP significantly on the first day, but it tended to rise again therealter." | ( Management of severe hypertension with nifedipine in combination with clonidine or propranolol. Abe, K; Chiba, S; Haruyama, T; Imai, Y; Irokawa, N; Ito, T; Miura, Y; Otsuka, Y; Saito, K; Sakurai, Y; Sato, M; Yasujima, M; Yoshinaga, K, 1980) | 0.87 |
"Pretreatment by nifedipine did not significantly influence the hypercalcemia-induced bradycardia and augmentation of the P-Q interval except a small and transient effect during relatively low calcium levels." | ( Electrocardiographic evidence for a cardioprotective effect of nifedipine during experimental hypercalcemia. Schäfer, A; Schäfer, H; Schäfer, W, ) | 0.7 |
"Treatment with nifedipine was successful in 6 patients of group 1, however, only in 6 out of 17 patients in group 2." | ( [Variant angina non-invasive assessment of coronary morphology]. Bergmann, H; Herbinger, W; Kramar, R; Leisch, F; Schützenberger, W, 1982) | 0.6 |
"Treatment with nifedipine 5 mg t.d.s." | ( Acute and long-term hypotensive effects and plasma concentrations of nifedipine in patients with essential hypertension. Aoki, K; Kawaguchi, Y; Sato, K; Yamamoto, M, 1982) | 0.84 |
"Treatment with nifedipine was given to six patients, with excellent results in four cases, and regular response in two." | ( [Variant angina pectoris with demonstration of coronary spasm. Diagnostic and therapeutic considerations]. Alegría, E; Elizalde, JM; Malpartida, F; Martínez Caro, D; Téllez, J; Vallés, V, ) | 0.47 |
"Pretreatment with nifedipine partially restores the analgesic action of morphine in morphine-tolerant rats." | ( Reduction of morphine dependence and potentiation of analgesia by chronic co-administration of nifedipine. Antkiewicz-Michaluk, L; Michaluk, J; Romańska, I; Vetulani, J, 1993) | 0.83 |
"Treatment with nifedipine was associated with the return of [Ca2+]i toward normal values in both the nondiabetic (51 +/- 4.5 nmol/L) and diabetic (54 +/- 2.5 nmol/L) hemodialysis patients." | ( Effect of treatment of hemodialysis patients with nifedipine on metabolism and function of polymorphonuclear leukocytes. Akmal, M; Alexiewicz, JM; Klin, M; Massry, SG; Smogorzewski, M, 1995) | 0.88 |
"Pretreatment with nifedipine (200 nM) only slightly inhibited the MO- (1.74 +/- 0.32 vs 2.88 +/- 0.56 g) or NA- (2.43 +/- 0.66 vs 3.60 +/- 0.82 g) induced contraction without statistical significance (P > 0.05)." | ( Inhibitory effects of calcium antagonists on alpha-adrenoceptor-mediated contraction in the human internal mammary artery. Acuff, TE; Bowman, RT; Douthit, MB; He, GW; Mack, MJ; Ryan, WH; Yang, CQ, 1994) | 0.61 |
"Treatment with nifedipine resulted in a prolongation of segment length." | ( Effect of nifedipine on coronary capillary geometry in normotensive and hypertensive rats. Cicutti, N; Kazda, S; Rakusan, K; Turek, Z, 1994) | 1.03 |
"Pretreatment with nifedipine (10(-6) M) did not reduce IPs formation." | ( Endothelin-1-induced phosphoinositide hydrolysis and contraction in isolated rabbit detrusor and urethral smooth muscle. Andersson, KE; Garcia-Pascual, A; Holmquist, F; Persson, K, 1993) | 0.61 |
"Pretreatment with nifedipine delayed the time of the peak plasma hormone responses after naloxone [ACTH, 32.1 +/- 2.1 vs." | ( Altered hypothalamic-pituitary-adrenal axis responsiveness in myotonic dystrophy: in vivo evidence for abnormal dihydropyridine-insensitive calcium transport. Crosbie, GV; Grice, JE; Hockings, GI; Jackson, RV; Walters, MM, 1993) | 0.61 |
"Pretreatment with nifedipine further inhibited (P < .01) the GHRH-induced increase in plasma concentrations of GH (P < .05), which, in keeping with previous data, had already been reduced by IV endothelin-1 alone (P < .05)." | ( Effect of endothelin-1 in man--impact on basal and stimulated concentrations of luteinizing hormone, follicle-stimulating hormone, thyrotropin, growth hormone, corticotropin, and prolactin with and without pretreatment with nifedipine. Vierhapper, H, 1996) | 0.8 |
"Rats treated with nifedipine alone had an increase in tail-flick latency of 122%, as measured by the area under the curve, compared to rats treated with DMSO alone." | ( Ondansetron blocks nifedipine-induced analgesia in rats. Hunt, TE; Wu, W; Zbuzek, VK, 1996) | 0.95 |
"Treatment with nifedipine consistently reduced the acute GtH response to either sGnRH or cGnRH-II." | ( Roles of calcium and calmodulin in the mediation of acute and sustained GnRH-stimulated gonadotropin secretion from dispersed goldfish pituitary cells. Chang, JP; Jobin, RM; Neumann, CM, 1996) | 0.63 |
"We treated with nifedipine or lisinopril 38 essential hypertensive patients with left ventricular hypertrophy. " | ( Lisinopril reverses left ventricular hypertrophy through improved aortic compliance. Shimamoto, H; Shimamoto, Y, 1996) | 0.64 |
"Rats treated with nifedipine or nimodipine exhibited a dose-dependent tendency to avoid the center of the field without modification of other parameters, suggesting an increased emotivity in the rats." | ( Behavioral and analgesic effects induced by administration of nifedipine and nimodipine. Alfaro, MJ; Colado, MI; del Val, VL; Goicoechea, C; Martín, MI, 1996) | 0.86 |
"Pretreatment with nifedipine partially prevented the hypoxia- and the inflammation-induced decrease in liver cytochrome P450; however, nifedipine did not prevent the decrease in theophylline clearance or the increase in liver malondialdehyde." | ( Effect of nifedipine on the elimination of theophylline in the rabbit subjected to hypoxia or to an inflammatory reaction. Barakat, M; du Souich, P, 1996) | 1.02 |
"Treatment with nifedipine effectively blocked both insulin and contraction stimulated glucose transport in soleus." | ( Role of dihydropyridine sensitive calcium channels in glucose transport in skeletal muscle. Balon, TW; Young, JC, 1997) | 0.64 |
"Pretreatment with nifedipine (10-30 mg/kg) produced dose-dependent rightward shifts of the (+/-)-Bay K 8644 dose-response curve." | ( Effects of dihydropyridine Ca2+ channel blockers on the discriminative stimulus and the motor impairing effects of (+/-)-Bay K 8644. Cohen, C; Perrault, G; Sanger, DJ, 1997) | 0.62 |
"Pretreatment with nifedipine nearly completely suppressed the histamine-induced increase in [Ca2+]i transient." | ( Histamine H1-receptor-mediated increase in the Ca2+ transient without a change in the Ca2+ current in electrically stimulated guinea-pig atrial myocytes. Hattori, Y; Houzen, H; Kanno, M; Yasuda, K; Yoshimoto, K, 1998) | 0.62 |
"The treatment with nifedipine retard increased the mean heart rate of patients." | ( Antihypertensive effect of amlodipine compared with nifedipine retard in patients with mild and moderate essential hypertension. Gross-Furek, V; Herman, ZS; Kalina, Z; Madej, A; Maślankiewicz, A; Okopień, B; Szwed, Z; Tokarz, D, ) | 0.7 |
"Treatment with nifedipine (10 mg/kg) and enalapril (5 mg/kg) for 15 days produced a significant reduction in T1/2." | ( Effect of nifedipine and enalapril on insulin-induced glucose disposal in spontaneous hypertensive and diabetic rats. Goyal, RK; Mehta, AA; Patel, S; Santani, DD, ) | 0.87 |
"Treatment with nifedipine completely restored 5-HT-induced vasodilation (113 +/- 13%), whereas it did not influence basal forearm vasomotion or SNP-induced vasodilation." | ( Nifedipine improves endothelial function in hypercholesterolemia, independently of an effect on blood pressure or plasma lipids. Honing, ML; Kastelein, JJ; Koomans, HA; Rabelink, TJ; van Dam, T; Verhaar, MC; Zwart, M, 1999) | 2.09 |
"The treatment with nifedipine GITS 30-60 mg/day (monotherapy or combination) lasted for 6 months." | ( [Treatment of chronic stable angina: follow-up study with nifedipine gastrointestinal therapeutic system. SENIOR Study Group]. de Lombera Romero, F; Fuertes García, A; González Juanatey, JR; Luengo Fernández, E; Palencia Pérez, MA; Sagués Cabarro, F; Vargas García, R; Wilke Delgado, M, 2000) | 0.87 |
"Treatment with nifedipine, a calcium-channel blocker, diminished the calcium current and caused the cell to lose its responsiveness to the orienting influence of gravity." | ( Gravity-directed calcium current in germinating spores of Ceratopteris richardii. Chatterjee, A; Porterfield, DM; Roux, SJ; Smith, PS, 2000) | 0.65 |
"Treatment with nifedipine resulted in a rise in LDL-ox of 7-11% as compared to baseline (P<0.05)." | ( Oxidation of low-density lipoprotein in normotensive type 2 diabetic patients. Comparative effects of enalapril versus nifedipine: a randomized cross-over over study. Brosh, D; Levi, Z; Lidar, M; Rachmani, R; Ravid, M, 2000) | 0.86 |
"Pretreatment with nifedipine (a calcium channel blocker) or extracellular Ca+2 removal by ethylenediaminetetraacetic acid (EDTA) greatly attenuated the relaxation effect, suggesting that calcium ion might be involved." | ( In vitro relaxation of rabbit and human internal anal sphincter by rutaecarpine, an alkaloid isolated from Evodia rutaecarpa. Chiu, JH; Jiang, JK; Lin, JK; Yu, IT, 2000) | 0.63 |
"Pretreatment with nifedipine (10 nmol/l) had no effect on the phasic contraction induced by NA, but it significantly reduced ATP- or high K(+)-induced contraction." | ( Modulatory effect of protein kinase C activator on contractility of rat vas deferens. Chan, FL; Chen, ZY; Huang, Y; Lau, CW; Pai, RK; Yao, XQ, 2001) | 0.63 |
"Treatment with nifedipine was interrupted significantly less often because of side effects (OR 0.12, 95% CI 0.05, 0.29) and led to better neonatal outcomes (fewer infants with respiratory distress syndrome: OR 0.57, 95% CI 0.37, 0.89) or transferred to neonatal intensive care units (OR 0.65, 95% CI 0.43, 0.97)." | ( Tocolysis with nifedipine or beta-adrenergic agonists: a meta-analysis. Carbonne, B; Dekker, G; Goffinet, F; Papatsonis, D; Tsatsaris, V, 2001) | 1 |
"Rats treated with nifedipine orally (700 mg/kg) for 19 days had a significant increase in urine output, whereas urinary osmolality and solute-free water reabsorption were markedly reduced." | ( Altered expression of renal aquaporins and Na(+) transporters in rats treated with L-type calcium blocker. Flyvbjerg, A; Frøkiaer, J; Knepper, MA; Kwon, TH; Li, C; Nielsen, S; Wang, W, 2001) | 0.63 |
"Pretreatment with nifedipine (low toxin concentration; acute denervation) significantly decreased intestinal MPO activity and number of RBCs." | ( Involvement of nerves and calcium channels in the intestinal response to Clostridium difficile toxin A: an experimental study in rats in vivo. Jodal, M; Lundgren, O; Sörensson, J, 2001) | 0.63 |
"Treatment with nifedipine and MDL-12330A caused additive inhibition of the PACAP-induced catecholamine responses." | ( Role of calcium channels and adenylate cyclase in the PACAP-induced adrenal catecholamine secretion. Fukushima, Y; Hikichi, H; Hisa, H; Kawashima, H; Kimura, T; Nagayama, T; Satoh, S; Suzuki-Kusaba, M; Yoshida, M, 2001) | 0.65 |
"Pretreatment with nifedipine (10-100 microg/kg per min, i.v.) dose-dependently attenuated SPP-induced renal blood flow reductions." | ( Nifedipine inhibits sphinogosine-1-phosphate-induced renovascular contraction in vitro and in vivo. Bischoff, A; Finger, J; Michel, MC, 2001) | 2.08 |
"Treatment with nifedipine alone appeared to have no effect on muscle mass or the amount of myofibrillar proteins." | ( Effect of treatment with nifedipine, an L-type calcium channel blocker, on muscular atrophy induced by hindlimb immobilization. Fujimoto, K; Wagatsuma, A; Yamada, S, 2002) | 0.96 |
"Treatment with nifedipine (30 mg/kg/day, p.o.) reduced the increased blood pressure of SHRs fed the high-salt diet to the level of SHRs fed the normal-salt diet." | ( High salt intake impairs vascular nitric oxide/cyclic guanosine monophosphate system in spontaneously hypertensive rats. Kagota, S; Kunitomo, M; Nakamura, K; Tamashiro, A; Yamaguchi, Y, 2002) | 0.65 |
"Treatment with nifedipine attenuated cyclosporine A-induced renal dysfunction and reduced urinary endothelin excretion." | ( Effect of nifedipine on cyclosporine A-induced nephrotoxicity, urinary endothelin excretion and renal endothelin receptor number. Brooks, DP; Caltabiano, M; Contino, LC; Nambi, P; Ohlstein, EH; Pullen, M; Storer, B, 1991) | 1.02 |
"Pretreatment with nifedipine (3 x 10(-8) M) prevented the rise in LVEDP induced by pacing tachycardia." | ( Effects of nifedipine on diastolic abnormalities in low-flow and pacing-induced ischemia in isolated rat hearts. Iizuka, M; Ikenouchi, H; Momomura, S; Serizawa, T; Sugimoto, T, 1991) | 0.99 |
"Rats treated by nifedipine starting 1 day preoperatively and continued for 1 week postoperatively had a mean necrosis of 10.0953%." | ( An experimental study on the effect of nifedipine on ischaemic skin flap survival in rats. Khazanchi, RK; Moudgil, K; Pal, S, ) | 0.73 |
"Treatment with nifedipine resulted in significant decreases in serum triglyceride concentrations." | ( Prevention of myocardial lesions in JCR:LA-corpulent rats by nifedipine. Amy, RM; Dolphin, PJ; Koeslag, DG; Russell, JC, ) | 0.71 |
"Treatment with nifedipine did not significantly change any of the pulmonary function values, except for the carbon monoxide diffusing capacity (DLCO)." | ( Diffusing capacity of the lung and nifedipine in systemic sclerosis. Georgiakodis, F; Kyriakidis, M; Papazoglou, S; Sfikakis, P; Sfikakis, PP; Toutouzas, P; Vergos, C, 1990) | 0.9 |
"Pretreatment with nifedipine inhibited the maximum contraction induced by endothelin, but did not affect the threshold dose or the half maximal effective dose (ED50)." | ( Myocardial ischaemia induced by endothelin in the intact rabbit: angiographic analysis. Akita, H; Fukuzaki, H; Hirata, K; Matsuda, Y; Yokoyama, M, 1990) | 0.6 |
"Pretreatment with nifedipine (7.5-50 mg/kg s.c.) markedly potentiated the effects of 4-AP." | ( Seizures and wet-dog shakes induced by 4-aminopyridine, and their potentiation by nifedipine. Alvarado, R; Fragoso-Veloz, J; Massieu, L; Tapia, R, 1990) | 0.83 |
"Treatment with nifedipine did not affect the response of peripheral airways to aerosolized acetylcholine, indicating that receptor-operated calcium channels (ROCC) and/or release of calcium from intracellular stores were unaffected by this drug." | ( Dry air-induced bronchoconstriction--a role for voltage-sensitive calcium channels? Freed, AN; Munakata, M, 1989) | 0.62 |
"Pretreatment with nifedipine or a reduction of external calcium, that either maintained or further enhanced the forskolin-induced increase in the cAMP level, abolished the forskolin-induced arrhythmia." | ( Arrhythmogenic effect of forskolin in the isolated perfused rat heart: influence of nifedipine or reduction of external calcium [corrected]. Huang, XD; Wong, TM, 1989) | 0.82 |
"Pretreatment with nifedipine, but not with trimetazidine, resulted in slightly but statistically not significant higher ATP-levels after global ischaemia in the working heart and in the heart-lung preparation." | ( Cardioprotective effect of trimetazidine and nifedipine in guinea-pig hearts subjected to ischaemia. Boddeke, HW; Bohnenn, VA; Heijnis, JB; Hugtenburg, JG; Jap, TJ; Mathy, MJ; van Heiningen, PN; van Zwieten, PA, ) | 0.71 |
"Treatment with nifedipine resulted in 63 patient withdrawals compared with 31 patient withdrawals during epanolol treatment; there were 5 patient withdrawals from both treatments." | ( Comparative multicentre study of the tolerability and efficacy of epanolol versus nifedipine in patients with stable angina pectoris. Readman, AS, 1989) | 0.84 |
"Pretreatment with nifedipine again abolished this response." | ( Ca++ utilization in the constriction of rat aorta to stimulation of protein kinase C by phorbol dibutyrate. Bozarth, JM; Chiu, AT; Forsythe, MS; Timmermans, PB, 1987) | 0.6 |
"Pretreatment with nifedipine antagonized the stimulatory effects of ethanol on the DA-system." | ( Biochemical and behavioral evidence for an interaction between ethanol and calcium channel antagonists. Engel, JA; Fahlke, C; Hård, E; Hulthe, P; Johannessen, K; Snape, B; Svensson, L, 1988) | 0.6 |
"Pretreatment with nifedipine (30 mg/kg), verapamil (50 mg/kg) or propranolol (20 mg/kg) completely prevented the occurrence of myocardial injury through the preservation of myocardial phospholipid composition, total phosphorus, CK activity and heart/body and protein/heart weight ratios." | ( Effects of phospholipase inhibitors and calcium antagonists on the changes in myocardial phospholipids induced by isoproterenol. Hashimoto, H; Ito, T; Miyazaki, Y; Ogawa, K; Satake, T; Takasu, N, ) | 0.45 |
"Treatment with nifedipine in combination with furosemide and propranolol led to a more significant decrease in calcium responses than that expressed with monotherapy." | ( Platelets as a model for studying the action of antihypertensive drugs. Avdonin, PV; Kravchenko, AN; Mazaev, AV; Nekrasova, AA; Shkhvatsabaya, IK, 1988) | 0.61 |
"Treatment with nifedipine in the early phase of acute myocardial infarction seems to have no effect on enzymatically measured infarct size." | ( Effect of nifedipine on enzymatically estimated infarct size in the early phase of acute myocardial infarction. Adgey, AA; MacKenzie, G; Walker, LJ, 1988) | 1.02 |
"Treatment with Nifedipine significantly increased heart rate at rest (p less than 0.05), under submaximal (p less than 0.05) and maximal load (p less than 0.05), with respect to treatment with Diltiazem and Verapamil." | ( [Comparative evaluation of 3 calcium antagonist drugs in patients with stable angina of effort. Double-blind placebo-controlled randomized study]. Buonamici, P; Buzzigoli, A; Fazzini, PF; Pucci, PD; Santoro, GM; Sarro, F, 1987) | 0.61 |
"The treatment with nifedipine induced a significant reduction in both systolic and diastolic blood pressures; the infusions of angiotensin II (0.150, 0.375 and 0.750 microgram/min, each rate for 30 min) and of potassium chloride (50 mmol in 500 ml of 5% glucose in 50 min) caused similar rises in plasma aldosterone before and during the administration of the calcium antagonist." | ( Calcium antagonists and responsiveness of the adrenal glands to aldosterone-releasing stimuli in hypertensive patients. Leonetti, G; Terzoli, L; Zanchetti, A, 1987) | 0.59 |
"Treatment with nifedipine over 3 years resulted in suppressing the pain almost totally." | ( [Long-term therapy of multiple piloleiomyomas with nifedipine]. Biltz, H; Kreysel, HW; Uerlich, M, 1987) | 0.86 |
"Treatment with nifedipine-propranolol was terminated in five cases due to deterioration or side effects after 6 and 12 months, respectively." | ( Effects of nifedipine and propranolol combined therapy in patients with hypertrophic cardiomyopathy. Hopf, R; Kaltenbach, M, 1987) | 1 |
"Treatment with nifedipine was less expensive and required less time in the ICU than treatment with nitroprusside and was accompanied by no associated increase in morbidity or mortality." | ( A randomized comparison of nifedipine and sodium nitroprusside in severe hypertension. Franklin, C; Mamdani, B; Nightingale, S, 1986) | 0.91 |
"Treatment with nifedipine did not diminish the diurnal variations in airway caliber, judged from peak expiratory flow rates, or in bronchial reactivity, judged from bronchodilator responsiveness." | ( Does nifedipine affect the diurnal variation of asthma in children? Landau, LI; Olinsky, A; Sly, PD, ) | 0.98 |
"Pretreatment with nifedipine significantly attenuated the hypoxia-induced increase in mean pulmonary artery pressure by 53% and of the mean pulmonary vascular resistance index by 50%." | ( Nifedipine attenuates acute hypoxic pulmonary vasoconstriction in patients with chronic obstructive pulmonary disease. Burghuber, OC, 1987) | 2.04 |
"Treatment with nifedipine and propranolol was terminated in five cases, due to deterioration or side effects after 6 and 12 months, respectively." | ( [Treatment of hypertrophic cardiomyopathy with nifedipine and propranolol in combination]. Hopf, R; Kaltenbach, M; Klepzig, H; Thomas, J, 1987) | 0.87 |
"Pretreatment with nifedipine postponed EMD until 120-150 seconds and was not observed in dogs on CPB." | ( Relation between power spectrum time course during ventricular fibrillation and electromechanical dissociation. Effects of coronary perfusion and nifedipine. Cosin, J; Hernandez, A; Llamas, P; Martin, G; Such, M, 1986) | 0.79 |
"Pretreatment with nifedipine significantly attenuated acetylcholine-induced changes in all four lung function parameters studied, but did not significantly influence the increase in thromboxane B2 plasma concentrations observed after the acetylcholine challenge." | ( Inhibition of acetylcholine-induced bronchoconstriction in asthmatics by nifedipine. Burghuber, OC; Haber, P; Harmuth, P; Kneussl, M; Silberbauer, K; Sinzinger, H, 1986) | 0.83 |
"Treatment with nifedipine inhibited both the development of hypertension and this specific change in the plasma proteins, in spite of continuous dietary salt loading." | ( Characteristic changes of plasma proteins in the Dahl hypertensive rat strain (DS) during the development of hypertension. Garthoff, B; Morich, FJ, 1985) | 0.61 |
Nicardipine is at least as safe and effective as nifedipine in the treatment of unstable angina.
The pharmacokinetic parameters (AUC, Cmax, Tmax, and t1/2) of nifedipine following single oral administration of a 10 mg capsule of test product were compared to those of the same amount of a reference product. In conclusion, the pharmacokinetics changes of n ifedipines may be modulated by the inhibitory effects of baicalin on plasma protein binding and CYP3A-mediated metabolism.
Excerpt | Reference | Relevance |
---|---|---|
" Nilvadipine has both pharmacokinetic and pharmacodynamic advantages compared to nifedipine (the prototype of the dihydropyridines)." | ( Pharmacodynamics of nilvadipine, a new dihydropyridine-type calcium antagonist. Honerjäger, P; Seibel, K, 1992) | 0.51 |
" No significant differences were observed among the three preparations in relation to the following pharmacokinetic parameters obtained from the plasma concentration-time curves: area under the curve (AUC), slope (beta) and half-life (T1/2) of the elimination phase, volume of distribution (Vd/F) and total body clearance (CL/F), both expressed as functions of the oral bioavailability (F) of nifedipine." | ( Comparative pharmacokinetics of different oral nifedipine preparations in healthy Brazilian volunteers. Melo, PA; Suarez-Kurtz, G; Sudo, RT; Vianna-Jorge, R, 1992) | 0.71 |
"This study characterizes the single dose pharmacokinetic characteristics of the dihydropyridine calcium antagonist drug amlodipine in a group of 16 elderly subjects, aged 65 to 86 years (8 M:8 F)." | ( An assessment of the pharmacokinetics and pharmacodynamics of single doses of amlodipine in elderly normotensives. Elliott, HL; Green, ST; Meredith, PA; Vincent, J, ) | 0.13 |
" There were no diazepam pharmacokinetic changes during restoration period." | ( [Pharmacokinetics of antipyrine, nifedipine and diazepam in experimental myocardial infarct]. Anan'ev, EA; Grek, OR; Kolpakov, MA; Sharapov, VI, 1992) | 0.56 |
" The results demonstrate the importance of defining the precise posture in studies in which pharmacokinetic and pharmacodynamic measurements are made on drugs which are absorbed rapidly and are subject to presystemic elimination." | ( The influence of posture on the pharmacokinetics of orally administered nifedipine. Ahsan, CH; Challenor, VF; Daniels, R; George, CF; Macklin, BS; Renwick, AG; Waller, DG, 1992) | 0.52 |
" Amlodipine is distinct from other calcium antagonists by its pharmacokinetic profile: slower onset of action with less acute vasodilatation associated side effects and a sustained antihypertensive and anti-anginal efficacy over 24 hours." | ( [Amlodipine: pharmacokinetic and pharmacodynamic profile of a calcium antagonist with prolonged effect]. Heynen, G, 1992) | 0.28 |
"Amlodipine is a dihydropyridine calcium antagonist drug with distinctive pharmacokinetic characteristics which appear to be attributable to a high degree of ionisation." | ( Clinical pharmacokinetics of amlodipine. Elliott, HL; Meredith, PA, 1992) | 0.28 |
" The slow rate of elimination (elimination half-life of 40-60 h) confers several pharmacokinetic characteristics that are not seen with other calcium-antagonist drugs." | ( Pharmacokinetics and pharmacodynamics of amlodipine. Abernethy, DR, 1992) | 0.28 |
" The small intraindividual variability in nifedipine pharmacokinetics allows crossover studies to detect pharmacokinetic relationships between nifedipine and other dihydropyridine calcium entry blockers." | ( Intraindividual variability in nifedipine pharmacokinetics and effects in healthy subjects. Breimer, DD; Cohen, AF; Schoemaker, HC; Soons, PA, 1992) | 0.83 |
" The pharmacokinetic characteristics of this new formulation of nifedipine-SR were compared with those of divided doses of conventional nifedipine." | ( New developments in sustained-release antihypertensive therapy: formulation and pharmacokinetic considerations. Davis, SS; Devane, JG; Kavanagh, M; Mulligan, S; Sparrow, RA; Wilding, IR, 1992) | 0.52 |
" The single dose of omeprazole had no significant effect on any pharmacokinetic parameter of nifedipine, nor on gastric pH, or blood pressure or heart rate." | ( Influence of single- and multiple-dose omeprazole treatment on nifedipine pharmacokinetics and effects in healthy subjects. Breimer, DD; Danhof, M; Jansen, JB; Lamers, CB; Soons, PA; van Brummelen, P; van den Berg, G, 1992) | 0.74 |
" A pharmacokinetic study on m-nifedipine was carried out in 8 rabbits." | ( [Determination of m-nifedipine and its pharmacokinetic study in rabbits by high-pressure liquid chromatography]. Liang, YB; Liu, DK; Ma, XY; Wang, LF; Wu, GJ; Xing, JF; Zhao, GS, 1992) | 0.9 |
"Pharmacokinetic and pharmacodynamic interactions of alcohol and nifedipine were assessed in 10 healthy human volunteers." | ( Effect of an acute dose of alcohol on the pharmacokinetics of oral nifedipine in humans. Caillé, G; Gossard, D; Lacasse, Y; Laganière, S; McGilveray, I; Qureshi, S, 1992) | 0.76 |
" A pharmacodynamic interaction may exist, inhibiting effective use of dihydropyridines as adjunctive therapy in epileptic patients." | ( Dihydropyridine calcium antagonists in mice: blood and brain pharmacokinetics and efficacy against pentylenetetrazol seizures. Brodie, MJ; Drennan, JE; Forrest, G; Larkin, JG; Scobie, G; Thompson, GG, ) | 0.13 |
"To evaluate the effect of diltiazem pretreatment (60 mg three times a day for 3 days) on pharmacokinetics and pharmacodynamic effect of nifedipine, six healthy subjects received 20 mg nifedipine orally on two occasions using a double-blind cross-over, placebo-controlled method." | ( Effects of diltiazem on the pharmacokinetics of nifedipine. Ebihara, A; Hosoda, S; Kumagai, Y; Ohashi, K; Sakamoto, K; Sudo, T; Sugimoto, K; Tateishi, T; Toyo-oka, T; Toyosaki, N, 1990) | 0.74 |
" Thus, amlodipine seems to provide a useful alternative to other agents currently available for the treatment of essential hypertension and chronic stable angina pectoris, with certain pharmacodynamic and tolerability properties that should be advantageous in many patients." | ( Amlodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. Heel, RC; Murdoch, D, 1991) | 0.28 |
" nifedipine were dependent on time of day: immediate-release nifedipine had higher Cmax (peak concentration) and shorter tmax (time-to-peak concentration) after morning than evening application, and bioavailability in the evening was reduced by about 40%." | ( Chronopharmacokinetics and cardiovascular effects of nifedipine. Behne, S; Kaiser, R; Lemmer, B; Nold, G, 1991) | 1.44 |
" In order to document its stability in vitro and to develop a pharmacokinetic model in rabbits, a new reversed-phase liquid chromatography (LC) assay with UV detection was developed." | ( Liquid chromatography assay for amlodipine: chemical stability and pharmacokinetics in rabbits. Mosher, SJ; Pollak, PT; Yeung, PK, 1991) | 0.28 |
"Pharmacokinetic and pharmacodynamic parameters of oral nifedipine were studied in the immediate postpartum period in eight women with preeclampsia." | ( Nifedipine pharmacokinetics and pharmacodynamics during the immediate postpartum period in patients with preeclampsia. Barton, JR; Prevost, RR; Sibai, BM; Whybrew, WD; Wilson, DA, 1991) | 1.97 |
"Ranitidine may be used at doses of up to 300 mg twice daily in the healing of duodenal ulcers, and this study investigated the potential for a pharmacokinetic or pharmacodynamic interaction between nifedipine 10 mg three times daily and ranitidine 300 mg twice daily compared with cimetidine 800 mg daily and placebo in a randomised crossover study in 18 healthy male subjects." | ( The pharmacokinetics and pharmacodynamics of nifedipine at steady state during concomitant administration of cimetidine or high dose ranitidine. Dixon, JS; Khan, A; Langley, SJ; Mullins, FG; Toon, S, 1991) | 0.73 |
" The niphedipine pharmacokinetics may be described in correspondence with the open pharmacokinetic model." | ( [Nifedipine pharmacokinetics in liver cirrhosis patients after the administration of a single oral dose]. Dumitraşcu, D; Grigorescu, M; Leucuţa, SE, ) | 1.04 |
"This double-blind randomized, crossover study was undertaken to determine the pharmacokinetic properties of nifedipine retard and atenolol when given separately, as a free or a fixed combination, compared with placebo in 15 healthy male volunteers." | ( A study of the pharmacokinetics and pharmacodynamics of nifedipine in combination with atenolol. Adam, HK; Fitzsimons, TJ; McAinsh, J; Norris, SC; Ryan, J, ) | 0.59 |
" There were no statistically significant differences in the saliva pharmacokinetic parameters of antipyrine on both occassions." | ( An examination of a possible pharmacokinetic interaction between nifedipine and antipyrine. Edeki, T; Johnston, A; Turner, P, 1990) | 0.52 |
" The mean apparent nifedipine elimination half-life was 16." | ( Pharmacokinetics of nifedipine derived from a new retard tablet formulation. Avgerinos, A; Gorrod, JW, ) | 0.78 |
" No remarkable deviation of NIF pharmacokinetic parameters from the normal ranges was found in CHF patients." | ( Nifedipine pharmacodynamics and pharmacokinetics in treatment of congestive heart failure. Chen, DG; Chen, K; Feng, QP; Wang, ZQ, 1990) | 1.72 |
" The pharmacokinetic parameters of nifedipine, after administration of a single oral dose of nifedipine-loaded hardened gelatin microspheres to volunteers, suggest that the preparation can be considered as a sustained release delivery system for nifedipine." | ( Controlled release of nifedipine from gelatin microspheres and microcapsules: in vitro kinetics and pharmacokinetics in man. Leucuţa, SE, ) | 0.72 |
"2 ng/ml) and terminal half-life of atenolol (9." | ( Interaction between nifedipine and atenolol: pharmacokinetics and pharmacodynamics in normotensive volunteers. Frölich, JC; Ledermann, H; Rosenkranz, B, ) | 0.45 |
" At the first intravenous nifedipine infusion a total systemic plasma clearance of 671 +/- 240 ml/min (mean +/- SD), an elimination half-life of 95 +/- 36 min, and a volume of distribution of 60." | ( Pharmacokinetics and hemodynamic effects of long-term nifedipine treatment in hypertensive patients. Breimer, DD; Faber, H; Kleinbloesem, CH; van Brummelen, P, 1987) | 0.82 |
" Pharmacokinetic studies were conducted with nonlabeled drug using specific high-pressure liquid chromatography or gas chromatographic procedures." | ( The metabolism and pharmacokinetics of amlodipine in humans and animals. Beresford, AP; Humphrey, MJ; Macrae, PV; Stopher, DA, 1988) | 0.27 |
" The elimination half-life was of the order of 50 h, similar to previously observed values, and did not vary with differences in renal function." | ( Pharmacokinetics of amlodipine in renal impairment. Carmody, M; Donohoe, JF; Doyle, GD; Greb, H; Kelly, JG; Laher, MS; Volz, M, 1988) | 0.27 |
" amlodipine, clearance tended to be decreased in elderly as compared with young patients with resulting prolongation in elimination half-life (64 +/- 20 vs." | ( Amlodipine in elderly hypertensive patients: pharmacokinetics and pharmacodynamics. Abernethy, DR; Gutkowska, J; Lambert, MD, 1988) | 0.27 |
"23 L/min (mean +/- SD), terminal half-life (t1/2) was 15." | ( Pharmacokinetics and hemodynamic effects of long-term nisoldipine treatment in hypertensive patients. Breimer, DD; Danhof, M; Quekel, RP; van Brummelen, P; van Harten, J, 1989) | 0.28 |
" The elimination half-life was of the order of 50 h, similar to previously reported values and did not vary with renal function." | ( Pharmacokinetics of amlodipine in renal impairment. Carmody, M; Donohue, J; Doyle, GD; Greb, H; Laher, M; Volz, M, 1989) | 0.28 |
"Amlodipine, a dihydropyridine calcium antagonist, was synthesized in an attempt to develop a compound with a pharmacokinetic profile characteristic of this class, which would also have an increased oral bioavailability and extended clearance time." | ( The pharmacokinetic profile of amlodipine. Abernethy, DR, 1989) | 0.28 |
" The mean elimination half-life of nifedipine prolonged significantly following diltiazem (2." | ( Dose dependent effect of diltiazem on the pharmacokinetics of nifedipine. Fujimura, A; Hosoda, S; Kumagai, Y; Ohashi, K; Sakamoto, K; Sudo, T; Sugimoto, K; Tateishi, T; Toyo-oka, T; Toyosaki, N, 1989) | 0.79 |
" The peak concentration of nifedipine during sublingual therapy ranged from 23." | ( Nifedipine pharmacokinetics during preterm labor tocolysis. Blaschke, T; Ferguson, JE; Pershe, R; Schutz, T; Stevenson, DK, 1989) | 2.02 |
" The pharmacokinetic profile of nifedipine was performed from venous blood samples obtained over a period of 8 hours, with a specific gas chromatographic assay." | ( Bioavailability and pharmacokinetics of nifedipine administered by different routes in healthy volunteers. León-Urrea, F; Montoya-Cabrera, MA; Palma-Aguirre, JA; Rodríguez, JM; Rosas-Alcázar, G, ) | 0.68 |
" In order to compare the pharmacokinetic properties of these compounds the dilation of the 'normal' coronary segments was correlated with the respective drug plasma levels; maximal plasma concentrations averaged 62 +/- 21 ng ml-1 (7th min) in group I and 17 +/- 7 ng ml-1 (4th min) in group II respectively." | ( Coronary vasodilation with dihydropyridines--a pharmacokinetic study. Bossaller, C; Hecker, H; Jost, S; Lichtlen, PR; Lippolt, P; Mogwitz, B; Nellessen, U; Rafflenbeul, W; Zwicky, P, 1989) | 0.28 |
" Both calcium antagonists tended to increase absorption rate and elimination rate, but none of the pharmacokinetic parameters of cyclosporine were significantly altered." | ( Short-term effects of calcium antagonists on hemodynamics and cyclosporine pharmacokinetics in heart-transplant and kidney-transplant patients. Browning, FM; Cardella, C; East, DS; Leenen, FH; Ogilvie, RI; Roy, LF; Shaw, D, 1989) | 0.28 |
" Experimental data were fitted and pharmacokinetic parameters were calculated using an open two compartment model." | ( Pharmacokinetics of oral nifedipine: relevance of the distribution phase. Castañeda-Hernández, G; Chávez, F; Herrera, JE; Hong, E; Hoyo-Vadillo, C; Moreno-Ramos, A; Salazar, LA; Tena, I; Vidal-Gárate, J, 1989) | 0.58 |
"We characterized the pharmacokinetic interaction between nifedipine and ethanol as a function of route of administration with pharmacokinetic monitoring of both compounds." | ( Characterization of the pharmacokinetic interaction between nifedipine and ethanol in the rat. Boje, KM; Fung, HL, 1989) | 0.76 |
"In the course of this trial the bioavailability and the essential pharmacokinetic parameters of a newly developed 10 mg nifedipine preparation were to be determined in comparison to a marketed reference preparation after single oral administration." | ( [Bioavailability and pharmacokinetics of a new nifedipine preparation in healthy volunteers]. Dilger, C; Hutt, V; Jaeger, H; Molz, KH; Mosberg, H; Pabst, G, 1989) | 0.74 |
" The findings of this study indicate that a variable liver blood flow response during the absorption phase of nisoldipine contributes to the pharmacokinetic variability of the drug, both on acute and multiple dose administration." | ( The contribution of nisoldipine-induced changes in liver blood flow to its pharmacokinetics after oral administration. Breimer, DD; Burggraaf, J; Danhof, M; van Brummelen, P; van Harten, J, 1989) | 0.28 |
" From tablets, the peak concentration was 79-88% lower and occurred 74-133 min after ingestion; also the bioavailability was lower, as indicated by on average 39% lower area under curve values after tablets." | ( Pharmacokinetics and acute side-effects of nifedipine given as slow-release tablets or liquid-filled capsules. Komulainen, H; Paronen, P; Raatikainen, O; Saano, V, 1989) | 0.54 |
" Pharmacokinetic data were analyzed by a nonlinear weighted least-square regression program (SAS-NLIN)." | ( Pharmacokinetics of vincristine in cancer patients treated with nifedipine. Aristei, C; Boschetti, E; Colozza, M; Del Favero, A; Fedeli, L; Guerciolini, R; Rambotti, P; Rossetti, R; Sabalich, I; Tonato, M, 1989) | 0.52 |
" A significant variability of the pharmacokinetic parameters in different patients was revealed." | ( [Pharmacokinetics of nifedipine after a single oral dose in patients with disorders of cerebral circulation]. Akopov, SE; Grigorian, GS; Ordukhanian, AA; Panosian, AG; Sarkissian, MA, ) | 0.45 |
"The pharmacokinetic and pharmacodynamic effects of nisoldipine, a 1,4-dihydropyridine calcium entry blocker, and the lipophilic beta-adrenoceptor blocker propranolol were assessed alone and in combination in 12 healthy men." | ( Pharmacokinetic and pharmacodynamic interactions between nisoldipine and propranolol. Leenen, FH; Levine, MA; Ogilvie, RI, 1988) | 0.27 |
"Pharmacokinetic and pharmacodynamic interactions between nifedipine and two beta-blocking agents were investigated." | ( Pharmacokinetic and pharmacodynamic interactions between nifedipine and propranolol or betaxolol. Canal, M; Carbon, C; Cascio, B; Domart, Y; Flouvat, B; Larribaud, J; Orofiamma, B; Roux, A; Vinceneux, P, 1986) | 0.76 |
"The purpose of this study was to determine the pharmacokinetic profile of nilvadipine and, using a chronic dog model, determine whether there was a correlation between plasma concentrations of the drug and hemodynamic effects." | ( Relationship between the pharmacokinetic and pharmacodynamic profile of nilvadipine in the dog. Garnes, D; Henderson, BM; Lanc, R; Silber, BM; Wu, WH; Yacobi, A, ) | 0.13 |
"Intravenous administration of amlodipine (single dose, 10 mg) to 12 volunteers gave a mean plasma half-life of 34 h, mean clearance of 7 ml min-1 kg-1 and a mean apparent volume of distribution of 21 l kg-1." | ( The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Chasseaud, LF; Faulkner, JK; McGibney, D; Perry, JL; Taylor, IW, 1986) | 0.27 |
"5 1 kg-1 and elimination half-life was 10." | ( The influence of infusion rate on the pharmacokinetics and haemodynamic effects of nisoldipine in man. Breimer, DD; Danhof, M; van Brummelen, P; van Harten, J; Zeegers, RR, 1988) | 0.27 |
" A pharmacokinetic study in rat and dog after oral and intravenous administrations revealed that KW-3049 was rapidly absorbed from the gastrointestinal tract, distributed into tissues moderately and comparatively quickly eliminated." | ( Pharmacokinetic study of benidipine hydrochloride in rats and dogs. Inoue, A; Kobayashi, H; Kobayashi, S; Nakamizo, N; Oka, T, 1988) | 0.27 |
" Pharmacokinetic parameters for nilvadipine were determined using model-independent methods." | ( Pharmacokinetics of nilvadipine after single oral doses in healthy volunteers. Cheung, WK; Desjardins, RE; Hibberd, M; Pearse, S; Shin, K; Silber, BM; Woodward, DL; Yacobi, A, 1988) | 0.27 |
" After each dose, clinical effects, hemodynamic changes and the pharmacokinetic profile of the drug were determined." | ( Importance of oral dosing rate on the hemodynamic and pharmacokinetic profile on nilvadipine. Cheung, WK; Desjardins, RE; Graveline, JF; Sia, LL; Silber, BM; Woodward, DL; Yacobi, A, 1988) | 0.27 |
" In the bioequivalence study with five volunteers, the pharmacokinetic parameters of a sustained release hydrophilic tablet of nifedipine and of immediate release capsules were determined." | ( The kinetics of nifedipine release from porous hydrophilic matrices and the pharmacokinetics in man. Leucuta, SE, 1988) | 0.83 |
"002) and Cmax in the elderly was significantly greater at 36." | ( Age-related changes in the pharmacokinetics and pharmacodynamics of nifedipine. George, CF; Renwick, AG; Robertson, DR; Waller, DG, 1988) | 0.51 |
" An elevation of the mean Cmax was found, from 73." | ( Pharmacokinetic interaction between nifedipine and propranolol. Koren, G; Levy, M; Turetz-Abramovitch, M; Zylber-Katz, E, 1988) | 0.55 |
" No significant differences were observed between Groups A, B and C (on an interdialysis day) in AUC (0-7h), tmax, Cmax and plasma protein binding." | ( Pharmacokinetics of nisoldipine in renal dysfunction. Ahr, G; Boelaert, J; Bogaert, MG; Dammekens, H; Daneels, R; De Vriese, G; Schurgers, M; Valcke, Y, 1988) | 0.27 |
" Pharmacokinetic parameters obtained in three beagle dogs after oral and intravenous administration are reported." | ( High performance liquid chromatography of a new 1,4-dihydropyridine: applications to pharmacokinetic study in dogs. Angignard, D; Cahn, J; Greiner, PO, 1988) | 0.27 |
" There was a fourfold increase in the elimination half-life (434 +/- 74 minutes in the cirrhotics compared with 102 +/- 11 minutes in the healthy subjects)." | ( Pharmacokinetics of nifedipine after oral administration in chronic liver disease. Ene, MD; Roberts, CJ, 1987) | 0.6 |
"The pharmacokinetics of nifedipine following intravenous administration can be represented by an open two-compartment model with a terminal elimination half-life of about two hours." | ( Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. A controlled-release formulation of nifedipine. Chung, M; Gaffney, M; Reitberg, DP; Singleton, W, 1987) | 0.87 |
" 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, ) | 0.4 |
" In patients with severe renal impairment, the maximal effect of nifedipine on diastolic blood pressure was more than doubled, which cannot be explained by differences in pharmacokinetics; therefore these patients appear to be more sensitive at the pharmacodynamic level." | ( Nifedipine. Relationship between pharmacokinetics and pharmacodynamics. Breimer, DD; Kleinbloesem, CH; van Brummelen, P, 1987) | 1.95 |
" The mean Cmax values for fasting, low-fat, and high-fat meals were 78." | ( Effect of food on nifedipine pharmacokinetics. Love, SJ; Quercia, GT; Reitberg, DP; Zinny, MA, 1987) | 0.61 |
" Assay suitability was assessed in a pharmacokinetic study in which four subjects were given a 6-mg oral dose of racemic nilvadipine." | ( Determination of (+)- and (-)-nilvadipine in human plasma using chiral stationary-phase liquid chromatography and gas chromatography-mass spectrometry, and a preliminary pharmacokinetic study in humans. Fujiwara, T; Noguchi, H; Tokuma, Y, 1987) | 0.27 |
" After pretreatment with cimetidine, which inhibits the activity of cytochrome P-450, the peak plasma concentration and area under the plasma-time concentration curve for nifedipine were increased by a mean 84%." | ( Factors affecting the pharmacokinetics of nifedipine. Challenor, VF; George, CF; Gruchy, B; Le Vie, J; Renwick, AG; Waller, DG, 1987) | 0.73 |
" 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) | 0.55 |
" The elimination half-life was dose-independent and averaged 11." | ( Pharmacokinetics of nilvadipine in healthy volunteers. Noguchi, H; Shishido, A; Terakawa, M; Tokuma, Y, 1987) | 0.27 |
"Pharmacokinetic, haemodynamic and radionuclide studies explored the acute pharmacokinetic and pharmacodynamic actions of nicardipine in patients with coronary heart disease." | ( Pharmacokinetic, haemodynamic and radionuclide studies with nicardipine in coronary artery disease. Finlayson, JR; Frais, MA; Graham, DJ; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986) | 0.27 |
" Intra- and inter-subject variability were assessed by comparing the pharmacokinetic parameters, AUC, Cmax and T50%AUC." | ( The intra- and inter-subject variability of nifedipine pharmacokinetics in young volunteers. Jack, DB; Kendall, MJ; Lobo, J, 1986) | 0.53 |
"In patients with essential hypertension, the pharmacokinetics of nifedipine in 2 forms (capsule, 10 mg nifedipine dissolved in an organic solvent; slow release tablet, 20 mg nifedipine) and their pharmacodynamic effectiveness on arterial pressure were studied." | ( Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients. Abe, K; Imai, Y; Nihei, M; Sasaki, S; Sekino, H; Yoshinaga, K, 1986) | 0.74 |
" In the fasting state, the time to peak concentration of nifedipine was not significantly different between the 20 mg biphasic and 20 mg sustained release tablets, but plasma concentrations were higher between 2 and 4 h after the biphasic tablet." | ( The effects of food and posture on the pharmacokinetics of a biphasic release preparation of nifedipine. Challenor, V; George, CF; Gruchy, BS; McEwen, J; McMurdo, ET; Renwick, AG; Waller, DG, 1986) | 0.74 |
" Nisoldipine had the lowest maximum plasma concentration and the longest elimination half-life among the four 1,4-dihydropyridines, resulting in no significant difference in the area under the plasma concentration-time curve." | ( Comparative study on acute antihypertensive effects and pharmacokinetics of nisoldipine, nifedipine, nimodipine and nicardipine administered orally to conscious renal hypertensive dogs. Kato, H; Takata, Y, 1986) | 0.49 |
"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 |
" Mean values for peak concentration, area under the serum concentration time curve (AUC), total serum clearance and the half-life of elimination of nifedipine did not differ before and concomitantly with digoxin administration." | ( Pharmacokinetic studies of nifedipine and digoxin co-administration. Granit, L; Koren, G; Levy, M; Zylber-Katz, E, 1986) | 0.77 |
"In a randomized three-way crossover study with twelve volunteers the bioavailability and main pharmacokinetic parameters of three different galenic formulations of nifedipine (hard gelatine capsule with pellets = preparation A, soft gelatine capsule with liquid nifedipine = preparation B, retard-tablet = preparation C) were determined." | ( Pharmacokinetics and bioavailability of three different galenic nifedipine preparations. Dahmen, W; Jaeger, H; Lutz, D; Molz, KH; Pabst, G, 1986) | 0.71 |
"The pharmacodynamic and pharmacokinetic profiles of nifedipine and nisoldipine were compared in a double blind, placebo-controlled study." | ( The pharmacodynamics and pharmacokinetics of a new calcium antagonist nisoldipine in normotensive and hypertensive subjects. Meredith, PA; Pasanisi, F; Reid, JL, 1985) | 0.52 |
" The relative bioavailabilities and important pharmacokinetic parameters were calculated and then statistically evaluated for significant differences between the preparations." | ( [Bioavailability of new nifedipine preparations in man. 1. Pharmacokinetics of nifedipine in the form of sustained-release tablets]. Dahmen, W; Jaeger, H; Lutz, D; Molz, KH; Pabst, G, 1985) | 0.58 |
" A compartment-independent pharmacokinetic analysis showed no difference in the absorption, elimination, or metabolism of nitrendipine between subjects with normal renal function and those with impaired renal function." | ( Pharmacokinetics of nitrendipine in patients with renal failure: comparison to normal subjects. Aronoff, GR, 1984) | 0.27 |
" The time to Cmax was not significantly different in the two groups." | ( Steady-state pharmacokinetics of nitrendipine in hepatic insufficiency. Burkholder, DE; Krol, GJ; Lasseter, KC; Murdoch, AA; Shamblen, EC; Taylor, RJ; Vanov, SK, 1984) | 0.27 |
" The present study did not show significant pharmacokinetic and pharmacodynamic interactions between nifedipine and lipophilic beta-adrenoceptor blockers." | ( Study of the influence of nifedipine on the pharmacokinetics and pharmacodynamics of propranolol, metoprolol and atenolol. Bellens, R; Degre, S; Degreve, M; Fitzsimons, TJ; Gangji, D; Herchuelz, A; Juvent, M; Niset, G; Poortmans, J; Wathieu, M, 1984) | 0.78 |
" 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 |
" The interaction of nifedipine and cimetidine is thus of clinical significance because of its pharmacodynamic effect." | ( [Effect of cimetidine and ranitidine on the pharmacokinetics and anti-hypertensive effect of nifedipine]. Heidemann, H; Janisch, HD; Kirch, W; Ohnhaus, EE; Rämsch, K, 1983) | 0.81 |
" The peak plasma concentrations and areas under the plasma concentration time curve were dose-dependent; kinetics were linear between 20 and 60 mg, and the half-life of nifedipine tablets was close to 10 hours." | ( Pharmacokinetic studies of nifedipine tablet. Correlation with antihypertensive effects. Banzet, O; Colin, JN; Corvol, P; Singlas, E; Taburet, AM; Thibonnier, M, ) | 0.62 |
" Although the profiles of the pharmacodynamic effects and of the kinetics of nicardipine were almost parallel in each individual after administration of both nicardipine formulations, there was no correlation between the nicardipine plasma relative bioavailability and its effects on brachial and carotid arteries blood flows when considering all subjects together." | ( Nicardipine: pharmacokinetics and effects on carotid and brachial blood flows in normal volunteers. Duhaze, P; Giudicelli, JF; Gueret, M; Kiechel, JR; Lhoste, F; Thuillez, C, 1984) | 0.27 |
" Plasma and urine drug concentrations were measured and the relevant pharmacokinetic parameters calculated." | ( Lack of a pharmacokinetic interaction between nifedipine and the beta-adrenoceptor blockers metoprolol and atenolol. Jack, DB; Kendall, MJ; Laugher, SJ; Lobo, J; Rolf Smith, S, 1984) | 0.53 |
" 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 |
" Pharmacodynamic steady states developed slowly within about 25 min." | ( A comparative study of the pharmacodynamic effects of nimodipine and nifedipine in the isolated spontaneously beating rabbit heart. Askholt, J; Jensen, PH; Nielsen-Kudsk, F, 1983) | 0.5 |
"25 hypertensive patients with normal or impaired renal function underwent pharmacokinetic and safety studies after single and multiple dose administration of nifedipine GITS (Gastro-Intestinal Therapeutic System) 60mg tablets." | ( Pharmacokinetic profile of nifedipine GITS in hypertensive patients with chronic renal impairment. Brendel, E; Griffel, L; Iaina, A; Kobelt, R; Schneider, R; Stolero, D, 1994) | 0.78 |
" Nicardipine increased significantly the AUC and Cmax of oral propranolol (1." | ( Influences of the calcium antagonists nicardipine and nifedipine, and the calcium agonist BAY-K-8644, on the pharmacokinetics of propranolol in rats. Dupont, AG; Massart, DL; Schoors, DF; Vercruysse, I, 1993) | 0.53 |
" Pharmacokinetic parameters were as follows: Cmax, 59." | ( [Effects of slow-release nifedipine on hemodynamics and pharmacokinetics in elderly hypertensives]. Nakamura, H; Shimamoto, H; Shimamoto, Y, 1994) | 0.59 |
" 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 |
" Drugs characterized by low accumulation indices (AI) showed virtually no change in the 90% confidence interval (CI) of AUC and CMAX upon multiple dosing." | ( Comparison of single and multiple dose pharmacokinetics using clinical bioequivalence data and Monte Carlo simulations. el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1994) | 0.29 |
" The calculated CLH values were then compared to literature values of clearance (CL) to the same metabolite obtained during pharmacokinetic studies in humans." | ( Predicting the hepatic clearance of xenobiotics in humans from in vitro data. Hoener, BA, 1994) | 0.29 |
" Grapefruit juice increased the AUC and cmax of 1 statistically significantly by 103 (SD 73, range 48 to 265)% and 94 (SD 83, range -23 to 259)%, respectively." | ( Influence of grapefruit juice on the pharmacokinetics of a slow release nifedipine formulation. Henschel, L; Hippius, M; Hoffmann, A; Kaufmann, K; Sigusch, H, 1994) | 0.52 |
"A comprehensive study was undertaken to examine the pharmacokinetic and pharmacodynamic interaction of propranolol and nifedipine in 11 patients with stable angina of effort who were treated for a long time." | ( [The pharmacokinetic interaction of propranolol and nifedipine in patients with angina of effort]. Belolipetskaia, VG; Kokurina, EV; Kukushkin, SK; Metelitsa, VI; Piotrovskiĭ, VK; Rumiantsev, DO, ) | 0.59 |
" Both the area under the plasma concentration-time curve (AUC) and terminal half-life of nifedipine were significantly higher in South Asians compared with Caucasian subjects after single oral doses of 10 and 20 mg." | ( The influence of dose and ethnic origins on the pharmacokinetics of nifedipine. Ahsan, CH; Amanullah, M; Challenor, VF; George, CF; Renwick, AG; Waller, DG, 1993) | 0.74 |
" These results suggest that quinidine inhibits nifedipine metabolism, and this pharmacokinetic interaction results in enhanced pharmacologic response." | ( Evaluation of the pharmacokinetic and pharmacodynamic interaction between quinidine and nifedipine. Bowles, SK; Cardozo, L; Edwards, DJ; Reeves, RA, 1993) | 0.77 |
" After nifedipine pretreatment, the maximum concentration (Cmax) of diltiazem was increased and the time of Cmax was shortened, and the area under the concentration curve (AUC) tended to be increased." | ( The effect of nifedipine on the pharmacokinetics and dynamics of diltiazem: the preliminary study in normal volunteers. Ebihara, A; Fujimura, A; Ohashi, K; Sakamoto, K; Sudo, T; Tateishi, T, 1993) | 1.1 |
" Cmax and AUC rose non-linearly with increasing doses in all three species." | ( Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human. Hashimoto, K; Higuchi, S; Teramura, T; Watanabe, T, 1995) | 0.29 |
" A pharmacokinetic characteristics of new drug adalate SL with two-step liberation of nifedipine." | ( [The pharmacokinetics of different drug forms of nifedipine when used singly and in a course as monotherapy and in combination with Cordanum and triampur preparations in patients with arterial hypertension]. Ignat'ev, VG; Kukes, VG; Pavlov, SS; Starodubtsev, AK, ) | 0.61 |
" After oral lidocaine, cirrhotic patients has a longer time to peak concentration (Tmax) and elimination half-life (t1/2), and a higher area under the curve (AUC)." | ( Pharmacokinetics of oral lidocaine and nifedipine in patients with liver cirrhosis. Klangwarnwong, D; Manorot, M; Praisontarangkul, OA; Tonsuwannont, W, 1996) | 0.56 |
"Comparative pharmacokinetic studies have been carried out with two 20 mg nifedipine active substance-containing retard film coated tablets, Cordaflex produced by EGIS Pharmaceuticals Co." | ( [Comparative human pharmacokinetic studies of 20 mg nifedipine-containing Cordaflex and Adalat film coated retared tablets]. Balogh, J; Baloghné, NK; Cseh, A; Farsang, C; Grézal, G; Horvai, G; Horváth, V; Klebovich, I; Kocsi, E, 1996) | 0.78 |
" Although it is recognised that CR drug formulations may enhance the treatment compliance of patients by reducing the number of daily doses, there are several pharmaceutical, pharmacokinetic and pharmacological considerations which may influence the ultimate selection of a particular dosage form." | ( The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Foster, RT; Grundy, JS, 1996) | 0.85 |
" In conclusion, isolated mesenteric arteries from obese Zucker rats do not show relevant structural changes, and the pharmacodynamic behaviour of such vessels appears to be the same as that of control preparations." | ( Pharmacodynamic behaviour of isolated resistance vessels obtained from hypertensive-diabetic rats. Kam, KL; Pfaffendorf, M; van Zwieten, PA, 1996) | 0.29 |
" The study demonstrated that axial stretching of an artery has impact on the pharmacodynamic reactivity to nifedipine in porcine coronary arteries." | ( Porcine coronary artery pharmacodynamics in vitro evaluated by a new intravascular technique: relation to axial stretch. Bagger, JP; Frøbert, O; Gregersen, H; Mikkelsen, EO; Nyborg, NC, 1996) | 0.51 |
"The plasma concentration time profiles and the pharmacokinetic parameters estimated for these drugs were in the expected range, except for furosemide, whose bioavailability was lower than reported in the literature." | ( Effect of the lipase inhibitor orlistat on the pharmacokinetics of four different antihypertensive drugs in healthy volunteers. Jonkmann, JH; Schmidtke-Schrezenmeier, G; Tam, YK; van Brummelen, P; Weber, C, 1996) | 0.29 |
" This communication highlights the possible pharmacokinetic basis of the reported digoxin-nifedipine interaction." | ( Pharmacokinetic basis of nifedipine-digoxin interaction: a commentary. Kokwaro, GO, 1995) | 0.82 |
" No statistically significant difference in pharmacokinetic parameters was observed between the three treatment groups." | ( Effects of nifedipine and diltiazem on pharmacokinetics of cefpodoxime following its oral administration. Camus, F; Carbon, C; Deslandes, A; Farinotti, R; Lacroix, C, 1996) | 0.68 |
"Calcium channel antagonists in different pharmacokinetic formulations are widely used in patients with coronary artery disease or hypertension." | ( Differential activation of cardiac and peripheral sympathetic nervous system by nifedipine: role of pharmacokinetics. Allegranza, G; Binggeli, C; Lüscher, TF; Noll, G; Shaw, S; Weidmann, P; Wenzel, RR, 1997) | 0.52 |
"The pharmacokinetic interaction of oral rifampicin (1200 mg) and oral nifedipine (10 mg capsules), given as single doses, was investigated in six healthy volunteers (mean age 28." | ( The effect of single does of rifampicin on the pharmacokinetics of oral nifedipine. Abdu-Aguye, I; Mustapha, A; Ndanusa, BU, 1997) | 0.76 |
"The aim of this series of studies was to determine the potential for pharmacokinetic interaction between candesartan (administered orally as the prodrug candesartan cilexetil) and hydrochlorothiazide (HCTZ), nifedipine, glibenclamide, warfarin, digoxin or the components of an oral contraceptive formulation." | ( Pharmacokinetic drug interaction studies with candesartan cilexetil. Högemann, A; Jonkman, JH; Lins, R; Sennewald, R; van Heiningen, PN; van Lier, JJ, 1997) | 0.48 |
"The pharmacokinetic parameters (AUC, Cmax, Tmax, and t1/2) of nifedipine following single oral administration of a 10 mg capsule of test product were compared to those of the same amount of a reference product." | ( Comparative pharmacokinetics of two nifedipine products in capsule form following single oral administration in healthy volunteers. al-Qato, MK; Battah, AH; Irshaid, YM; Rawashdeh, NM, ) | 0.65 |
" To test this hypothesis, we conducted three randomized, double-masked, placebo-controlled studies to evaluate how coadministration of tamsulosin would affect the pharmacodynamic profiles of nifedipine, enalapril, and atenolol." | ( Coadministration of tamsulosin and three antihypertensive agents in patients with benign prostatic hyperplasia: pharmacodynamic effect. Lowe, FC, ) | 0.32 |
"A light breakfast produced a delay in gastric emptying (indicated by the rate of paracetamol absorption) compared with the fasting state but did not alter the tmax or Cmax for nifedipine significantly." | ( The influence of two types of meal on the pharmacokinetics of a modified-release formulation of nifedipine (Adalat Retard). Armstrong, J; Challenor, VF; Macklin, BS; Renwick, AG; Waller, DG, 1997) | 0.71 |
" The food interaction pharmacokinetic study of Cordaflex 20 mg retard filmtablet was carried out in 12 healthy male volunteers treated with a single dose of the preparation both after fasting and after food ingestion, in a crossover design allowing 1 week of wash-out period between the 2 treatments." | ( Food interaction pharmacokinetic study of cordaflex 20 mg retard filmtablet in healthy volunteers. Balogh Nemes, K; Csörgö, M; Drabant, S; Grézal, G; Horvai, G; Horváth, V; Hrabéczy-Páll, A; Klebovich, I; Kocsi, E; Renczes, G, 1998) | 0.3 |
" Prediction of food effect response on the basis of the physicochemical and pharmacokinetic characteristics of the drug molecule or formulations is discussed." | ( [Role of food interaction pharmacokinetic studies in drug development. Food interaction studies of theophylline and nifedipine retard and buspirone tablets]. Drabant, S; Farsang, C; Gachályi, B; Klebovich, I; Renczes, G, 1998) | 0.51 |
" doses, respectively, thereby increasing AUC0-infinity, Cmax and half-life." | ( Effects of hyperlipidemia on the pharmacokinetics of nifedipine in the rat. Eliot, LA; Foster, RT; Jamali, F, 1999) | 0.55 |
"In the present study, Diabecon (D-400), a herbomineral anti-diabetic preparation, was studied for its pharmacokinetic interaction with the commonly used drugs rifampicin and nifedipine." | ( Pharmacokinetic interaction of Diabecon (D-400) with rifampicin and nifedipine. Gopumadhavan, S; Mitra, SK; Sundaram, R; Venkataranganna, MV, ) | 0.56 |
" In general, the pharmacokinetic consequences of hyperlipidemia include increased total drug concentrations and decreased unbound fraction in plasma." | ( Pharmacokinetics and pharmacodynamics of nifedipine in untreated and atorvastatin-treated hyperlipidemic rats. Eliot, LA; Jamali, F, 1999) | 0.57 |
"34) or time to peak concentration compared with nifedipine alone." | ( Rosiglitazone has no clinically significant effect on nifedipine pharmacokinetics. Finnerty, D; Freed, MI; Harris, RZ; Inglis, AM; Jorkasky, DK; Miller, AK; Patterson, S; Thompson, KA, 1999) | 0.81 |
" A Cmax > or = 878 ng/ml was the best predictor for the appearance of tremor." | ( Impact of cyclosporin A pharmacokinetics on the presence of side effects in pediatric renal transplantation. Arai Furusawa, E; Cavalcante, JS; David-Neto, E; Ianhez, LE; Lemos, FBC; Romano, P; Schwartzman, BS; Yagyu, EM, 2000) | 0.31 |
" The method is sensitive and reliable for pharmacokinetic studies and therapeutic drug monitoring of nifedipine in humans after the oral administration of immediate-release capsules and sustained-release tablets to five healthy subjects." | ( Liquid chromatographic assay of nifedipine in human plasma and its application to pharmacokinetic studies. Abou-Auda, HS; Al-Fawzan, NF; Al-Hadiya, BM; Al-Khamis, KI; Ghilzai, NM; Najjar, TA, 2000) | 0.81 |
" UVA irradiation did not significantly affect any of the other measured pharmacokinetic parameters (Cmax, t 1/2, tmax)." | ( The effect of whole-body sunbed ultraviolet A exposure on the pharmacokinetics of the photolabile drug nifedipine. Al-Ajmi, HS; Dawe, RS; Ferguson, J; Gibbs, NK; Macklin, BS; Renwick, AG, 2000) | 0.52 |
" Twenty-four hours after LPS injection, the pharmacokinetic parameters of the four drugs were obtained following intravenous administrations of antipyrine (7 mg/kg), theophylline (5 mg/kg), phenytoin (10 mg/kg) and nifedipine (1 mg/kg)." | ( The impact of acute phase response on the plasma clearance of antipyrine, theophylline, phenytoin and nifedipine in rabbits. Kokue, E; Saitoh, T; Shimoda, M, 2000) | 0.71 |
" The method has been applied to pharmacokinetic study." | ( [Determination of nifedipine in human plasma by gas chromatography and its pharmacokinetic study]. Wang, Y; Wu, J; Zhang, ZX, 1997) | 0.63 |
"It has been reported that grapefruit juice (GJ) causes a pharmacokinetic interaction with many drugs after co-ingestion." | ( Effects of furanocoumarin derivatives in grapefruit juice on nifedipine pharmacokinetics in rats. Mohri, K; Uesawa, Y, 2001) | 0.55 |
"The pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme (ACE) inhibitor imidapril with other therapeutic principles used in hypertension and heart failure were evaluated." | ( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine. Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001) | 0.31 |
" Plasma concentrations of imidaprilat and H were followed up to 48 h, those of B and N up to 24 h and area under the concentration time curve (AUC), maximum plasma concentration (Cmax) and time to Cmax (tmax) were determined." | ( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine. Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001) | 0.31 |
"The combination of imidapril with a diuretic, beta-adrenoceptor antagonist or calcium-channel blocker seems a reasonable and safe treatment option when striving for additive pharmacodynamic effects not accompanied by relevant pharmacokinetic interactions." | ( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine. Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001) | 0.31 |
"Our objective was to investigate ethnic differences in the oral pharmacokinetics of nifedipine and erythromycin, both typical cytochrome P4503A (CYP3A) substrates, in Koreans and Caucasians and to identify the nature of any correlations between the pharmacokinetic parameters of the two drugs." | ( Ethnic differences and relationships in the oral pharmacokinetics of nifedipine and erythromycin. Bae, KS; Cho, JY; Jang, IJ; Lim, HS; Shin, SG; Shon, JH; Yi, SY; Yu, KS, 2001) | 0.77 |
" Pharmacokinetic evaluations were performed, and parameters were compared for the two ethnic groups." | ( Ethnic differences and relationships in the oral pharmacokinetics of nifedipine and erythromycin. Bae, KS; Cho, JY; Jang, IJ; Lim, HS; Shin, SG; Shon, JH; Yi, SY; Yu, KS, 2001) | 0.55 |
" Hemodynamic changes after nifedipine administration paralleled those of the pharmacokinetic differences, with significantly greater decreases in blood pressure and total peripheral resistance noted in Koreans." | ( Ethnic differences and relationships in the oral pharmacokinetics of nifedipine and erythromycin. Bae, KS; Cho, JY; Jang, IJ; Lim, HS; Shin, SG; Shon, JH; Yi, SY; Yu, KS, 2001) | 0.84 |
"A suitable, convenient and simple HPLC assay for pharmacokinetic study of mebudipine in rabbits was developed." | ( High performance liquid chromatography of mebudipine: application to pharmacokinetic study. Bohlooli, S; Keyhanfar, F; Mahmoudian, M, ) | 0.13 |
" For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater Cmax and AUC0-24 than did subjects in the control group." | ( [Effect of grapefruit pulp on the pharmacokinetics of the dihydropyridine calcium antagonists nifedipine and nisoldipine]. Itou, K; Kariya, S; Kasuyama, K; Kawabata, S; Kotaki, H; Morikawa, A; Nishida, N; Ohtani, M; Seo, I; Uchino, K, 2002) | 0.53 |
" Calculation of pharmacokinetic parameters was conducted model-independently." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.57 |
" Under fed conditions the differences in bioavailability between the two products as characterized by the pharmacokinetic parameters AUC(0,tn) and Cmax were greater than after fasting conditions with point estimates of 69." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.57 |
" The classical pharmacokinetic model for designing CRDDS [Drug Dev." | ( Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index. Panchagnula, R; Sood, A, 2003) | 0.32 |
" The method was not interfered with by other plasma components and was applied for the determination of nifedipine in pharmacokinetic study after single oral administration of 10 mg nifedipine to 18 healthy male subjects." | ( Determination of nifedipine in human plasma by solid-phase extraction and high-performance liquid chromatography: validation and application to pharmacokinetic studies. Daftsios, AC; Niopas, I, 2003) | 0.87 |
" Pharmacokinetic study: plasma samples were collected periodically after intravenous (0." | ( Application of a new high performance liquid chromatography method to the pharmacokinetics of dibudipine in rats. Bohlooli, S; Ghiaee, S; Keyhanfar, F; Mahmoudian, M, ) | 0.13 |
"To examine the reproducibility of nifedipine absorption from gastrointestinal therapeutic system (GITS) tablets by comparing the single-dose pharmacokinetic profiles of 4 different dosages administered orally." | ( Reproducibility of nifedipine absorption from GITS tablets: comparison of single-dose pharmacokinetics using 10, 20, 40 and 60 mg nifedipine. Okumura, K; Orii, Y; Tanaka, T; Tateishi, T, 2004) | 0.93 |
" Coefficients of variation (CV) of dose-corrected area under the concentration-time curve (AUC) and peak plasma drug concentrations (Cmax) were calculated from the pharmacokinetic profiles." | ( Reproducibility of nifedipine absorption from GITS tablets: comparison of single-dose pharmacokinetics using 10, 20, 40 and 60 mg nifedipine. Okumura, K; Orii, Y; Tanaka, T; Tateishi, T, 2004) | 0.65 |
"Mean AUC and mean Cmax were dose-proportional from 10 to 60 mg." | ( Reproducibility of nifedipine absorption from GITS tablets: comparison of single-dose pharmacokinetics using 10, 20, 40 and 60 mg nifedipine. Okumura, K; Orii, Y; Tanaka, T; Tateishi, T, 2004) | 0.65 |
" Pharmacokinetic parameters derived from Adalat administration were calculated by non-compartmental analysis with the WinNonlin program." | ( Pharmacokinetics of nifedipine in Taiwanese. Chien, SC; Hsu, KY; Lin, HY; Uang, YS, 2004) | 0.65 |
" 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 |
" These modifications are generally responsible for reduced plasma concentration and reduced half-life of most drugs." | ( Pharmacokinetics of tocolytic agents. Cabrol, D; Carbonne, B; Tsatsaris, V, 2004) | 0.32 |
" The pharmacokinetic parameters were calculated by 3P97 software." | ( [Pharmacokinetics of m-nifedipine in Beagle dogs]. Mei, QB; Yang, TH; Yang, ZF; Zhou, SY, 2004) | 0.63 |
" Simultaneous oral ingestion of GBE (240 mg) did not significantly affect any of the mean pharmacokinetic parameters of either NFP or dehydronifedipine, a major metabolite of NFP, after oral administration of NFP (10 mg)." | ( Studies on interactions between functional foods or dietary supplements and medicines. IV. Effects of ginkgo biloba leaf extract on the pharmacokinetics and pharmacodynamics of nifedipine in healthy volunteers. Koishi, T; Kuroda, K; Matsumoto, T; Nakagawa, M; Obata, Y; Ohkuni, T; Ohnishi, N; Tagagi, K; Takara, K; Yokoyama, T; Yoshioka, M, 2004) | 0.72 |
" This new extended-release formulation has interesting pharmacokinetic parameters and may be effective in conditions in which dihydropyridine calcium channel blockers are indicated." | ( Pharmacokinetics of a new extended-release nifedipine formulation following a single oral dose, in human volunteers. Bartiromo, M; Bertolini, A; Cainazzo, MM; Forgione, A; Pinetti, D; Savino, G, 2005) | 0.59 |
" There was a dosing time dependency on the tissue distribution 30 min after administration, showing a similar tendency to the pharmacokinetic behavior." | ( Circadian variations in the pharmacokinetics, tissue distribution and urinary excretion of nifedipine after a single oral administration to rats. Cao, QR; Choi, JS; Kim, TW; Lee, BJ, 2005) | 0.55 |
"It has been reported that grapefruit juice (GJ) causes pharmacokinetic interactions with many drugs after co-ingestion, but the effects of the juice of sweetie fruit, a cross between a pomelo and a grapefruit, on the pharmacokinetics of medicines have not been clear." | ( [Effects of sweetie juice on nifedipine pharmacokinetics in rats]. Mohri, K; Uesawa, Y, 2005) | 0.62 |
" On the other hand, there were no significant differences in the mean peak value time in plasma (T(max)) and the elimination half-life (t1/2(ke)) between the control and the treated groups." | ( [Effect of kaempferol on the pharmacokinetics of nifedipine in rats]. Xu, M; Yang, M; Zheng, YF; Zhu, HJ; Zhu, XQ, 2006) | 0.59 |
"The concomitant oral use of kaempferol with NFP may influence the pharmacokinetic parameters of NFP in rats, which suggests that kaempferol might reduce the first-pass metabolism of NFP." | ( [Effect of kaempferol on the pharmacokinetics of nifedipine in rats]. Xu, M; Yang, M; Zheng, YF; Zhu, HJ; Zhu, XQ, 2006) | 0.59 |
" 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 |
" Grapefruit juice in quartz vessels was UV irradiated (302 nm) with a transilluminator for 0 to 6 h at 4 degrees C, and furanocoumarins, potent contributors to the pharmacokinetic interaction, in each juice sample were measured using HPLC." | ( UV-irradiated grapefruit juice loses pharmacokinetic interaction with nifedipine in rats. Mohri, K; Uesawa, Y, 2006) | 0.57 |
" In addition, the pharmacokinetic interaction between CJ and NFP in vivo was confirmed in rats." | ( Effects of cranberry juice on nifedipine pharmacokinetics in rats. Mohri, K; Uesawa, Y, 2006) | 0.62 |
" The aim of this study was to evaluate the pharmacokinetic interactions between Sairei-to and nifedipine (NFP), a substrate for CYP3A, in rats." | ( Effects of Sairei-to on the pharmacokinetics of nifedipine in rats. Ikehata, M; Kawakita, T; Kiyohara, Y; Maeda, A; Matsumoto, T; Ohnishi, N; Takara, K; Yokoyama, T, 2008) | 0.82 |
" Pharmacokinetic parameters were calculated by non-compartmental methods, and the potential interaction by silymarin was handled as an equivalence problem." | ( The effect of silymarin on oral nifedipine pharmacokinetics. Beckmann-Knopp, S; Fuhr, U; Jetter, A; Lück, H; Mengs, U, 2007) | 0.62 |
"GITS tablets 90 mg/d are an alternative dosage regimen to previous used slow-release tablets 60 mg/d for tocolysis with similar pharmacokinetic profile and a good tolerance." | ( Nifedipine gastrointestinal therapeutic system (GITS) as an alternative to slow-release for tocolysis--tolerance and pharmacokinetic profile. Burkhardt, T; Juon, AM; Krähenmann, F; Kühn-Velten, WN; von Mandach, U; Zimmermann, R, 2008) | 1.79 |
" 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 method was successfully applied to a clinical pharmacokinetic study of lacidipine in healthy volunteers following oral administration." | ( Ultra-performance liquid chromatography-tandem mass spectrometry for the determination of lacidipine in human plasma and its application in a pharmacokinetic study. Cheng, G; Peng, W; Tang, J; Zhao, R; Zhu, R, 2008) | 0.35 |
" The aim of this study was to investigate the pharmacokinetic characteristics of these derivatives to provide reference for their further evaluation and modification." | ( Pharmacokinetics of the analogs at C3 and C5 of m-nifedipine in beagle dogs. Liu, XY; Mei, QB; Yang, TH; Yang, ZF; Zhou, SY, 2008) | 0.6 |
" Serum concentrations of nifedipine and lidocaine were determined by a high-performance liquid chromatography method in order to calculate pharmacokinetic parameters." | ( Pharmacokinetics of anorectal nifedipine and lidocaine (lignocaine) ointment following haemorrhoidectomy: an open-label, single-dose, phase IV clinical study. Antropoli, C; Cerutti, R; Cusato, M; Dominici, P; Giannotti, G; Grossi, E; Perrotti, P; Regazzi, M, 2009) | 0.94 |
"8%), consistent with therapeutically negligible concentrations and insufficient to permit calculation of any pharmacokinetic parameters." | ( Pharmacokinetics of anorectal nifedipine and lidocaine (lignocaine) ointment following haemorrhoidectomy: an open-label, single-dose, phase IV clinical study. Antropoli, C; Cerutti, R; Cusato, M; Dominici, P; Giannotti, G; Grossi, E; Perrotti, P; Regazzi, M, 2009) | 0.64 |
"The objective of this study was to evaluate whether pharmacokinetic parameters (clearance and volume of distribution of the central compartment) from a sparse sampling population pharmacokinetic study can be obtained with a very small sample size." | ( Population pharmacokinetics with a very small sample size. Duan, J; Mahmood, I, 2009) | 0.35 |
"The pharmacokinetic characteristics were found by a two-compartment model following the oral administration of NF-loaded N-succinyl chitosan/alginate hydrogel beads in rabbits." | ( Pharmacokinetics of a novel nifedipine and pH-sensitive N-succinyl chitosan/alginate hydrogel bead in rabbits. He, JQ; Li, P; Liu, X; Yuan, W; Zhu, XJ, 2010) | 0.65 |
" Pharmacokinetic parameters of nifedipine were determined in rats following an oral gavage (3 mg/kg) or intravenous administration (0." | ( Effect of diallyl trisulfide on the pharmacokinetics of nifedipine in rats. Cheng, G; Ren, JG; Wang, Y; Zhao, N; Zhou, H; Zou, MJ, ) | 0.66 |
" The method was fully validated and successfully applied to a clinical pharmacokinetic study of nifedipine sustained-release tablet in healthy male volunteers." | ( Determination of nifedipine in human plasma by ultra performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. Jiang, K; Li, F; Lu, X; Qin, F; Wang, D; Yang, S, 2011) | 0.93 |
" Non-compartmental pharmacokinetic analysis was used to estimate nifedipine exposure at steady state." | ( A pilot study of the impact of genotype on nifedipine pharmacokinetics when used as a tocolytic. Haas, DM; Jones, DR; McCormick, CL; Quinney, SK; Renbarger, JL, 2012) | 0.88 |
" However, the formulation of nifedipine has undergone a number of modifications over time to improve the pharmacokinetic profile and administration regimen from 3 times daily to once daily." | ( Once daily nifedipine: the formulation dictates the pharmacokinetic characteristics and the therapeutic responses. Elliott, HL; Meredith, PA; Toal, CB, 2012) | 1.06 |
" Thus, this study was performed to investigate the pharmacokinetic and pharmacodynamic interactions between nifedipine and metformin, since both drugs were commonly metabolized via hepatic CYP2C and 3A subfamilies in rats." | ( Pharmacokinetic and pharmacodynamic interaction between nifedipine and metformin in rats: competitive inhibition for metabolism of nifedipine and metformin by each other via CYP isozymes. Choi, YH; Lee, MG, 2012) | 0.84 |
" The aim of the current study was to use in vitro data on a number of CYP3A4 substrates to develop mechanistic population pharmacokinetic models which are capable of integrating various attributes of drugs and estimating the statistical power of in vivo studies designed to discern sex differences in the clearance of CYP3A4 substrates." | ( Sex differences in the clearance of CYP3A4 substrates: exploring possible reasons for the substrate dependency and lack of consensus. Chetty, M; Mattison, D; Rostami-Hodjegan, A, 2012) | 0.38 |
"Pregnant women receiving oral nifedipine underwent steady-state pharmacokinetic testing over one dosing interval." | ( Nifedipine pharmacokinetics are influenced by CYP3A5 genotype when used as a preterm labor tocolytic. Caritis, SN; Clark, S; Clay, JM; Haas, DM; Hebert, MF; Quinney, SK; Renbarger, JL; Umans, JG, 2013) | 2.12 |
" The validated assay method was successfully applied to a pharmacokinetic study in humans." | ( Sensitive LC-MS/MS-ESI method for simultaneous determination of nifedipine and atenolol in human plasma and its application to a human pharmacokinetic study. Inamadugu, JK; Kallem, RR; Ramesh, M; Seshagirirao, JV, 2013) | 0.63 |
"A more rapid, sensitive and specific high-performance liquid chromatography coupled to -tandem mass spectrometry (HPLC-MS/MS) was developed and validated for the quantification of nifedipine in human plasma, and applied to the pharmacokinetic study of nifedipine in Chinese healthy volunteers." | ( A more rapid, sensitive, and specific HPLC-MS/MS method for nifedipine analysis in human plasma and application to a pharmacokinetic study. Chen, R; Guo, R; Huang, J; Li, R; Liu, X; Lv, C; Wang, B; Wei, C; Yuan, G, 2013) | 0.82 |
" The pharmacokinetic parameters of repaglinide and blood glucose concentrations were also determined in rats after oral (0." | ( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine. Choi, DH; Choi, I; Choi, JS, 2013) | 0.78 |
" In conclusion, the pharmacokinetic changes of nifedipine may be modulated by the inhibitory effects of baicalin on plasma protein binding and CYP3A-mediated metabolism." | ( Contribution of baicalin on the plasma protein binding displacement and CYP3A activity inhibition to the pharmacokinetic changes of nifedipine in rats in vivo and in vitro. Cheng, ZY; Gao, J; Jia, LJ; Li, HM; Qiao, HL; Tian, X, 2014) | 0.86 |
" A physiologically based pharmacokinetic (PBPK) model was developed to project the dynamics and magnitude of CYP3A4 induction in vivo from in vitro data generated with primary human hepatocytes." | ( Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: influence of time between substrate and inducer administration. Baneyx, G; Iliadis, A; Lavé, T; Meille, C; Parrott, N, 2014) | 0.4 |
" The pharmacokinetic parameters of nifedipine and/or dehydronifedipine were determined after oral and intravenous administration of nifedipine to rats in the absence (control) and presence of licochalcone A (0." | ( Effects of licochalcone A on the bioavailability and pharmacokinetics of nifedipine in rats: possible role of intestinal CYP3A4 and P-gp inhibition by licochalcone A. Choi, DH; Choi, JS, 2014) | 0.91 |
" The aim of this study was to determine nifedipine slow-release half-life and distribution volume in pregnant women and to compare these with pharmacokinetic parameters of nifedipine in non-pregnant subjects described in the literature." | ( Pharmacokinetics of nifedipine slow-release during sustained tocolysis. Kwee, A; Lotgering, FK; Mol, BW; Papatsonis, DN; Porath, MM; Roos, C; Spaanderman, ME; ter Laak, MA; Touw, DJ; van 't Veer, NE; van der Post, JA; van Hattum, PR; van Pampus, MG, 2015) | 1.01 |
" Exclusion criteria for the pharmacokinetic study were contra-indications for nifedipine, impaired liver function, and concomitant intake of inhibitors or inducers of the cytochrome P450 3A4 isoenzyme." | ( Pharmacokinetics of nifedipine slow-release during sustained tocolysis. Kwee, A; Lotgering, FK; Mol, BW; Papatsonis, DN; Porath, MM; Roos, C; Spaanderman, ME; ter Laak, MA; Touw, DJ; van 't Veer, NE; van der Post, JA; van Hattum, PR; van Pampus, MG, 2015) | 0.97 |
"Pharmacokinetic parameters were estimated using iterative two-stage Bayesian population pharmacokinetic analysis by MWPharm© software." | ( Pharmacokinetics of nifedipine slow-release during sustained tocolysis. Kwee, A; Lotgering, FK; Mol, BW; Papatsonis, DN; Porath, MM; Roos, C; Spaanderman, ME; ter Laak, MA; Touw, DJ; van 't Veer, NE; van der Post, JA; van Hattum, PR; van Pampus, MG, 2015) | 0.74 |
"The pharmacokinetic parameters of nifedipine slow-release tablets were determined from the data of 8 pregnant women." | ( Pharmacokinetics of nifedipine slow-release during sustained tocolysis. Kwee, A; Lotgering, FK; Mol, BW; Papatsonis, DN; Porath, MM; Roos, C; Spaanderman, ME; ter Laak, MA; Touw, DJ; van 't Veer, NE; van der Post, JA; van Hattum, PR; van Pampus, MG, 2015) | 1.02 |
"Pregnant subjects in this study, using nifedipine slow-release tablets, showed a larger volume of distribution and a shorter elimination half-life than for non-pregnant subjects as published in the literature." | ( Pharmacokinetics of nifedipine slow-release during sustained tocolysis. Kwee, A; Lotgering, FK; Mol, BW; Papatsonis, DN; Porath, MM; Roos, C; Spaanderman, ME; ter Laak, MA; Touw, DJ; van 't Veer, NE; van der Post, JA; van Hattum, PR; van Pampus, MG, 2015) | 1.01 |
" The pharmacokinetic parameters of nifedipine and dehydronifedipine were determined after oral and intravenous administrations of nifedipine to rats in the presence and absence of pioglitazone (0." | ( Effects of pioglitazone on the pharmacokinetics of nifedipine and its main metabolite, dehydronifedipine, in rats. Choi, DH; Choi, I; Choi, JS, 2016) | 0.96 |
"We determined the pharmacokinetic parameters of nifedipine and dehydronifedipine in rats after oral and intravenous administration of nifedipine without and with HMG-CoA reductase inhibitors." | ( Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of nifedipine in rats: Possible role of P-gp and CYP3A4 inhibition by HMG-CoA reductase inhibitors. Choi, DH; Choi, JS; Lee, CK, 2015) | 0.91 |
"Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
" The estimated pharmacokinetic parameters of nifedipine showed a mean AUC(0-12) of 250." | ( Analysis of nifedipine in human plasma and amniotic fluid by liquid chromatography-tandem mass spectrometry and its application to clinical pharmacokinetics in hypertensive pregnant women. Carvalho, DM; Cavalli, RC; Duarte, G; Filgueira, GC; Filgueira, OA; Lanchote, VL; Marques, MP; Moisés, EC, 2015) | 1.06 |
" The pharmacokinetic crossover study in healthy volunteers (N = 6) did not show a significant effect of the water volume administered with the capsule (50 vs." | ( Effect of Gastric Fluid Volume on the In Vitro Dissolution and In Vivo Absorption of BCS Class II Drugs: a Case Study with Nifedipine. Fadda, HM; Foster, DR; Nader, AM; Quinney, SK, 2016) | 0.64 |
"The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to examine the influence of the biopharmaceutics classification system class on the simulation success." | ( Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models. Aarons, L; Darwich, A; Dressman, J; Hansmann, S; Margolskee, A, 2016) | 0.43 |
"To investigate the pharmacokinetic (PK) profiles and safety of nifedipine and candesartan after a single oral dose of nifedipine gastrointestinal therapeutic system (GITS) 30 mg/candesartan cilexetil 8 mg (N30/C8 mg) fixed-dose combination (FDC) in adults with mild to moderate hepatic impairment." | ( Pharmacokinetics and safety of nifedipine GITS/candesartan fixed-dose combination in subjects with hepatic impairment
. Blode, H; Boettcher, MF; Brendel, E; Halabi, A; Liu, Y; Schmidt, A; Unger, S, 2017) | 0.98 |
" A physiologically based pharmacokinetic (PBPK) model that includes inhibition constant evaluated in cryopreserved hepatocytes was used to predict drug-drug interactions (DDIs) between orally administered nifedipine, a CYP substrate, and fluconazole or ketoconazole, CYP inhibitors, in rats." | ( Quantitative prediction of the extent of drug-drug interaction using a physiologically based pharmacokinetic model that includes inhibition of drug metabolism determined in cryopreserved hepatocytes. Amano, N; Hirabayashi, H; Iwasaki, S, 2018) | 0.67 |
"Physiologically based pharmacokinetic modeling is considered a valuable tool for predicting pharmacokinetic changes in pregnancy to subsequently guide in-vivo pharmacokinetic trials in pregnant women." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
"Quantitative information on gestation-specific changes in enzyme activity available in the literature was incorporated in a pregnancy physiologically based pharmacokinetic model and the pharmacokinetics of eight drugs metabolized via one or multiple cytochrome P450 enzymes was predicted." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
"The pregnancy physiologically based pharmacokinetic model successfully predicted the pharmacokinetics of all tested drugs." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
"The presented pregnancy physiologically based pharmacokinetic model can quantitatively predict the pharmacokinetics of drugs that are metabolized via one or multiple cytochrome P450 enzymes by integrating prior knowledge of the pregnancy-related effect on these enzymes." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
"Concomitant administration of P-glycoprotein substrates and inhibitors may cause pharmacokinetic drug interactions leading to increased concentrations associated with serious side effects and toxicities." | ( Pharmacokinetics of talinolol is modified by barnidipine: implication of P-glycoprotein modulation. Okyar, A; Ozturk, D; Ozturk, N; Pala-Kara, Z, 2017) | 0.46 |
"9 g/kg SY, nifedipine clearance decreased by 34% and half-life increased by 142%." | ( Shenmai-Yin decreased the clearance of nifedipine in rats: The involvement of time-dependent inhibition of nifedipine oxidation. Chen, AC; Chen, WC; Lu, CK; Ueng, YF; Wang, HJ, 2019) | 1.17 |
" Owing to the risk of pharmacokinetic drug-drug interactions based on CYP3A4/CYP2C9 inhibition by apatinib, caution is advised in the concurrent use of apatinib with either CYP2C9 or CYP3A4 substrates." | ( Effects of Apatinib on the Pharmacokinetics of Nifedipine and Warfarin in Patients with Advanced Solid Tumors. Chen, XY; Guo, LX; Li, W; Liu, YP; Mao, SY; Qu, XJ; Teng, Z; Wang, QR; Zhang, YF; Zhong, DF; Zhu, YT, 2020) | 0.82 |
"The purpose of this research work was to evaluate the Pharmacokinetic (PK), Pharmacodynamic (PD), and the distribution pattern of mucoadhesive microspheres of nifedipine." | ( Pharmacokinetic and Pharmacodynamic Studies of Nifedipine Loaded Microspheres for the Treatment of Hypertension. Garg, R; Gupta, GD; Lal, C, 2021) | 1.08 |
" The purpose of this study is to apply a physiologically based pharmacokinetic (PBPK) modeling approach to investigate the DDI mechanism for an immediate release formulation of nifedipine with omeprazole." | ( Physiologically Based Pharmacokinetic Modeling Approach to Identify the Drug-Drug Interaction Mechanism of Nifedipine and a Proton Pump Inhibitor, Omeprazole. Babiskin, A; Le Merdy, M; Lee, SC; Ni, Z; Sun, D; Tan, ML; Zhao, L, 2021) | 1.03 |
"In the present era of drug development, quantification of drug concentrations following pharmacokinetic studies has preferentially been performed using plasma as a matrix rather than whole blood." | ( Whole blood or plasma: what is the ideal matrix for pharmacokinetic-driven drug candidate selection? Dash, RP; Mehta, N; Rosenfeld, C; Srinivas, NR; Thomas, JA; Veeravalli, V, 2021) | 0.62 |
"A series of small pharmacokinetic studies illustrate higher oral clearance of labetalol and nifedipine during pregnancy." | ( The Impact of Pregnancy on Antihypertensive Drug Metabolism and Pharmacokinetics: Current Status and Future Directions. Daubert, MA; Fashe, MM; Garcia, JE; Lee, CR; Loop, MS; Mulrenin, IR; Urrutia, RP, 2021) | 0.84 |
" This study aimed to elucidate the impact of SMS on nifedipine/felodipine treatment by the findings from rat pharmacokinetic study of nifedipine to the retrospective cohort study of patients with hypertension." | ( Effect of repeated Shengmai-San administration on nifedipine pharmacokinetics and the risk/benefit under co-treatment. Chen, WC; Chia-Hui Tan, E; Chiang, TY; Shen, CC; Ueng, YF; Wang, HJ, 2022) | 1.23 |
"This study employed population pharmacokinetic (PopPK) modeling to delineate potential changes in CYP3A activity in patients with CKD." | ( Population Pharmacokinetic Modelling for Nifedipine to Evaluate the Effect of Parathyroid Hormone on CYP3A in Patients with Chronic Kidney Disease. Fu, C; Guo, C; Li, W; Liang, W; Liu, J; Pei, Q; Tan, H; Yang, B; Yang, G; Zhang, H, 2022) | 0.99 |
" Pharmacokinetic parameters were obtained using a noncompartmental model and log-transformed pharmacokinetic parameters (maximum plasma concentration, area under the plasma concentration-time curve (AUC) from time 0 to the last measurable concentration, AUC from time 0 to infinity) were used to evaluate bioequivalence." | ( Pharmacokinetics and Bioequivalence of 2 Nifedipine Controlled-Release Tablets: A Randomized, Single-Dose, 2-Period Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions. Chen, D; Chen, Q; Jia, J; Li, Y; Liu, Y; Wang, W; Wu, Q; Xin, L; Yu, C; Zou, Y, 2023) | 1.18 |
" We investigated potential effects of comedication on pharmacokinetic exposure of nifedipine ER products with different formulation designs and manufacturing processes." | ( Effect of Omeprazole Administration on the Pharmacokinetics of Oral Extended-Release Nifedipine in Healthy Subjects. Feng, K; Kinjo, M; Lionberger, R; Sun, D; Tan, ML; Wang, H; Xu, M; Zhao, L, 2023) | 1.36 |
" This work presents, for the first time, a universal LC-MS/MS method for analysis of haemanthamine in plasma, bile and urine which has been verified in a pilot pharmacokinetic experiment on rats." | ( LC-MS/MS method for the determination of haemanthamine in rat plasma, bile and urine and its application to a pilot pharmacokinetic study. Cahlíková, L; Cermanová, J; Havelek, R; Hošťálková, A; Hroch, M; Hulcová, D; Mičuda, S; Řezáčová, M, 2016) | 0.43 |
Nifedipine in combination with atenolol precipitated LV failure only in those with the lowest EF and highest LVEDP. The cytotoxic drug combination of methotrexate and melphalan, or nifingipine alone (0.5 mg/kg) did not cause LV failure.
Nifedipine (NI) is a poorly water-soluble drug and its oral bioavailability is very low. The data suggest gastroretention as a promising approach to enhance bioavailability of nifedipsine.
Excerpt | Reference | Relevance |
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"Nilvadipine is absorbed rapidly and completely and its absolute bioavailability is about 14-19% because of its high first-pass metabolism." | ( Pharmacokinetics of nilvadipine. Huber, HJ; Stanislaus, F; von Nieciecki, A, 1992) | 0.28 |
" No significant differences were observed among the three preparations in relation to the following pharmacokinetic parameters obtained from the plasma concentration-time curves: area under the curve (AUC), slope (beta) and half-life (T1/2) of the elimination phase, volume of distribution (Vd/F) and total body clearance (CL/F), both expressed as functions of the oral bioavailability (F) of nifedipine." | ( Comparative pharmacokinetics of different oral nifedipine preparations in healthy Brazilian volunteers. Melo, PA; Suarez-Kurtz, G; Sudo, RT; Vianna-Jorge, R, 1992) | 0.71 |
" After comparison with other methods, we used the program to evaluate the influence of nifedipine on the absorption and bioavailability of amoxicillin." | ( Adaptive computer program for determination of absorption profiles by numerical deconvolution: application to amoxicillin absorption. Deslandes, A; Farinotti, R; Trouvin, JH; Westphal, JF, 1992) | 0.51 |
"We studied the action of nifedipine on the bioavailability of cefixime, a molecule absorbed via the gut wall dipeptide carrier system in the rat, and on the bioavailability of D-xylose, which is absorbed via a pH (and Na(+)-)-dependent transporter." | ( Modification of cefixime bioavailability by nifedipine in humans: involvement of the dipeptide carrier system. Bouten, A; Carbon, C; Deslandes, A; Duverne, C; Farinotti, R; Trouvin, JH; Westphal, JF, 1992) | 0.85 |
" Following oral administration, bioavailability is 60 to 65% and plasma concentrations rise gradually to peak 6 to 8h after administration." | ( Clinical pharmacokinetics of amlodipine. Elliott, HL; Meredith, PA, 1992) | 0.28 |
" It has high oral bioavailability (60-80%) and accumulates to a steady-state with once-daily administration over a period of 1-1 1/2 weeks." | ( Pharmacokinetics and pharmacodynamics of amlodipine. Abernethy, DR, 1992) | 0.28 |
" bioavailability of the dihydropyridine calcium antagonists nifedipine and felodipine." | ( Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavonoids found in grapefruit juice. Edgar, B; Eriksson, UG; Lundahl, J; Miniscalco, A; Regårdh, CG, 1992) | 0.53 |
" The relative bioavailability of nifedipine, measured as AUC, was increased by 54% (533 vs 346 ng." | ( Effect of an acute dose of alcohol on the pharmacokinetics of oral nifedipine in humans. Caillé, G; Gossard, D; Lacasse, Y; Laganière, S; McGilveray, I; Qureshi, S, 1992) | 0.8 |
" The mean felodipine bioavailability with grapefruit juice was 284 (range 164-469)% of that with water." | ( Interaction of citrus juices with felodipine and nifedipine. Arnold, JM; Bailey, DG; Munoz, C; Spence, JD, 1991) | 0.54 |
" nifedipine were dependent on time of day: immediate-release nifedipine had higher Cmax (peak concentration) and shorter tmax (time-to-peak concentration) after morning than evening application, and bioavailability in the evening was reduced by about 40%." | ( Chronopharmacokinetics and cardiovascular effects of nifedipine. Behne, S; Kaiser, R; Lemmer, B; Nold, G, 1991) | 1.44 |
" A high oral bioavailability of amlodipine has been demonstrated in a number of animal species and man, together with a long elimination half-life." | ( Amlodipine: a once daily calcium antagonist. Burges, RA, 1991) | 0.28 |
" The relative bioavailability [correction of biodisponibility] of niphedipine was double in the patients with hepatic cirrhosis versus the healthy subjects." | ( [Nifedipine pharmacokinetics in liver cirrhosis patients after the administration of a single oral dose]. Dumitraşcu, D; Grigorescu, M; Leucuţa, SE, ) | 1.04 |
" Thus, it is concluded that the fixed combination of nifedipine and atenolol is bioequivalent to the free combination and that the bioavailability of both drugs in the fixed combination is equivalent to that of the single entities." | ( A study of the pharmacokinetics and pharmacodynamics of nifedipine in combination with atenolol. Adam, HK; Fitzsimons, TJ; McAinsh, J; Norris, SC; Ryan, J, ) | 0.63 |
"In a prematurely discontinued bioavailability study of 40 mg nifidepine retard dragees, it was shown in four subjects that cardiovascular side effects may occur at nifedipine levels equal to or higher than some 80 ng/ml serum." | ( [Side effects of nifedipine in healthy probands within the scope of a discontinued bioavailability study]. Banditt, P; Meyer, FP; Walther, H, 1991) | 0.82 |
" In order to assess the in vivo relevance of these data, we studied, in healthy volunteers, the influence of nifedipine, a calcium channel blocking agent, on the intestinal uptake of amoxicillin, a commonly prescribed and well-absorbed aminopenicillin." | ( Nifedipine enhances amoxicillin absorption kinetics and bioavailability in humans. Carbon, C; Deslandes, A; Trouvin, JH; Westphal, JF, 1990) | 1.93 |
" 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) | 0.28 |
" The results suggest that important differences in bioavailability exist amongst dihydropyridines which may have important therapeutic implications." | ( Cardiovascular actions of a new dihydropyridine calcium antagonist, 8363-S: comparison with nifedipine and nicardipine in awake, unsedated dogs. Hardman, HF; Preuss, KC; Shimshak, TM; Warltier, DC; Wynsen, JC, 1987) | 0.49 |
" Bioavailability of unchanged drug after oral administration was high with values of 63, 88, 100, and 100% in humans, dogs, mice, and rats, respectively." | ( The metabolism and pharmacokinetics of amlodipine in humans and animals. Beresford, AP; Humphrey, MJ; Macrae, PV; Stopher, DA, 1988) | 0.27 |
"The oral bioavailability of amlodipine in healthy volunteers was compared in two separate studies after solution and capsule doses, and after capsule doses in fed and fasting states." | ( Absorption of amlodipine unaffected by food. Solid dose equivalent to solution dose. Chasseaud, LF; Faulkner, JK; Hayden, ML; Taylor, T, 1989) | 0.28 |
"Amlodipine, a dihydropyridine calcium antagonist, was synthesized in an attempt to develop a compound with a pharmacokinetic profile characteristic of this class, which would also have an increased oral bioavailability and extended clearance time." | ( The pharmacokinetic profile of amlodipine. Abernethy, DR, 1989) | 0.28 |
" Amlodipine, a new member of this family of dihydropyridines, has a unique pharmacokinetic profile with high bioavailability and an extended period of pharmacodynamic activity." | ( The efficacy of amlodipine in myocardial ischemia. Taylor, SH, 1989) | 0.28 |
"The paper reports on the bioavailability of niphedipine in various pharmaceutic preparations administered in a single dose of 10 mg, per os, to volunteer subjects: Niphedipine dragees (Terapia, Cluj-Napoca), Adalat capsules (Bayer); Adalat coated tablets (Bayer and Birlaşik Alman Ilac Fabricalari, Istanbul) and Corinfar dragées (VEB Arzneimittelwerk, Dresden)." | ( [The bioavailability of nifedipine in different solid pharmaceutical preparations for oral use]. Baloescu, C; Bugnariu, S; Făgărăşan, E; Leucuta, SE; Mocan, A; Olinic, N; Vida-Simiti, L; Vlaicu, R, ) | 0.44 |
" Bioavailability of nifedipine from this preparation was satisfactory, as shown by plasma concentrations which remained constantly in the therapeutic range." | ( Evaluation of the efficacy of slow-release nifedipine in systemic hypertension by ambulatory intraarterial blood pressure monitoring. Bonaduce, D; Canonico, V; Chiariello, M; Condorelli, M; Ferrara, N; Mazza, F; Nicolino, A, ) | 0.72 |
"Absolute bioavailability (F) of 10 mg nifedipine capsules was studied in six adult healthy male volunteers." | ( Bioavailability and pharmacokinetics of nifedipine administered by different routes in healthy volunteers. León-Urrea, F; Montoya-Cabrera, MA; Palma-Aguirre, JA; Rodríguez, JM; Rosas-Alcázar, G, ) | 0.67 |
" The bioavailability of the controlled-release pellets is a little higher than that of the conventional pellets." | ( [Studies on the controlled-release pellets of nifedipine]. Chen, G; Liu, GJ; Yang, TH; Zhang, JS, 1989) | 0.54 |
" 95% confidence intervals for indices of bioavailability based on AUC and Cmax overlapped, indicating that the two preparations are bioequivalent." | ( [The bioequivalence of two nifedipine fluid capsules]. Bacracheva, N; Thürmann, P, 1989) | 0.57 |
" Both calcium antagonists tended to increase absorption rate and elimination rate, but none of the pharmacokinetic parameters of cyclosporine were significantly altered." | ( Short-term effects of calcium antagonists on hemodynamics and cyclosporine pharmacokinetics in heart-transplant and kidney-transplant patients. Browning, FM; Cardella, C; East, DS; Leenen, FH; Ogilvie, RI; Roy, LF; Shaw, D, 1989) | 0.28 |
"In the course of this trial the bioavailability and the essential pharmacokinetic parameters of a newly developed 10 mg nifedipine preparation were to be determined in comparison to a marketed reference preparation after single oral administration." | ( [Bioavailability and pharmacokinetics of a new nifedipine preparation in healthy volunteers]. Dilger, C; Hutt, V; Jaeger, H; Molz, KH; Mosberg, H; Pabst, G, 1989) | 0.74 |
"The absolute and relative bioavailability of nifedipine (1) from different formulations administered as single oral doses in healthy volunteers was determined." | ( Bioavailability of nifedipine from different oral dosage forms in healthy volunteers. Căprioară, MG; Făgărăşan, E; Leucuţa, SE; Manasia, M; Olinic, N; Vida-Simiti, L; Vlaicu, R, 1989) | 0.87 |
" From tablets, the peak concentration was 79-88% lower and occurred 74-133 min after ingestion; also the bioavailability was lower, as indicated by on average 39% lower area under curve values after tablets." | ( Pharmacokinetics and acute side-effects of nifedipine given as slow-release tablets or liquid-filled capsules. Komulainen, H; Paronen, P; Raatikainen, O; Saano, V, 1989) | 0.54 |
"The effect of food on the bioavailability of a nifedipine sustained-release preparation was studied." | ( Effect of food on nifedipine sustained-release preparation. Ikada, T; Kawashima, S; Matsumoto, K; Miyai, K; Nakata, I; Uemoto, K; Ueno, K; Wada, K; Yamazaki, K, 1989) | 0.87 |
" Nifedipine significantly enhanced propranolol bioavailability and Cmax, but reduced its tmax, in three out of six subjects who were also good absorbers of beta-blockers when taken alone." | ( Pharmacokinetic and pharmacodynamic interactions between nifedipine and propranolol or betaxolol. Canal, M; Carbon, C; Cascio, B; Domart, Y; Flouvat, B; Larribaud, J; Orofiamma, B; Roux, A; Vinceneux, P, 1986) | 1.43 |
" The absolute bioavailability of nilvadipine decreased from 67 to 27% after increasing oral doses (6 and 24 mg), probably because of reduced drug absorption from the gastrointestinal tract." | ( Relationship between the pharmacokinetic and pharmacodynamic profile of nilvadipine in the dog. Garnes, D; Henderson, BM; Lanc, R; Silber, BM; Wu, WH; Yacobi, A, ) | 0.13 |
" Oral bioavailability approached 100%, and hemodynamic responses were gradual in onset and long-lasting in effect." | ( Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents. Arrowsmith, JE; Blackburn, KJ; Burges, RA; Campbell, SF; Cross, PE; Gardiner, DG; Stubbs, JK, 1986) | 0.27 |
" The drug was well absorbed by the oral route while the mean oral bioavailability for unchanged drug was 62." | ( Metabolism and kinetics of amlodipine in man. Beresford, AP; Humphrey, MJ; Macrae, PV; McGibney, D; Stopher, DA, 1988) | 0.27 |
"In the present study we investigated the pharmacokinetics and comparative bioavailability of three oral doses of amlodipine in 12 healthy male volunteers." | ( Amlodipine pharmacokinetics in healthy volunteers. Cubeddu, LX; Williams, DM, 1988) | 0.27 |
" After oral administration, non-linearity of bioavailability with increment of doses was observed in both rat and dog." | ( Pharmacokinetic study of benidipine hydrochloride in rats and dogs. Inoue, A; Kobayashi, H; Kobayashi, S; Nakamizo, N; Oka, T, 1988) | 0.27 |
"The bioavailability of nifedipine in man is highly variable." | ( Complexation of nifedipine with substituted phenolic ligands. Boje, KM; Fung, HL; Sak, M, 1988) | 0.93 |
" Although the bioavailability of the two preparations is similar, the therapeutic effects may differ." | ( The kinetics of nifedipine release from porous hydrophilic matrices and the pharmacokinetics in man. Leucuta, SE, 1988) | 0.62 |
" 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) | 0.48 |
" Bioavailability was low in male rats (3-4%) and rabbits (2%), but in other species was 29-44%." | ( Pharmacokinetics of nilvadipine, a new dihydropyridine calcium antagonist, in mice, rats, rabbits and dogs. Niwa, T; Noguchi, H; Sekiguchi, M; Tokuma, Y, 1988) | 0.27 |
" The trend towards an increased bioavailability in elderly subjects (36%) was supported by a significantly lower nitropyridine metabolite/nifedipine ratio in the elderly." | ( Age-related changes in the pharmacokinetics and pharmacodynamics of nifedipine. George, CF; Renwick, AG; Robertson, DR; Waller, DG, 1988) | 0.71 |
" Since the bioavailability of P is 97% the two preparations are bioequivalent." | ( [A model study of bioequivalence of dissolved nifedipine from soft gelatin capsules]. Kausch, M; Menke, G; Rietbrock, N, 1988) | 0.53 |
" The most likely explanation for increased bioavailability of nifedipine when coadministered with propranolol is by a reduction of the hepatic "first-pass" clearance, as a result of changes in hepatic blood flow." | ( Pharmacokinetic interaction between nifedipine and propranolol. Koren, G; Levy, M; Turetz-Abramovitch, M; Zylber-Katz, E, 1988) | 0.79 |
" The rate of absorption and peak plasma concentrations were similar in the two groups." | ( Pharmacokinetics of nifedipine after oral administration in chronic liver disease. Ene, MD; Roberts, CJ, 1987) | 0.6 |
"The pharmacokinetics and bioavailability of intravenous, intraduodenal, buccal, rectal and percutaneous nifedipine were studied in rats to evaluate the influence of route of administration." | ( Moment analysis of intravenous, intraduodenal, buccal, rectal and percutaneous nifedipine in rats. Kondo, S; Sugimoto, I, 1987) | 0.71 |
" The bioavailability of percutaneous nifedipine in rats was determined from the drug solutions containing different proportions of EtOH and DES." | ( Enhancement of transdermal delivery by superfluous thermodynamic potential. II. In vitro-in vivo correlation of percutaneous nifedipine transport. Kondo, S; Sugimoto, I; Yamasaki-Konishi, H, 1987) | 0.75 |
"The bioavailability of percutaneous nifedipine was studied in rats." | ( Enhancement of transdermal delivery by superfluous thermodynamic potential. III. Percutaneous absorption of nifedipine in rats. Kondo, S; Sugimoto, I; Yamanaka, C, 1987) | 0.76 |
" Although nifedipine is almost completely absorbed from the gastrointestinal tract, oral bioavailability ranges from 45 to 68 percent because of first-pass metabolism." | ( Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. A controlled-release formulation of nifedipine. Chung, M; Gaffney, M; Reitberg, DP; Singleton, W, 1987) | 0.97 |
" 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, ) | 0.4 |
" Pharmacokinetic parameters which describe bioavailability and general kinetic behaviour of the drug (AUC, Cmax, tmax, beta, MRT) were calculated from individual plasma profiles." | ( The bioavailability of oral nifedipine formulations: a statistical and simulation approach. Janezic, A; Karba, R; Kozjek, F; Mrhar, A; Primozic, S; Raemsch, KD, ) | 0.43 |
"The effect of food on the bioavailability of nifedipine (Procardia), 10 mg capsules, was studied." | ( Effect of food on nifedipine pharmacokinetics. Love, SJ; Quercia, GT; Reitberg, DP; Zinny, MA, 1987) | 0.87 |
" Moreover, in 8 additional subjects free of cardiovascular and other diseases, the formulation was compared to a commercial sustained release product in order to evaluate its bioavailability after a single 20 mg dose." | ( Clinical efficacy and bioavailability of a sustained release nifedipine formulation. Piovella, C, 1987) | 0.51 |
"The effect of two different meals on the bioavailability of nilvadipine, a new antihypertensive and antianginal drug, was examined in 16 healthy male volunteers in two separate studies." | ( Effect of two different meals on bioavailability of nilvadipine in healthy volunteers. Noguchi, H; Shishido, A; Terakawa, M; Tokuma, Y; Yasuda, K, 1987) | 0.27 |
" In the six volunteers, the mean bioavailability was 46% (range 29-86%), the mean CL was 588." | ( The bioavailability and pharmacokinetics of slow release nifedipine during chronic dosing in volunteers. Abrams, SM; Debbas, NM; Jackson, SH; Johnston, A; Shah, K; Turner, P, 1986) | 0.52 |
" The absorption rate of nifedipine from the capsule tended to be larger than that from the retard tablet." | ( Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients. Abe, K; Imai, Y; Nihei, M; Sasaki, S; Sekino, H; Yoshinaga, K, 1986) | 0.8 |
" A pharmacokinetic study performed in 15 elderly patients showed a fast rate of absorption and also higher plasma levels than those observed in hypertensive adults (mean age, 54 years)." | ( Effect of nicardipine in elderly hypertensive patients. Bellet, M; Bouchacourt, P; Forette, F; Guerret, M; Henry, JF; Hervy, MP; Poyard-Salmeron, C, 1985) | 0.27 |
" 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 |
" This corresponds to a bioavailability of 73%." | ( Intranasal delivery of nicardipine in the rat. Bajka, E; Benjamin, E; Visor, GC, 1986) | 0.27 |
"In a randomized three-way crossover study with twelve volunteers the bioavailability and main pharmacokinetic parameters of three different galenic formulations of nifedipine (hard gelatine capsule with pellets = preparation A, soft gelatine capsule with liquid nifedipine = preparation B, retard-tablet = preparation C) were determined." | ( Pharmacokinetics and bioavailability of three different galenic nifedipine preparations. Dahmen, W; Jaeger, H; Lutz, D; Molz, KH; Pabst, G, 1986) | 0.71 |
" Steady-state plasma levels and bioavailability show a nonlinear relationship with doses over the range 10-40 mg three times daily." | ( The metabolism and pharmacokinetics of nicardipine hydrochloride in man. Alexander, OF; Dow, RJ; Freedman, D; Graham, DJ; Hall, DJ; Mroszczak, EJ, 1985) | 0.27 |
"Relative bioavailability of 5-, 10-, and 20-mg nitrendipine tablets was determined in a four-way crossover bioequivalence study involving 22 normal male volunteers." | ( Bioequivalence and metabolism of nitrendipine administered orally to healthy volunteers. Burkholder, DE; Kann, J; Krol, GJ; Levitt, MJ; Raemsch, KD, 1984) | 0.27 |
" 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) | 0.54 |
" 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, ) | 0.51 |
" Simultaneously, nicardipine plasma levels and relative bioavailability were determined." | ( Nicardipine: pharmacokinetics and effects on carotid and brachial blood flows in normal volunteers. Duhaze, P; Giudicelli, JF; Gueret, M; Kiechel, JR; Lhoste, F; Thuillez, C, 1984) | 0.27 |
" These results suggest that the rate of absorption of this drug varies widely among individuals." | ( Specific HPLC assay for serum nifedipine. Fernandez, PG; Galway, BA; Kim, BK; Snedden, W, 1984) | 0.56 |
" The oral bioavailability of nicardipine determined by reference to a co-administered intravenous radiolabelled dose was found to be non-linearly related to dose." | ( Pharmacokinetics of nicardipine following oral and intravenous administration in man. Dow, RJ; Freedman, D; Graham, DJ; Ling, T; Mroszczak, E, 1984) | 0.27 |
" Absorption curves were classified into 3 types: a rapid absorption rate (2 subjects) in which the maximum measured nifedipine concentration (70-80 ng/ml) was obtained, within 20-40 min after administration, a slower absorption rate (3 subjects) and an intermediate absorption rate (3 subjects) and an intermediate absorption rate (3 subjects)." | ( Nifedipine serum concentration; effects upon blood pressure and heart rate in normotensive volunteers. Inoki, M; Nakanishi, Y; Nakashima, T, ) | 1.78 |
" Nifedipine bioavailability was 56% +/- 25% for the capsule and 52% +/- 13% for the tablet, but there were large interindividual differences." | ( Nifedipine: kinetics and dynamics in healthy subjects. Breimer, DD; Kleinbloesem, CH; van Brummelen, P; van de Linde, JA; Voogd, PJ, 1984) | 2.62 |
" We conclude that although the bioavailability in general of the two preparations is similar, the therapeutic equivalence may differ." | ( Bioavailability of nifedipine: a comparison between two preparations. Granit, L; Koren, G; Levy, M; Zylber-Katz, E, ) | 0.46 |
" 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 |
" Absorption, bioavailability and elimination were linear between the 20 and 60 mg doses." | ( Acute antihypertensive effect and pharmacokinetics of a tablet preparation of nifedipine. Alexandre, JM; Banzet, O; Colin, JN; Corvol, P; Singlas, E; Thibonnier, M, 1983) | 0.49 |
" Because of presystemic metabolism, the bioavailability is about 56% to 77%." | ( Pharmacokinetics and metabolism of nifedipine. Raemsch, KD; Sommer, J, ) | 0.41 |
" Therefore, we evaluated the kinetics and bioavailability of nifedipine in 12 normal subjects after single intravenous (1 mg/5 min) and oral (10 mg) doses." | ( Nifedipine kinetics and bioavailability after single intravenous and oral doses in normal subjects. Bryant, PJ; Foster, TS; Graves, DA; Hamann, SR; McAllister, RG; Richards, VR, 1983) | 1.95 |
" Administration of the test drugs in combination slightly increased the bioavailability of both--nifedipine [N] to 18% and quinidine [Q] to 16%--and decreased the clearance of both drugs." | ( Pharmacokinetic interactions of nifedipine and quinidine. Brendel, E; Henschel, L; Hippius, M; Hoffmann, A; Sigusch, H; Tepper, J, 1995) | 0.79 |
" Impaired renal function did not affect the maximum plasma concentrations or bioavailability of nifedipine after single or multiple dose administration of nifedipine GITS, nor was there any evidence of excessive drug accumulation in the presence of renal impairment." | ( Pharmacokinetic profile of nifedipine GITS in hypertensive patients with chronic renal impairment. Brendel, E; Griffel, L; Iaina, A; Kobelt, R; Schneider, R; Stolero, D, 1994) | 0.8 |
" Nifedipine also significantly increased the AUC and Cmax of oral propranolol (15 mg/kg), whereas with BAY-K-8644 there was only a slight increase in the bioavailability of oral propranolol (15 mg/kg)." | ( Influences of the calcium antagonists nicardipine and nifedipine, and the calcium agonist BAY-K-8644, on the pharmacokinetics of propranolol in rats. Dupont, AG; Massart, DL; Schoors, DF; Vercruysse, I, 1993) | 1.44 |
" It is especially suited for bioavailability studies because of its stability and high sampling rate." | ( Determination of nifedipine in human serum by gas chromatography-mass spectrometry: validation of the method and its use in bioavailability studies. Banditt, P; Martens, J; Meyer, FP, 1994) | 0.63 |
" The addition of 40 mg foridon, a calcium antagonist from dihydropyridine series increased the absorption rate of glucose, Na+ and water by 28." | ( [Stimulating effects of a calcium antagonist foridon on absorption detected by segmental perfusion of the small intestine]. Fazylov, AV; Parfenov, AI; Poleva, NI, 1994) | 0.29 |
" Owing to a marked first-pass effect, the absolute bioavailability is 14-19%." | ( Nilvadipine: profile of a new calcium antagonist. An overview. Rosenthal, J, 1994) | 0.29 |
"To modify the release rate of nifedipine, a potent calcium channel antagonist, a double-layer tablet was designed, anticipating a more balanced oral bioavailability and a prolonged efficacy than the simple plain tablet." | ( Design and in-vitro evaluation of a modified-release oral dosage form of nifedipine by hybridization of hydroxypropyl-beta-cyclodextrin and hydroxypropylcellulose. Hirayama, F; Horikawa, T; Uekama, K; Wang, Z, 1993) | 0.81 |
"5) was selected as an appropriate modified-release formulation because it elicited almost comparable retarding effects with superior oral bioavailability compared with those of a commercially available slow-release nifedipine product." | ( In-vivo and in-vitro evaluations of a modified-release oral dosage form of nifedipine by hybridization of hydroxypropyl-beta-cyclodextrin and hydroxypropylcelluloses in dogs. Hirayama, F; Uekama, K; Wang, Z, 1994) | 0.7 |
" In study 1, 22 healthy male volunteers took part in an open, multiple-dose, randomized, crossover study to determine the relative bioavailability of two 10 mg controlled-release nifedipine tablets (Adalat Retard, Bayer), administered 12 hourly, and one 20 mg controlled-release nifedipine tablet (Adalat Retard, Bayer) administered 12 hourly." | ( Relative bioavailability of four controlled-release nifedipine products. Duursema, L; Groenewoud, G; Hundt, HK; Müller, FO; Schall, R; Van Dyk, M; Van Schalkwyk, AM, 1994) | 0.73 |
" Nilvadipine has an asymmetric center at the C-4 position of the dihydropyridine ring, and characterization of the optical isomers with regard to their activity and bioavailability is of interest." | ( Studies on nilvadipine. IV. Synthesis of deuteriated and optically active isopropyl 2-cyano-3-methoxycarbonyl-4-(3-nitrophenyl)-6-methyl-1,4- dihydropyridine-5-carboxylate (nilvadipine). Okumura, K; Satoh, Y; Shiokawa, Y, 1994) | 0.29 |
"The objective of this study was to investigate in a twoway randomized crossover whether repeated uptake of grapefruit juice (200 ml at 0, 2, 4, 8 and 12 h enhances bioavailability of a nifedipine (1) slow release formulation (20 mg) in ten healthy volunteers." | ( Influence of grapefruit juice on the pharmacokinetics of a slow release nifedipine formulation. Henschel, L; Hippius, M; Hoffmann, A; Kaufmann, K; Sigusch, H, 1994) | 0.71 |
" Both a decreased hepatic clearance and an increased bioavailability of diltiazem probably accounts for the increase in the Cmax and AUC of diltiazem after nifedipine pretreatment, and that might affect the pharmacodynamics of diltiazem." | ( The effect of nifedipine on the pharmacokinetics and dynamics of diltiazem: the preliminary study in normal volunteers. Ebihara, A; Fujimura, A; Ohashi, K; Sakamoto, K; Sudo, T; Tateishi, T, 1993) | 0.84 |
" Increased nifedipine bioavailability in the nonwhite populations is likely due to nutritional habits." | ( Pharmacokinetics of oral nifedipine in different populations. Castañeda-Hernández, G; Flores-Murrieta, FJ; Hoyo-Vadillo, C; Palma-Aguirre, JA, 1993) | 0.98 |
"05) and bioavailability (0." | ( Factors affecting the absolute bioavailability of nifedipine. Clarke, H; George, CF; Martin, U; Rashid, TJ; Renwick, AG; Waller, DG, 1995) | 0.54 |
" The absolute bioavailability was low (11-18% in the rat and 6-9% in the dog), suggesting a marked first-pass metabolism." | ( Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human. Hashimoto, K; Higuchi, S; Teramura, T; Watanabe, T, 1995) | 0.29 |
" The pharmacokinetic parameters and the relative bioavailability were determined in 15 and 16 healthy male volunteers, respectively after single and repeated administration in open, randomized cross over study." | ( [Comparative human pharmacokinetic studies of 20 mg nifedipine-containing Cordaflex and Adalat film coated retared tablets]. Balogh, J; Baloghné, NK; Cseh, A; Farsang, C; Grézal, G; Horvai, G; Horváth, V; Klebovich, I; Kocsi, E, 1996) | 0.54 |
" To assess the effect of orlistat on the bioavailability of nifedipine GITS, a third party-blind, placebo-controlled, randomized, two-way crossover study was performed in 18 healthy volunteers." | ( Lack of effect of orlistat on the bioavailability of a single dose of nifedipine extended-release tablets (Procardia XL) in healthy volunteers. Melia, AT; Mulligan, TE; Zhi, J, 1996) | 0.77 |
"In humans, oral bioavailability of nifedipine has been reported to be around 60%, although the organ(s) contributing to its first-pass metabolism have not been determined." | ( Lack of presystemic metabolism of nifedipine in the rabbit. Caillé, G; Dépôt, M; du Souich, P; Héroux, L; Maurice, H, 1995) | 0.85 |
" Absorption was less rapid from the colon than from the upper part of the gut, but this was not associated with a decrease in absorption and/or bioavailability: Absolute bioavailability, calculated from the normalised AUC values, ranged from 42 to 56%, and bioavailability relative to oral solution was 100 to 126% (medians of the application sites)." | ( Investigation of nifedipine absorption in different regions of the human gastrointestinal (GI) tract after simultaneous administration of 13C- and 12C-nifedipine. Ahr, G; Bode, H; Brendel, E; Fuhr, U; Harder, S; Staib, AH, 1996) | 0.63 |
"The bioavailability of a nifedipine extended release capsule-formulation (CAS 21829-25-4, Aprical retard) was investigated in comparison to a standard retard tablet." | ( [Bioequivalence of nifedipine sustained-release formulations in comparison to standard preparations in solid state]. Herrmann, R, 1996) | 0.93 |
" Drug delivery by the nifedipine GITS is unaffected by changes in pH and gastrointestinal (GI) motility, but the rate of drug release can increase slightly with food intake (although absolute bioavailability remains unchanged)." | ( The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Foster, RT; Grundy, JS, 1996) | 1.17 |
"The plasma concentration time profiles and the pharmacokinetic parameters estimated for these drugs were in the expected range, except for furosemide, whose bioavailability was lower than reported in the literature." | ( Effect of the lipase inhibitor orlistat on the pharmacokinetics of four different antihypertensive drugs in healthy volunteers. Jonkmann, JH; Schmidtke-Schrezenmeier, G; Tam, YK; van Brummelen, P; Weber, C, 1996) | 0.29 |
"01) and bioavailability decreased from 41." | ( The nifedipine-rifampin interaction. Evidence for induction of gut wall metabolism. Fromm, MF; Heidemann, H; Holtbecker, N; Kroemer, HK; Ohnhaus, EE, 1996) | 0.85 |
" Relative bioavailability was significantly increased with Eudragit nanoparticles compared to the nifedipine/PEG solution." | ( The antihypertensive effect of orally administered nifedipine-loaded nanoparticles in spontaneously hypertensive rats. Atkinson, J; Fluckiger, L; Hoffman, M; Kim, YI; Lartaud-Idjouadiene, I; Maincent, P, 1997) | 0.77 |
" These data suggest that the absorption of the SR formulation is slightly reduced but that its bioavailability is comparable to that of the normal formulation." | ( Metabolism and pharmacokinetics of barnidipine hydrochloride, a calcium channel blocker, in man following oral administration of its sustained release formulation. Hashimoto, K; Higuchi, S; Teramura, T; Watanabe, T, 1997) | 0.3 |
" The mean relative bioavailability of nifedipine following pre-treatment with rifampicin 1200 mg was 35." | ( The effect of single does of rifampicin on the pharmacokinetics of oral nifedipine. Abdu-Aguye, I; Mustapha, A; Ndanusa, BU, 1997) | 0.8 |
") bioavailability of nifedipine is reported to range from about 45 to 58% in the rat; this compares favourably to human beings." | ( Extrahepatic first-pass metabolism of nifedipine in the rat. Eliot, LA; Foster, RT; Grundy, JS, 1997) | 0.89 |
" Co-administration of candesartan cilexetil with HCTZ produced a statistically significant increase in the bioavailability and Cmax values for candesartan (18% and 25%, respectively)." | ( Pharmacokinetic drug interaction studies with candesartan cilexetil. Högemann, A; Jonkman, JH; Lins, R; Sennewald, R; van Heiningen, PN; van Lier, JJ, 1997) | 0.3 |
" Thus, the two products could be considered bioequivalent regarding absorption rate (Cmax and Tmax), extent of absorption (Cmax and AUC) and elimination (t1/2)." | ( Comparative pharmacokinetics of two nifedipine products in capsule form following single oral administration in healthy volunteers. al-Qato, MK; Battah, AH; Irshaid, YM; Rawashdeh, NM, ) | 0.41 |
" Neither meal influenced the bioavailability of nifedipine." | ( The influence of two types of meal on the pharmacokinetics of a modified-release formulation of nifedipine (Adalat Retard). Armstrong, J; Challenor, VF; Macklin, BS; Renwick, AG; Waller, DG, 1997) | 0.77 |
" After pre-administration of erythromycin the relative bioavailability of nifedipine after oral administration was increased compared with injection into the peritoneal cavity." | ( Inhibition of nifedipine metabolism in dogs by erythromycin: difference between the gut wall and the liver. Arimori, K; Nakamura, K; Nakano, M; Tsuruta, S, 1997) | 0.89 |
"Previous studies with rats indicate that nifedipine undergoes both hepatic and extrahepatic presystemic metabolism after peroral (po) administration, and that its bioavailability is increased and absorption delayed by concomitant administration of grapefruit juice concentrate (GJC)." | ( Grapefruit juice and orange juice effects on the bioavailability of nifedipine in the rat. Eliot, LA; Foster, RT; Grundy, JS; Kulmatycki, KM, 1998) | 0.8 |
" 1994], food ingestion increased the relative bioavailability and maximum plasma concentration (Cmax)." | ( Food interaction pharmacokinetic study of cordaflex 20 mg retard filmtablet in healthy volunteers. Balogh Nemes, K; Csörgö, M; Drabant, S; Grézal, G; Horvai, G; Horváth, V; Hrabéczy-Páll, A; Klebovich, I; Kocsi, E; Renczes, G, 1998) | 0.3 |
" They are very liposoluble molecules which are well absorbed after oral prescription (90-100%); they show an important effect in their first step, they join the serum proteins in a high proportion, present a wide tissue distribution, they are quickly biotransformed in the liver and only a minimum proportion is discharged by urine without any modification." | ( [Clinical pharmacokinetics of calcium antagonists]. Sesin, J; Tamargo, J, 1997) | 0.3 |
" With the use of the highly accurate and specific technique of IDMS it can now be unequivocally established that the different progestins in the tested oral contraceptives have no influence on the bioavailability of EE2 (area under EE2 serum concentration curves, as usually defined in pharmacokinetics)." | ( Gestodene and desogestrel do not have a different influence on concentration profiles of ethinylestradiol in women taking oral contraceptives--results of isotope dilution mass spectrometry measurements. Albring, M; Bidlingmaier, F; Brill, K; Siekmann, A; Siekmann, L, 1998) | 0.3 |
"The aim of the present study was to compare the bioavailability of nifedipine when administered as a hydrophilic matrix tablet (ER) and a push-pull osmotic pump tablet (XL) administrated after fasting, and to evaluate the effect of food for the hydrophilic matrix tablet." | ( Drug absorption from nifedipine hydrophilic matrix extended-release (ER) tablet-comparison with an osmotic pump tablet and effect of food. Abrahamsson, B; Alpsten, M; Bake, B; Eriksson-Lepkowska, M; Jonsson, UE; Larsson, A, 1998) | 0.86 |
" Well known example, that bioavailability of theophylline can be influenced in different way (either increased, decreased or unchanged) by concomitant intake of food in the case of different sustained release products." | ( [Role of food interaction pharmacokinetic studies in drug development. Food interaction studies of theophylline and nifedipine retard and buspirone tablets]. Drabant, S; Farsang, C; Gachályi, B; Klebovich, I; Renczes, G, 1998) | 0.51 |
" The in vivo results in eight healthy volunteers showed that the relative bioavailability of the nifedipine sustained-release microspheres against commercial retard tablet as a control was 102." | ( [Studies on oral sustained-release microspheres of nifedipine]. Fu, CD; Hu, JH; Jiang, XT; Wu, W, 1996) | 0.76 |
" Absolute bioavailability and Vdss remained unchanged." | ( Effects of hyperlipidemia on the pharmacokinetics of nifedipine in the rat. Eliot, LA; Foster, RT; Jamali, F, 1999) | 0.55 |
" A male Caucasian who participated in six bioavailability studies in our laboratory over a period of several years showed extremely low clearance of two drugs: phenytoin and glipizide (both substrates of CYP2C9), but not for nifedipine (a CYP3A4 substrate) and chlorpheniramine (a CYP2D6 substrate)." | ( Pharmacokinetics of chlorpheniramine, phenytoin, glipizide and nifedipine in an individual homozygous for the CYP2C9*3 allele. Blaisdell, J; Dalton, JT; Goldstein, JA; Kidd, RS; Meyer, MC; Straughn, AB, 1999) | 0.73 |
" Also, it appeared that mebudipine had a slower rate of absorption compared with nifedipine (the time to reach peak hypotensive action at 2, 4 and 8 mg kg(-1) orally administered doses were, respectively, 24." | ( Effects of mebudipine and dibudipine, two new calcium-channel blockers, on rat left atrium, rat blood pressure and human internal mammary artery. Ghiaee, S; Mahmoudian, M; Mirkhani, H; Omrani, GR, 1999) | 0.53 |
"The extrapolated area under the concentration-time curve (AUC0-infinity) for any drug is considered by operating guidelines as the primary parameter related to the extent of absorption in single-dose bioavailability and bioequivalence trials." | ( Experimental, extrapolated and truncated areas under the concentration-time curve in bioequivalence trials. Marzo, A; Monti, NC; Vuksic, D, 1999) | 0.3 |
" This occurs with most extended-release formulations, endogenous substances, and poorly absorbed drugs." | ( Experimental, extrapolated and truncated areas under the concentration-time curve in bioequivalence trials. Marzo, A; Monti, NC; Vuksic, D, 1999) | 0.3 |
" In conclusion, short-term id exposure to GJ resulted in increased NFP bioavailability, whereas long-term administration of GJ resulted in reduced bioavailability and increased CL." | ( Effects of long-term grapefruit juice ingestion on nifedipine pharmacokinetics: induction of rat hepatic P-450 by grapefruit juice. Mohri, K; Sagawa, Ki; Uesawa, Y, 2000) | 0.56 |
" Absolute bioavailability and comparative bioavailability of the tested tablet were studied." | ( Preparation and evaluation of a sustained-release formulation of nifedipine HPMC tablets. Ding, D; Li, H; Yan, G; Zhang, R, 2000) | 0.54 |
"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 |
"The aim of the present study was to investigate the effect of hydroxypropylmethylcellulose (HPMC-2208), used as an excipient for controlled release of drug, on the release profiles and bioavailability of the poorly water-soluble nifedipine (NP) from a tablet prepared using macrogol 6000 (PEG) and HPMC." | ( Effect of hydroxypropylmethylcellulose (HPMC) on the release profiles and bioavailability of a poorly water-soluble drug from tablets prepared using macrogol and HPMC. Endo, H; Ishikawa, T; Matsumoto, M; Takayama, K; Watanabe, Y, 2000) | 0.49 |
" treatment, it can be envisaged to apply this effect to increase bioavailability of poorly absorbed peptidomimetic drugs in man." | ( Chronic nifedipine dosing enhances cephalexin bioavailability and intestinal absorption in conscious rats. Berlioz, F; Carbon, C; Farinotti, R; Julien, S; Lepére-Prevot, B; Rozé, C; Tsocas, A, 2000) | 0.74 |
"Experimental controlled release nifedipine microcapsules composed of ethylcellulose and eudragit RL were explored for the assessment of bioavailability on rabbit." | ( Assessment of bioavailability of experimental controlled release microcapsules of nifedipine. Ghosal, SK; Gupta, BK; Mallick, S, ) | 0.64 |
"05), mimicking the effect of an apparent decrease in bioavailability of endogenous NO." | ( Chronic nicotine alters NO signaling of Ca(2+) channels in cerebral arterioles. Gerzanich, V; Simard, JM; West, GA; Zhang, F, 2001) | 0.31 |
" In contrast with several other calcium antagonists, barnidipine does not affect the steady-state kinetics of digoxin, whereas, like other calcium antagonists its bioavailability may be increased by the concomitant administration of cimetidine." | ( Interaction profile and tolerability of barnidipine. Beudeker, HJ; van der Aar, EM; van der Velden, JW, 2000) | 0.31 |
" We conclude that the calcium antagonist nifedipine enhances the bioavailability of endothelial NO without significantly altering the NOS (type III) mRNA and protein expression, possibly via an antioxidative protection." | ( Nifedipine increases endothelial nitric oxide bioavailability by antioxidative mechanisms. Bartels, H; Berkels, R; Egink, G; Klaus, W; Marsen, TA; Roesen, R, 2001) | 2.02 |
" The method was validated for accuracy, sensitivity, selectivity and reproducibility and finally was utilized and proved to be suitable in a bioavailability study of two products of nifedipine following oral administration to healthy male subjects." | ( Trace-level determination of nifedipine in human serum by reversed phase high performance liquid chromatography. Hasan, E; Najib, N; Zaater, M, ) | 0.61 |
" A flow-through apparatus containing a piece of small intestine (ileum) of a rat was used for the absorption rate measurements." | ( Influence of surfactants additions on the absorption process of nifedipine in vitro. Gadomska-Nowak, M; Wojdak, H, ) | 0.37 |
"Because rifampicin may greatly decrease the oral bioavailability of nilvadipine, caution is needed when these two drugs are to be coadministered." | ( The effects of rifampicin on the pharmacokinetics and pharmacodynamics of orally administered nilvadipine to healthy subjects. Echizen, H; Fukuda, J; Furuie, K; Hayashi, T; Saima, S; Yoshimoto, H, 2002) | 0.31 |
" Therefore, inhibition of hepatic extraction of NIF by the KTZ treatment mainly results in substantial increase in systemic bioavailability in dogs." | ( Effect of oral ketoconazole on first-pass effect of nifedipine after oral administration in dogs. Kayaba, H; Khalil, WF; Kishimoto, S; Kokue, E; Kuroha, M; Shimoda, M, 2002) | 0.57 |
"The objective of this study was a comparative investigation of the influence of concomitant food intake on the bioavailability of two nifedipine-containing controlled-release formulations." | ( Formulation-dependent food effects demonstrated for nifedipine modified-release preparations marketed in the European Union. Blume, HH; Brendel, E; Schug, BS; Wargenau, M; Wolf, D; Wonnemann, M, 2002) | 0.77 |
"Grapefruit juice is known to increase the oral bioavailability of dihydropyridine calcium channel blockers, including nifedipine, by reducing presystemic clearance." | ( Clinical effects of grapefruit juice-nifedipine interaction in a 54-year-old Nigerian: a case report. Adigun, AQ; Mudasiru, Z, 2002) | 0.8 |
" Within- and between-product comparisons were determined for fed versus fasted administration considering bioavailability and tolerability of all treatments." | ( Dosage form-related food interaction observed in a marketed once-daily nifedipine formulation after a high-fat American breakfast. Blume, HH; Brendel, E; Dingler, A; Schug, BS; Wargenau, M; Wolf, D; Wonnemann, M, 2002) | 0.55 |
"Under fasted conditions the comparison of test and reference products showed a similar extent of bioavailability with a mean ratio of AUC((0-)(infinity)()) of 99% [95% confidence interval (CI) 86%, 114%], but significantly higher C(max) values resulting in a mean ratio of 169% (95% CI 139%, 206%)." | ( Dosage form-related food interaction observed in a marketed once-daily nifedipine formulation after a high-fat American breakfast. Blume, HH; Brendel, E; Dingler, A; Schug, BS; Wargenau, M; Wolf, D; Wonnemann, M, 2002) | 0.55 |
" The aim of this study was to examine whether CCBs of several kinds directly increase the bioavailability of NO in forearm resistance vessels." | ( Nitric oxide plays an insignificant role in direct vasodilator effects of calcium channel blockers in healthy humans. Arakawa, N; Hiramori, K; Nagano, M; Naganuma, Y; Nakamura, M; Yoshida, H, 2002) | 0.31 |
"The aim of this study was to investigate the effect of concomitant food intake on the bioavailability of two nifedipine containing modified release dosage forms for once daily administration." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.79 |
"After fasted administration the extent of bioavailability of nifedipine as characterized by AUC(0,infinity) was slightly lower for Slofedipine XL compared with Adalat OROS with a point estimate of 82." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.81 |
"Nifedipine (NF) is a poorly water-soluble drug, of low and irregular bioavailability after oral administration." | ( Improving the dissolution and bioavailability of nifedipine using solid dispersions and solubilizers. Badr, RM; Elbary, AA; Emara, LH, 2002) | 2.01 |
" The human pharmacokinetics and relative bioavailability of MOTS containing nifedipine were compared with a commercial Adalat osmotic tablet system containing an equivalent dose of nifedipine following an oral single dose of 30 mg given to each of 11 healthy volunteers in an open, randomized crossover study in vivo." | ( Evaluation of monolithic osmotic tablet system for nifedipine delivery in vitro and in vivo. Chen, D; Liu, X; Zhang, R, 2003) | 0.8 |
" The release characteristics of oral controlled-release medications are destroyed when crushed, resulting in the rapid bioavailability of the total drug amount." | ( Fatality from administration of labetalol and crushed extended-release nifedipine. Hoffman, RS; Howland, MA; Nelson, LS; Schier, JG, 2003) | 0.55 |
" Oral bioavailability was low." | ( Application of a new high performance liquid chromatography method to the pharmacokinetics of dibudipine in rats. Bohlooli, S; Ghiaee, S; Keyhanfar, F; Mahmoudian, M, ) | 0.13 |
" The oral bioavailability was low (< 2%) suggesting a marked first-pass effect." | ( Pharmacokinetics of mebudipine, a new calcium antagonist, following single intravenous and oral administrations in rats. Bohlooli, S; Keyhanfar, F; Mahmoudian, M, 2004) | 0.32 |
" The influence of the Ca(2+) channel antagonists on pancreatic beta cell functions is dependent on lipophilicity, interactions with the cell membrane lipid bilayer, with SNAREs protein complexes in cell and vesicle membranes, with intracellular receptors, bioavailability and time of elimination from several organs and the bloodstream." | ( Effect of new and known 1,4-dihydropyridine derivatives on blood glucose levels in normal and streptozotocin-induced diabetic rats. Bisenieks, E; Briede, J; Duburs, G; Makarova, N; Poikāns, J; Stivriņa, M; Stoldere, D; Uldriķis, J, ) | 0.13 |
" The absolute bioavailability of m-Nif given orally was very low." | ( [Pharmacokinetics of m-nifedipine in Beagle dogs]. Mei, QB; Yang, TH; Yang, ZF; Zhou, SY, 2004) | 0.63 |
" Nifedipine, a dihydropyridine-type calcium antagonist, improves endothelial function in hypercholesterolemia by enhancing nitric oxide function, and increases endothelial nitric oxide bioavailability by antioxidative mechanisms." | ( Long-term treatment with nifedipine modulates procoagulant marker and C-C chemokine in hypertensive patients with type 2 diabetes mellitus. Iwasaka, T; Nishikawa, M; Nomura, S; Omoto, S; Shouzu, A, 2005) | 1.54 |
" The increased release or bioavailability of NO may causally result from elevated endothelial [Ca(2+)](i) in arteries." | ( Cilnidipine, a slow-acting Ca2+ channel blocker, induces relaxation in porcine coronary artery: role of endothelial nitric oxide and [Ca2+]i. Chen, ZY; Gollasch, M; Huang, Y; Ko, WH; Leung, FP; Leung, HS; Yao, X, 2006) | 0.33 |
"The objective of this study was to compare the rate and extent of nifedipine bioavailability after single dose administration of Adalat OROS 30 (Reference) and Nifedipine Sandoz retard 30 tablets (Test)." | ( Significant food interactions observed with a nifedipine modified-release formulation marketed in the European Union. Blume, H; Brendel, E; Schmücker, K; Schug, B; van Zwieten, PA; Wonnemann, M, 2006) | 0.83 |
" DCMTs successfully sustained the absorption of NiD longer than IR tablets, while they did not decrease the bioavailability of NiD." | ( Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): in vivo evaluation. Higaki, K; Ibuki, R; Imai, K; Kimura, T; Okimoto, K; Tanaka, N; Tokunaga, Y; Ueda, S, 2006) | 0.33 |
" The bioavailability of the compound following the colon administration in dogs, relative to the same formulation administered orally (relative bioavailability), was determined." | ( Dog colonoscopy model for predicting human colon absorption. Evans, LA; Fortner, JH; McCarthy, JM; Sutton, SC; Sweeney, K, 2006) | 0.33 |
"Except for atenolol, a small hydrophillic molecule, the relative bioavailability from administration to the colon of the dog correlated well with the following compound properties: high solubility and high, passive permeability > high solubility, low permeability > low solubility, high, passive permeability approximately low solubility, low permeability." | ( Dog colonoscopy model for predicting human colon absorption. Evans, LA; Fortner, JH; McCarthy, JM; Sutton, SC; Sweeney, K, 2006) | 0.33 |
" However, no human intubation or dog colon studies are required for Class 1 (HS/HP), as these compounds are likely to be well absorbed from the colon." | ( Dog colonoscopy model for predicting human colon absorption. Evans, LA; Fortner, JH; McCarthy, JM; Sutton, SC; Sweeney, K, 2006) | 0.33 |
"The human ATP-binding cassette transporter, ABCG2, confers resistance to multiple chemotherapeutic agents and also affects the bioavailability of different drugs." | ( The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2. Ambudkar, SV; Bates, SE; Robey, RW; Shukla, S, 2006) | 0.33 |
"Crystallization of drugs formulated in the amorphous form may lead to reduced apparent solubility, decreased rate of dissolution and bioavailability and compromise the physical integrity of the solid dosage form." | ( Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility. Marsac, PJ; Shamblin, SL; Taylor, LS, 2006) | 0.33 |
"The results of this study report the novel use of electrostatic layer-by-layer nanoassembly of biocompatible nanoparticulate TiO2 multilayers to coat irregular nifedipine (NF) microcrystals to increase the photostability of the drug when exposed to simulated sunlight and to increase the dissolution rate and possibly the bioavailability of the drug after oral administration." | ( Nanoparticle multilayers: surface modification of photosensitive drug microparticles for increased stability and in vitro bioavailability. De Villiers, MM; Kommireddy, DS; Li, N; Liebenberg, W; Lvov, Y; Tiedt, LR, ) | 0.33 |
"Nifedipine, a dihydropyridine calcium antagonist, improves endothelial function in patients with hypercholesterolaemia by enhancing nitric oxide (NO) activity, and increases endothelial NO bioavailability by antioxidant mechanisms." | ( Effect of nifedipine on adiponectin in hypertensive patients with type 2 diabetes mellitus. Inami, N; Iwasaka, T; Kimura, Y; Nishikawa, M; Nomura, S; Omoto, S; Shouzu, A, 2007) | 2.18 |
"Grapefruit juice (GJ) contains components that may increase the bioavailability of drugs; however, approaches to the removal of these components have been little investigated." | ( The use of heat treatment to eliminate drug interactions due to grapefruit juice. Mohri, K; Uesawa, Y, 2006) | 0.33 |
" Guidance for Bioavailability and Bioequivalence Studies for Chemical Drug Products in Human Being." | ( Determination of nifedipine in human plasma and its use in bioequivalence study. Dai, J; Guo, N; Guo, X; Guo, Y; Ma, Z; Qian, G, 2007) | 0.68 |
"To determine the effect of intestinal cytochrome P450 (P450) enzymes on the bioavailability of oral drugs, we have examined the metabolism of nifedipine, an antihypertensive drug and a model substrate of CYP3A4, in mouse models having deficient expression of the NADPH-cytochrome P450 reductase." | ( Role of small intestinal cytochromes p450 in the bioavailability of oral nifedipine. Ding, X; Dunbar, D; Kaminsky, LS; Zhang, J; Zhang, QY, 2007) | 0.77 |
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects." | ( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007) | 0.34 |
" After oral administration of both tablet formulations in the fed state, marked differences in rate and extent of bioavailability were observed." | ( Comparison of two marketed nifedipine modified-release formulations: an exploratory clinical food interaction study. Anschütz, M; Blume, H; Brendel, E; De Nucci, G; Schug, B; Wonnemann, M, 2008) | 0.64 |
"Many generic drugs have been released to decrease medical expenses, but some problems have been reported with regard to bioavailability and safety." | ( Evaluation of zero-order controlled release preparations of nifedipine tablet on dissolution test, together with cost benefit point of view. Matsuyama, K; Naruto, I; Sakurai, M, 2008) | 0.59 |
"This study reports the use of para-sulphonato calix[8]arene to produce stable complexes with improved bioavailability for nifedipine, a calcium-channel blocker that is practically insoluble in water." | ( Effect of para-sulfonato-calix[n]arenes on the solubility, chemical stability, and bioavailability of a water insoluble drug nifedipine. de Villiers, MM; Liebenberg, W; Otto, DP; Yang, W, 2008) | 0.76 |
" It is interesting to note that the expression of CYP1A1 was also increased in the liver, kidney, and lung of the IE-Cpr-null mice compared with wild-type (WT) littermates, a result strongly supporting the notion that SI metabolism of putative dietary CYP1A1 inducers can influence the systemic bioavailability of these inducers." | ( An intestinal epithelium-specific cytochrome P450 (P450) reductase-knockout mouse model: direct evidence for a role of intestinal p450s in first-pass clearance of oral nifedipine. Ding, X; Dunbar, D; Fang, C; Kaminsky, L; Zhang, J; Zhang, QY, 2009) | 0.55 |
" The dissolution test and the bioavailability of the coated microcapsule in rats were evaluated compared to nifedipine powder." | ( Development of nifedipine-loaded coated gelatin microcapsule as a long acting oral delivery. Choi, HG; Choi, JS; Hong, MJ; Kang, JY; Kim, JO; Lee, WS; Li, DX; Oh, DH; Woo, JS; Yong, CS, 2009) | 0.92 |
"Nifedipine (NI) is a poorly water-soluble drug and its oral bioavailability is very low." | ( Freeze-dried nifedipine-lipid nanoparticles with long-term nano-dispersion stability after reconstitution. Itai, S; Iwao, Y; Kurita, T; Makino, Y; Miyagishima, A; Ohshima, H; Sonobe, T, 2009) | 2.16 |
" P-gp is a drug transporter, which determines the absorption and bioavailability of many drugs that are substrates for P-gp." | ( Effect of cyclosporine on drug transport and pharmacokinetics of nifedipine. Dorababu, M; Naruhashi, K; Nishimura, A; Prabha, T; Shibata, N; Sugioka, N; Takada, K, 2009) | 0.59 |
"The poor water solubility of many drugs requires a specific formulation to achieve a sufficient bioavailability after oral administration." | ( Use of hydrophobins in formulation of water insoluble drugs for oral administration. Haas Jimoh Akanbi, M; Meter-Arkema, A; Post, E; Rink, R; Robillard, GT; Scholtmeijer, K; Wang, X; Wösten, HA, 2010) | 0.36 |
"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 |
"This study was designed to evaluate and compare the bioavailability of two osmotically active formulations of 60 mg nifedipine, Gen-Nifedipine extended release Test tablets (Genpharm ULC, Etobicoke, ON, Canada) and Adalat XL Reference tablets (Bayer Healthcare AG, Leverkusen, Germany) after single dose fasted and fed administration." | ( Differences in bioavailability between 60 mg of nifedipine osmotic push-pull systems after fasted and fed administration. Anschütz, M; Blume, H; Brendel, E; Donath, F; Pauli, K; Pontius, A; Schug, B; Toal, C; Wonnemann, M, 2010) | 0.83 |
" Food components and dosing time significantly altered the oral pharmacokinetics of nifedipine in rats, implying that the altered bioavailability and higher plasma concentrations in the morning time may influence dosing regimens of nifedipine for hypertension patients." | ( Effect of food components and dosing times on the oral pharmacokinetics of nifedipine in rats. Cao, QR; Cui, JH; Han, HK; Lee, BJ; Lee, J; Oh, KT; Park, I; Park, JB, 2010) | 0.82 |
"To develop the long acting nifedipine oral delivery with bioavailability enhancement, a nifedipine dry elixir (NDE) containing nifedipine ethanol solution in dextrin shell was prepared using a spray-dryer, and then coated nifedipine dry elixir (CNDE) was prepared by coating NDE with Eudragit acrylic resin." | ( Development of coated nifedipine dry elixir as a long acting oral delivery with bioavailability enhancement. Choi, JY; Jin, SE; Kim, CK; Lee, HJ; Maeng, HJ; Park, Y, 2011) | 0.98 |
" Considering pharmacokinetic properties of nifedipine such as rapid onset and long duration of action, the good oral bioavailability and less frequent side effects, it looks more preferable in hypertension emergencies of pregnancy than hydralazine." | ( Comparison of the efficacy of nifedipine and hydralazine in hypertensive crisis in pregnancy. Esmaeili, S; Khazaeipour, Z; Motevalian, M; Pourmojieb, M; Rezaei, Z; Sharbaf, FR; Youefzadeh-Fard, Y, 2011) | 0.92 |
" DHB also reduced the absorption rate at 450 nm in a CO-binding spectrum assay without alteration of the wavelength of maximum absorption." | ( Inhibition of CYP3A4 by 6',7'-dihydroxybergamottin in human CYP3A4 over-expressed hepG2 cells. Araki, N; Enosawa, S; Fujimura, A; Hasegawa, G; Omasa, T; Tsuruoka, S; Yamazoe, Y; Yanagihara, H, 2012) | 0.38 |
"Arterial stiffness and impaired nitric oxide (NO) bioavailability contribute to the high risk for cardiovascular disease in CKD." | ( Endothelin-A receptor antagonism modifies cardiovascular risk factors in CKD. Blackwell, S; Dhaun, N; Goddard, J; Johnston, NR; Melville, V; Talwar, DK; Webb, DJ, 2013) | 0.39 |
" Furthermore, the oral bioavailability of F7 and F8 was significantly improved." | ( Formulation and pharmacokinetic evaluation of once-daily sustained-released system of nifedipine with solid dispersion and coating techniques. Wang, P; Wei, YM; Xue, ZK; Zhao, L, 2013) | 0.61 |
" A comparison of the pharmacokinetic parameters of the NI-LN suspensions with those of the NI solution prepared using only the surfactant polysorbate 80 revealed that although the AUC and bioavailability (59%) values were almost identical, a rapid absorption rate was still observed in the NI-LN suspensions." | ( Lipid nanoparticles with no surfactant improve oral absorption rate of poorly water-soluble drug. Funakoshi, Y; Itai, S; Iwao, Y; Noguchi, S, 2013) | 0.39 |
"The aim of this investigation was to examine the efficacy of PhytoSolve and Phosal-based formulation (PBF) to enhance the oral bioavailability of mebudipine, which is a poorly water-soluble calcium channel blocker." | ( Improved oral bioavalability of mebudipine upon administration in PhytoSolve and Phosal-based formulation (PBF). Keyhanfar, F; Khani, S, 2014) | 0.4 |
"The aim of this study was to investigate the effects of nifedipine on the bioavailability and pharmacokinetics of repaglinide in rats." | ( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine. Choi, DH; Choi, I; Choi, JS, 2013) | 1.03 |
" Nifedipine also increased the absolute bioavailability (AB) of repaglinide by 50." | ( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine. Choi, DH; Choi, I; Choi, JS, 2013) | 1.69 |
"Nifedipine enhanced the oral bioavailability of repaglinide, which may be mainly attributable to inhibition of CYP3A4-mediated metabolism of repaglinide in the small intestine and/or in the liver and to inhibition of the P-gp efflux transporter in the small intestine and/or reduction of total body clearance by nifedipine." | ( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine. Choi, DH; Choi, I; Choi, JS, 2013) | 2.22 |
"The bioavailability of nifedipine is significantly increased by a simultaneous oral co-administration of DCT." | ( Da-Chaihu-Tang alters the pharmacokinetics of nifedipine in rats and a treatment regimen to avoid this. Akao, T; Hattori, M; He, JX; Ohno, K; Tang, J; Tani, T, 2014) | 0.97 |
" On oral administration it undergoes extensive first pass metabolism, which outweighs its absorbance through gastrointestinal tract (GIT) and bioavailability of the drug in systemic circulation." | ( A novel vesicular transdermal delivery of nifedipine - preparation, characterization and in vitro/in-vivo evaluation. Jain, K; Jakki, SL; Kuppusamy, G; Natarajan, J; Sood, S; Venkatachalam, S; Yasam, VR, 2016) | 0.7 |
"Amorphous drugs are used to improve the solubility, dissolution, and bioavailability of drugs." | ( A method to evaluate the effect of contact with excipients on the surface crystallization of amorphous drugs. de Villiers, MM; Derdour, L; Huang, J; Hussain, MA; Qian, F; Yu, L; Zhang, SW, 2014) | 0.4 |
"The objective of this paper was to prepare nifedipine-loaded oral copolymer micelles and to improve bioavailability of hydrophobic drugs." | ( Study on the preparation of nifedipine-loaded oral copolymer micelles and its pharmacokinetics in rats. Ding, PT; Yang, YH, 2015) | 0.97 |
"The commercial and clinical success of amorphous solid dispersions (ASD) in overcoming the low bioavailability of poorly soluble molecules has generated momentum among pharmaceutical scientists to advance the fundamental understanding of these complex systems." | ( Impact of polymers on the crystallization and phase transition kinetics of amorphous nifedipine during dissolution in aqueous media. Alonzo, DE; Gao, Y; Raina, SA; Taylor, LS; Zhang, GG, 2014) | 0.63 |
" Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP." | ( Spontaneous emulsification of nifedipine-loaded self-nanoemulsifying drug delivery system. Kumpugdee-Vollrath, M; Limmatvapirat, S; Sriamornsak, P; Weerapol, Y, 2015) | 0.71 |
" Consequently, the absolute bioavailability (AB) of nifedipine in the presence of pioglitazone (1." | ( Effects of pioglitazone on the pharmacokinetics of nifedipine and its main metabolite, dehydronifedipine, in rats. Choi, DH; Choi, I; Choi, JS, 2016) | 0.94 |
"The increased bioavailability of nifedipine may be mainly due to inhibition of both P-gp in the small intestine and CYP3A subfamily-mediated metabolism of nifedipine in the small intestine and/or in the liver and to the reduction of the CL/F of nifedipine by fluvastatin and simvastatin." | ( Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of nifedipine in rats: Possible role of P-gp and CYP3A4 inhibition by HMG-CoA reductase inhibitors. Choi, DH; Choi, JS; Lee, CK, 2015) | 0.93 |
"The objective of this study was to prepare spontaneous emulsifying powder (SEP) for improving dissolution and enhancing oral bioavailability of a poorly water-soluble drug, nifedipine (NDP)." | ( Enhanced dissolution and oral bioavailability of nifedipine by spontaneous emulsifying powders: effect of solid carriers and dietary state. Jansakul, C; Limmatvapirat, S; Sriamornsak, P; Takeuchi, H; Weerapol, Y, 2015) | 0.86 |
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates." | ( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. Bharate, SS; Vishwakarma, RA, 2015) | 0.42 |
" The intestinal absorption rate for each drug was acquired by deconvolution, using historical intravenous data as reference, and used with the intestinal surface area and the dose remaining in the lumen to estimate the Peff." | ( Human in vivo regional intestinal permeability: quantitation using site-specific drug absorption data. Dahlgren, D; Lennernäs, H; Roos, C; Sjögren, E, 2015) | 0.42 |
") administration studies were conducted to calculate the oral bioavailability (BA)." | ( An Assessment of the Oral Bioavailability of Three Ca-Channel Blockers Using a Cassette-Microdose Study: A New Strategy for Streamlining Oral Drug Development. Imai, H; Inano, A; Kataoka, M; Morimoto, T; Mutaguchi, K; Ohashi, K; Sugiyama, Y; Suzaki, Y; Togashi, K; Yamashita, S, 2015) | 0.42 |
" The primary factor leading to increased bioavailability is the administration of the drug in a pre-dissolved state thereby avoiding the dissolution limiting step." | ( Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity. Belotti, S; Chavant, Y; Chevrier, S; Demarne, F; Dumont, C; Jannin, V; Michenaud, M, 2015) | 0.42 |
"4 h and oral bioavailability of (F) 56." | ( Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. Bansode, R; Bhargavi, G; Chikhale, R; Jadhav, A; Karodia, N; Khedekar, P; Pant, A; Paradkar, A; Rajasekharan, MV; Thatipamula, KC; Thorat, S, 2015) | 0.42 |
"A nanoemulsion drug delivery system was developed to increase the oral bioavailability of mebudipine as a calcium channel blocker with very low bioavailability profile." | ( Design and evaluation of oral nanoemulsion drug delivery system of mebudipine. Amani, A; Keyhanfar, F; Khani, S, 2016) | 0.43 |
"The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to examine the influence of the biopharmaceutics classification system class on the simulation success." | ( Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models. Aarons, L; Darwich, A; Dressman, J; Hansmann, S; Margolskee, A, 2016) | 0.43 |
" In some cases, the formation of crystals will impact the bioavailability of the active pharmaceutical ingredient in these formulations." | ( Frozen in Time: Kinetically Stabilized Amorphous Solid Dispersions of Nifedipine Stable after a Quarter Century of Storage. Anantharaman, S; Dreis-Kühne, SH; Kyeremateng, SO; Mägerlein, M; Rosenberg, J; Theil, F; van Lishaut, H; Woehrle, GH, 2017) | 0.69 |
" Furthermore, the in vivo pharmacokinetic results suggested that these cubosomes led to a considerable increase in the systemic oral bioavailability of the drugs compared with pure dispersions of the same materials." | ( Enhancing the Solubility and Oral Bioavailability of Poorly Water-Soluble Drugs Using Monoolein Cubosomes. Ali, MA; Itai, S; Iwao, Y; Kataoka, N; Noguchi, S; Oka, T; Ranneh, AH, 2017) | 0.46 |
" These nanodroplets, present as a dispersed phase, can potentially enhance oral bioavailability of poorly soluble drugs by serving as a drug reservoir that efficiently feeds the continuous aqueous solution phase following absorption of drug." | ( Origin of Nanodroplet Formation Upon Dissolution of an Amorphous Solid Dispersion: A Mechanistic Isotope Scrambling Study. Gao, Y; Indulkar, AS; Mo, H; Raina, SA; Taylor, LS; Waters, JE; Zhang, GGZ, 2017) | 0.46 |
" Increment of talinolol bioavailability upon low and high doses of barnidipine co-administration may be due to P-glycoprotein inhibition." | ( Pharmacokinetics of talinolol is modified by barnidipine: implication of P-glycoprotein modulation. Okyar, A; Ozturk, D; Ozturk, N; Pala-Kara, Z, 2017) | 0.46 |
"Amorphous solid dispersions (ASD) are intended to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients." | ( In-situ determination of crystallization kinetics in ASDs via water sorption experiments. Luebbert, C; Sadowski, G, 2018) | 0.48 |
" If gut microbes are involved in the metabolism of nifedipine, plateau hypoxia may regulate the bioavailability and the therapeutic effect of nifedipine by altering the metabolic activity of the gut microbiota." | ( Plateau hypoxia attenuates the metabolic activity of intestinal flora to enhance the bioavailability of nifedipine. Chen, Y; Jia, Z; Sun, Y; Wang, R; Zhang, J, 2018) | 0.95 |
"Wet milling is a multifunctional and the most common method to prepare a drug nanosuspension for improving the bioavailability of poorly water soluble drugs." | ( A quality-by-design study to develop Nifedipine nanosuspension: examining the relative impact of formulation variables, wet media milling process parameters and excipient variability on drug product quality attributes. Dave, RH; Gajera, BY; Patel, PJ, 2018) | 0.75 |
"In this study, a nanoemulsion containing mebudipine [composed of ethyl oleate (oil phase), Tween 80 (T80), Span 80 (S80) (surfactants), polyethylene glycol 400, ethanol (cosurfactants), and deionized water] was prepared with the aim of improving its bioavailability for an effective antihypertensive therapy." | ( Use of artificial neural networks for analysis of the factors affecting particle size in mebudipine nanoemulsion. Abbasi, S; Amani, A; Keyhanfar, F; Khani, S, 2019) | 0.51 |
"Liquid-liquid phase separation (LLPS) occurs following amorphous solid dispersion (ASD) dissolution when the drug concentration exceeds the "amorphous solubility", and is emerging as an important characteristic of formulations that may enhance the oral bioavailability of poorly soluble drugs." | ( Congruent release of drug and polymer: A "sweet spot" in the dissolution of amorphous solid dispersions. Kestur, US; Mugheirbi, NA; Saboo, S; Taylor, LS; Zemlyanov, DY, 2019) | 0.51 |
" Hence, the data suggest gastroretention as a promising approach to enhance bioavailability of nifedipine." | ( Formulation, Optimization, and In vivo Evaluation of Gastroretentive Drug Delivery System of Nifedipine for the Treatment of Preeclampsia. Avari, JG; Karemore, MN, 2019) | 0.95 |
"Co amorphous systems are supersaturated drug delivery systems which offer a basic platform for delivery of multicomponent adducts (combination of more than one active pharmaceutical ingredient (API)) and/or as a fixed dose combination therapy, in addition to their potential to improve the apparent solubility, dissolution rate and ultimately bioavailability of poorly water soluble APIs." | ( Co amorphous valsartan nifedipine system: Preparation, characterization, in vitro and in vivo evaluation. Chavan, RB; Chella, N; Lodagekar, A; Mannava, MKC; Nangia, AK; Shastri, NR; Yadav, B, 2019) | 0.82 |
"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 |
"Proliposomes were used to improve the solubility and oral bioavailability of nifedipine." | ( A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine. Bi, Y; Lee, RJ; Li, L; Lv, B; Qiu, Z; Teng, L; Xie, J, 2020) | 1.02 |
"Drug release plays a critical role in defining bioavailability for an extended release solid oral drug products and predictive dissolution tests are desired to establish clinically relevant quality standards for batch release." | ( Nifedipine Release From Extended-Release Solid Oral Formulations Using In Vitro Dissolution Testing Under Simulated Gastrointestinal Compression. Gao, Z; Rodriguez, JD; Tian, L, 2020) | 2 |
" It suggested that the potential interactions of SMS with CYP 3A drug substrates should be noticed, especially the drugs whose bioavailability depends heavily on intestinal CYP3A." | ( Effects of Shengmai San on key enzymes involved in hepatic and intestinal drug metabolism in rats. Chia-Hui Tan, E; Chiang, TY; Lee, IJ; Ueng, YF; Wang, HJ; Wang, YC; Yun, CH, 2021) | 0.62 |
"Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility." | ( Microemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: Structural and in vitro study. Antunes de Souza Araújo, A; Cavalcante Duarte, M; de Souza Nunes, R; Mendonça da Cruz Macieira, G; Moreira Lira, AA; Nery Dos Santos, Q; Otubo, L; Santos Matos, S; Souza de Araujo, GR; Vitorino Sarmento, VH; Xavier de Oliveira, D, 2022) | 2.38 |
" However, their performance is limited by the low physical stability of the amorphous phase which can lead to recrystallization which in turn results in decreased solubility and bioavailability of the drug." | ( Polyvinylpyrrolidone as co-inhibitor of crystallization of nifedipine in paper tablets. Castro-Camus, E; Heidrich, L; Keck, CM; Koch, M; Ornik, J, 2023) | 1.15 |
"Polymers like poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA) or hydroxypropyl methylcellulose acetate succinate (HPMCAS) are commonly used as a matrix for amorphous solid dispersions (ASDs) to enhance the bioavailability of the active pharmaceutical ingredients (APIs)." | ( Water Sorption in Rubbery and Glassy Polymers, Nifedipine, and Their ASDs. Danzer, A; Fahrig, I; Fritschka, E; Grönniger, B; Sadowski, G, 2023) | 1.17 |
Nifedipine gastrointestinal therapeutic system (GITS) is a once-daily formulation. It provides sustained plasma nifedipsine concentrations throughout the 24-hour dosing interval. The needle and syringe methods were the most reproducible and efficient procedures.
Excerpt | Relevance | Reference |
---|---|---|
" When nifedipine dosage was decreased." | ( Nifedipine therapy for refractory coronary arterial spasm. Heupler, FA; Proudfit, WL, 1979) | 2.18 |
" 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) | 0.75 |
"3-3 mg/kg), dose-response curves of the antihypertensive effect did not change and body weight gain was equal to that of the vehicle-treated group." | ( Antihypertensive effects of MPC-1304, a novel calcium antagonist, in experimental hypertensive rats and dogs. Haruno, A; Kanda, A; Miyake, H; Nagasaka, M, 1992) | 0.28 |
" Adequate blood pressure reductions were achieved with nilvadipine 8 mg once daily in 13 patients; 7 required a doubling of the dosage to 16 mg/day." | ( 24-hour blood pressure control after single daily doses of nivaldipine in patients with essential hypertension. Huber, HJ; Kuchlbauer, R; Lossnitzer, K; Quitzdorff, G, 1992) | 0.28 |
" This dosage was well tolerated." | ( Nilvadipine in hypertension with renal dysfunction. Albert, FW; Berger, HH, 1992) | 0.28 |
" 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 results indicate that the maximal stimulation of transcaltachia occurs at 50 pM PTHrP(1-40), and that the dose-response curve is biphasic in nature." | ( A parathyroid-related peptide induces transcaltachia (the rapid, hormonal stimulation of intestinal Ca2+ transport). Nemere, I; Norman, AW; Zhou, LX, 1992) | 0.28 |
" Increase in extracellular K+ concentration (10, 15 mM) shifted the dose-response relationship for the ET-1-induced contraction to the left." | ( A pertussis toxin-sensitive mechanism of endothelin action in porcine coronary artery smooth muscle. Goto, K; Kasuya, Y; Masaki, T; Takuwa, Y; Yanagisawa, M, 1992) | 0.28 |
" These results suggest that HP-beta-CyD is particularly useful in solving problems encountered on storage of amorphous nifedipine in solid dosage forms." | ( Inhibitory effect of 2-hydroxypropyl-beta-cyclodextrin on crystal-growth of nifedipine during storage: superior dissolution and oral bioavailability compared with polyvinylpyrrolidone K-30. Hirayama, F; Horiuchi, Y; Ikegami, K; Uekama, K; Wang, Z, 1992) | 0.72 |
" The acute or chronic administration of phenoxybenzamine alone displaced the dose-response curve to cirazoline to the right in a dose-dependent manner, while reducing the slope function and maximum response to the agonist." | ( A comparison of the effects of acute versus chronic administration of phenoxybenzamine on pressor responses elicited by the selective alpha 1-adrenoceptor agonist cirazoline in the pithed rat preparation. Tabrizchi, R; Triggle, CR, 1992) | 0.28 |
" Dosing with 25 mg carvedilol once daily or 20 mg nifedipine SR twice daily resulted in mean peak reductions in supine blood pressure of 21/11 and 20/16 mm Hg, respectively, after 1 week of treatment with each respective monotherapy." | ( Safety of the coadministration of carvedilol and nifedipine sustained-release in the treatment of essential hypertension. de Vries Robles, P; Juttmann, JR; Venuti, RP, 1992) | 0.79 |
" Treatment with captopril was found to attenuate pressor responses produced by the administration of either alpha 1- or alpha 2-adrenoceptor agonists, resulting in the displacement to the right of the agonist dose-response curves and significantly increasing the calculated ED50 values." | ( The interrelationship between the effects of captopril and nifedipine on pressor responses elicited by selective alpha-adrenoceptor agonists in the pithed rat preparation. Tabrizchi, R; Triggle, CR, 1992) | 0.53 |
" Patients received a daily oral dosage of either 4 to 8 mg of perindopril or 40 to 80 mg of nifedipine in slow-release form." | ( Relation of regression of left ventricular hypertrophy to changes in ambulatory blood pressure after long-term therapy with perindopril versus nifedipine. Gotzen, R; Lenz, T; Liederwald, K; Meyer-Sabellek, W; Schulte, KL; van Gemmeren, D, 1992) | 0.7 |
" 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 |
" Gingival changes in the nifedipine patients were not related to drug dosage or plaque scores." | ( The incidence and severity of nifedipine-induced gingival overgrowth. Barclay, S; Idle, JR; Seymour, RA; Thomason, JM, 1992) | 0.88 |
" Due to the low incidence of side effects and the once-daily dosage regimen, an improvement in patient compliance can be expected." | ( [Effectiveness and tolerance of amlodipine in treatment of patients with mild to moderate hypertension. Results of a long-term study with a new calcium antagonist]. Ganzinger, U; Habeler, G; Lenzhofer, R; Pall, H; Tomaschek, A; Ziebart-Schroth, A; Zirm, B, 1992) | 0.28 |
" Amlodipine shows linear dose-related pharmacokinetic characteristics and, at steady-state, there are relatively small fluctuations in plasma concentrations across a dosage interval." | ( Clinical pharmacokinetics of amlodipine. Elliott, HL; Meredith, PA, 1992) | 0.28 |
" Fluctuation of plasma drug concentration between doses is between 20 and 25% when once-daily dosing is used." | ( Pharmacokinetics and pharmacodynamics of amlodipine. Abernethy, DR, 1992) | 0.28 |
" This study established that the large intestine is the major site of residence and absorption for this dosage form." | ( New developments in sustained-release antihypertensive therapy: formulation and pharmacokinetic considerations. Davis, SS; Devane, JG; Kavanagh, M; Mulligan, S; Sparrow, RA; Wilding, IR, 1992) | 0.28 |
" Automated ambulatory blood pressure recordings performed in 221 of the patients showed that the blood pressure was lowered evenly through the entire 24-hour dosing period." | ( Effectiveness of once-daily monotherapy with a new nifedipine sustained release calcium antagonist. Bottini, PB; Carr, AA; Devane, JG; Feig, P; Fisher, L; MacCarthy, EP; Mulligan, S; Prisant, LM; Rhoades, RB, 1992) | 0.54 |
"1 mg/kg) occurred during an 8-week repeated daily dosing to RHD and plasma renin activity, and aldosterone levels were not elevated during this period." | ( Y-27152, a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state. Aoki, K; Fukunari, A; Katoh, A; Nakajima, T; Setoguchi, M; Shinagawa, K; Shinohara, T; Tahara, T; Yamanaka, T; Yaoka, O, 1992) | 0.28 |
" 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) | 0.57 |
" Therapeutic doses of nifedipine are associated with measurable shifts in the dose-response curves to these two alpha-adrenergic agonists in the hand vein." | ( Responsiveness of peripheral veins to vasodilators and the effect of nifedipine on alpha-adrenergic responsiveness in hypertension. Blaschke, TF; Ford, GA; Hoffman, BB; Katzir, D, 1991) | 0.83 |
" Oral dosing of nilvadipine suppressed carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen." | ( Inhibition by nilvadipine of ischemic and carrageenan paw edema as well as of superoxide radical production from neutrophils and xanthine oxidase. Oyanagui, Y; Sato, S, 1991) | 0.28 |
" Administration of nifedipine to Sprague-Dawley and WKY rats did not affect the dose-response curve to AVP, but nifedipine administration in SHR led to a significant inhibition of the pressor responses to AVP." | ( Pressor actions of arginine vasopressin in pithed Sprague-Dawley, Wistar-Kyoto and spontaneously hypertensive rats before and after treatment with nifedipine or pertussis toxin. Tabrizchi, R; Triggle, CR, 1991) | 0.81 |
" In a subgroup of sheep, chronic dosing with phenobarbital increased maternal nifedipine clearance 3-fold." | ( Pharmacokinetics and pharmacodynamics of nifedipine in pregnant sheep. Abramson, FP; Hill, M; Hursey, T; Nugent, CE, ) | 0.63 |
" The ED50 value for the dose-response curves to B-HT 920 and St587 were found to be significantly increased after the administration of staurosporine." | ( Effects of staurosporine on the pressor responses to alpha-adrenoceptor agonists in pithed rats: a comparison with nifedipine. Tabrizchi, R; Triggle, CR, 1991) | 0.49 |
"Effects of Bay K 8644, partial depolarization with high potassium, and nifedipine on the dose-response curves of the rat vas deferens to norepinephrine, methacholine and KCI were investigated in HEPES-buffered physiological salt solution (PSS) with or without 20 mM sodium bicarbonate." | ( Bicarbonate-dependent action of Bay K 8644 in the smooth muscle of the rat vas deferens. Gomi, Y; Suzuki, N, 1990) | 0.51 |
" Doxazosin produced rightward shifts of the PE pressor dose-response curves but had no effect on responses to AII." | ( Vascular pressor responses in treated and untreated essential hypertension. Donnelly, R; Elliott, HL; Howie, CA; Reid, JL; Sumner, DJ, 1990) | 0.28 |
" Treatment with pertussis toxin caused the DBP dose-response curve to SRTX-b to be displaced to the right." | ( Effects of nifedipine, BAY K 8644, and pertussis toxin on pressor response to sarafotoxin-b in pithed rats. Tabrizchi, R; Triggle, CR, 1990) | 0.67 |
" Sixty percent D2O also depressed a calcium contraction dose-response curve by approximately 25%." | ( Deuterium oxide reduces agonist and depolarization-induced contraction of rat aortic rings. Liepins, A; McWilliam, TM; Rankin, AJ, 1990) | 0.28 |
"The dose-response effects of BAY K 8644 and nifedipine on diaphragmatic contractility were assessed in vitro." | ( Multiple effects of BAY K 8644 and nifedipine on isolated diaphragmatic fibers in vitro. Aubier, M; Pavlovic, D; Viires, N, 1991) | 0.82 |
" 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) | 0.28 |
"; n = 4) in antagonizing cumulative dose-response curve for Ca2+ in the depolarized aorta strips." | ( Ca2+ channel blocking effects of hirsutine, an indole alkaloid from Uncaria genus, in the isolated rat aorta. Aimi, N; Horie, S; Horiuchi, H; Sakai, S; Watanabe, K; Yano, S, 1991) | 0.28 |
"Sixty patients (31 male, 29 female) were studied in a 4-week double-blind parallel dose-response study." | ( A double-blind dose-response study of amlodipine in patients with stable angina pectoris. Alfiero, R; Cocco, G, 1991) | 0.28 |
"2 mg/kg/day for 20 days) chronically receiving AML, there was an enhancement of the antihypertensive effect of AML within a few days after starting chronic dosing, and thereafter a significant reduction of BP at 24 hr after dosing and constant effects of AML during subsequent treatment." | ( [Antihypertensive effects of amlodipine, a new calcium antagonist]. Ishiko, J; Munehasu, S; Suzuki, M; Yamanaka, K, 1991) | 0.28 |
" The pharmacokinetics of the molecule mean that effective blood levels and hence good control of blood pressure are maintained throughout the dosing interval." | ( Amlodipine: an effective once-daily antihypertensive agent. Tyler, HM, 1991) | 0.28 |
" Ambulatory monitoring studies have confirmed that once-daily dosing provides 24-h control of blood pressure." | ( Amlodipine in the treatment of hypertension. Kaplan, NM, 1991) | 0.28 |
"In a patient with a gastroplasty, gastric outlet obstruction developed after the dosage of nifedipine GITS (gastrointestinal therapeutic system) was increased from 30 to 60 mg/d." | ( Nifedipine GITS (gastrointestinal therapeutic system) bezoar. Bottini, PB; Carr, AA; Kaesemeyer, WH; Prisant, LM, 1991) | 1.94 |
" 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) | 0.52 |
" We conclude that a therapeutic oral dosage of nifedipine has a significant relaxing effect on the human gallbladder." | ( Effect of nifedipine on interdigestive gallbladder volume and postprandial gallbladder emptying in man. Jonderko, K; Kasicka-Jonderko, A; Kucio, C; Nowak, A; Sliwiński, Z, 1991) | 0.94 |
" A dosing interval of every 3 to 4 hours is suggested when rapid-release nifedipine is used in the postpartum patient with preeclampsia." | ( Nifedipine pharmacokinetics and pharmacodynamics during the immediate postpartum period in patients with preeclampsia. Barton, JR; Prevost, RR; Sibai, BM; Whybrew, WD; Wilson, DA, 1991) | 1.96 |
" In contrast, conventional drug dosage forms exert no control, permitting the familiar peak-and-trough concentration cycle, often resulting in side effects or suboptimal therapy or both." | ( Overview and evolution of therapeutic systems. Zaffaroni, A, 1991) | 0.28 |
" Plasma concentrations of Diltiazem were 328 +/- 35 ng/l with the 360 mg/day dosage and 137 +/- 52 ng/l with the 180 mg/day dosage." | ( [Comparative study of effects of diltiazem, nifedipine and their combination on exercise stable angina]. Bonnet, JL; Bory, M; Djiane, P; Gillet, T; Habib, G; Sebag, CL, 1991) | 0.54 |
" 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 |
" In a double-blind dose-finding study, 58 patients were treated in five consecutive dosage steps each lasting 1-3 months." | ( Responders and non-responders to metoprolol, propranolol and nifedipine treatment in migraine prophylaxis: a dose-range study based on time-series analysis. Diener, HC; Gerber, WD; Niederberger, U; Scholz, E, 1991) | 0.52 |
" Thus the results indicate that nifedipine in clinical therapeutic dosage may directly reduce Ca2+ conductance and then in higher concentration may also depress secondarily Ca(2+)-dependent potassium conductance." | ( [Nifedipine inhibits calcium-dependent potentials in guinea pig sympathetic neurons]. Ma, RC; Zhai, J, 1991) | 1.48 |
" Each drug was given separately in a random fashion in fixed dosage for 4 weeks with a washout period of 2 weeks in between the drugs." | ( The effects of antihypertensive agents on the quality of life in Indian hypertensives. Kumar, K; Rajan, AG; Somani, PN; Sundar, S, 1991) | 0.28 |
" Newer agents including calcium channel blockers, which exert potent antihypertensive effects without adversely affecting metabolic parameters unfavorably, are used with increasing frequency in hypertensive patients, but their clinical utility has been limited by the need for multiple daily dosing with attendant fluctuations in plasma levels thought to be associated with nuisance side effects and possible gaps in therapeutic protection." | ( Endocrine and renal effects of nifedipine gastrointestinal therapeutic system in patients with essential hypertension. Results of a multicenter trial. The Modern Approach to the Treatment of Hypertension Study Group. Bravo, EL; Friedman, CP; Krakoff, LR; Tuck, ML, 1990) | 0.57 |
" Nifedipine was administered in the third group at a dosage of 46 micrograms/kg body weight/h." | ( Positive influence of nifedipine on early-stage minipig shock lung. Rüfer, R; Widjaja, B; Wuthe, J, 1990) | 1.5 |
" Six patients had negative results; out of the remaining six, three exhibited a significant increase in the dosage required for provoking ischemia." | ( Intravenous nifedipine prevents ergonovine-induced myocardial ischemia in patients with stable effort angina. Brunelli, C; Caponnetto, S; Caudullo, M; Ghigliotti, G; Iannetti, M; Spallarossa, P, 1990) | 0.66 |
" Under this aspect we examined 44 patients by right heart catheterisation at rest and at exercise before and after sublingual application of a single dose of 20 mg nifedipine (Corinfar) as well as under continuous dosage of 30-60 mg daily." | ( The influence of nifedipine (Corinfar) on pulmonary hypertension in chronic obstructive lung disease. Evers, H; Harzbecker, K; Orschekowski, H; Schauer, J; Schilling, W; Steiniger, L; Winkler, J, 1990) | 0.81 |
" In this dosage peripheral effects--decrease of peripheral vascular resistance and mean aortic pressure--did not differ significantly between them." | ( [Myocardial effects of the calcium antagonists nifedipine, nisoldipine and isradipine in coronary heart disease]. Ickrath, O; Karsch, KR; Kühlkamp, V; Mauser, M; Voelker, W, 1990) | 0.54 |
" Thus, it is concluded that isradipine, administered in an equally effective antihypertensive dosage regimen is superior to nifedipine with regard to the incidence of adverse effects, resulting in greater patient satisfaction with treatment." | ( The calcium antagonist isradipine in the therapy of hypertension. A double-blind crossover comparison with nifedipine. Burger, KJ; Welzel, D, 1990) | 0.7 |
" To determine the mechanism of action of nifedipine and its dose-response relation, 14 patients with stable angina were treated with nifedipine 10, 20 and 30 mg 4 times daily as single-agent therapy in a double-blind, randomized, placebo-controlled crossover trial." | ( Effects of nifedipine on myocardial perfusion during exercise in chronic stable angina pectoris. Gervino, E; Jarisch, WR; Rice, KR; Stone, PH, 1990) | 0.93 |
" At week 8, if the target diastolic pressure of less than 90 mm Hg was not achieved, the dosage of hydrochlorothiazide was increased to 50mg." | ( Comparative efficacy and safety of enalapril and sustained-release nifedipine in patients with mild to moderate hypertension. The Enalapril vs Nifedipine French Study Group. Artigou, JY; Benichou, M; Berland, J; Fressinaud, P; Grollier, G; Gueret, P; Nguyen, CD, 1990) | 0.52 |
"This randomized multicentre study in elderly hypertensives with two unbalanced groups (2 patients under labetalol for 1 patient under nifedipine) compared the efficacy and safety of labetalol, whose dosage could be adjusted (1, 2, then 3 tablets/day) according to blood pressure level (BP greater than or equal to 160/95 mmHg), to that of nifedipine given at its recommended dosage (2 tablets/day)." | ( [Hypertension in the elderly. Comparison of the efficacy and tolerability of labetalol and nifedipine. A multicenter, randomized, single-blind study]. d'Allens, H; Decoulx, M; Godon, P; Pappo, M, 1990) | 0.7 |
" Sitting (and standing) blood pressure and heart rate one to four hours after dosing were recorded at entry (191/95 mmHg) and at the end of the run-in period (186/93 mmHg)." | ( Hypertension in the elderly: a study of a combination of atenolol and nifedipine. Cheadle, B; Duckett, GK, 1990) | 0.51 |
" 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 |
" Blood pressure reduction was still significant in both groups during the early morning hours at the end of the dosage interval." | ( Influence of co-dergocrine mesilate/nifedipine compared to mefruside/nifedipine on circadian blood pressure in patients with essential hypertension. Heintz, B; Heller, A; Kirsten, R; Nelson, K, 1990) | 0.55 |
" The dosage of felodipine or nifedipine was doubled if seated diastolic blood pressure exceeded 95 mmHg, 2 or 4 weeks after randomisation." | ( Control of blood pressure in hypertensive patients with felodipine extended release or nifedipine retard. Littler, WA, 1990) | 0.79 |
"Behavioral performances of normotensive and hypertensive adult male baboons were tested before, during, and following chronic oral dosing with nifedipine." | ( Behavioral performance effects of nifedipine in normotensive and renovascular hypertensive baboons. Hienz, RD; Turkkan, JS, 1990) | 0.76 |
" Relaxation dose-response curves for D600 or nifedipine were generated, and IC50 values were calculated." | ( Factors affecting rabbit mesenteric artery smooth muscle sensitivity to calcium antagonists. Cipkus-Dubray, LA; Meisheri, KD; Sage, GP, 1990) | 0.54 |
"Nifedipine was embedded in a gelatin matrix to develop a prolonged release dosage form." | ( Controlled release of nifedipine from gelatin microspheres and microcapsules: in vitro kinetics and pharmacokinetics in man. Leucuţa, SE, ) | 1.89 |
" During 12 weeks of prednisone treatment in a dosage of 40 mg daily, her condition markedly deteriorated clinically and hemodynamically as manifested by pulmonary artery pressure (PAP), pulmonary vascular resistance (PVR), cardiac output (CO), mixed venous O2 saturation, and systemic vascular resistance (SVR)." | ( Nifedipine and prazosin in the management of pulmonary hypertension in CREST syndrome. Dresner-Feigin, R; Galun, E; Glikson, M; Pollack, A; Rubinow, A, 1990) | 1.72 |
" Nifedipine (3 X 10(-7) M) produced a parallel shift to the right of the dose-response curve to BAY-K-8644, whereas 5 X 10(-6)M verapamil markedly reduced the responses evoked by all concentrations of this drug." | ( The effects of BAY-K-8644 on the contraction of cat middle cerebral and femoral arteries. Marin, J; Reviriego, J; Salaices, M; Sanchez-Ferrer, CF, 1985) | 1.18 |
" Both vasodilators depressed the pressor dose-response curves to BHT 920, while sparing those to methoxamine." | ( Calcium entry blockade and alpha-adrenergic responsiveness in vivo. Pedrinelli, R; Tarazi, RC, 1985) | 0.27 |
" In the isolated rat mesenteric artery, perfused with a depolarizing solution, vasoconstrictor Ca2+ dose-response curves are shifted to the right by nifedipine." | ( In vitro comparative studies of the calcium-entry activators YC-170, CGP 28392, and BAY K 8644. Criscione, L; Meier, M; Rogg, H; Truog, A, 1985) | 0.47 |
" 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, ) | 0.13 |
" BAY K 8644, in either potassium buffer, induced a statistically significant shift to the left in the norepinephrine dose-response curve." | ( The facilitative actions of Bay K 8644 on norepinephrine and KCl-induced contractures of rabbit aortic rings. Babich, M; Piascik, MT, 1986) | 0.27 |
" Dose-response curves to K+ show that following differentiation, cells become more sensitive, releasing transmitter at lower K+ concentrations." | ( Nerve growth factor modulates the drug sensitivity of neurotransmitter release from PC-12 cells. Kongsamut, S; Miller, RJ, 1986) | 0.27 |
" 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) | 0.27 |
" The dose-response curve for BAY K 8644 was established in 5 mM K+-containing medium and for 30 min exposure to 45Ca." | ( BAY K 8644-induced enhancement of 45Ca uptake by rabbit aortic rings. Anderson, CL; Janis, RA; Scriabine, A, ) | 0.13 |
" The antihypertensive response to BRL 34915 in these models is reproducible on repeat once daily dosing without rebound hypertension on cessation of dosing." | ( BRL 34915, a novel antihypertensive agent: comparison of effects on blood pressure and other haemodynamic parameters with those of nifedipine in animal models. Buckingham, RE; Clapham, JC; Hamilton, TC; Longman, SD; Norton, J; Poyser, RH, ) | 0.34 |
" When the effect of nifedipine on the dose-response curve for Bay k 8644 was determined in WKY femoral artery, there was a similar extent of rightward displacement of the dose-response curve to that seen in SHR." | ( Contractile effects of Bay k 8644, a dihydropyridine calcium agonist, on isolated femoral arteries from spontaneously hypertensive rats. Aoki, K; Asano, M; Matsuda, T, 1986) | 0.59 |
" The effect of ANP on the dose-response curve of aldosterone stimulated by ANG II, ACTH, and potassium on isolated rat adrenal glomerulosa cells was studied." | ( Role of calcium in effects of atrial natriuretic peptide on aldosterone production in adrenal glomerulosa cells. Chartier, L; Schiffrin, EL, 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 |
" When dosing regimens that produced stable plasma levels of both drugs were used, the observed effects were closely related to the plasma concentrations of the individual agents." | ( Nifedipine-propranolol interaction: dependence of cardiovascular effects on plasma drug concentrations. Hamann, SR; Kaltenborn, KE; McAllister, RG, 1987) | 1.72 |
" At the end of the 2-week control period, exercise performance was assessed with treadmill exercise testing and measurement of oxygen consumption during the final third of the dosing interval." | ( Comparison of nitroglycerin patches and nifedipine. Burdick, DC; Eldridge, JE; Hossack, KF; Jones, RH, 1987) | 0.54 |
" Higher concentrations of these antagonists shifted the Ca2+ dose-response curve to the right." | ( Adrenergic-cholinergic interactions in left atria. II. Comparison of the antagonism of inotropic responses to alpha- and beta-adrenoceptor stimulation and BAY K 8644 by carbachol, D-600, and nifedipine. MacLeod, KM, 1987) | 0.46 |
" The dose-response curve of nifedipine was shifted parallel to the right by the infusion of Bay K 8644 and the dose-ratio was the greatest of the 4 drugs." | ( Differential antagonism by Bay K 8644 of vasodilator effects of nifedipine, diltiazem, nicorandil and nitroglycerin in dog femoral circulation. Ishii, K; Sato, Y; Taira, N, 1988) | 0.81 |
" When the effects of an elevation in the level of extracellular K+ on the contractile responses to BAY were determined in SHR and WKY rat femoral arteries, dose-response curves for BAY were not significantly different between the SHR and WKY rats." | ( Increased responsiveness to calcium agonist BAY k 8644 and calcium antagonist nifedipine in femoral arteries of spontaneously hypertensive rats. Aoki, K; Asano, M, 1987) | 0.5 |
" Twenty-one patients with concentric LVH (thickness of interventricular septum, IVS, and left posterior wall, LPW, above 11 mm) were given a 2D and M-mode echocardiogram before (pre) and 12 and 24 weeks, respectively, after therapy was initiated (mean oral cl dosage 150 micrograms; nf, 30 mg/day)." | ( Effects of clonidine and nifedipine on left ventricular hypertrophy and muscle mass in hypertensive patients. Brückner, S; Kleine, P; Meissner, E; von Bruchhausen, V, 1987) | 0.58 |
" At 6 h post DE, there were no differences between the dose-response curves obtained from aortic rings with or without endothelium." | ( Effect of endothelium removal on stimulatory and inhibitory modulation of rat aortic prostacyclin synthesis. Dandona, P; Jeremy, JY, 1989) | 0.28 |
" It is concluded that once-daily dosing with either amlodipine or atenolol significantly reduces blood pressures." | ( Multicenter placebo-controlled comparison of amlodipine and atenolol in mild to moderate hypertension. Cocco, G; de Bruijn, B; Tyler, HM, 1988) | 0.27 |
" After intravenous administration, the percentages of the dosed radioactivity recovered in urine were 62% in humans, 45% in dogs, 38% in rats, and 25% in mice." | ( The metabolism and pharmacokinetics of amlodipine in humans and animals. Beresford, AP; Humphrey, MJ; Macrae, PV; Stopher, DA, 1988) | 0.27 |
" These results suggest that once-daily administration of amlodipine is suitable for all degrees of renal function and that dosage adjustment is not necessary in renal impairment." | ( Pharmacokinetics of amlodipine in renal impairment. Carmody, M; Donohoe, JF; Doyle, GD; Greb, H; Kelly, JG; Laher, MS; Volz, M, 1988) | 0.27 |
" Ambulatory blood pressure recordings revealed adequate blood pressure control throughout the 24-h dosing interval." | ( A double-blind evaluation of the effect of amlodipine on ambulatory blood pressure in hypertensive patients. Allenby, KS; Burris, JF; Mroczek, WJ, 1988) | 0.27 |
" In contrast, isoproterenol shifted the entire dose-response curve for nifedipine to the right." | ( Interaction between isoproterenol and dihydropyridines in heart cells. Briand, V; Laurent, S; Schmitt, H, 1989) | 0.51 |
" The dog was given only the alcohol solvent portion of the nifedipine solution at a dosage and rate equivalent to that of the first day of the experiment." | ( Does nifedipine enhance the cardiovascular depressive effects of bupivacaine? Candler, EM; Frolicher, DA; Howie, MB; McSweeney, TD; Mortimer, W, ) | 0.89 |
" However, 2 h after dosing there was a significant prolongation during stress testing in the time to onset of both 1 mm ST depression on the ECG (by 28%) and to angina (by 37%) compared with atenolol alone, but no benefit was apparent by 12 h after dosing." | ( Slow release nifedipine plus atenolol in chronic stable angina pectoris. Challenor, VF; George, CF; Renwick, AG; Waller, DG, 1989) | 0.65 |
"The antihypertensive efficacy and suitability for once daily dosing of amlodipine, a new calcium antagonist, was studied in a series of 205 patients with mild to moderate hypertension." | ( A dose-response study of amlodipine in mild to moderate hypertension. Frick, MH; McGibney, D; Tyler, HM, 1989) | 0.28 |
" These results suggest that once daily administration of amlodipine is suitable for all degrees of renal function and that dosage adjustment is not necessary in renal impairment." | ( Pharmacokinetics of amlodipine in renal impairment. Carmody, M; Donohue, J; Doyle, GD; Greb, H; Laher, M; Volz, M, 1989) | 0.28 |
" With chronic oral dosing of amlodipine once daily for 14 days, support was provided for the linearity of amlodipine's pharmacokinetics and absence of such with chronic oral dosing with verapamil, diltiazem, and nifedipine." | ( The pharmacokinetic profile of amlodipine. Abernethy, DR, 1989) | 0.46 |
"We examined renal responses to a pharmacological dosage of human atrial natriuretic peptide (hANP) and the potential interference of nifedipine administration with the effects of hANP on kidney function in healthy subjects and normoglycemic patients with type 1 diabetes mellitus." | ( Effects of nifedipine on renal responses to human atrial natriuretic peptide in healthy subjects and normoglycemic patients with type 1 diabetes mellitus. Hofmann, E; Jungmann, E; Scheuermann, EH; Schöffling, K; Seel, K, 1989) | 0.87 |
" Benextramine (3, 6 and 12 mg/Kg) displaced the dose-response curve to methoxamine to the right." | ( Benextramine and nifedipine distinguish between sub-classes of alpha 1-adrenoceptors. Tabrizchi, R; Triggle, CR, 1989) | 0.62 |
" Thus, there is evidence that application of concentration-effect analysis is useful in predicting the steady-state antihypertensive effect from the first dose-response to the drug." | ( Prediction of response to antihypertensive therapy with enalapril and nifedipine. Donnelly, R; Elliott, HL; Meredith, PA; Reid, JL, 1989) | 0.51 |
" At clinically high dosage levels, the incidence of peripheral edema was comparable for both nifedipine and diltiazem, although low-dose nifedipine resulted in a significantly greater incidence of edema compared with low-dose diltiazem." | ( High-dose monotherapy and combination therapy with calcium channel blockers for angina. A comprehensive review of the literature. Temkin, LP, 1989) | 0.5 |
" Dosage modifications are unnecessary in renal impairment, but the dosage regimen for patients with hepatic impairment is not yet established." | ( The safety of amlodipine. Osterloh, I, 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 |
"When the dose-response curve of adrenocorticotropin (ACTH)-induced aldosterone secretion is compared to that of ACTH-induced intracellular cAMP, the ED50 for intracellular cAMP is more than 10 times as high as that for aldosterone production." | ( Role of calcium and cAMP in the action of adrenocorticotropin on aldosterone secretion. Kojima, I; Kojima, K; Rasmussen, H, 1985) | 0.27 |
" NE- and KCI-induced dose-response relationships were differentially depressed by SG-75 (NE much greater than KCI) and NIF (KCI much greater than NE)." | ( Effects of 2-nicotinamidoethyl nitrate on agonist-sensitive Ca++ release and Ca++ entry in rabbit aorta. Hester, RK, 1985) | 0.27 |
"Nifedipine, in a slow release preparation, was given at a mean daily dosage of 47 +/- 4 mg to 12 patients with severe hypertension in whom arterial pressure was not satisfactorily controlled (mean arterial pressure 132 +/- 4 4 mm Hg) by the combination of a converting enzyme inhibitor and a diuretic." | ( Effect of chronic nifedipine in patients inadequately controlled by a converting enzyme inhibitor and a diuretic. Mimran, A; Ribstein, J, 1985) | 2.05 |
" 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, ) | 0.39 |
"7 min) during three dosing periods: 15 min, 2 h, and 4 h postocclusion." | ( Effects of nisoldipine, a new calcium antagonist, on myocardial infarct size and cardiac dynamics following acute myocardial infarction. Deth, R; Kloner, RA; Tumas, J, ) | 0.13 |
"Chronic dosing studies in normal volunteers have shown that both nifedipine and diltiazem exert a small effect on serum theophylline concentrations, which tend to be higher during concurrent nifedipine therapy." | ( The influence of nifedipine and diltiazem on serum theophylline concentration-time profiles. Haffner, CA; Kendall, MJ; Smith, SR, 1989) | 0.85 |
" The needle and syringe methods were the most reproducible and efficient procedures for obtaining a desired milligram dosage of nifedipine from the capsules." | ( Evaluation of five procedures for measuring nonstandard doses of nifedipine liquid. Johnson, CE; Rosen, WJ, 1989) | 0.72 |
" Both placebo and nifedipine dosed during the continued water deprivation and stabilized urinary osmolarity condition caused an increase in the urinary excretions of solutes." | ( Effect of nifedipine on urinary concentrating ability: a placebo controlled study. Iizuka, T; Ishizaki, T; Okaniwa, T; Yasuda, K, 1989) | 1.01 |
" The method was applied to plasma samples obtained from a human subject who had been dosed with a 10-mg nifedipine capsule every 8 h for eight doses." | ( Gas chromatographic-mass spectrometric analysis of plasma nifedipine. Jarvi, EJ; Meyer, MC; Patrick, KS; Straughn, AB, 1989) | 0.74 |
" dosing with 1 mg/kg of the 14C-labelled compound." | ( Sex differences in the metabolism and excretion of nilvadipine, a new dihydropyridine calcium antagonist, in rats. Noguchi, H; Sekiguchi, M; Terashita, S; Tokuma, Y, 1989) | 0.28 |
" Thus, nifedipine GITS represents a sound pharmacologic approach to the management of ischemic disease; and with once-daily dosing and a favorable side-effect profile this agent affords the potential for better patient compliance and efficacy without concern about the development of tolerance." | ( Once-daily therapy for angina pectoris with nifedipine gastrointestinal therapeutic system. Dosing and clinical efficacy. Vetrovec, GW, 1989) | 0.99 |
" A study drug dosage was titrated in each patient and maintained throughout the trial." | ( Therapy of chronic idiopathic urticaria with nifedipine: demonstration of beneficial effect in a double-blinded, placebo-controlled, crossover trial. Bressler, RB; Huston, DP; Sowell, K, 1989) | 0.54 |
" Treatment was titrated to produce at least a 30% increase in treadmill exercise duration over placebo baseline and then maintained at that dosage for an additional 3 weeks." | ( Comparison of atenolol and nifedipine in chronic stable angina pectoris. Kostis, JB; Narahara, KA; Shapiro, W; Thandroyen, F; Zohman, LR, 1989) | 0.57 |
" Nifedipine (100 nM) inhibited the vasoconstriction and shifted the dose-response curve to the right." | ( Effect of endothelin as a coronary vasoconstrictor in the Langendorff-perfused rat heart. Fukuda, K; Handa, S; Hori, S; Kusuhara, M; Kyotani, S; Nakamura, Y; Oono, H; Satoh, T; Yamaguchi, K, 1989) | 1.19 |
" 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) | 0.48 |
"For effective treatment of coronary heart disease with calcium antagonists, knowledge of both the dose-response relationship of a remedy and equipotent dosage for comparison of different drugs is necessary." | ( [Dose-response relation of gallopamil in comparison with nifedipine, diltiazem and tiapamil in patients with coronary heart disease]. Fleischer, K; Forster, A; Hopf, R; Kaltenbach, M; Mohler, C; Schulz, PC, 1989) | 0.52 |
" 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) | 0.5 |
" The results show that an adequate characterization of the distribution phase is required if one pretends to use pharmacokinetic data for dosage regimen design." | ( Pharmacokinetics of oral nifedipine: relevance of the distribution phase. Castañeda-Hernández, G; Chávez, F; Herrera, JE; Hong, E; Hoyo-Vadillo, C; Moreno-Ramos, A; Salazar, LA; Tena, I; Vidal-Gárate, J, 1989) | 0.58 |
" The pharmacokinetics of ethanol were also examined in the animal preparation in order to design a suitable ethanol dosing protocol for the interaction study." | ( Characterization of the pharmacokinetic interaction between nifedipine and ethanol in the rat. Boje, KM; Fung, HL, 1989) | 0.52 |
" These preliminary data suggest that in patients with severe hypertension, effective long-term control of BP with a once-a-day dosage of nifedipine in the GITS formulation may be achieved without adverse hemodynamic effects." | ( Cardiac and hemodynamic adjustments to rapid and sustained blood pressure reduction. Ardeljan, M; Eison, HB; Goldman, ME; Krakoff, LR; Phillips, RA, 1989) | 0.48 |
" The necessity of cautious introduction of vasodilating drugs in pulmonary hypertension and of gradual dosage increase is stressed." | ( Paradoxical elevation of pulmonary vascular resistance after nifedipine in primary pulmonary hypertension. A case study. Grad, A; Horvat, M; Mozina, M; Pohar, B; Rakovec, P, 1989) | 0.52 |
" Pharmacokinetics of nisoldipine was assessed and liver blood flow (ICG clearance) was measured before dosing and at the end of the infusion or during absorption." | ( Variability in the pharmacokinetics of nisoldipine as caused by differences in liver blood flow response. Blauw, GJ; Breimer, DD; Danhof, M; Ooms, P; van Brummelen, P; van Harten, J, 1989) | 0.28 |
" Treadmill exercise testing was performed, 24-hour ambulatory electrocardiograms were recorded, and serum propranolol levels were assessed at 1 and 2 hours after dosing with propranolol alone, and after 2 weeks of combined therapy with either nifedipine, 10 or 20 mg, or diltiazem, 60 or 120 mg, administered every 8 hours." | ( Comparative study of the effect of nifedipine versus diltiazem on exercise performance, serum propranolol levels, and ST-segment abnormalities in patients with chronic stable angina taking propranolol. Krikler, DM; Krikler, S; Robinson, K, 1989) | 0.74 |
" 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) | 0.28 |
" In the presence of Ang II, the NE dose-response curve shifted to the left twofold and the maximal response was not changed." | ( Angiotensin II amplification of alpha-adrenergic vasoconstriction: role of receptor reserve. Purdy, RE; Weber, MA, 1988) | 0.27 |
"The effect of nifedipine on pressor dose-response curves to phenylephrine, alpha-methylnoradrenaline and angiotensin II was determined in anaesthetized cats pretreated with propranolol and atropine." | ( Lack of differential inhibition by nifedipine of pressor responses induced by alpha 1- and alpha 2-adrenoceptor agonists and by angiotensin II in anaesthetized cats. Alabaster, VA; Solca, AM, 1985) | 0.91 |
" During long term treatment, blood pressure was significantly decreased after felodipine during the dosing interval (12h), irrespective of concomitant treatment." | ( Antihypertensive effects of felodipine compared with placebo. Elmfeldt, D; Hedner, T, 1985) | 0.27 |
" Further increase in the dosage resulted in 63% of the captopril- and 81% of the nifedipine-treated patients achieving target blood pressure." | ( Comparison of nifedipine and captopril as third-line agents in hypertensive patients uncontrolled with beta-blocker and diuretic therapy. Beevers, DG; Potter, JF, ) | 0.72 |
" Exercise testing 24 hours after dosing showed significant improvement in time to angina and total exercise time for patients receiving 60-mg and 90-mg doses but not for the 30-mg or placebo categories." | ( Efficacy of nifedipine gastrointestinal therapeutic system in combination with beta blockers in the management of exertional angina. A multicenter study of 54 patients. Bittar, N; Corder, CN; Eich, R; McGrew, FA; Paulk, EA; Zellner, S, 1987) | 0.65 |
" It was possible to pursue the same nifedipine daily dosage for 2 months in 10 patients, who were re-evaluated after 8 wk of treatment and after nifedipine withdrawal the following week." | ( Nifedipine reduces pulmonary pressure and vascular tone during short- but not long-term treatment of pulmonary hypertension in patients with chronic obstructive pulmonary disease. Agostoni, P; Doria, E; Galli, C; Guazzi, MD; Tamborini, G, 1989) | 1.99 |
" Thus, maximum tolerated doses of diltiazem or nifedipine do not impair the metabolism of theophylline to a clinically relevant degree and adjustment of theophylline dosage is not required after the addition or discontinuation of diltiazem or nifedipine." | ( Clinical relevance of the interaction of theophylline with diltiazem or nifedipine. Christopher, MA; Harman, E; Hendeles, L, 1989) | 0.77 |
" Nine patients were treated for 42 days at a fixed dosage of 1 tablet/day." | ( [Nitrendipine, a new calcium antagonist, in the therapy of arterial hypertension]. Aimi, M; Bianco, C; Conti, G; Corbacelli, C; Cosmi, F; Mollaioli, M; Ricca, M, 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) | 0.27 |
" At the end of the dosing interval, supine and standing blood pressures were lowered 6/4 and 6/3 mm Hg respectively with the former regimen, and 2/3 mm Hg with the latter." | ( Once- and twice-daily nitrendipine in patients with hypertension and noninsulin-dependent diabetes. Conrad, KA; Crook, J; Fagan, TC; Lasseter, KC; Morledge, J; Nelson, EB, ) | 0.13 |
" Dose-response comparisons against nifedipine in 21 patients and against isosorbide dinitrate in 14 patients demonstrate that PN 200-110 has a similar antianginal efficacy profile to both drugs." | ( Efficacy of a new calcium antagonist PN 200-110 (isradipine) in angina pectoris. Allen, J; Jackson, NC; Pool, PE; Taylor, SH, 1987) | 0.55 |
" Dose-response curves were obtained with 4 doses of each drug in 6 animals." | ( Comparison of cardiodepressant and vasodilator effects of PN 200-110 (isradipine), nifedipine and diltiazem in anesthetized rabbits. Hof, RP, 1987) | 0.5 |
"The haemodynamic dose-response effects of a new long-acting slow-calcium channel blocking agent, amlodipine were evaluated in 20 patients with angiographically confirmed coronary heart disease." | ( A haemodynamic dose finding study with a new slow-calcium channel blocker (amlodipine) in coronary artery disease. Frais, MA; Jackson, NC; Reynolds, G; Sharma, SK; Silke, B; Taylor, SH; Verma, SP, 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 |
" Renal elimination was the major route of excretion with about 60% of the dosed radioactivity recovered in urine." | ( Metabolism and kinetics of amlodipine in man. Beresford, AP; Humphrey, MJ; Macrae, PV; McGibney, D; Stopher, DA, 1988) | 0.27 |
" The unchanged drug was neither detected in the urine nor in the bile, but nisoldipine was present in plasma of the rat 30 min after dosing and up to 24 h in man." | ( Pharmacokinetics of nisoldipine. III. Biotransformation of nisoldipine in rat, dog, monkey, and man. Ahr, G; Ahr, HJ; Karl, W; Scherling, D; Wehinger, E, 1988) | 0.27 |
"3 mg/kg) in presence of prazosin shifted the norepinephrine pressor dose-response curves to the right whereas it was ineffective in yohimbine-pretreated animals." | ( Calcium entry blockade by nitrendipine and alpha adrenergic responsiveness in vivo: comparison with noncalcium entry blocker vasodilators in absence and presence of phenoxybenzamine pretreatment. Pedrinelli, R; Tarazi, RC, 1985) | 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) | 0.27 |
" Mastoparan, a known facilitator of phospholipase A2 enzymatic activity, shifted the bee venom phospholipase A2 dose-response curve to the left." | ( Inhibition of [3H]nitrendipine binding by phospholipase A2. Goldman, ME; Pisano, JJ, 1985) | 0.27 |
"Nifedipine, in a slow release preparation, was given at a mean daily dosage of 47 +/- 4 mg to 12 patients with severe hypertension in whom arterial pressure was not satisfactorily controlled (mean blood pressure, 172 +/- 6/111 +/- 4 mmHg) by the association of a converting enzyme inhibitor and a diuretic." | ( Effect of nifedipine in hypertension not controlled by converting enzyme inhibitor and diuretic. Mimran, A; Ribstein, J, 1986) | 2.12 |
"Combinations of antianginal drugs may be used for an additive effect against angina, but also to off-set unwanted effects of one drug with another, either by direct effects or by a reduction of dosage of each drug." | ( Interactions of vasodilators with calcium entry- and beta-blockers in patients with coronary heart disease. Adam, WE; Haerer, W; Henze, E; Hermann, T; Kohler, J; Kress, P; Stauch, M, 1986) | 0.27 |
" The dose-response curve for neonatal islets was steeper than for adult islets and the maximal response was clearly shifted towards lower glucose concentrations." | ( Effects of glucose on insulin release and 86Rb permeability in cultured neonatal and adult rat islets. Atwater, I; Boschero, AC; Tombaccini, D, 1988) | 0.27 |
" A reduction in prescribed dosage was required in 37% of nifedipine-treated compared with 6% of diltiazem-treated patients." | ( A randomized double-blind comparison of diltiazem and nifedipine in stable angina. Dempsey, EE; Grace, M; Klinke, WP; Kvill, L, 1988) | 0.77 |
" Nifedipine pharmacokinetics after a single oral dose and sustained dosing (three times daily for five days) were not significantly different." | ( Haemodynamic effects of combined oral nifedipine and sublingual nitroglycerin in patients with chronic stable angina. Boje, KM; Fung, HL; Parker, JO; Yoshitomi, K, 1987) | 1.45 |
" Ninety-one patients (93 percent), 80 men and 11 women, mean age 62 +/- 1 years, completed the trial, which included two weeks receiving standard nifedipine followed by 12 weeks receiving nifedipine GITS starting at a dosage equal to the 24-hour total dose of nifedipine capsules and titrated upward as necessary." | ( Nifedipine gastrointestinal therapeutic system in stable angina pectoris. Results of a multicenter open-label crossover comparison with standard nifedipine. Cole, S; Parker, VE; Procacci, PM; Tabatznik, B; Terry, R; Vetrovec, GW, 1987) | 1.92 |
" After a 2-week placebo run-in period, each patient was randomized to either nicardipine or nifedipine; each drug was titrated up to either blood pressure normalization, appearance of adverse effects, or maximal dosage (40 mg, three times a day with nicardipine and 30 mg, three times a day with nifedipine) and then administered for 4 weeks." | ( A randomized double-blind crossover study of nicardipine and nifedipine in patients with angina pectoris and concomitant essential hypertension. Bonandi, L; Dei Cas, L; Feroldi, P; Metra, M; Nodari, S; Nordio, G; Raddino, R; Visioli, O, 1988) | 0.74 |
" At a higher dosage there is an increase of the arterial flow, eliciting a reflex sympathetic stimulation with heart rate increase and venoconstriction." | ( Peripheral vascular effects of calcium entry blockers in normal volunteers. Clement, DL; Colardyn, F; Everaert, J, ) | 0.13 |
" It shifted the dose-response curve of vasopressin to the right in a noncompetitive manner." | ( Effect of nisoldipine on large coronary arteries in situ: inhibition of vasoconstriction induced by vasopressin. Bing, RJ; Saeed, M; Saito, T, 1988) | 0.27 |
" The radioactivity in the tissues at 1 h after last dosing was compared with that at 1 h after single administration." | ( Absorption, distribution and excretion of 14C-benidipine hydrochloride after repeated administration to rats. Inoue, A; Kobayashi, H; Kobayashi, S; Nakamizo, N; Nishiie, H; Ohishi, T; Oka, T, 1988) | 0.27 |
" After nifedipine, both the mSBP and the mDBP decreased, with onset of effect five minutes after dosage and maximum decrease at 60 min (mSBP 134." | ( Treatment of hypertensive crisis in children with nifedipine. Albajara, L; Cagigas, P; Garcia, S; Lopez-Herce, J; Ruza, F, 1988) | 0.98 |
" In higher Ca2+ solution, dose-response curves for MPC-2101 on dV/dt of slow action potentials were shifted to the right." | ( Effects of a newly synthetized calcium antagonist, cyclopropylmethyl 4-(3-nitrophenyl) 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate (MPC-2101), on action potentials of rabbit's myocardial tissues in vitro. Kano, T; Nakamura, S; Nishi, K, ) | 0.13 |
" This shows that the dosage form may be formulated as a drug-polymer system which exhibits constant release at a desired rate." | ( The kinetics of nifedipine release from porous hydrophilic matrices and the pharmacokinetics in man. Leucuta, SE, 1988) | 0.62 |
" 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) | 0.48 |
" 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 |
" In one of the groups a dose-response curve to nifedipine was obtained." | ( [Comparative cardiovascular effects of nifedipine in anesthetized dogs]. Cingolani, HE; Gelpi, RJ; Mosca, SM, 1987) | 0.8 |
" It is concluded that an antihypertensive dosage of nifedipine administered to animals with atherosclerosis does not suppress subsequent atherogenesis." | ( Hypertension and atherosclerosis in cholesterol-fed rabbits. II. One-kidney, one clip Goldblatt hypertension treated with nifedipine. Overturf, M; Schaper, J; Sybers, H; Taegtmeyer, H, 1987) | 0.73 |
" Once or twice daily dosage possible with nitrendipine and nisoldipine offers a convenient administration schedule, which encourages patient compliance in long-term therapy of hypertension." | ( Differential effects of 1,4-dihydropyridine calcium channel blockers: therapeutic implications. Katz, AM; Leach, NM, 1987) | 0.27 |
" dosing (0." | ( Pharmacokinetics of nilvadipine, a new dihydropyridine calcium antagonist, in mice, rats, rabbits and dogs. Niwa, T; Noguchi, H; Sekiguchi, M; Tokuma, Y, 1988) | 0.27 |
"To assess the dosing equivalency and the early and late antianginal efficacy of a gastrointestinal therapeutic system for once-daily, continuous-release nifedipine (N-GITS), 10 patients with stable angina pectoris, who were previously receiving chronic treatment with nifedipine, completed a 12-week trial comparing N-GITS with standard nifedipine." | ( Comparative dosing and efficacy of continuous-release nifedipine versus standard nifedipine for angina pectoris: clinical response, exercise performance, and plasma nifedipine levels. Alpert, DA; Parker, VE; Vetrovec, GW, 1988) | 0.72 |
" Healthy young and elderly volunteers received 20 mg nifedipine (slow release) orally for 2 weeks with concomitant dosing of atenolol 50 mg orally during the second week." | ( The effect of ageing on the disposition of nifedipine and atenolol. Adam, HK; Castleden, CM; Fitzsimons, TJ; Scott, M; Smith, RP, 1988) | 0.79 |
" The linear distribution and disposition of nifedipine was found within the dosing range tested (0." | ( Moment analysis of intravenous, intraduodenal, buccal, rectal and percutaneous nifedipine in rats. Kondo, S; Sugimoto, I, 1987) | 0.76 |
", after dosing with 14C-nilvadipine." | ( Metabolism of nilvadipine, a new dihydropyridine calcium antagonist, in rats and dogs. Fujiwara, T; Noguchi, H; Okumura, K; Shiokawa, Y; Terashita, S; Tokuma, Y, 1987) | 0.27 |
" Indomethacin (5 microM) shifted the dose-response curve to norepinephrine to the right in arteries from all groups of animals." | ( Effect of diabetes on vascular smooth muscle function in normotensive and spontaneously hypertensive rat mesenteric artery. Agrawal, DK; McNeill, JH, 1987) | 0.27 |
" In contrast, no appreciable increases in the percutaneous absorption of nifedipine from PG or IPM above controls were observed for pretreatment of the dosing site with acetone." | ( Enhancement of transdermal delivery by superfluous thermodynamic potential. III. Percutaneous absorption of nifedipine in rats. Kondo, S; Sugimoto, I; Yamanaka, C, 1987) | 0.72 |
" Pharmacokinetic studies on the gastrointestinal therapeutic system (GITS) show that the bioavailability of the GITS dosage form (relative to the capsule) is about 65 percent after a single dose, but increases to about 86 percent at steady-state because of residual absorption more than 24 hours after dosing." | ( Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. A controlled-release formulation of nifedipine. Chung, M; Gaffney, M; Reitberg, DP; Singleton, W, 1987) | 0.56 |
"Convenient once-a-day dosage regimens are highly desirable in general, and especially for the treatment of asymptomatic diseases such as essential hypertension." | ( Nifedipine gastrointestinal therapeutic system. Barclay, BL; Swanson, DR; Theeuwes, F; Wong, PS, 1987) | 1.72 |
" In three patients not achieving the diastolic BP goal during combination therapy with dosing every 8 hours, automatic 24-hour ambulatory BP monitoring demonstrated lack of antihypertensive control for only the last 2 to 3 hours of the dosing interval." | ( Effects of combination therapy with captopril and nifedipine in severe or resistant hypertension. Lane, TJ; Podesla, S; Viadero, JJ; White, WB, 1986) | 0.52 |
" 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) | 0.27 |
" It is also possible that the plasma level-effect correlations for the drug may differ with single and sustained dosing regimens." | ( Aspects of the clinical pharmacology of nifedipine, a dihydropyridine calcium-entry antagonist. Hamann, SR; McAllister, RG; Piascik, MT, ) | 0.4 |
" On separate days cumulative dose-response curves to methacholine were constructed, basal and 20 min after nifedipine administration; on both occasions basal FEV1 varied less than 5%." | ( Nifedipine decreases sensitivity and reactivity to methacholine in mild asthmatics. Marco, V; Pellicer, C; Perpiñá, M, 1987) | 1.93 |
" The dosage of active medication was guided by a "third party observer" to avoid iatrogenic hypotension." | ( Enhancement of metabolism of jeopardized myocardium by nifedipine. Biello, DR; Geltman, EM; Jaffe, AS; Sobel, BE, 1987) | 0.52 |
" Cimetidine produced a significant increase in the AUC of both single and steady state dosing of nifedipine." | ( Ranitidine and cimetidine; drug interactions with single dose and steady-state nifedipine administration. Beerahee, A; Jack, DB; Kendall, MJ; Lobo, J; Smith, SR; Wilkins, MR, 1987) | 0.72 |
" The simulation proved to be an efficient tool to substitute in vivo multiple dosing studies for assessment of bioavailability." | ( The bioavailability of oral nifedipine formulations: a statistical and simulation approach. Janezic, A; Karba, R; Kozjek, F; Mrhar, A; Primozic, S; Raemsch, KD, ) | 0.43 |
" All patients then received treatment for a further 6 weeks with a combination of the two drugs in the same dosage as before." | ( Effect of nifedipine and mefruside on renal function and platelet function in hypertensive patients. Anderton, JL; Burnet, ME; Fiskerstrand, CE; Notghi, A, 1987) | 0.68 |
" Additionally the pharmacokinetic profiles of the enantiomers in the plasma up to 12 h after dosing were examined in three subjects." | ( Plasma levels of (+)- and (-)-nilvadipine after oral dosing with racemic (+)-nilvadipine in man. Fujiwara, T; Noguchi, H; Tokuma, Y, 1987) | 0.27 |
" Both nisoldipine and the diuretic had a flat dose-response curve." | ( Monotherapy with the calcium channel antagonist nisoldipine for systemic hypertension and comparison with diuretic drugs. Daniels, AR; Opie, LH, 1987) | 0.27 |
" It is concluded that the new formulation can be successfully applied to the treatment of hypertensive and/or coronary diseases with a considerable simplification of the dosing schedule and an improved patient compliance." | ( Clinical efficacy and bioavailability of a sustained release nifedipine formulation. Piovella, C, 1987) | 0.51 |
" The pharmacokinetics of nilvadipine were generally linear over the dosage range studied." | ( Pharmacokinetics of nilvadipine in healthy volunteers. Noguchi, H; Shishido, A; Terakawa, M; Tokuma, Y, 1987) | 0.27 |
" infusion of lysine theophylline, equivalent to 197 mg anhydrous theophylline, both before (day 1) and during (day 5) steady state chronic oral dosing with slow release nifedipine 20 mg 12 hourly." | ( The interaction between i.v. theophylline and chronic oral dosing with slow release nifedipine in volunteers. Debbas, NM; Jackson, SH; Johnston, A; Peverel-Cooper, CA; Shah, K; Turner, P, 1986) | 0.69 |
" The absence of reflex tachycardia found in previous chronic oral dosing studies with this drug appears to take some days to develop in humans." | ( PY 108-068--acute effects of a single oral dose in chronic stable angina. de Buitleir, M; Krikler, DM; Krikler, S, 1986) | 0.27 |
" Urinary excretion was the favoured route comprising about 60% of the dosed radioactivity." | ( The metabolism of nicardipine hydrochloride in healthy male volunteers. Alexander, O; Cairncross, L; Dow, RJ; Graham, DJ; Hall, DJ; Rush, WR, 1986) | 0.27 |
" 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 |
" Plasma concentrations of nifedipine, measured 12 hr after the dosing of the retard tablet during chronic treatment, were not different from those after the acute administration of the retard tablet, suggesting that no accumulation of nifedipine occurs." | ( Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients. Abe, K; Imai, Y; Nihei, M; Sasaki, S; Sekino, H; Yoshinaga, K, 1986) | 0.8 |
"The sensitivity of the uterus to the inhibition of contractions by salbutamol, diltiazem or nifedipine was assessed in the ovariectomized, post-partum rat by dose-response curves following bolus intravenous (i." | ( The effects of long-term infusion of salbutamol, diltiazem and nifedipine on uterine contractions in the ovariectomized, post-partum rat. Abel, MH; Hollingsworth, M, 1986) | 0.73 |
"05) was decreased for the entire dosing interval after nifedipine dosing." | ( Pharmacokinetics and pharmacodynamics of nifedipine in patients at steady state. Carliner, N; Fisher, M; Gutierrez, LM; Lesko, LJ; Whipps, R, ) | 0.64 |
" Using this device, we were able to obtain the direct-writing dose-response curve of respiratory resistance measured during quiet breathing." | ( Effect of nifedipine on dose-response curves to acetylcholine and histamine measured during quiet breathing. Arai, M; Fueki, R; Kobayashi, S; Kuroiwa, H; Tomioka, S, 1986) | 0.67 |
" The small time lag in absorption that may be attributed to the dissolution of the nifedipine capsule may be obviated by biting through the capsule and swallowing the contents; this bite-and-swallow approach to dosing provides the most rapid rise in plasma nifedipine concentrations, and produces peak levels well above those achieved with sublingual administration." | ( Kinetics and dynamics of nifedipine after oral and sublingual doses. McAllister, RG, 1986) | 0.8 |
"The serum concentrations and urinary excretion of nifedipine and 3 of its metabolites have been compared in two groups of hypertensive patients, one receiving prolonged (1-2 years) nifedipine monotherapy, the second receiving the same dosage of nifedipine in conjunction with a variety of other antihypertensive and cardioactive drugs." | ( The metabolism of nifedipine during long-term therapy. Fernandez, PG; Nath, C; Snedden, W, 1986) | 0.86 |
" 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 |
" In this study, placebo and nifedipine in 10-, 20-, 30-, and 40-mg doses were administered sublingually to ten normal subjects with at least three days between dosing periods." | ( Correlation of plasma levels of nifedipine and cardiovascular effects after sublingual dosing in normal subjects. Hongo, M; McAllister, RG; McCallum, RW; Traube, M, 1985) | 0.85 |
"The dose-response effects of oral nicardipine on the systemic blood pressure were examined in 54 patients with uncomplicated essential hypertension (DBP greater than or equal to 100 mm Hg)." | ( Anti-hypertensive dose-response effects of nicardipine in stable essential hypertension. Frais, MA; Jackson, N; Lee, P; Silke, B; Taylor, SH; Verma, SP, 1985) | 0.27 |
" In the first study, the effect of acute dosing (via an intravenous infusion of 5 mg h-1 for 3 h) on the glucose, insulin, hormonal, and intermediary metabolite responses to an intravenous glucose tolerance test was determined in six healthy male volunteers." | ( The effect of nicardipine on glucose and drug-stimulated insulin secretion in normal volunteers. Baty, J; Dow, RJ; Isles, TE, 1985) | 0.27 |
" These results suggest that nifedipine, when given in standard dosage for 3 months, has minor effects on carbohydrate metabolism in non-insulin dependent diabetic patients." | ( [Effects of nifedipine on carbohydrate metabolism in the non-insulin dependent diabetic]. Abadie, E; Fiet, J; Gauville, C; Passa, P; Tabuteau, F; Villette, JM, 1985) | 0.94 |
" 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) | 0.8 |
" Side effects were noted in 5 patients taking nifedipine, leading to a decrease in the dosage to 30 mg per day in 3, and in one patient taking placebo." | ( Nifedipine in chronic bronchial asthma: a randomized double-blind crossover trial against placebo. Boismare, F; Lemercier, JP; Leprevost, A; Moore, ND; Ozenne, G; Pasquis, P; Tardif, C, 1985) | 1.97 |
" The average daily dosage of nicardipine for optimal angina relief was 89 mg (range 40 to 160)." | ( Nicardipine for angina pectoris at rest and coronary arterial spasm. Feldman, RL; Gelman, JS; Pepine, CJ; Scott, E, 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) | 0.51 |
" The pancreatic vascular resistances declined significantly for the 3 doses, but no dose-response could be registered." | ( [Calcium antagonists and glycoregulation: dissociated effects of nicardipine on vascular tonus and insulin secretion]. Gauville, C; Marre, M; Passa, P, 1985) | 0.27 |
" Plasma concentrations of nifedipine were measured by capillary gas-liquid chromatography up to 24 h after single dosing as well as up to 48 h after multiple doses of the drugs (steady state)." | ( Pharmacokinetics and bioavailability of three different galenic nifedipine preparations. Dahmen, W; Jaeger, H; Lutz, D; Molz, KH; Pabst, G, 1986) | 0.81 |
"To determine whether nifedipine or diltiazem affect digoxin kinetics, glycoside plasma concentrations and renal excretion were measured before and during dosing in 23 patients with cardiac insufficiency achieving steady-state conditions." | ( Effects of nifedipine and diltiazem on plasma levels and renal excretion of beta-acetyldigoxin. Kuhlmann, J, 1985) | 0.98 |
" 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) | 0.54 |
" Enzyme leakage was appreciated by creatine-kinase (CK) dosage in the effluent from each compartment." | ( [Effects of nicardipine on electrophysiologic alterations and enzyme leakage induced in vitro in the guinea pig]. Adamantidis, MM; Aniq-Filali, O; Dupuis, BA; Duriez, PR; Rouet, RH, ) | 0.13 |
" At the maximum dosage used, nisoldipine injection caused a decrease of the regional washout rate of Xenon-133 of 63 +/- 8% (SEM) in the Walker carcinoma and an increase of 80 +/- 41% in the muscle of the hind leg." | ( Selective drug-induced reduction of blood flow in tumor transplants. Altmann, A; Debatin, J; Helus, F; Knapp, WH; Layer, K; Ostertag, H; Sinn, HJ, 1985) | 0.27 |
" Nicardipine at 10(-7) mol/l shifted to the right the dose-response curve for Ca of the phasic contraction evoked by electrical stimulation with an alternating current, and at higher concentration it reduced the maximum tension and slope of the dose-response curve." | ( Calcium antagonistic properties of nicardipine, a dihydropyridine derivative assessed in isolated cerebral arteries and cardiac muscle. Ishii, K; Kato, H; Kurihara, J; Miyajima, Y; Nakayama, K, 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 |
" Plasma nicardipine concentration, blood pressure, heart rate, and systolic time intervals were measured before dosing and at frequent intervals between 1 and 360 min post dosing." | ( Noninvasive assessment of the haemodynamic effects of nicardipine in normotensive subjects. Campbell, BC; Hillis, WS; Kelman, AW, 1985) | 0.27 |
"To establish dosage recommendations in patients with end-stage renal disease undergoing chronic haemodialysis, nifedipine kinetics were studied between and during haemodialysis sessions." | ( Haemodialysis does not affect the pharmacokinetics of nifedipine. Jacobs, C; Martre, H; Sari, R; Singlas, E; Taburet, AM, 1985) | 0.73 |
" Antihypertensive efficacy was demonstrated after acute dosing and was maintained over 4 weeks of twice daily treatment as monotherapy." | ( The pharmacodynamics and pharmacokinetics of a new calcium antagonist nisoldipine in normotensive and hypertensive subjects. Meredith, PA; Pasanisi, F; Reid, JL, 1985) | 0.27 |
" The method was applied to urine collected from rats (n = 4, 0-24 h) after oral dosing of [14C] felodipine (5 mumol/kg)." | ( Bimodal column switching liquid chromatographic assay of six metabolites of [14C] felodipine in rat urine. Weidolf, L, 1985) | 0.27 |
" In 10 patients resting cardiac stroke output (thermodilution) and pulmonary artery occluded pressure were determined following four intravenous nisoldipine injections (cumulative dosage of 1, 2, 4 and 8 micrograms kg-1)." | ( Haemodynamic dose-response effects of intravenous nisoldipine in coronary artery disease. Frais, MA; Muller, P; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1985) | 0.27 |
" In six anaesthetized sheep, the dose-response curve comparing vascular resistance to nifedipine dose showed greater sensitivity than that reported for either dogs or humans." | ( The effects of nifedipine on the systemic and coronary vascular beds of the sheep: a potential method for induction of ischaemia. Fu, WK; Gangell, P; Kilpatrick, D; Roberts, MS; Yong, AC, ) | 0.71 |
" An extrapolation with the obtained data for the expected steady state plasma levels after a twice-a-day dosing showed that the above mentioned therapeutically relevant plasma levels of the unchanged drug are in general achieved for most of the dosage interval." | ( [Bioavailability of new nifedipine preparations in man. 1. Pharmacokinetics of nifedipine in the form of sustained-release tablets]. Dahmen, W; Jaeger, H; Lutz, D; Molz, KH; Pabst, G, 1985) | 0.58 |
" Only a leftward shift of the dose-response curves was observed, which was most pronounced for (-)-phenylephrine and Sgd 101/75." | ( Interactions between the putative calcium entry promotor Bay k 8644 and pressor responses produced by alpha 1- and alpha 2-adrenoceptor agonists in the pithed normotensive rat. de Jonge, A; Mathy, MJ; Thoolen, MJ; Timmermans, PB; van Heiningen, PN; van Zwieten, PA; Wilffert, B, 1984) | 0.27 |
" Where pA2 values (-log dose antagonist evoking a twofold shift for the agonist dose-response curve) could be calculated, no significantly different pA2 values against either agonist resulted." | ( Calcium influx-dependent and -independent alpha 1-adrenoceptor-mediated processes of vasoconstriction in vivo do not operate via different alpha 1-adrenoceptor subtypes. de Jonge, A; Korstanje, C; Thoolen, MJ; Timmermans, PB; van Zwieten, PA; Wilffert, B, ) | 0.13 |
" Blood pressure variation through one dosing interval increased 42% when hydralazine was given but was not altered by nitrendipine." | ( Efficacy and safety comparison of nitrendipine and hydralazine as antihypertensive monotherapy. Deedwania, PC; Fagan, TC; Mehta, JL; Sternleib, C; Vlachakis, N, 1984) | 0.27 |
" Since 35 to 43% of both the liquid and tablet doses was recovered in the urine of volunteers, excretion of urinary metabolites appears to be independent of the dosage form." | ( Bioequivalence and metabolism of nitrendipine administered orally to healthy volunteers. Burkholder, DE; Kann, J; Krol, GJ; Levitt, MJ; Raemsch, KD, 1984) | 0.27 |
"As a calcium antagonist, nitrendipine will be used in the treatment of various diseases in patients with hepatic insufficiency, and it is important to know if they require modified dosing schedules." | ( Steady-state pharmacokinetics of nitrendipine in hepatic insufficiency. Burkholder, DE; Krol, GJ; Lasseter, KC; Murdoch, AA; Shamblen, EC; Taylor, RJ; Vanov, SK, 1984) | 0.27 |
" The influence of bepridil on the dose-response curves of mesenteric arterial strips for CaCl2, norepinephrine and serotonin differed from the influence seen with nifedipine, another Ca++ blocker." | ( Effects on calmodulin of bepridil, an antianginal agent. Hidaka, H; Ishikawa, T; Itoh, H, 1984) | 0.46 |
" Nifedipine shifted the pressor dose-response curves of all three agonists to the right." | ( Nifedipine and alpha adrenoceptor antagonism. Brown, MJ; Dollery, CT; Heavey, DJ; Murphy, MB; Scriven, AJ, 1984) | 2.62 |
" The dosage and choice of drugs are based on pharmaco-kinetic and dynamic data in animals and man." | ( Clinical pharmacology of beta-adrenoceptor antagonism in angina pectoris: an overview. Oh, VM, 1980) | 0.26 |
"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) | 1.71 |
" 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) | 0.27 |
"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 |
"The dose-response effects of a new slow-calcium-channel blocker, nicardipine, on the resting blood pressure and on the pressor responses induced by skin cold, isometric exertion, and dynamic exercise were examined in a single-blind placebo-controlled study in six male patients with stable uncomplicated essential hypertension." | ( Influence of nicardipine on the blood pressure at rest and on the pressor responses to cold, isometric exertion, and dynamic exercise in hypertensive patients. Ahuja, RC; Okoli, R; Silke, B; Taylor, SH, ) | 0.13 |
" The relationship to dosage and possible mechanisms for this effect are discussed." | ( Nifedipine reduces arrhythmias but does not alter prostanoid release during coronary artery occlusion and reperfusion in anaesthetised greyhounds. Coker, SJ; Parratt, JR, ) | 1.57 |
" All patients were then given a combination of half the initial dosage of both drugs for an additional period of 6 weeks." | ( Controlled trial of nifedipine and bendroflumethiazide in hypertension. Andrén, L; Hallin, L; Hansson, L, ) | 0.45 |
" 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 |
" The dose-response curve for isoprenaline was shifted to the right and downward in the presence of YC-93 in a concentration-dependent manner, and the positive inotropic action of calcium was also inhibited markedly by YC-93." | ( Dissociation of cyclic AMP and contractile responses to isoprenaline: effects of a dihydropyridine derivative, nicardipine (YC-93), on canine ventricular muscle. Endoh, M; Taira, N; Yanagisawa, T, 1980) | 0.26 |
"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 |
" Full PH dose-response curves for standard antihypertensive drugs were explored and were compared to their hypotensive dose-response curves." | ( Antihypertensive drugs: their postural hypotensive effect and their blood pressure lowering activity in conscious normotensive rats. Carver, LA; Lee, CH; Strosberg, AM, 1983) | 0.27 |
" After a second 1-week placebo period, there was a crossover to the alternative dosage (20 or 40 mg respectively), and active therapy was again given for 3 weeks." | ( Pharmacokinetic and pharmacodynamic parameters in patients treated with nitrendipine. Andrén, L; Hansson, L; Orö, L; Ryman, T, ) | 0.13 |
" The acute blood-pressure-lowering effect of nifedipine in the Dahl salt-sensitive rat was characterized by a rapid onset of action, the minimal effective oral dosage (0." | ( Factors involved in the antihypertensive action of calcium antagonists. Garthoff, B; Kazda, S; Knorr, A; Thomas, G, ) | 0.39 |
" The fall in pressure after oral nifedipine was maximal within 1 hr or less and was generally accompanied by palpitation and increase in pulse rate; with a six hourly dosing regimen the tendency of blood pressure to recover after each dose was interrupted by the next dose, so that values remained significantly reduced throughout the 24 hr, although pressure fluctuations were evident." | ( Calcium-channel blockade with nifedipine and angiotensin converting-enzyme inhibition with captopril in the therapy of patients with severe primary hypertension. Bartorelli, A; De Cesare, N; Galli, C; Guazzi, MD; Salvioni, A; Tamborini, G; Tramontana, C, 1984) | 0.84 |
" Adverse reactions may be reduced by the use of long-acting nifedipine, which would permit a reduction in the dosage of captopril and minoxidil." | ( Long acting nifedipine in the treatment of severe hypertension. Bursztyn, M; Grossmann, E; Rosenthal, T, 1984) | 0.89 |
" 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) | 0.66 |
" As revealed by the dose-response curves in SHR both drugs produce similar maximal drops in blood pressure by about 54%." | ( Differential influence of the calcium antagonist nitrendipine and the vasodilator hydralazine on normal and elevated blood pressure. Garthoff, B; Knorr, A, 1984) | 0.27 |
" Thus at the dosage used felodipine was a potent dilator of systemic arterioles but had no direct effect on left ventricular function." | ( Acute haemodynamic effects of felodipine during beta blockade in patients with coronary artery disease. Culling, W; Ruttley, MS; Sheridan, DJ, 1984) | 0.27 |
" 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) | 0.5 |
" 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 |
"We describe two patients in whom spontaneous angina following acute myocardial infarction (postinfarction angina caused by coronary artery spasm) and worsening angina were successfully eliminated after clinical dosage of oral diltiazem, while marked sinus node suppression developed and temporary pacing was performed." | ( Elimination of unstable angina by diltiazem under temporary pacing. Imamura, T; Ishikawa, T; Koiwaya, Y; Tanaka, K, 1984) | 0.27 |
"The haemodynamic dose-response effects of the slow channel blocking agent nicardipine were evaluated in 10 male patients with angiographically confirmed coronary artery disease." | ( Haemodynamic dose-response effects of i.v. nicardipine in coronary artery disease. Hussain, M; Nelson, GI; Silke, B; Taylor, SH; Verma, SP, 1984) | 0.27 |
"The haemodynamic dose-response effects of the slow-calcium channel blocker nicardipine were evaluated in fifteen male patients with uncomplicated acute myocardial infarction." | ( Haemodynamic effects of nicardipine in acute myocardial infarction. Frais, MA; Hafizullah, M; Jackson, NC; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 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) | 0.27 |
" 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) | 0.88 |
" 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 |
"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) | 0.27 |
" This dosage produced a minimal increase in heart rate and reduced the PR interval." | ( The search for a digitalis substitute II milrinone (Win 47203). Its action on the heart-lung preparation of the dog. Farah, A; Kabela, E; Mendez, R; Pastelin, G, 1983) | 0.27 |
" Some calcium antagonists have been shown to alter digoxin kinetics and changes in digoxin dosage have been recommended." | ( The effect of nifedipine on serum digoxin concentrations in patients. Akers, S; Raizner, A; Schwartz, JB, 1984) | 0.63 |
" infusion of either NF at three dosage levels [0." | ( Effects of nifedipine on total cardiac output distribution in conscious rat. Flaim, SF; Kanda, K, 1984) | 0.66 |
" Large interindividual differences have been observed in the effective dosage of the drug." | ( Nifedipine plasma concentration in patients treated for angina pectoris. Levy, M; Stern, Z; Zylber-Katz, E, 1984) | 1.71 |
" 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 |
" 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 |
" When used in standard recommended oral dosage nifedipine has no significant effect on glucose tolerance." | ( Effect of nifedipine on glucose tolerance and insulin secretion in diabetic and non-diabetic patients. Donnelly, T; Harrower, AD, 1980) | 0.92 |
" 4 The synergistic effect was even more pronounced after reduction in propranolol dosage to 50% of the beta-adrenoceptor blocking dose, reflecting the myocardial depressant effects of beta-adrenoceptor blocking drugs in these patients with coronary heart disease, some of whom had poor left ventricular function." | ( The combination of nifedipine and propranolol in the management of patients with angina pectoris. Beattie, JM; Hutton, I; Murray, RG; Tweddel, AC, 1981) | 0.59 |
" The daily dosage of nifedipine during this phase was 10 mg 3 times daily." | ( Effects of treatment with nifedipine and metoprolol in essential hypertension. Eggertsen, R; Hansson, L, 1982) | 0.88 |
" A clinical trial of nifedipine on patients with achalasia was carried out taking nifedipine sublingually in a daily dosage of 30 to 60 mg before meal." | ( [Clinical effect of nifedipine in patients with achalasia]. Hongo, M, 1982) | 0.91 |
" Substantial and prolonged falls in blood pressure were observed following oral dosing with 3 mg/kg of nifedipine in renal hypertensive rats, with 10 mg/kg of nifedipine in normotensive and spontaneously hypertensive rats and with 10 mg/dg of hydralazine in all three groups of animals." | ( Antihypertensive effects of nifedipine on conscious normotensive and hypertensive rats. Fujie, K; Kubo, T; Misu, Y; Yamashita, M, 1981) | 0.77 |
" dosage to rats, dogs, monkeys and humans." | ( Comparative pharmacokinetics of nicardipine hydrochloride, a new vasodilator, in various species. Higuchi, S; Shiobara, Y, 1980) | 0.26 |
" Dosage of all drugs was adjusted to reduce mean aortic pressure by no more than 5 mmHg." | ( Improved performance of ischemic canine myocardium in response to nifedipine and diltiazem. Henry, PD; Pérez, JE; Sobel, BE, 1980) | 0.5 |
"The anti-anginal activity of nifedipine was studied after a dosage of 10 and 20 mg in nine patients suffering from a typical, stable effort angina pectoris." | ( [Effectiveness and duration of action of nifedipine in effort angina (author's transl)]. Arosio, G; Ciampalini, G; Di Girolamo, A; Ettori, F; Fappani, A; Oneglia, C, 1980) | 0.82 |
"00mM resulted in a dose-response relationship with regard to LDH release (243% to 750% of control) and to the loss of cell viability (0 to 67% of control)." | ( Protective effect of nifedipine against cytotoxicity and intracellular calcium alterations induced by acetaminophen in rat hepatocyte cultures. Claude, JR; Dutertre-Catella, H; Ellouk-Achard, S; Mawet, E; Thevenin, M; Thibault, N, ) | 0.45 |
" First, dose-response curves were constructed; from these data the EC50 concentration for the three calcium antagonists was calculated." | ( Hemodynamic and antiischemic effects of nifedipine, lacidipine, and nisoldipine in rat isolated working heart. Pfaffendorf, M; Pijl, AJ; van Zwieten, PA, 1993) | 0.55 |
" The content of cAMP in MIN6 cells was also elevated significantly by genistein and the dose-response relationship between the genistein and cAMP accumulation was consistent with the relationship between the genistein and insulin release." | ( Genistein augments cyclic adenosine 3'5'-monophosphate(cAMP) accumulation and insulin release in MIN6 cells. Ishii, C; Ito, Y; Kato, N; Kawazu, S; Ohno, T; Shimizu, M; Tomono, S, 1993) | 0.29 |
" 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) | 1.2 |
" At the end of the dosing interval, felodipine lowered office DBP (mm Hg) by -18 +/- 12/14 +/- 1 compared to -14 +/- 2/11 +/- 1 for nifedipine (P < or = ." | ( Differential effects of felodipine and nifedipine on 24-h blood pressure and left ventricular mass. Leenen, FH; Myers, MG; Tanner, J, 1995) | 0.76 |
"Although the combined administration of atenolol and nifedipine has been shown to be effective in the treatment of angina pectoris the optimum dosage level of the combination has not yet been established." | ( A cross-over study comparing the efficacy of a combination of atenolol and nifedipine at different doses in angina pectoris. Jennings, K; Metcalfe, MJ, 1995) | 0.77 |
" The daily dosage of enalapril was increased, if required, from 10 to 20 to 40 mg and that of nifedipine from 40 to 60 to 80 mg at 4-week intervals during the 12-week titration period." | ( Factors determining the blood pressure response to enalapril and nifedipine in hypertension associated with NIDDM. Chan, JC; Cheung, CK; Cockram, CS; Law, LK; Nicholls, MG; Swaminathan, R, 1995) | 0.75 |
" Following 4 weeks of wash-out/run-in period, patients from the carvedilol group received this drug once a day at a dosage of 25 mg/day for 8 consecutive weeks." | ( [Use of carvedilol compared to nifedipine in the treatment of mild and moderate essential arterial hypertension]. Dantas, M; Freitas, AF; Furtado, MR; Kohlmann, NE; Kohlmann, O; Plavnik, FL; Portela, JE; Spritzer, N; Spritzer, T, 1994) | 0.57 |
"A parallel-group, randomized, double-blind, forced-titration, multicenter study was done to compare the efficacy and safety of once-daily nifedipine coat-core (NIF CC) and once-daily nifedipine gastrointestinal therapeutic system (NIF GITS) dosed in the fasting state in patients with mild-to-moderate essential hypertension." | ( The efficacy and safety of once-daily nifedipine administered without food: the coat-core formulation compared with the gastrointestinal therapeutic system formulation in patients with mild-to-moderate hypertension. Nifedipine Study Group. Allenby, KS; Commins, BM; Glasser, SP; Jungerwirth, S; Ripa, SR; Schwartz, LA, ) | 0.6 |
" Nifedipine (100 micrograms/kg, 300 micrograms/kg, and 1000 micrograms/kg) inhibited in a dose-dependent manner the pressor responses to the alpha 1- and alpha 2-adrenoceptor agonists, the dose-response curves to the alpha 2-adrenoceptor agonists being shifted further to the right." | ( A comparison of the effects of TMB-8 and nifedipine on pressor responses to alpha 1- and alpha 2-adrenoceptor agonists in pithed rats. Aleixandre, MA; Pintado, A; Puerro, M, 1995) | 1.47 |
"We restricted the dose-response meta-analysis to the 16 randomized secondary-prevention trials of nifedipine for which mortality data were available." | ( Nifedipine. Dose-related increase in mortality in patients with coronary heart disease. Furberg, CD; Meyer, JV; Psaty, BM, 1995) | 1.95 |
" These results suggested that AJ-2615 has potential as a long-acting (once daily dosage regimen) antihypertensive drug without causing a steep blood pressure fall and tachycardia." | ( Antihypertensive effects of AJ-2615, a new calcium antagonist with alpha 1-adrenergic blocking activity in experimental hypertensive animals. Fukuya, F; Hosoki, K; Ikeno, A; Karasawa, T; Minato, H; Nose, I; Takeyama, K, 1993) | 0.29 |
" After 12 weeks of artificial sunlight exposure, less than 3% of NDNIF (w/w initial NIF content) was present in each of the 10 tested dosage forms." | ( Photostability determination of commercially available nifedipine oral dosage formulations. Foster, RT; Grundy, JS; Kherani, R, 1994) | 0.54 |
" The exercise tests were performed at the end of dosage interval (i." | ( 24 h anti-anginal and anti-ischaemic effects with once daily felodipine. A double-blind comparison with nifedipine, twice daily, and placebo in patients with stable exercise induced angina pectoris. Schulte, KL, 1995) | 0.51 |
" Nicardipine was given at a daily dosage of 80-120 mg, and nifedipine 40-60 mg, for up to one month." | ( [The efficacy and safety of slow-release nicardipine vs nifedipine in angina]. Maddalena, F; Rocco, CG; Villanova, C, 1994) | 0.78 |
" Both formulations were well tolerated and reduced blood pressure over the 24-hour dosing interval even when coadministered with food." | ( The efficacy and safety of once-daily nifedipine: the coat-core formulation compared with the gastrointestinal therapeutic system formulation in patients with mild-to-moderate diastolic hypertension. Nifedipine Study Group. Allenby, KS; Glasser, SP; Jain, A; MacCarthy, EP; Pettis, PP; Pride, K; Schwartz, LA; Shannon, T, ) | 0.4 |
" First, because the frequency of treatment regimens has been shown to be the most important determinant of long-term compliance with calcium channel blocker medications, it was desirable to compare drugs having identical dosing regimens." | ( The costs and effects of switching calcium channel blockers: evidence from Medicaid claims data. Rizzo, JA; Simons, WR; Smith, ME; Stoddard, M, ) | 0.13 |
" The effects of three long-acting calcium antagonists, amlodipine, lacidipine and nifedipine GITS (gastrointestinal therapeutic system), on vascular reactivity were assessed over 24h and 48h dosage intervals." | ( Vascular reactivity: a measurement of calcium channel blockade. Elliott, HL, 1995) | 0.52 |
" It allows instant evaluation of a patient's dosing record, at the patient's return to the practice." | ( Patterns of drug compliance with medications to be taken once and twice daily assessed by continuous electronic monitoring in primary care. Kruse, W; Rampmaier, J; Ullrich, G; Weber, E, 1994) | 0.29 |
" The individual control showed no effect in 5 patients, an unfavorable effect by a decrease of Rs exceeding that of Rp in 2 patients, and a favorable net effect in only 3 patients, induced in 1 patient only after a very high dosage of nifedipine and leading to a certain increase of arterial oxygen saturation in only 1 other patient." | ( [Comparative studies of hemodynamics under prostacyclin and nifedipine in patients with Eisenmenger syndrome]. Gildein, HP; Mocellin, R; Wildberg, A, 1995) | 0.72 |
" The analysis was further extended to simulate the blood pressure responses to alternative fixed dosage regimens." | ( Prediction and optimisation of the antihypertensive response to nifedipine. Donnelly, R; Elliott, HL; Meredith, PA, 1994) | 0.53 |
" The dose-response curves were analyzed for differences in active force development (kg/cm2)." | ( Developmental changes in gastric fundus smooth muscle contractility and involvement of extracellular calcium in fetal and adult guinea pigs. Ierardi, JA; Parkman, HP; Paul, DA; Ryan, JP, 1994) | 0.29 |
" dose of M3 (the 3-carboxylic acid pyridine derivative), and the dosed M3 was excreted only by glomerular filtration." | ( Interaction of renal excretion between nilvadipine metabolites, M3 and M7 in rats: characterization of sex-dependent and sex-independent active secretion in the kidney. Hata, T; Sawamoto, T; Terashita, S; Tokuma, Y; Tozuka, Z, 1994) | 0.29 |
" At a daily dosage of 8-16 mg, the responder rate (RRdiast < 90 mm Hg) is 60-70% in single-drug therapy and up to 80% in combination therapy." | ( Nilvadipine: profile of a new calcium antagonist. An overview. Rosenthal, J, 1994) | 0.29 |
" Pretreatment with captopril reduced the pressor responses to cirazoline and displaced the dose-response curve for this agonist to the right, significantly increasing the ED50 without altering the maximum response." | ( Pressor responses to the alpha 1-adrenoceptor agonist cirazoline: effects of captopril, phenoxybenzamine and nifedipine. Tabrizchi, R; Triggle, CR, 1994) | 0.5 |
"1 microM), a selective alpha 2-adrenoceptor antagonist, shifted the dose-response curves for clonidine to the right." | ( Effects of pertussis and cholera toxins on alpha-adrenoceptor function in rat tail artery: differences in hypertension. Li, XF; Triggle, CR, ) | 0.13 |
" The variability in plasma concentrations over the dosing interval was found to be markedly less with the felodipine-metoprolol combination than with the combination of nifedipine and atenolol." | ( Aiming for steady 24-hour plasma concentrations: a comparison of two calcium antagonist and beta-blocker combinations. Bergstrand, R; Eriksson, M; Lidman, K; Nyberg, G; Olofsson, B, 1993) | 0.48 |
" In the beta cell of aged rats, the following abnormalities were found: (a) right shift of the dose-response curve (depressed sensitivity) of glucose-induced insulin release, (b) no increase of the maximum response to glucose in the face of increased insulin content of the islets (reduced responsiveness), (c) no response to forskolin and normal response to the phorbol ester and glyburide, and (d) increased sensitivity to nifedipine." | ( Insulin secretion by the pancreatic beta cell of aged rats. Aizawa, T; Hashizume, K; Ishihara, F; Komatsu, M; Nishii, N; Sato, Y; Suzuki, N; Yamada, T, 1994) | 0.45 |
" About 8% of patients had a low compliance rate, irrespective of the dosage regimen." | ( [Time of drug intake in hypertension and angina pectoris. A controlled monitoring study]. Erne, P; Heynen, G; Saxenhofer, H; Waeber, B, 1994) | 0.29 |
" N-acetyl-beta-glucosaminidase (beta-NAG) activity showed a similar change in the high dosage group." | ( [Effects of nifedipine on hepatic hyaluronic acid, hydroxyproline and glucosaminidase contents in rats with liver fibrosis]. Che, J; Li, D; Lu, H, 1994) | 0.67 |
" The synergistic action of magnesium sulphate and nifedipine in the dosage employed in this study may be used to reduce maternal and perinatal mortality and morbidity in women with eclampsia." | ( A safer and more effective treatment regimen for eclampsia. Bhalla, AK; Dhall, GI; Dhall, K, 1994) | 0.54 |
" After a 3-week washout period, patients were randomized to receive felodipine-ER (5 mg once daily) or nifedipine GITS (30 mg once daily); during a subsequent 6-week titration phase, the once-daily felodipine-ER dose could be increased to 10 mg and the nifedipine GITS dose to 60 or 90 mg in an attempt to achieve adequate blood pressure response (SiDBP < or = 90 mm Hg, or < 100 mm Hg with a > 10-mm Hg reduction from baseline, as measured 24 hours after dosing [trough])." | ( Efficacy and tolerability of extended-release felodipine and extended-release nifedipine in patients with mild-to-moderate essential hypertension. Fagan, TC; Haggert, BE; Liss, C, ) | 0.57 |
" After 3 months the drug dosage was doubled if the systolic blood pressure goal (SBP < 160 mmHg and SBP reduction of at least 20 mmHg) had not been reached." | ( Antihypertensive efficacy and tolerability of different drug regimens in isolated systolic hypertension in the elderly. Alli, C; Avanzini, F; Bettelli, G; Colombo, F; Corso, R; Mariotti, G; Radice, M; Tognoni, G; Torri, V, 1994) | 0.29 |
" Thus, compared with other agents, amlodipine with its relatively smooth concentration-time profile and long elimination half-life will be superior in maintaining blood pressure control both with perfect compliance and when dosage regimens are perturbed due to missed drug doses." | ( Therapeutic coverage: reducing the risks of partial compliance. Elliott, HL; Meredith, PA, 1994) | 0.29 |
" In a randomized, double-blind trial, 15 type 1 diabetic patients were treated with either nifedipine (n = 8; dosage 30 mg/day) or placebo (n = 7) for 12 months." | ( Long-term treatment with nifedipine reduces urinary albumin excretion and glomerular filtration rate in normotensive type 1 diabetic patients with microalbuminuria. Banyai, M; Capek, M; Kautzky-Willer, A; Prager, R; Schernthaner, G; Schnack, C, 1994) | 0.81 |
"To present the efficacy and tolerability of a new oral dosage form of the calcium antagonist nitrendipine compared to nifedipine capsules in patients with hypertensive emergency." | ( Treatment of hypertensive emergency. Comparison of a new dosage form of the calcium antagonist nitrendipine with nifedipine capsules. Blanke, P; Reimnitz, P; Rohr, G, 1994) | 0.71 |
"The new dosage form of nitrendipine (vial with 1 ml of alcoholic solution) represents an alternative in the treatment of hypertensive emergency." | ( Treatment of hypertensive emergency. Comparison of a new dosage form of the calcium antagonist nitrendipine with nifedipine capsules. Blanke, P; Reimnitz, P; Rohr, G, 1994) | 0.5 |
" Nifedipine and captopril were administered as monotherapy in increasing dosage while a diuretic was added after 8 weeks in patients who failed to reach the target BP (24-h mean diastolic BP < 90 mm Hg) on monotherapy." | ( Nifedipine versus captopril in the management of moderate hypertension in black patients. Davis, J; Eitzman, L; Sareli, P; Skoularigis, J; Strugo, V, 1994) | 2.64 |
" Furthermore, these models take account of placebo effects and time-dependent changes in blood pressure and drug concentrations during a dosage interval." | ( Concentration-effect analysis of antihypertensive drug response. Focus on calcium antagonists. Donnelly, R; Elliott, HL; Meredith, PA, 1994) | 0.29 |
" Tissues were precontracted with carbachol or KCl, and relaxation dose-response curves to nifedipine, Mn2+, or Cd2+ were obtained." | ( Expression of dihydropyridine resistance differs in porcine bronchial and tracheal smooth muscle. Croxton, TL; Fleming, C; Hirshman, CA, 1994) | 0.51 |
" 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 |
" Beginning at 5 mg once daily for enalapril and 30 mg once daily for nifedipine-ER, the dosage was titrated every 4 weeks for 16 weeks, up to a maximum of 40 mg for enalapril and 120 mg for nifedipine-ER." | ( Efficacy and safety of enalapril versus extended-release nifedipine for the treatment of mild-to-moderate essential hypertension: a multicenter 22-week study. Multicenter Cooperative Study Group. Leon, AS, ) | 0.61 |
" The nifedipine coat-core tablet provided good control of blood pressure for the entire 24-hour dosing interval and was well tolerated by the majority of patients in the study." | ( The efficacy and safety of once-daily nifedipine coat-core in the treatment of mild-to-moderate hypertension. Adalat CC Cooperative Study Group. Feig, PU; Gibson, L; Mac Carthy, EP; Pettis, PP; Schwartz, L, ) | 0.92 |
" Nifedipine coat-core, when combined with ATN in patients not controlled by ATN alone, had significant antihypertensive activity for the entire 24-hour dosing interval and was well tolerated by the majority of patients in the study." | ( The safety and efficacy of once-daily nifedipine coat-core in combination with atenolol in hypertensive patients. Adalat CC Cooperative Study Group. Feig, PU; Gibson, L; Mac Carthy, EP; Pettis, PP; Schwartz, L, ) | 1.31 |
" Nifedipine at a dosage of 200 micrograms or placebo was added to each 1000 ml of St." | ( Cardioprotection by nifedipine cardioplegia during coronary artery surgery. Haider, W; Laczkovics, A; Moritz, A; Trubel, W; Zwoelfer, W, 1994) | 1.52 |
" More controlled trials with less aggressive dosing regimens and placebo controls need to be performed to assess the most appropriate treatment for HUs with the fewest adverse effects." | ( Oral antihypertensives for hypertensive urgencies. Gales, MA, 1994) | 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) | 0.79 |
" Intracarotid administration of cisplatin to rat did not cause acute vascular damage in either the brain or brain tumor at the dosage used." | ( Capillary permeability in experimental rat glioma and effects of intracarotid CDDP administration on tumor drug delivery. Aoyagi, M; Hirakawa, K; Ichimura, K; Ohno, K; Suzuki, R; Tamaki, M, 1993) | 0.29 |
" In the three areas of efficacy that the study compared-24-hour post dose blood pressure, control of blood pressure over the dosing period with particular reference to the waking day and attenuation of systolic blood pressure on exercise-atenolol and the fixed combination demonstrated greater efficacy than enalapril." | ( A double-blind crossover trial of atenolol, enalapril and the fixed combination of atenolol and nifedipine in mild and moderate hypertension. Brennand-Roper, D; Chapman, CM; Flora, HK; Gupta, S; Jackson, G; Jackson, PG; Manivannan, A; Taylor, DJ; Thirkettle, JL; Vella, R, ) | 0.35 |
" Dose-response curves induced by bolus injection (i." | ( Effects of a K+ATP channel opener, lemakalim, on systemic, coronary and regional vascular dynamics in conscious dogs: comparison with nifedipine, adenosine, nitroglycerin and acetylcholine. Shen, YT; Vatner, SF, 1993) | 0.49 |
" At the end of the 4th week, the non-responders (diastolic blood pressure > 90 mmHg or reduction in diastolic pressure < 10 mmHg), had the dosage increased to 60 mg/day." | ( [Multicenter National Study for the evaluation of the efficacy and tolerance of nifedipine oral release osmotic system in mild to moderate hypertension]. Amodeo, C; Ayoub, JC; Brandão, AP; Chaves, H; de Andradre, J; Giorge, DM; Lima Júnior, E; Mion Júnior, D; Nobre, F; Ribeiro, JM, 1995) | 0.52 |
" Fifty nine percent were considered responders at the end of the 4th week with nifedipine oros 30 mg/day and 41% needed dosage increment to 60 mg/day." | ( [Multicenter National Study for the evaluation of the efficacy and tolerance of nifedipine oral release osmotic system in mild to moderate hypertension]. Amodeo, C; Ayoub, JC; Brandão, AP; Chaves, H; de Andradre, J; Giorge, DM; Lima Júnior, E; Mion Júnior, D; Nobre, F; Ribeiro, JM, 1995) | 0.75 |
" The pharmacokinetics of a new calcium antagonist barnidipine hydrochloride, a stereochemically pure enantiomer, was studied after intravenous and oral dosing to the rat and dog, and oral to man." | ( Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human. Hashimoto, K; Higuchi, S; Teramura, T; Watanabe, T, 1995) | 0.29 |
" The fentanyl dose-response curve was unchanged by opioid receptor blockade with 10(-6)M naloxone and by alpha and beta adrenoceptor blockade produced by 10(-6)M prazosin and 10(-6)M propranolol." | ( Direct effects of fentanyl on canine coronary artery rings. Bridges, MT; Grover, TE; Introna, RP; Pruett, JK; Yodlowski, EH, 1995) | 0.29 |
" This close temporal and dose-response relationship strongly suggests that delta-opioid receptor-mediated increases in intracellular [Ca2+] results from inositol 1,4,5-trisphosphate-induced Ca2+ release from intracellular stores, in undifferentiated NG108-15 cells." | ( delta-Opioids stimulate inositol 1,4,5-trisphosphate formation, and so mobilize Ca2+ from intracellular stores, in undifferentiated NG108-15 cells. Lambert, DG; Smart, D, 1996) | 0.29 |
"2 mM) produced a concentration dependent rightward shift of contraction dose-response curves to KCl but not to carbachol." | ( MgSO4 relaxes porcine airway smooth muscle by reducing Ca2+ entry. Clancy, J; Croxton, TL; Hirshman, CA; Kumasaka, D; Lande, B; Lindeman, KS, 1996) | 0.29 |
"Photochemical degradation reactions and the chemical structure of the decomposition products were studied in the 1,4-dihydropyridine series for Nifedipine drug substances and for various dosage of it (Cordaflex product family)." | ( [Photostability of nifedipine]. Bárczay, E; Hoffmanné, FV; Tömpe, P, 1996) | 0.82 |
" Dose-response studies were performed using previously reported inhibitors of cytosolic calcium oscillation mechanisms." | ( The mechanisms underlying Bay K 8644-stimulated phasic myometrial contractions. Chien, EK; Phillippe, M; Saunders, T, ) | 0.13 |
" Although it is recognised that CR drug formulations may enhance the treatment compliance of patients by reducing the number of daily doses, there are several pharmaceutical, pharmacokinetic and pharmacological considerations which may influence the ultimate selection of a particular dosage form." | ( The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Foster, RT; Grundy, JS, 1996) | 0.85 |
" In the majority of those patients for whom dosage reduction, or drug discontinuation or substitution is not possible, and for whom prophylactic measures have failed, surgical excision of gingival tissue remains the only treatment of choice." | ( Gingival enlargement induced by drugs. Berini, L; Brunet, L; Farré, M; Mendieta, C; Miranda, J, 1996) | 0.29 |
" Dosing of oral nifedipine capsules in medical and surgical inpatients was studied prospectively in three central Connecticut hospitals (University, community-teaching, and private nonteaching) during a 60-day period from January to March, 1994." | ( "Inappropriate" physician habits in prescribing oral nifedipine capsules in hospitalized patients. Mansoor, GA; Rehman, F; White, WB, 1996) | 0.89 |
" For both drug classes, we suggest that long-acting agents be considered, providing therapeutic coverage well beyond the normal dosing interval." | ( 1,4-Dihydropyridines versus beta-blockers for hypertension: are either safe for the heart? Leenen, FH, 1996) | 0.29 |
"Nifedipine, a calcium-channel blocking drug was analysed in dog plasma after oral dosing with two different formulations." | ( Sensitive high-performance liquid chromatographic determination of nifedipine in dog plasma using an automated sample preparation system with laboratory robot. Balogh-Nemes, K; Gödörházy, L; Horvai, G; Horváth, V; Hrabéczy-Páll, A; Klebovich, I; Kocsi, E; Niegreisz, Z; Tolokán, A, 1996) | 1.97 |
"The gastrointestinal therapeutic system formulation of nifedipine enables a once-daily dosing resulting in predictable, relatively constant plasma concentrations." | ( Nifedipine gastrointestinal therapeutic system versus atenolol in stable angina pectoris. The Netherlands Working Group on Cardiovascular Research (WCN). Bernink, PJ; Claessens, RJ; de Vries, RJ; Dunselman, PH; Kingma, JH; Lok, DJ; Pasteuning, WH; van den Heuvel, AF, 1996) | 1.98 |
" All of the nanoparticle dosage forms decreased Cmax and increased Tmax and the mean residence time (MRT) values." | ( The antihypertensive effect of orally administered nifedipine-loaded nanoparticles in spontaneously hypertensive rats. Atkinson, J; Fluckiger, L; Hoffman, M; Kim, YI; Lartaud-Idjouadiene, I; Maincent, P, 1997) | 0.55 |
" An incremental dose-response effect was observed both in clinic and ambulatory blood pressure parameters during treatment with mibefradil and nifedipine GITS alone and combined with lisinopril." | ( The antihypertensive efficacy of the novel calcium antagonist mibefradil in comparison with nifedipine GITS in moderate to severe hypertensives with ambulatory hypertension. Archambault, F; Dalle Ave, S; Lacourcière, Y; Lefebvre, J; Lindberg, E; Poirier, L; Ward, C, 1997) | 0.72 |
" The hypotensive effect of YM430 reached its maximum about 2 hr after dosing and lasted for over 10 hr." | ( Hypotensive effects of YM430, a 1,4-dihydropyridine derivative, in spontaneously hypertensive rats and renal hypertensive dogs. Shibasaki, K; Takenaka, T; Takizawa, K; Uchida, W, 1997) | 0.3 |
" Heterogeneity of trial results appeared to be due to differences in the severity of initial pulmonary artery pressures and to differences in the dosage of nifedipine rather than the type of disease state." | ( Meta-analysis of the long-term effect of nifedipine for pulmonary hypertension. Lehrman, S; Malik, AS; Warshafsky, S, 1997) | 0.76 |
" An analysis was also performed on 84 outpatients with stable angina pectoris, who were included in an open, parallel study and received the same dosing regimen of either amlodipine or nifedipine SR as the patients in the hypertension arm of the study." | ( Patient compliance and therapeutic coverage: amlodipine versus nifedipine SR in the treatment of hypertension and angina: interim results. Steering Committee and Cardiologists and General Practitioners involved in the Belgium Multicentre Study on Patient Detry, JM, 1994) | 0.72 |
"Nifedipine decreased the daily and cumulative dosage requirement of tacrolimus." | ( Nifedipine interaction with tacrolimus in liver transplant recipients. Gordon, FD; Jenkins, RL; Lewis, WD; Marcos-Alvarez, A; Seifeldin, RA, 1997) | 3.18 |
" As the dose-response relationship shows clinical saturation at a daily dose of 16 mg, the recommended dose is 8 mg taken once daily." | ( Nilvadipine in hypertension--experience in ambulatory treatment. Burkardt, I; Hoffmann, A; Kraul, H, 1997) | 0.3 |
"65 microM, close to that obtained from the dose-response curve." | ( Characterization of nifedipine block of the human heart delayed rectifier, hKv1.5. Anderson, JW; Fedida, D; Zhang, X, 1997) | 0.62 |
"To investigate the effect of 7 to 14 days of therapy with nifedipine (sustained-release preparation) on the 24-hour blood pressure patterns of pregnant women with pre-eclampsia or chronic hypertension, and to test the utility of blood pressure monitoring in modulating the timing and dosage of the drug." | ( 24-hour blood pressure monitoring to evaluate the effects of nifedipine in pre-eclampsia and in chronic hypertension in pregnancy. Benedetto, C; Carandente, F; Chiarolini, L; Giarola, M; Maulà, V; Zonca, M, 1997) | 0.78 |
" 24-hour blood pressure monitoring allowed adjustment, when necessary, to the timing and dosage of nifedipine in accordance with the blood pressure patterns of each patient, using the hyperbaric index and percent time elevation as objective parameters for the evaluation of treatment efficacy." | ( 24-hour blood pressure monitoring to evaluate the effects of nifedipine in pre-eclampsia and in chronic hypertension in pregnancy. Benedetto, C; Carandente, F; Chiarolini, L; Giarola, M; Maulà, V; Zonca, M, 1997) | 0.76 |
" Additionally, mean blood pressures at 4-hour intervals after drug administration and heart rate during the first 8 hours of the dosage interval were compared." | ( Nifedipine gastrointestinal therapeutic system versus nifedipine coat-core: comparison of efficacy via 24-hour ambulatory blood pressure monitoring. Bookstaver, DA; Coffey, TA; Defina, LF; Goldfinger, MP, ) | 1.57 |
" Neither dosage nor treatment order had an effect on the results." | ( Nifedipine gastrointestinal therapeutic system versus nifedipine coat-core: comparison of efficacy via 24-hour ambulatory blood pressure monitoring. Bookstaver, DA; Coffey, TA; Defina, LF; Goldfinger, MP, ) | 1.57 |
"Accurate, precise first-derivative ultraviolet spectrophotometric, gas-liquid and high performance liquid chromatographic methods for the determination of nifedipine and mefruside in tablet dosage form were described." | ( Simultaneous determination of the binary mixture of nifedipine and mefruside using derivate spectroscopy, capillary gas-liquid chromatography and high performance liquid chromatography. el Walily, AF, ) | 0.58 |
" No tolerance to the antihypertensive effect of KRN4884 was observed during a 15-day repeated dosing period." | ( KRN4884, a novel K channel opener: antihypertensive effects in conscious renal hypertensive dogs. Endo, M; Izawa, T; Izumi, H; Jinno, Y; Kawahara, J; Takeuchi, A, 1997) | 0.3 |
" dosing was 10." | ( Extrahepatic first-pass metabolism of nifedipine in the rat. Eliot, LA; Foster, RT; Grundy, JS, 1997) | 0.57 |
" Pelliculation frequently differs in soft shell capsules from hard shell capsules because of the larger mass of gelatin in the softshell dosage form." | ( Dissolution testing of soft shell capsules-acetaminophen and nifedipine. Bottom, CB; Carstensen, JT; Clark, M, 1997) | 0.54 |
"Nifedipine gastrointestinal therapeutic system (GITS) is a once-a-day formulation of nifedipine providing stable plasma concentrations over the entire 24 h dosing interval." | ( Efficacy of a low dose nifedipine GITS (20 mg) in patients with mild to moderate hypertension. Toal, CB, 1997) | 2.05 |
" The good anti-anginal and hypotensive efficacy and safety of amiodipine with once daily dosage regimen makes this drug an excellent choice of treatment for hypertensive patients with severe coronary artery disease." | ( [Comparative study to assess the efficacy and adverse effects of amlodipine and nifedipine retard in patients with stable exertional angina and hypertension]. Hlawaty, M; Kubler, G; Negrusz-Kawecka, M; Olszowska, M; Salamon, P; Tracz, W; Witkowska, M, 1997) | 0.52 |
" Pretreatment with nifedipine (10-30 mg/kg) produced dose-dependent rightward shifts of the (+/-)-Bay K 8644 dose-response curve." | ( Effects of dihydropyridine Ca2+ channel blockers on the discriminative stimulus and the motor impairing effects of (+/-)-Bay K 8644. Cohen, C; Perrault, G; Sanger, DJ, 1997) | 0.63 |
"Nifedipine gastrointestinal therapeutic system (GITS) is an extended-release dosage formulation that provides sustained blood concentrations of nifedipine over 24 hours." | ( Nifedipine gastrointestinal therapeutic system (GITS) for hypertensive patients in a primary care setting: results of the Extended Release Adalat Canadian Trial (EXACT). Barnes, C; Burelle, D; Mahon, WA; Toal, CB, ) | 3.02 |
" The experiments were of randomized cross-over design with a two-week wash-out period between dosing regimens." | ( Inhibition of nifedipine metabolism in dogs by erythromycin: difference between the gut wall and the liver. Arimori, K; Nakamura, K; Nakano, M; Tsuruta, S, 1997) | 0.66 |
" The decrease in arterial pressure was smooth and sustained over the entire 24-h dosing interval." | ( Differential properties of mibefradil in hypertension and angina. Kobrin, I, 1997) | 0.3 |
" Compared with placebo, barnidipine lowered blood pressure, with a trend toward a dose-response relationship over the dose range 10-30 mg." | ( Barnidipine, a novel calcium antagonist for once-daily treatment of hypertension: a multicenter, double-blind, placebo-controlled, dose-ranging study. Dutch Barnidipine Multicenter Study Group. Hart, W; Holwerda, NJ, 1997) | 0.3 |
" The interpretation of the results of these studies and their application to clinical practice requires an understanding of study design constraints, conflicting results and limitations in extrapolating study findings to other dosage strengths, formulations or agents within the calcium channel antagonist class." | ( Calcium channel antagonists: morbidity and mortality--what's the evidence? Parra, D; Straka, RJ; Swanson, AL, 1998) | 0.3 |
" Once-daily dosing improves compliance, but 24-h antihypertensive activity should be provided." | ( Compliance and antihypertensive efficacy of amlodipine compared with nifedipine slow-release. Bernaud, C; Carré, A; Charpentier, JC; Hotton, JM; Lequeuche, B; Mounier-Vehier, C, 1998) | 0.53 |
" The results obtained show that Adalat in dosage 60 mg daily during 7 days is most effective in cases with concomitant border-line hypertension." | ( [Premedication with different groups of hypotensive drugs in preparation of patients with concomitant arterial hypertension to planned surgical treatment]. Eliutin, DV; Mil'tsyn, AS; Sadchikov, DV, 1998) | 0.3 |
" At presumed ICG steady state (t=45 min), subjects were dosed with oral nifedipine (20 mg), captopril (50 mg) or placebo." | ( The influence of nifedipine and captopril on liver blood flow in healthy subjects. Burggraaf, J; Cohen, AF; Kroon, JM; Schoemaker, RC, 1998) | 0.87 |
" Plaque index and bleeding index showed a significant association with GO, while nifedipine dosage and duration of nifedipine therapy were not found to be significant predictors of GO." | ( Subgingival microflora associated with nifedipine-induced gingival overgrowth. Andronikaki, A; Kamma, JJ; Mitsis, F; Nakou, M, 1998) | 0.8 |
" The suitability of barnidipine for once-daily dosing was confirmed in a randomized, double-blind, placebo-controlled, crossover study of 20 patients." | ( Efficacy and tolerability of once-daily barnidipine in the clinical management of patients with mild to moderate essential hypertension. Spieker, C, 1998) | 0.3 |
" Duration of treatment, dosage of drugs per kg body weight and serum cyclosporin levels were recorded." | ( Contribution of individual drugs to gingival overgrowth in adult and juvenile renal transplant patients treated with multiple therapy. Ashley, FP; Koffman, CG; Morel, A; Ogg, CS; Rigden, SP; Smith, D; Wilson, RF, 1998) | 0.3 |
"cm-5) were noted in both groups, whereby in the F group the therapeutic goal could be achieved more quickly with the dosage regimen chosen." | ( DA1-receptor stimulation by fenoldopam in the treatment of postcardiac surgical hypertension. Berger, J; Gombotz, H; Mahla, E; Metzler, H; Plaza, J, 1998) | 0.3 |
" Animals in each group daily received NIF in dimethyl sulfoxide by gastric feeding at a dosage of 0 (control), 30, or 50 mg/kg body weight for 9 weeks." | ( Nifedipine-induced gingival overgrowth in rats: brief review and experimental study. Fu, E; Hsiao, CT; Hsieh, YD; Nieh, S; Shen, EC; Wikesjö, UM, 1998) | 1.74 |
" This might resemble the inverted U-shaped dose-response curve observed with another dihydropyridine, nimodipine, by other authors." | ( L-type voltage-dependent calcium channel blocker nifedipine enhances memory retention when infused into the hippocampus. Born, AG; Daroit, D; Kuyven, CR; Quevedo, J; Quillfeldt, JA; Roesler, R; Vianna, M, 1998) | 0.55 |
" Three protocols were employed to examine the inhibitory effect of thiopentone: (a) concentration-dependent effect on 10(-7) M noradrenaline (NA)- or high-K+ (40 mM)-induced contractions: (b) effect on NA-induced extra-and intracellular Ca(2+)-dependent contractions and (c) effect on the dose-response curve when Ca2+ is restored to Ca(2+)-depleted rings in Ca(2+)-free 40 mM K(+)-depolarizing medium." | ( Vasorelaxant effect of thiopentone in isolated human epigastric arteries. Ebeigbe, AB; Ehigiegba, AE; Olele, NE, 1998) | 0.3 |
" The daily dosage of rilmenidine was 1 mg, and could be increased to 2 mg/day." | ( Regression of left ventricular hypertrophy in hypertensive patients after 1 year of treatment with rilmenidine: a double-blind, randomized, controlled (versus nifedipine) study. Balazovjech, I; Dubai, G; Dvorak, I; Januszewicz, W; Krupa-Wojciechowska, B; Kubasik, A; Kuch-Wocial, A; Polak, G; Sadowski, Z; Simon, K; Stejfa, M; Szwed, H, 1998) | 0.5 |
"One-year treatment with a daily dosage of 1 or 2 mg rilmenidine achieves a significant reduction of left ventricular mass, which is not statistically different than that occurring with a daily dosage of 40 mg of slow-release nifedipine." | ( Regression of left ventricular hypertrophy in hypertensive patients after 1 year of treatment with rilmenidine: a double-blind, randomized, controlled (versus nifedipine) study. Balazovjech, I; Dubai, G; Dvorak, I; Januszewicz, W; Krupa-Wojciechowska, B; Kubasik, A; Kuch-Wocial, A; Polak, G; Sadowski, Z; Simon, K; Stejfa, M; Szwed, H, 1998) | 0.68 |
" Dose-response curves were performed for each drug." | ( Postcardioplegic myocardial recovery: effects of halothane, nifedipine, HOE 694, and quinacrine. Genade, S; Lochner, A; Theron, S; Trollip, G; Tromp, E, 1998) | 0.54 |
"Dissolution testing is an essential requirement for the development, establishment of in vitro dissolution and in vivo performance (IVIVR), registration and quality control of solid oral dosage forms." | ( Evaluation and comparison of dissolution data derived from different modified release dosage forms: an alternative method. Fassihi, R; Pillay, V, 1998) | 0.3 |
" Consequently, mibefradil dosage adjustment is not required for patients with renal impairment." | ( Steady-state trough plasma mibefradil concentrations and correlation to blood pressure response in hypertensive patients with chronic renal disease. Pordy, R; Woittiez, A, 1998) | 0.3 |
" Moreover, it was suggested that duration of nifedipine therapy (more than 2 months) and drug dosage (90 mg per day) could be important (1,2,3)." | ( [Gingival hyperplasia during treatment with nifedipine]. Bokor-Bratić, M; Selaković, S; Vucković, N, ) | 0.65 |
"Patients stabilized with Nif-GITS 30, 60, or 90 mg were monitored over 24 hours with an ambulatory blood pressure monitor and were then switched to an equivalent dosage of Nif-CC." | ( Comparison of 24-hour ambulatory blood pressure data in hypertensive patients switched from nifedipine-GITS to nifedipine-CC. Hilleman, DE; Lucas, BD; Mohiuddin, SM; Mooss, AN; Ryschon, KL; Wurdeman, RL, 1999) | 0.52 |
"No differences in average 24 hour-blood pressure readings were observed but significant differences in blood pressure control during the first 4 and last 8 hours of the dosing interval were seen." | ( Comparison of 24-hour ambulatory blood pressure data in hypertensive patients switched from nifedipine-GITS to nifedipine-CC. Hilleman, DE; Lucas, BD; Mohiuddin, SM; Mooss, AN; Ryschon, KL; Wurdeman, RL, 1999) | 0.52 |
"This study suggests that patients switched from Nif-GITS to Nif-CC could experience increased blood pressure during the night or toward the end of the dosing interval." | ( Comparison of 24-hour ambulatory blood pressure data in hypertensive patients switched from nifedipine-GITS to nifedipine-CC. Hilleman, DE; Lucas, BD; Mohiuddin, SM; Mooss, AN; Ryschon, KL; Wurdeman, RL, 1999) | 0.52 |
"To evaluate the appropriate dosing of amlodipine when converting patients from nifedipine extended-release (nifedipine ER) to amlodipine in the treatment of hypertension." | ( Evaluation of amlodipine dosing for conversion of nifedipine extended-release to amlodipine in the treatment of hypertension. Enlow, AM; Halverson, VJ; Kilpatrick, DM; Lower, DL; Montopoli, G; Yamreudeewong, W, 1999) | 0.78 |
" Dosing titration of amlodipine was required in 16 of 27 patients after the switch." | ( Evaluation of amlodipine dosing for conversion of nifedipine extended-release to amlodipine in the treatment of hypertension. Enlow, AM; Halverson, VJ; Kilpatrick, DM; Lower, DL; Montopoli, G; Yamreudeewong, W, 1999) | 0.56 |
"This study indicates the amlodipine dosage of 5 or 10 mg once daily can be used when nifedipine ER is converted to amlodipine in the treatment of hypertension." | ( Evaluation of amlodipine dosing for conversion of nifedipine extended-release to amlodipine in the treatment of hypertension. Enlow, AM; Halverson, VJ; Kilpatrick, DM; Lower, DL; Montopoli, G; Yamreudeewong, W, 1999) | 0.78 |
" 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) | 0.3 |
" In one case, nifedipine monotherapy prevented hypoglycaemia; in the second case, the dosage and the side-effects of other substances could be reduced, thus circumventing surgical therapy." | ( Treatment of hyperinsulinaemic hypoglycaemia with nifedipine. Eichmann, D; Hufnagel, M; Quick, P; Santer, R, 1999) | 0.92 |
" According to the experts in this roundtable discussion, the GITS formulation provides continuous delivery of nifedipine, ensuring relatively constant drug levels and 24-hour efficacy with a once-daily dosage regimen." | ( P&T Committee review of nifedipine GITS: new modality for angina and hypertension. Horn, J; Krakoff, L; Vetrovec, G; Weintraub, M, 1990) | 0.8 |
" Rats in each group received daily NIF, at a dosage of 0, 10, 30 or 50 mg/kg body weight, by gastric feeding for nine weeks." | ( Alterations of gingival morphology in nifedipine-fed rats. Fu, E; Hsiao, CT; Hsieh, YD; Lin, FG; Nieh, S, 1999) | 0.57 |
" Dimensional alterations of gingivae were noted among the different dosage groups, but significant differences were mainly observed in those groups compared to the 50 mg/kg group." | ( Alterations of gingival morphology in nifedipine-fed rats. Fu, E; Hsiao, CT; Hsieh, YD; Lin, FG; Nieh, S, 1999) | 0.57 |
"001) at 1 hour after nifedipine dosing (99 +/- 99 mL) compared with labetalol (44." | ( A randomized, double-blind trial of oral nifedipine and intravenous labetalol in hypertensive emergencies of pregnancy. Chauhan, SP; Newman, RB; Scardo, JA; Vermillion, ST, 1999) | 0.89 |
" Hemodynamic parameters at dosing and at 15, 30, 60, and 120 minutes were recorded." | ( A randomized, double-blind, hemodynamic evaluation of nifedipine and labetalol in preeclamptic hypertensive emergencies. Chauhan, SP; Hogg, BB; Newman, RB; Scardo, JA; Vermillion, ST, 1999) | 0.55 |
"Nifedipine gastrointestinal therapeutic system (GITS) is a once-daily formulation of nifedipine that provides stable plasma concentrations over the entire 24 h dosing interval." | ( Effectiveness of nifedipine GITS in combination with atenolol in chronic stable angina. Baird, MG; Bélanger, L; Erne, P; Klinke, P; Kostuk, WJ; Lotan, C; Marmor, A; Motro, M; Palant, A; Sclarowski, S; Stolero, D; Toal, CB; Turpie, A; Weiss, A; Zilberman, A, 1999) | 2.09 |
" Dosage of nifedipine or efonidipine was chosen after preliminary studies demonstrated that it showed moderate antihypertensive action (more than a 20% decrease in systemic blood pressure after treatment)." | ( Effects of the antihypertensive drug nifedipine on albuminuria and renal histopathology in young spontaneously hypertensive rats with diabetes. Kaneko, S; Shou, I; Takeda, M; Takizawa, H; Tomino, Y, 1999) | 0.97 |
"To examine the effects of repeat oral dosing of rosiglitazone on the pharmacokinetics of nifedipine, a prototype CYP3A4 substrate, a randomized, open-label, crossover study was performed with two treatment phases separated by a washout period of at least 14 days." | ( Rosiglitazone has no clinically significant effect on nifedipine pharmacokinetics. Finnerty, D; Freed, MI; Harris, RZ; Inglis, AM; Jorkasky, DK; Miller, AK; Patterson, S; Thompson, KA, 1999) | 0.77 |
"An original dosage form for oral delivery based on the encapsulation of both, lipophilic and hydrophilic drugs, in poly(epsilon-caprolactone) (PCL) microparticles prepared either by the oil-in-water (o/w) or the water-in-oil-in-water (w/o/w) solvent evaporation method was developed." | ( The preparation and evaluation of poly(epsilon-caprolactone) microparticles containing both a lipophilic and a hydrophilic drug. Astier, A; Bodmeier, R; Hoffman, M; Hombreiro Pérez, M; Lamprecht, A; Maincent, P; Ubrich, N; Zinutti, C, 2000) | 0.31 |
" The age, gender, current drug regimen and dosage were recorded for each participant and alginate impressions taken of both arches." | ( The calcium channel blocker used with cyclosporin has an effect on gingival overgrowth. Boomer, S; Campbell, BA; Hull, PS; Irwin, CR; Jamal, S; James, JA; Johnson, RW; Linden, GJ; Marley, JJ; Maxwell, AP; Short, CD; Spratt, H, 2000) | 0.31 |
") was administered prior to a cumulative DZP or PCP dose-response determination." | ( Modulation of the ethanol-like discriminative stimulus effects of diazepam and phencyclidine by L-type voltage-gated calcium-channel ligands in rats. Grant, KA; Green-Jordan, K, 2000) | 0.31 |
" It was also found that PEO and nifedipine were miscible, which may support the application of PEO in nifedipine dosage forms." | ( Sandwiched osmotic tablet core for nifedipine controlled delivery. Khang, G; Lee, HB; Liu, L; Rhee, JM, 1999) | 0.86 |
" Adalat GITS 30 was used as a reference dosage form." | ( Preparation and evaluation of a sustained-release formulation of nifedipine HPMC tablets. Ding, D; Li, H; Yan, G; Zhang, R, 2000) | 0.54 |
"A stability indicating high performance thin layer chromatographic (HPTLC) method for quantification of nifedipine, as bulk drug and from solid oral dosage forms has been developed." | ( High performance thin layer chromatographic determination of nifedipine from bulk drug and from pharmaceuticals. Gore, SP; Nair, VB; Patravale, VB, 2000) | 0.76 |
" The dose-response curves indicated IGF-I was more potent than insulin, favoring the assignment of the former as the physiological protective agent." | ( Insulin-like growth factor I prevents the development of sensitivity to kainate neurotoxicity in cerebellar granule cells. Baer, JD; Coyle, JT; Leski, ML; Valentine, SL, 2000) | 0.31 |
" In addition, data were collected and analyzed with regard to adverse drug reactions, average dosage of the alternative calcium channel blocker, number of additional antihypertensives begun or discontinued, and number of dosage changes in antihypertensives within the two visits after conversion, and the overall cost impact of conversion." | ( Retrospective evaluation of the conversion of amlodipine to alternative calcium channel blockers. Beckey, NP; Korman, L; Parra, D, 2000) | 0.31 |
" Conversion to calcium channel antagonists other than felodipine or less than equal dosages of felodipine may require dosage titration." | ( Retrospective evaluation of the conversion of amlodipine to alternative calcium channel blockers. Beckey, NP; Korman, L; Parra, D, 2000) | 0.31 |
" At high (>300 mmHg) vs low (<55 mmHg) oxygen tension the dose-response curves to NO- and SNP-induced relaxations were biphasic and shifted leftward." | ( Nitric oxide and sodium nitroprusside-induced relaxation of the human umbilical artery. Lovren, F; Triggle, C, 2000) | 0.31 |
" The dose-response profile of V(1) receptor agonist-induced neurotrophism exhibited a biphasic function, with lower concentrations inducing a significant increase while higher concentrations generally induced no significant effect." | ( Vasopressin-induced neurotrophism in cultured neurons of the cerebral cortex: dependency on calcium signaling and protein kinase C activity. Brinton, RD; Chen, Q; Kim, J; Monreal, AW; Oji, G; Patel, R; Sales, A, 2000) | 0.31 |
" The area under the field potentials was reduced only at a dosage of 60micromol/l (n=11)." | ( Effects of nifedipine on rhythmic synchronous activity of human neocortical slices. Ebner, A; Höhling, JM; Köhling, R; Lücke, A; Oppel, F; Pannek, H; Speckmann, EJ; Straub, H; Tuxhorn, I; Wolf, P, 2000) | 0.7 |
"Nifedipine gastrointestinal therapeutic system (GITS) is a once-daily formulation of nifedipine that provides sustained plasma nifedipine concentrations throughout the 24-hour dosing interval." | ( Blood pressure control in patients with mild to moderate essential hypertension switched from nifedipine gastrointestinal therapeutic system (GITS) 30 mg to nifedipine GITS 20 mg. Toal, CB, 2001) | 1.97 |
" In the first 3 months, drug dosage was titrated to achieve a decrease in diastolic blood pressure of at least 5 mm HG: Thirty-three patients had a minimum of 24 months' data, and 25 patients were followed up beyond 36 months (mean, 67 +/- 4 months)." | ( Long-term comparison between perindopril and nifedipine in normotensive patients with type 1 diabetes and microalbuminuria. Allen, TJ; Campbell, DJ; Cooper, ME; Gilbert, RE; Hammond, JJ; Jerums, G; Raffaele, J; Tsalamandris, C, 2001) | 0.57 |
"Ninety male Sprague-Dawley rats were divided into 6 groups: the first group received 8 mg/kg of CsA daily by gastric feeding for 6 weeks; the second and third groups received NIF daily at a dosage of 10 or 50 mg/kg; the fourth and fifth groups received CsA (8 mg/kg) and NIF (10 or 50 mg/kg); and the sixth group received solvents as a negative control." | ( Does nifedipine aggravate cyclosporin--induced gingival overgrowth? An experiment in rats. Chiang, CY; Chiu, HC; Fu, E; Liu, D, 2001) | 0.82 |
" Given the lower incidence of adverse events with amlodipine and its convenient once daily dosing regimen, however, amlodipine may help to enhance patient compliance." | ( [Amlodipine versus nifedipine retard. A randomized double-blind comparative study on long-term efficacy and safety of amlodipine and nifedipine retard in the monotherapy of chronic stable angina pectoris]. Kupper, W; Sauerbrey-Wullkopf, N, 2001) | 0.64 |
"The extent and severity of hyperplasia was significantly correlated with the dosage and serum level of CsA at 3, 6 and 12 months post-transplantation; last recorded dosage, however (p<0." | ( Cyclosporin A-induced gingival overgrowth is unrelated to allograft function in renal transplant recipients. Baboolal, K; Newcombe, RG; Subramanian, N; Thomas, DW, 2001) | 0.31 |
" glabra saponins at a dosage of 200mg/Kg of body weight." | ( [Antihypertensive effect of Herniaria glabra saponins in the spontaneously hypertensive rat]. Cherrah, Y; Hassar, M; Lyoussi, B; Rhiouani, H; Settaf, A, 2001) | 0.31 |
" A similar dose-response relationship was determined for nifedipine, an L-type calcium channel antagonist." | ( Pharmacological involvement of the calcium channel blocker flunarizine in dopamine transmission at the striatum. Armando, I; Belforte, JE; Buño, W; Magariños-Azcone, C; Pazo, JH, 2001) | 0.56 |
" Responders continued on the same dosage for 16 additional weeks, while non-responders were titrated to 60 mg NI or 10 mg AM." | ( Efficacy, tolerability and influence on "quality of life" of nifedipine GITS versus amlodipine in elderly patients with mild-moderate hypertension. Boari, L; De Dominicis, E; Giusti, C; Kilama, MO; Marchesi, M; Marelli, G; Mattarei, M; Mos, L; Novo, S; Pessina, AC; Pirrelli, A; Santini, M; Santonastaso, M; Semeraro, S; Uslenghi, E, 2001) | 0.55 |
" Blood pressure was measured at the end of the dosing interval that is 24 hours and 12 hours after Felodipine and Nifedipine respectively." | ( A randomised trial to compare the efficacy and safety of Felodipine (Plendil) and Nifedipine (Adalat) retard in patients with mild-to-moderate hypertension. Danbauchi, SS; Mbakwem, AC; Obodo, JO; Oke, DA; Okeahialam, BN; Onwubere, BJ, ) | 0.57 |
" Dose-response curves of nifedipine in the range from 2 to 50 microM showed a residual current that represented, in the presence of 2 microM nifedipine, 16." | ( Reexpression of the nifedipine-resistant calcium channel during dedifferentiation of adult rat ventricular cardiomyocytes. Ancey, C; Bescond, J; Fares, N; Pignier, C; Potreau, D, 2002) | 0.94 |
"The aim of this study was to investigate the effect of concomitant food intake on the bioavailability of two nifedipine containing modified release dosage forms for once daily administration." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.79 |
" The two dosage forms as well as the two administration conditions were compared by calculating point estimates and 90% confidence intervals for the relevant pharmacokinetic parameters." | ( The effect of food on the pharmacokinetics of nifedipine in two slow release formulations: pronounced lag-time after a high fat breakfast. Blume, HH; Brendel, E; Chantraine, E; Martin, W; Schall, R; Schug, BS; Wolf, D, 2002) | 0.57 |
"A new simple, sensitive and reproducible spectrophotometric method for the determination of nifedipine in pure and dosage forms has been proposed." | ( Spectrophotometric method for the determination of nifedipine with 4-(methylamino)phenol and potassium dichromate. Hoda, MN; Rahman, N, 2002) | 0.79 |
"Development of an extended release oral dosage form for nifedipine using the non-uniform drug distribution matrix method was conducted." | ( Development of extended release dosage forms using non-uniform drug distribution techniques. Huang, KK; Meng, CL; Wang, DP, 2002) | 0.56 |
"Nifedipine is a highly photosensitive drug that requires restricted protection from light during manufacturing, storage and handling of its dosage forms." | ( Effect of inclusion complexation with cyclodextrins on photostability of nifedipine in solid state. Abanumay, KA; Al-Angary, AA; Bayomi, MA, 2002) | 1.99 |
" Discontinuation of atenolol, and nifedipine dosage reduction by 50% were effective in managing his orthostatic changes." | ( Symptomatic orthostasis with extended-release nifedipine and protease inhibitors. Rathbun, RC; Rossi, DR; Slater, LN, 2002) | 0.85 |
"Nifedipine can be prepared in two liquid dosage forms and stored for up to 3 months under refrigeration or at room temperature." | ( Stability of nifedipine in two oral suspensions stored at two temperatures. Morosco, RS; Nahata, MC; Willhite, EA, ) | 1.94 |
" The nifedipine gastrointestinal therapeutic system (GITS) formulation provides a once-daily dosing regimen with a continuous and slow release of the drug, resulting in a smooth plasma concentration/time profile." | ( Clinical use of nifedipine GITS in the treatment of hypertension: an overview. Levenson, J; Simon, A, 2003) | 1.18 |
" Doses were increased to 20 mg/day, 10 mg/day or 60 mg/day, respectively, if the office BP remained 160/90 mmHg or greater at the end of the dosing interval." | ( Differential effects of once-daily antihypertensive drugs on blood pressure, left ventricular mass and sympathetic activity: Nifedipine-GITS versus felodipine-ER versus enalapril. Joyner, CD; Leenen, FH; Myers, MG; Toal, CB, 2002) | 0.52 |
"On 24 h ambulatory BP monitoring, nifedipine-GITS caused a consistent decrease in BP throughout the 24 h dosing interval, whereas felodipine-ER caused a more marked fall in BP during the day, and enalapril's effects diminished during the night and had disappeared by the morning." | ( Differential effects of once-daily antihypertensive drugs on blood pressure, left ventricular mass and sympathetic activity: Nifedipine-GITS versus felodipine-ER versus enalapril. Joyner, CD; Leenen, FH; Myers, MG; Toal, CB, 2002) | 0.8 |
"The photostability of drugs has been widely studied while less attention is devoted to the possible modifications that UV light may induce on the excipients of a dosage form, in particular, on the functional polymers used to modulate drug delivery." | ( Photostability of extended-release matrix formulations. Albini, A; Conte, U; Fasani, E; Maggi, L; Ochoa Machiste, E; Segale, L, 2003) | 0.32 |
"Eighty-four patients with threatened premature labor were randomly divided into three groups according to the dosage of NIF." | ( [Clinical observations on the prevention and treatment of premature labor with nifedipine]. Liu, M; Zhang, X, 2002) | 0.54 |
" However, injection of nifedipine into the vPAG potentiated the antinociceptive effect of endomorphin-1, producing a significant leftward shift in the dose-response curve of endomorphin-1 in both the tail-flick and tail-pressure tests." | ( Nifedipine potentiates the antinociceptive effect of endomorphin-1 microinjected into the periaqueductal gray in rats. Cousins, MJ; Fink, DJ; Hao, S; Iwasaki, H; Mamiya, K; Mata, M; Takahata, O, 2003) | 2.07 |
" Rightward shift of the dose-response curves due to coinfusion of inhibitors served to assess contribution of different pathways: trimethoxybenzoate (TMB-8) against Ca2+ mobilization, nifedipine against Ca2+ influx, staurosporine and Ro-318220 against PKC, and Y-27632 and HA-1077 against ROK." | ( Variations in cell signaling pathways for different vasoconstrictor agonists in renal circulation of the rat. Bauer, J; Parekh, N, 2003) | 0.51 |
" They shifted dose-response curves of Ang II, norepinephrine, and AVP to sevenfold and higher values." | ( Variations in cell signaling pathways for different vasoconstrictor agonists in renal circulation of the rat. Bauer, J; Parekh, N, 2003) | 0.32 |
"The objectives of peroral controlled release drug delivery systems (CRDDS) are to maintain therapeutically effective plasma drug concentration levels for a longer duration thereby reducing the dosing frequency and to minimise the plasma drug concentration fluctuations at steady state by delivering drug in a controlled and a reproducible manner." | ( Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index. Panchagnula, R; Sood, A, 2003) | 0.32 |
" There was no statistically significant difference in the pharmacokinetic parameters between two dosage forms." | ( Evaluation of monolithic osmotic tablet system for nifedipine delivery in vitro and in vivo. Chen, D; Liu, X; Zhang, R, 2003) | 0.57 |
"3-fold in the dose-response curves." | ( A comparative assessment of the duration of action of amlodipine and nifedipine GITS in normotensive subjects. Elliott, HL; Howie, CA; Meredith, PA; Ueda, S, 1993) | 0.52 |
" At doses with equivalent effects on heart rate (2 microg kg(-1) nisoldipine; 10 microg kg(-1) nifedipine) acute dosing with nisoldipine caused a significantly greater fall in systemic vascular resistance and increase in cardiac index, whilst nifedipine caused a greater reduction in stroke volume index and left ventricular stroke work index." | ( A comparison of the acute haemodynamic effects of nisoldipine and nifedipine during treatment with atenolol in patients with coronary artery disease. Dawkins, KD; Donaldson, KM; Waller, DG, 1993) | 0.74 |
" 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) | 0.54 |
"A previously described model for simulating drug dissolution, absorption, and pharmacokinetics has been expanded beyond the original application of simulating immediate-release dosage forms to include simulation of drug precipitation, water absorption from the gastrointestinal tract, changing gastrointestinal permeability, disintegration, and controlled-release and dissolution from a GITS-type dosage form." | ( Dissolution and absorption modeling: model expansion to simulate the effects of precipitation, water absorption, longitudinally changing intestinal permeability, and controlled release on drug absorption. Johnson, KC, 2003) | 0.32 |
" After oral administration of an immediate-release dosage form of a 10 mg nifedipine capsule to Taiwan residents, a skewed distribution with no clear evidence of bimodality of pharmacokinetic parameters was observed." | ( Pharmacokinetics of nifedipine in Taiwanese. Chien, SC; Hsu, KY; Lin, HY; Uang, YS, 2004) | 0.88 |
"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 |
" Data were abstracted from published reports and meeting abstracts, assessing method of randomization, blinding, "intention to treat" and dropouts, therapies, supportive measures, dosing and frequency, and crossovers." | ( A systematic review of medical therapy for anal fissure. Nelson, R, 2004) | 0.32 |
"Since beta1-blockade by nebivolol is larger after repeated dosing than after a single oral intake, we have explored its effect on pulmonary function after a 2-week treatment in hypertensive patients with mild to moderate COPD." | ( Comparative effects of a two-week treatment with nebivolol and nifedipine in hypertensive patients suffering from COPD. Cazzola, M; Girbino, G; Matera, MG; Ruggeri, P; Sanduzzi, A; Spicuzza, L; Vatrella, A, ) | 0.37 |
" Medical records (from five Canadian pediatric hospitals) of all pediatric hypertensive hospitalized children who were treated with short-acting nifedipine from January 1995 to December 1998 were retrospectively reviewed for patient demographics, dosing regimen, use of concomitant medications, co-morbid conditions, and presence/absence of minor and serious adverse events." | ( The safety and use of short-acting nifedipine in hospitalized hypertensive children. Filler, G; Girardin, C; Goodyer, P; Gowrishankar, M; Harley, F; MacLaine, P; Midgley, J; Ogborn, M; Orrbine, E; Rosychuk, RJ; Yiu, V, 2004) | 0.8 |
" After oral dosing (10 mg/kg), the C(max) of mebudipine was 25." | ( Pharmacokinetics of mebudipine, a new calcium antagonist, following single intravenous and oral administrations in rats. Bohlooli, S; Keyhanfar, F; Mahmoudian, M, 2004) | 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 |
"The release of Adalat Oros 60 on the Belgian market was justified since it has been clearly demonstrated that the dosage of 60 mg significantly increases the proportion of responders to nifedipine monotherapy." | ( [Medication of the month. Adalat Oros 60 mg]. Kulbertus, H, 2004) | 0.51 |
" The influence of CsA dosage and its trough level, HLA phenotype, gender and the administered calcium channel blocker on incidence and severity of overgrowth were studied." | ( Risk factors of gingival overgrowth in kidney transplant recipients treated with cyclosporine A. Boratyńska, M; Klinger, M; Radwan-Oczko, M; Zietek, M, 2003) | 0.32 |
" Total yearly CsA dosage was significantly higher in patients with overgrowth." | ( Risk factors of gingival overgrowth in kidney transplant recipients treated with cyclosporine A. Boratyńska, M; Klinger, M; Radwan-Oczko, M; Zietek, M, 2003) | 0.32 |
" Mean sodium diclofenac dosage per patient in groups 1 to 3 was 19." | ( Nifedipine versus tamsulosin for the management of lower ureteral stones. Fiori, C; Fontana, D; Ghignone, G; Porpiglia, F; Scarpa, RM, 2004) | 1.77 |
" The dose-response curves were shifted to the right by muscarinic antagonists in the following order of affinity: darifenacin (M(3))>methocramine (M(2)) >pirenzepine (M(1))." | ( Mechanisms mediating cholinergic antral circular smooth muscle contraction in rats. Ouyang, A; Tandon, T; Wrzos, HF, 2004) | 0.32 |
" Such data in pregnant women may affect the choice of optimal drug dosage and route of administration." | ( Pharmacokinetics of tocolytic agents. Cabrol, D; Carbonne, B; Tsatsaris, V, 2004) | 0.32 |
" The effect size may have been small because of low dosing in studies." | ( Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis. Pope, JE; Thompson, AE, 2005) | 0.33 |
" Throughout the dosing range, ATI22-107 induced much smaller, if any, increases in diastolic [Ca(2+)](i), T(25), and T(75)." | ( Pharmacological effects of ATI22-107 [2-(2-{2-[2-chloro-4-(6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)-phenoxy]-acetylamino}-ethoxymethyl)-4-(2-chloro-phenyl)-6-methyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester)], a novel dual pharmacophore, o Bednarik, DP; Houser, SR; Jung, AS; Margulies, KB; Mills, GD; Quaile, MP, 2005) | 0.33 |
"Controlled-release dosage forms may enhance persistence with therapy because of reduced dosing frequency and fewer adverse effects." | ( Persistence with antihypertensives related to formulation: the case of nifedipine. Breekveldt-Postma, NS; Herings, RM, 2005) | 0.56 |
" Patients with unaltered formulation and dosing frequency of nifedipine in the first year of follow-up with at least 2 prescriptions were included in the cohort." | ( Persistence with antihypertensives related to formulation: the case of nifedipine. Breekveldt-Postma, NS; Herings, RM, 2005) | 0.8 |
" It is desirable for antihypertensives to have a long duration of action so that once-daily dosing is possible." | ( Barnidipine: a new calcium channel blocker for hypertension treatment. Liau, CS, 2005) | 0.33 |
" We suggest that a reasonable approach is ongoing use of nifedipine capsules, with perhaps an initial dosage of 5 mg rather than 10 mg." | ( Nifedipine for severe hypertension in pregnancy: emotion or evidence? Côté, AM; Magee, LA; von Dadelszen, P, 2005) | 2.02 |
" Once-daily dosing with nifedipine GITS has been shown to achieve smooth and continuous blood pressure control, identical to conventional first-line diuretic therapy." | ( Nifedipine gastrointestinal therapeutic system--hypertension management to improve cardiovascular outcomes. Heagerty, AM, 2005) | 2.08 |
"Circadian variations in the pharmacokinetics, tissue distribution and urinary excretion of nifedipine were examined in fasted rats after administering a single oral dose at three different dosing times (08:00 am, 16:00 pm, 00:00 am)." | ( Circadian variations in the pharmacokinetics, tissue distribution and urinary excretion of nifedipine after a single oral administration to rats. Cao, QR; Choi, JS; Kim, TW; Lee, BJ, 2005) | 0.77 |
") dosing of nifedipine." | ( Nifedipine represses ion channels, transporters and Ca(2+)-binding proteins in hearts of spontaneously hypertensive rats. Borlak, J; Zwadlo, C, 2006) | 2.16 |
" Dose-response curves for carbachol revealed a lower peak response in new-born bladders compared with adults." | ( Developmental regulation of nerve and receptor mediated contractions of mammalian urinary bladder smooth muscle. Andersson, KE; Arner, A; Ekman, M, 2006) | 0.33 |
" Experiments with adenosine demonstrated that the selected dose of SPT elicited marked rightward shifts in the dose-response curves for both the inotropic and vascular actions." | ( Acute dilatory and negative inotropic effects of homocysteine are inhibited by an adenosine blocker. Boerma, M; Hauer-Jensen, M; Joseph, J; Kennedy, RH; Melchert, RB; Owings, R, 2006) | 0.33 |
" In mice given high drug dosing (100 mg/kg), seminiferous tubules showed immaturity with spermatogenic arrest at elongating spermatid stage and poorly developed lumen." | ( Effects of calcium channel blockers on the spermatogenesis and gene expression in peripubertal mouse testis. Gye, MC; Kim, DH; Kim, H; Lee, JH, ) | 0.13 |
" Only glycerol showed dose-response and effects potentially better than no treatment." | ( Anti-irritants I: Dose-response in acute irritation. Andersen, F; Andersen, KE; Bindslev-Jensen, C; Fullerton, A; Hedegaard, K; Petersen, TK, 2006) | 0.33 |
" The dose-response effect of 4 alleged AI (nifedipine, (-)-alpha-bisabolol, canola oil and glycerol) was studied on experimentally induced acute irritation in healthy volunteers, and only glycerol showed dose-related response and effects potentially better than no treatment." | ( Anti-irritants II: Efficacy against cumulative irritation. Andersen, F; Andersen, KE; Bindslev-Jensen, C; Fullerton, A; Hedegaard, K; Petersen, TK, 2006) | 0.6 |
"Crystallization of drugs formulated in the amorphous form may lead to reduced apparent solubility, decreased rate of dissolution and bioavailability and compromise the physical integrity of the solid dosage form." | ( Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility. Marsac, PJ; Shamblin, SL; Taylor, LS, 2006) | 0.33 |
" HAC particles were spherical and their surface appeared scale-worked; thermal studies demonstrated the existence of relevant interactions among the system components and the dissolution experiments led to the hypothesis that the drug is released primarily by diffusion through the lipid coating: the poloxamer and its concentration have a significant influence on the pharmaceutical properties of the dosage form, as shown by the a parameter of Weibull model." | ( Effect of poloxamers on nifedipine microparticles prepared by Hot Air Coating technique. Bellomi, S; Giovannelli, L; Pattarino, F, 2007) | 0.65 |
" These results indicate that in vivo experiments using the extract of herbal medicine prepared with the same dosage form as patients take are necessary to provide proper information about herb-drug interaction." | ( Does a kampo medicine containing schisandra fruit affect pharmacokinetics of nifedipine like grapefruit juice? Makino, T; Mizukami, H; Mizuno, F, 2006) | 0.56 |
" But at the dosage of 2 and 5 mg/kg animals do not exhibit this effect." | ( Involvement of hypothalamic pituitary adrenal axis on the nifedipine-induced antinociception and tolerance in rats. Ahmadiani, A; Mahani, SE; Motamedi, F, 2006) | 0.58 |
" 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 |
"Addition of CGRP stimulated rhythmic contractility but only in the presence of calcium, with a dose-response to the level of calcium ions." | ( The role of sympathetic innervation in the developing rat gubernaculum. Clarke, MC; Hutson, JM; Sasaki, Y, 2007) | 0.34 |
" Despite the standardised dosage and standardised blood sampling nifedipine serum levels spread in a wide range." | ( Nifedipine serum levels in pregnant women undergoing tocolysis with nifedipine. Burkhardt, T; Kraehenmann, F; Marin, TZ; Meier, R; Zimmermann, R, 2007) | 2.02 |
"To investigate the effect of nifedipine of therapeutic dosage on the plasma membrane functional integrity and osmosensitive calcium influx in human sperm in vitro." | ( [Nifedipine modifies plasma membrane functional integrity and inhibits osmosensitive calcium influx in human sperm]. Li, HC; Liu, XJ; Mi, ZG; Wang, HY; Xu, JX; Xu, N, 2007) | 1.54 |
" However, the short-acting formulations of nifedipine had pharmacokinetic properties that were far from ideal and in 1995, several studies involving various dosing regimens reported possible dangerous effects in secondary prevention." | ( Nifedipine Gastrointestinal Therapeutic System (GITS) in the treatment of coronary heart disease and hypertension. Dunselman, PH; Kragten, JA, 2007) | 2.05 |
"Previous chronotherapy studies have shown that the circadian pattern of blood pressure (BP) remains unchanged after either morning or evening dosing of several calcium channel blockers (CCB), including amlodipine, isradipine, verapamil, nitrendipine, and cilnidipine." | ( Dose- and administration time-dependent effects of nifedipine gits on ambulatory blood pressure in hypertensive subjects. Ayala, DE; Calvo, C; Chayán, L; Fernández, JR; Fontao, MJ; Hermida, RC; López, JE; Mojón, A; Rodríguez, M, 2007) | 0.59 |
" The objectives of this paper are to analyze the behavior of these turnover models from a mathematical/analytical point of view and to make simulations with different parameter settings and dosing regimens in order to highlight the intrinsic behavior of these models and draw some general conclusions." | ( A nonlinear feedback model capturing different patterns of tolerance and rebound. Gabrielsson, J; Peletier, LA, 2007) | 0.34 |
" NE dose-response curves determined in femoral arteries from PTX-treated WKY rats were shifted to the right compared to those from control WKY." | ( Nifedipine-sensitive vascular reactivity of femoral arteries in WKY: the effects of pertussis toxin pretreatment and endothelium removal. Kunes, J; Líšková, S; Zicha, J, 2007) | 1.78 |
" Recent evidence has established the tolerability and efficacy of once-daily dosage forms, which provide stable plasma nifedipine concentrations, in the management of coronary artery disorders." | ( [Clinical experience with nifedipine in the treatment of angina pectoris in Japan]. Hosoda, S, 2006) | 0.84 |
" It compared the antihypertensive effect between increasing ARB dosage and the addition of controlled-release nifedipine." | ( [NICE-Combi study: effect of nifedipine in combination with an angiotensin II receptor blocker on BP control and renal protection]. Hasebe, N, 2006) | 0.84 |
"GITS dosage titrated to clinical response (30-150 mg/day)." | ( Nifedipine concentration in maternal and umbilical cord blood after nifedipine gastrointestinal therapeutic system for tocolysis. Juon, AM; Kühn-Velten, WN; Silberschmidt, AL; von Mandach, U; Zimmermann, R, 2008) | 1.79 |
"Steady-state plasma nifedipine concentrations after repeated dosing with nifedipine GITS 30-150 mg/day in pregnant women with preterm labour do not exceed 100 micrograms/l; fetal levels are 77% of maternal levels." | ( Nifedipine concentration in maternal and umbilical cord blood after nifedipine gastrointestinal therapeutic system for tocolysis. Juon, AM; Kühn-Velten, WN; Silberschmidt, AL; von Mandach, U; Zimmermann, R, 2008) | 2.11 |
" These results provided some useful information on parameters which can be modulated in the design of a controlled release dosage form for NP." | ( Dissolution kinetics and physical characterization of three-layered tablet with poly(ethylene oxide) core matrix capped by Carbopol. Hong, SI; Oh, SY, 2008) | 0.35 |
"The objective of this study was to compare the in vitro and in vivo characteristics of 2 nifedipine modified-release tablet formulations for once-daily dosing marketed in the European community, which were expected to be bioequivalent." | ( Comparison of two marketed nifedipine modified-release formulations: an exploratory clinical food interaction study. Anschütz, M; Blume, H; Brendel, E; De Nucci, G; Schug, B; Wonnemann, M, 2008) | 0.86 |
"GITS tablets 90 mg/d are an alternative dosage regimen to previous used slow-release tablets 60 mg/d for tocolysis with similar pharmacokinetic profile and a good tolerance." | ( Nifedipine gastrointestinal therapeutic system (GITS) as an alternative to slow-release for tocolysis--tolerance and pharmacokinetic profile. Burkhardt, T; Juon, AM; Krähenmann, F; Kühn-Velten, WN; von Mandach, U; Zimmermann, R, 2008) | 1.79 |
" When each drug was prescribed at a dosage of 20 mg once daily for two weeks, the difference in the copayment for the patient was only 10 yen." | ( Evaluation of zero-order controlled release preparations of nifedipine tablet on dissolution test, together with cost benefit point of view. Matsuyama, K; Naruto, I; Sakurai, M, 2008) | 0.59 |
" Dosing 3 mg/kg/d cediranib for 4 days induced a marked hypertension of 35 to 50 mmHg." | ( Inhibition of vascular endothelial growth factor-a signaling induces hypertension: examining the effect of cediranib (recentin; AZD2171) treatment on blood pressure in rat and the use of concomitant antihypertensive therapy. Curwen, JO; Kendrew, J; Musgrove, HL; Ogilvie, DJ; Richmond, GH; Wedge, SR, 2008) | 0.35 |
"Previous studies have shown that the circadian pattern of blood pressure (BP) remains unchanged after either morning or evening dosing of several calcium-channel blockers (CCBs), including amlodipine, isradipine, verapamil, nitrendipine, and cilnidipine." | ( Chronotherapy with nifedipine GITS in hypertensive patients: improved efficacy and safety with bedtime dosing. Ayala, DE; Fernández, JR; Hermida, RC; Mojón, A, 2008) | 0.67 |
" In all cases the calcium antagonist Nifedipine was used in dosage 4 x 10 mg per os." | ( [Treatment of preterm delivery with calcium channel blockers--Nifedipine]. Diavolov, V; Dimitrov, A; Ivanov, S; Markov, D; Nikolov, A, 2007) | 0.85 |
" Hypertensive patients received daily treatment with an oral dosage of 30 mg nifedipine GITS for 16 days." | ( Arg347Cys polymorphism of alpha1A-adrenoceptor gene is associated with blood pressure response to nifedipine GITS in Chinese hypertensive patients. Hong, X; Huo, Y; Liu, H; Xu, X; Zhang, Y, 2009) | 0.8 |
"The BP reduction after the treatment was significantly greater with bedtime dosing (P<0." | ( Reduction of morning blood pressure surge after treatment with nifedipine GITS at bedtime, but not upon awakening, in essential hypertension. Alonso, I; Ayala, DE; Fernández, JR; Hermida, RC; Mojón, A, 2009) | 0.59 |
" The dosage form related food effects for Coral 60 mg tablets that were previously observed in human bioequivalence studies could be predicted with the two non-compendial dissolution test devices." | ( Comparison of dissolution profiles obtained from nifedipine extended release once a day products using different dissolution test apparatuses. Abrahamsson, B; Axell, M; Garbacz, G; Golke, B; Söderlind, E; Wedemeyer, RS; Weitschies, W, 2009) | 0.61 |
" Overall, a minimal effect of CD dosed as a physical mixture was observed and predicted." | ( Modeling the influence of cyclodextrins on oral absorption of low solubility drugs: II. Experimental validation. Ahmed, I; Carrier, RL; Gamsiz, ED; Miller, L; Thombre, AG, 2010) | 0.36 |
" In both age groups, chronic nifedipine administration reduced neurogenic contractions of isolated superior mesenteric artery, but did not significantly affect the dose-response curve to exogenous noradrenaline in 8-week-old rats." | ( Effect of chronic nifedipine treatment on blood pressure and adrenergic responses of isolated mesenteric artery in young rats with developing spontaneous hypertension. Török, J; Zemančíková, A, 2009) | 0.98 |
" Nifedipine dosage was based on the value of CYP3A4 gene expression." | ( [Methyldopa-induced acute reactive hepatitis in pregnancy, drug-metabolizing capacity of the liver]. Monostory, K; Ozsvár, Z; Solymossi, Z, 2010) | 1.27 |
" To evaluate the contribution of Gi-proteins and L-VDCC to vasoconstriction induced by exogenous norepinephrine, dose-response curves were determined before and after acute nifedipine administration." | ( Role of nifedipine-sensitive sympathetic vasoconstriction in maintenance of high blood pressure in spontaneously hypertensive rats: effect of Gi-protein inactivation by pertussis toxin. Karen, P; Kunes, J; Pintérová, M; Zicha, J, 2010) | 0.99 |
" In both strains, PTX pretreatment as well as acute nifedipine administration caused substantial rightward shift of norepinephrine dose-response curves (without additive effects of both treatments)." | ( Role of nifedipine-sensitive sympathetic vasoconstriction in maintenance of high blood pressure in spontaneously hypertensive rats: effect of Gi-protein inactivation by pertussis toxin. Karen, P; Kunes, J; Pintérová, M; Zicha, J, 2010) | 1.05 |
"The present study was aimed to investigate the effect of food components and dosing time on the oral exposure of nifedipine in rats." | ( Effect of food components and dosing times on the oral pharmacokinetics of nifedipine in rats. Cao, QR; Cui, JH; Han, HK; Lee, BJ; Lee, J; Oh, KT; Park, I; Park, JB, 2010) | 0.8 |
" Two additional groups (nifedipine 10 and 100mg/kg/day) were included to explore a possible dose-response relationship." | ( Effect of nifedipine on gingival enlargement and periodontal breakdown in ligature-induced periodontitis in rats. Fernandes, MI; Gaio, EJ; Oppermann, RV; Rados, PV; Rösing, CK; Susin, C, 2010) | 1.07 |
"The prediction of the in vivo drug release characteristics of modified release (MR) oral dosage forms by in vitro dissolution tests is a prerequisite for successful product development." | ( A biorelevant dissolution stress test device - background and experiences. Garbacz, G; Klein, S; Weitschies, W, 2010) | 0.36 |
"To improve the predictive power of dissolution testing, the authors recently developed a new dissolution test apparatus that simulates physical conditions of the gastrointestinal (GI) passage of MR dosage forms." | ( A biorelevant dissolution stress test device - background and experiences. Garbacz, G; Klein, S; Weitschies, W, 2010) | 0.36 |
" Results of these experiments thus indicated that a high sensitivity of dosage forms to GI-specific physical conditions has to be regarded as a major cause of irregularities in the drug release profiles, which may result in fluctuations of the individual drug plasma concentration profiles, as, for example, caused by dose dumping." | ( A biorelevant dissolution stress test device - background and experiences. Garbacz, G; Klein, S; Weitschies, W, 2010) | 0.36 |
" RPTEC/TERT1 cells were cultured with either the dosing vehicle (DMSO) or with exposure to one of six compounds (nifedipine, potassium bromate, monuron, D-mannitol, ochratoxin A and sodium diclofenac), several of which are known to cause renal effects." | ( Metabolic response to low-level toxicant exposure in a novel renal tubule epithelial cell system. Athersuch, TJ; Cavill, R; Ebbels, TM; Ellis, JK; Jennings, P; Keun, HC; McMorrow, T; Radford, R; Ryan, MP; Slattery, C, 2011) | 0.58 |
" To optimize the dose regimens of these inducers for use in DDI studies, their effect at various doses and dosing durations on the area under the curve (AUC) of multiple probe substrates was simulated using a population-based simulator." | ( Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs. Hayashi, M; Shou, M; Skiles, GL; Xu, Y; Zhou, Y, 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 |
" Over one dosing interval, drug concentrations, clinical data, and genotype for Cytochrome P450 (CYP)3A5 polymorphisms were obtained." | ( A pilot study of the impact of genotype on nifedipine pharmacokinetics when used as a tocolytic. Haas, DM; Jones, DR; McCormick, CL; Quinney, SK; Renbarger, JL, 2012) | 0.64 |
" In this study, we retrospectively investigated data from SSc patients who had undergone therapy with high-dose intravenous N-acetylcysteine (NAC) at a dosage of 15 mg/Kg/h for 5 consecutive hours every 14 days." | ( Long-term N-acetylcysteine therapy in systemic sclerosis interstitial lung disease: a retrospective study. Giovannetti, A; Molinaro, I; Pisarri, S; Rosato, E; Rossi, C; Salsano, F, ) | 0.13 |
" On the other hand, under the condition of Ang II-induced hypertension, administration of a hypotensive dosage of cilnidipine showed no effect on the plasma aldosterone levels, whereas a hypotensive dosage of nifedipine significantly increased the plasma aldosterone levels." | ( L/N-type calcium channel blocker suppresses reflex aldosterone production induced by antihypertensive action. Aritomi, S; Konda, T; Yoshimura, M, 2012) | 0.57 |
" We determined from brand names and dosage forms whether nifedipine was prescribed in an immediate-release or sustained-release formulation." | ( The frequency of prescription of immediate-release nifedipine for elderly patients in Germany: utilization analysis of a substance on the PRISCUS list of potentially inappropriate medications. Abbas, S; Hein, R; Schubert, I; Thürmann, P, 2012) | 0.88 |
" Preincubation with receptor antagonist for M(3) but not for M(2) attenuated contraction significantly, shifting the dose-response curve to the right." | ( The effect of hypercholesterolemia on carbachol-induced contractions of the detrusor smooth muscle in rats: increased role of L-type Ca2+ channels. Balkanci, ZD; Bayrak, S; Erdem, A; Karabulut, I; Karaismailoğlu, S; Pehlivanoğlu, B, 2012) | 0.38 |
"Pregnant women receiving oral nifedipine underwent steady-state pharmacokinetic testing over one dosing interval." | ( Nifedipine pharmacokinetics are influenced by CYP3A5 genotype when used as a preterm labor tocolytic. Caritis, SN; Clark, S; Clay, JM; Haas, DM; Hebert, MF; Quinney, SK; Renbarger, JL; Umans, JG, 2013) | 2.12 |
"Hydrophobic drugs present a challenge due to: (i) adhesion and agglomeration; hence the choice of the suitable processing technique to have the drugs into orally administered dosage forms is critical." | ( In situ lyophilisation of nifedipine directly in hard gelatine capsules. Crum, M; Elkordy, AA; Elkordy, EA; Zarara, M, ) | 0.43 |
"Although continuous intravenous (IV) calcium infusion is recommended for calcium channel blocker (CCB) overdose, its clinical efficacy is inconsistent and the dosage required is unclear." | ( A novel dosing regimen for calcium infusion in a patient of massive overdose of sustained-release nifedipine. Li, GQ; Liu, Y; Wei, LQ; Zhou, H, 2013) | 0.61 |
"49 healthy, white, male subjects received: 60 mg nifedipine and 32 mg candesartan FDC, the loose combination of 60 mg nifedipine GITS and 32 mg candesartan, 60 mg nifedipine GITS alone, or 32 mg candesartan alone in a randomized, non-blinded, 4-period, 4-way crossover design with each dosing following overnight fasting." | ( Investigation of bioequivalence of a new fixed-dose combination of nifedipine and candesartan with the corresponding loose combination as well as the drug-drug interaction potential between both drugs under fasting conditions. Brendel, E; Dietrich, H; Froede, C; Thomas, D; Weimann, B, 2013) | 0.88 |
" When comparing AUC(0-tlast) and Cmax of nifedipine and candesartan after dosing with the loose combination vs." | ( Investigation of bioequivalence of a new fixed-dose combination of nifedipine and candesartan with the corresponding loose combination as well as the drug-drug interaction potential between both drugs under fasting conditions. Brendel, E; Dietrich, H; Froede, C; Thomas, D; Weimann, B, 2013) | 0.89 |
" Moreover, fasudil pretreatment shifted norepinephrine dose-response curves to the right more in WKY than in SHR." | ( Ca2+ sensitization and Ca2+ entry in the control of blood pressure and adrenergic vasoconstriction in conscious Wistar-Kyoto and spontaneously hypertensive rats. Behuliak, M; Bencze, M; Karen, P; Kuneš, J; Líšková, S; Petrová, M; Pintérová, M; Vaněčková, I; Zicha, J, 2013) | 0.39 |
" Though the main criterion for combining drugs in a single dosage form is the rationale, but consideration like stability of formulation is equally important, due to an added aspect of drug-drug interaction." | ( Characterization of a new degradation product of nifedipine formed on catalysis by atenolol: A typical case of alteration of degradation pathway of one drug by another. Handa, T; Singh, IP; Singh, S, 2014) | 0.66 |
" We have recently found that supersaturating dosage forms can exhibit the phenomenon of liquid-liquid phase separation (LLPS)." | ( Enhancements and limits in drug membrane transport using supersaturated solutions of poorly water soluble drugs. Alonzo, DE; Catron, ND; Gao, Y; Raina, SA; Taylor, LS; Wu, J; Zhang, GGZ; Zhu, D, 2014) | 0.4 |
" Another important focus for future trials is identifying optimal dosage regimens of different types of CCBs (high versus low, particularly addressing speed of onset of uterine quiescence) and formulation (capsules versus tablets)." | ( Calcium channel blockers for inhibiting preterm labour and birth. Carbonne, B; Flenady, V; Jardine, LA; Murray, L; Papatsonis, DN; Stock, OM; Wojcieszek, AM, 2014) | 0.4 |
"To investigate the influence of co-administrated Da-Chaihu-Tang (DCT; a traditional Chinese formulation) on the pharmacokinetics of nifedipine, as well as the safe optimal dosing interval to avoid the adverse interactions." | ( Da-Chaihu-Tang alters the pharmacokinetics of nifedipine in rats and a treatment regimen to avoid this. Akao, T; Hattori, M; He, JX; Ohno, K; Tang, J; Tani, T, 2014) | 0.86 |
" Further study on the optimal dosing interval for nifedipine and DCT revealed that administration of DCT 30 min before or after nifedipine did not significantly change the AUC of nifedipine." | ( Da-Chaihu-Tang alters the pharmacokinetics of nifedipine in rats and a treatment regimen to avoid this. Akao, T; Hattori, M; He, JX; Ohno, K; Tang, J; Tani, T, 2014) | 0.91 |
"DISTINCT (reDefining Intervention with Studies Testing Innovative Nifedipine GITS - Candesartan Therapy) aimed to determine the dose-response and tolerability of nifedipine GITS and/or candesartan cilexetil therapy in participants with hypertension." | ( Nifedipine plus candesartan combination increases blood pressure control regardless of race and improves the side effect profile: DISTINCT randomized trial results. Cha, G; Gil-Extremera, B; Haller, H; Harvey, P; Heyvaert, F; Kjeldsen, SE; Lewin, AJ; Mancia, G; Sica, D; Villa, G, 2014) | 2.08 |
" A positive dose-response was observed, with all combinations providing statistically better blood pressure (BP) reductions from baseline versus respective monotherapies (P < 0." | ( Nifedipine plus candesartan combination increases blood pressure control regardless of race and improves the side effect profile: DISTINCT randomized trial results. Cha, G; Gil-Extremera, B; Haller, H; Harvey, P; Heyvaert, F; Kjeldsen, SE; Lewin, AJ; Mancia, G; Sica, D; Villa, G, 2014) | 1.85 |
" Measurements at 20-60 and 61-120 min were compared to assess the differential effects of dosing on hemodynamics and reflected the effects of the initial and complete loading doses, respectively." | ( Hemodynamic effects of nifedipine tocolysis. Burlingame, J; Kaneshiro, B; Yamasato, K, 2015) | 0.73 |
"001), but differential dosing effects were not observed." | ( Hemodynamic effects of nifedipine tocolysis. Burlingame, J; Kaneshiro, B; Yamasato, K, 2015) | 0.73 |
" The maintenance dosage was 20 mg of oral nifedipine administered every 6 hours for 48 hours, for a total dose of 80 mg/day." | ( The effect of nifedipine tocolysis on Doppler indices of the uterine and umbilical arteries. Kaya, C; Özmen Bayar, Ü; Ulubaşoğlu, H; Ungan, B, 2015) | 1.04 |
" In all cases the calcium antagonist Nifedipine was used in dosage 4 x 10 mg per os." | ( [Tocolysis with nifedipin; its use in current practice]. Dimitrov, G; Ivanov, S; Jordanova, D; Karamisheva, V; Marinov, B; Nachev, A, 2014) | 0.68 |
" It is a major determinant of half-life and dosing frequency of a drug." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
"Literature data relevant to the biopharmaceutical properties of the active pharmaceutical ingredient (API) nifedipine are reviewed to evaluate whether a waiver of in vivo bioequivalence (BE) testing of immediate-release (IR) dosage forms formulated as tablets and soft gelatin capsules is warranted." | ( Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Nifedipine. Abrahamsson, B; Cristofoletti, R; Dressman, JB; Gajendran, J; Groot, DW; Krämer, J; Langguth, P; Mehta, M; Polli, J; Shah, VP, 2015) | 0.87 |
" Water-soluble and water-dispersible surfactants are able to dissolve the target dose of each drug in the dosage form and efficiently keep it in solution during dispersion." | ( Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity. Belotti, S; Chavant, Y; Chevrier, S; Demarne, F; Dumont, C; Jannin, V; Michenaud, M, 2015) | 0.42 |
"With the increased reliance on in vitro dissolution testing as an indicator of in vivo drug behavior and the trend towards the in silico modeling of dosage form performance, the need for bioperformance dissolution methodology development has been enhanced." | ( Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect. Ilić, M; Kovačević, I; Parojčić, J, 2015) | 0.8 |
" Media composition was varied in terms of pH and content, to mimic the dosage form intake with water or non-alcoholic beverages (orange juice) and alcoholic beverages (orange juice/ethanol mixture (47% v/v))." | ( An in vitro-in vivo correlation study for nifedipine immediate release capsules administered with water, alcoholic and non-alcoholic beverages: Impact of in vitro dissolution media and hydrodynamics. Bresciani, M; Fares, R; Fotaki, N; Mercuri, A, 2016) | 0.7 |
" A trend to dose-response relationship was observed in each subgroup." | ( Nifedipine GITS/Candesartan Combination Therapy Lowers Blood Pressure Across Different Baseline Systolic and Diastolic Blood Pressure Categories: DISTINCT Study Subanalyses. Cha, G; Kjeldsen, SE; Mancia, G; Villa, G, 2016) | 1.88 |
" On top of the previous stable treatment regimen (which excluded calcium-channel blockers), a 10 mg dosing of barnidipine hydrochloride at bedtime was added to all subjects during a 12-week period." | ( Effect of bedtime dosing of barnidipine hydrochloride in non-dipper hypertensive patients with obstructive sleep apnoea not treated with continuous positive airway pressure. Bravi, E; Cassi, A; Crippa, G; Zabzuni, D, 2016) | 0.43 |
"Bedtime dosing of the calcium-channel blocker (CCB) barnidipine significantly reduced mean nighttime systolic and diastolic ABP in hypertensive patients presenting with non-dipper pattern and OSA--not on CPAP treatment." | ( Effect of bedtime dosing of barnidipine hydrochloride in non-dipper hypertensive patients with obstructive sleep apnoea not treated with continuous positive airway pressure. Bravi, E; Cassi, A; Crippa, G; Zabzuni, D, 2016) | 0.43 |
"Food intake is known to have various effects on gastrointestinal luminal conditions in terms of transit times, hydrodynamic forces and/or luminal fluid composition and can therefore affect the dissolution behavior of solid oral dosage forms." | ( Can dosage form-dependent food effects be predicted using biorelevant dissolution tests? Case example extended release nifedipine. Andreas, CJ; Dressman, JB; Mueck, W; Muenster, U; Tomaszewska, I; van der Mey, D, 2016) | 0.64 |
" Using Level II biorelevant media the dosage form dependent food effect for nifedipine was described well when studied with the USP apparatus III, whereas the USP apparatus IV failed to detect the positive food effect for the matrix-type dosage form." | ( Can dosage form-dependent food effects be predicted using biorelevant dissolution tests? Case example extended release nifedipine. Andreas, CJ; Dressman, JB; Mueck, W; Muenster, U; Tomaszewska, I; van der Mey, D, 2016) | 0.87 |
"Nifedipine (NIF) is a typical light-sensitive drug requiring protection from light during manufacture, storage, and handling of its dosage forms." | ( Photostable Solid Dispersion of Nifedipine by Porous Calcium Silicate. Fujimoto, Y; Hirai, N; Takahashi, K; Takatani-Nakase, T, 2016) | 2.16 |
" It was concluded that the formulated nifedipine pulsatile dosage form could be useful in the treatment of hypertension." | ( Development and Characterization Pulsatile Microspheres of Nifedipine for Hypertension. Gupta, GD; Taneja, R, 2017) | 0.97 |
" This study examined the validity of the assumption that these interchangeable, but different, delivery technologies are therapeutically equivalent in maintaining systolic blood pressure (SBP) control throughout the entire dosing interval." | ( Therapeutic Differences in 24-h Ambulatory Blood Pressures in Patients Switched Between Bioequivalent Nifedipine Osmotic Systems With Differing Delivery Technologies. Feldman, RD; Herman, RJ; Pollak, PT, 2017) | 0.67 |
"The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug." | ( Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form. Dorożyński, P; Garbacz, G; Haznar-Garbacz, D; Kaminska, E; Kaminski, K; Kulinowski, P; Lachmann, M; Zakowiecki, D, 2018) | 0.68 |
"Drug half-life has important implications for dosing regimen and peak-to-trough ratio at the steady state." | ( Relevance of Half-Life in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2018) | 0.48 |
" Nifedipine and irbesartan were taken after discharge, and the dosage was reduced gradually under supervision." | ( Hypertensive crisis with 2 target organ impairment induced by glycyrrhizin: A case report. Fan, X; Li, J; Wang, Q, 2018) | 1.39 |
"In contrast to nifedipine matrix-based extended-release dosage forms, the osmotic pump drug delivery systems have a zero-order drug release independent of external variables such as pH, agitation rate, and dissolution media." | ( Effects of Dissolution Medium pH and Simulated Gastrointestinal Contraction on Drug Release From Nifedipine Extended-Release Tablets. Gao, Z; Jiang, W; Keire, D; Ngo, C; Rodriguez, JD; Sun, D; Wen, H; Ye, W, 2019) | 1.08 |
" Oral Nifedipine may be a better alternative because of its ease of oral administration and a flat dosing regimen." | ( IV labetalol and oral nifedipine in acute control of severe hypertension in pregnancy-A randomized controlled trial. Sowjanya, R; Tatapudi, R; Zulfeen, M, 2019) | 1.31 |
"Dissolution experiments were designed to reflect clinical practice in a paediatric hospital, with respect to dosage forms, feeding regimens and methods of administration." | ( Potential prediction of formulation performance in paediatric patients using biopharmaceutical tools and simulation of clinically relevant administration scenarios of nifedipine and lorazepam. Fotaki, N; Hanff, LM; Van der Vossen, AC; Vulto, AG, 2019) | 0.71 |
" OXTRrisk-allele dosage was associated with more severe autism diagnostics observation schedule (ADOS) scores only in the OXTRA group." | ( Cumulative Risk of the Oxytocin Receptor Gene Interacts with Prenatal Exposure to Oxytocin Receptor Antagonist to Predict Children's Social Communication Development. Feldstein, O; Friedlander, E; Harel-Gadassi, A; Israel, S; Laiba, E; Mankuta, D; Yaari, M; Yirmiya, N, 2019) | 0.51 |
" If BP is not at goal during 4 week's visit, dosage of antihypertensive agents will be doubled." | ( A comparative study for the effects of nifedipine GITS and amlodipine besylate administrated in daytime or at nighttime on recovery of blood pressure rhythm and arterial stiffness in the young and middle-aged subjects with non-dipper hypertension (NARRAS) Liu, J, 2020) | 0.83 |
"Proton pump inhibitors (PPIs) can affect the intragastric release of other drugs from their dosage forms by elevating the gastric pH." | ( Physiologically Based Pharmacokinetic Modeling Approach to Identify the Drug-Drug Interaction Mechanism of Nifedipine and a Proton Pump Inhibitor, Omeprazole. Babiskin, A; Le Merdy, M; Lee, SC; Ni, Z; Sun, D; Tan, ML; Zhao, L, 2021) | 0.83 |
" The objective of the current work was to design a rapidly dissolving solid dosage formulation for the treatment of AD as an alternative to the off-license "bite and swallow" use of currently available commercial products." | ( Design and characterisation of an amorphous formulation of nifedipine for the treatment of autonomic dysreflexia. Browne, E; Cheyne, S; Healy, AM; Quinn, S, 2021) | 0.86 |
" The current investigations clarified the efficiency of this novel and unique NF loaded in situ gel for the control of the IOP compared to the conventional ophthalmic dosage forms." | ( Repurposing of nifedipine loaded in situ ophthalmic gel as a novel approach for glaucoma treatment. Ahmed, KA; El-Feky, YA; El-Telbany, DFA; El-Telbany, RFA; Fares, AR; Zayed, G, 2021) | 0.97 |
"This research study utilized a light-sensitive drug, nifedipine (NFD), to understand the impact of processing parameters and formulation composition on drug degradation, crystallinity, and quality attributes (dimensions, hardness, disintegration time) of selective laser sintering (SLS)-based three-dimensional (3D)-printed dosage forms." | ( Selective Laser Sintering of a Photosensitive Drug: Impact of Processing and Formulation Parameters on Degradation, Solid State, and Quality of 3D-Printed Dosage Forms. Davis, DA; Maniruzzaman, M; Thakkar, R; Williams, RO, 2021) | 0.87 |
" However, antihypertensive drugs lack pregnancy-specific dosing recommendations due to critical knowledge gaps surrounding the extent of gestational changes in antihypertensive drug pharmacokinetics and underlying mechanisms." | ( The Impact of Pregnancy on Antihypertensive Drug Metabolism and Pharmacokinetics: Current Status and Future Directions. Daubert, MA; Fashe, MM; Garcia, JE; Lee, CR; Loop, MS; Mulrenin, IR; Urrutia, RP, 2021) | 0.62 |
"This review (1) summarizes currently recommended medications and dosing strategies for non-emergent HDP treatment, (2) reviews and synthesizes existing literature identified via a comprehensive PubMed search evaluating gestational changes in the maternal pharmacokinetics of commonly prescribed HDP drugs (notably labetalol and nifedipine), and (3) offers insight into the metabolism and clearance mechanisms underlying altered HDP drug pharmacokinetics during pregnancy." | ( The Impact of Pregnancy on Antihypertensive Drug Metabolism and Pharmacokinetics: Current Status and Future Directions. Daubert, MA; Fashe, MM; Garcia, JE; Lee, CR; Loop, MS; Mulrenin, IR; Urrutia, RP, 2021) | 0.79 |
" Future research is needed to address various evidence gaps and inform the development of more precise antihypertensive drug dosing strategies." | ( The Impact of Pregnancy on Antihypertensive Drug Metabolism and Pharmacokinetics: Current Status and Future Directions. Daubert, MA; Fashe, MM; Garcia, JE; Lee, CR; Loop, MS; Mulrenin, IR; Urrutia, RP, 2021) | 0.62 |
" Extended-release (ER) solid oral dosage forms are normally subjected to physical shear and grinding forces as well as pressure exerted by peristaltic movements when passing through the GI tract." | ( An In Vitro Dissolution Method for Testing Extended-Release Tablets Under Mechanical Compression and Sample Friction. Cao, LNY; Gao, Z; Liu, X; Rodriguez, JD; Tian, L, 2022) | 0.72 |
"This network meta-analysis aimed to compare the efficacy and safety of intravenous (IV) hydralazine, oral nifedipine, and IV labetalol with different dosage regimens in the treatment of severe hypertension during pregnancy." | ( Different dosage regimens of nifedipine, labetalol, and hydralazine for the treatment of severe hypertension during pregnancy: a network meta-analysis of randomized controlled trials. Cheng, Y; Jiang, YF; Li, JB; Wu, HZ; Yu, D; Zhu, ZN, 2022) | 1.23 |
" In comparison with the reference level, it was observed that the dosage of nifedipine should be reduced with the maximum boundary value of PTH, after a Monte Carlo simulation." | ( Population Pharmacokinetic Modelling for Nifedipine to Evaluate the Effect of Parathyroid Hormone on CYP3A in Patients with Chronic Kidney Disease. Fu, C; Guo, C; Li, W; Liang, W; Liu, J; Pei, Q; Tan, H; Yang, B; Yang, G; Zhang, H, 2022) | 1.22 |
" Aiming for evidence-based and personalized dosing of antihypertensive medication in the future, further studies on the relationship of both PK and pharmacodynamics (including the optimal blood pressure targeting) during pregnancy and pregnancy-related pathology are urgently needed to prevent undertreatment, overtreatment, and side effects." | ( Pharmacokinetics of the most commonly used antihypertensive drugs throughout pregnancy methyldopa, labetalol, and nifedipine: a systematic review. Allegaert, K; Flint, RB; Mian, P; Schoenmakers, S; van de Vusse, D; Versmissen, J; Visser, W, 2022) | 0.93 |
" Blood samples were collected before dosing and up to 72 hours after administration." | ( Pharmacokinetics and Bioequivalence of 2 Nifedipine Controlled-Release Tablets: A Randomized, Single-Dose, 2-Period Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions. Chen, D; Chen, Q; Jia, J; Li, Y; Liu, Y; Wang, W; Wu, Q; Xin, L; Yu, C; Zou, Y, 2023) | 1.18 |
"Oral extended-release (ER) dosage forms have been used to sustain blood drug levels, reduce adverse events, and improve patient compliance." | ( Effect of Omeprazole Administration on the Pharmacokinetics of Oral Extended-Release Nifedipine in Healthy Subjects. Feng, K; Kinjo, M; Lionberger, R; Sun, D; Tan, ML; Wang, H; Xu, M; Zhao, L, 2023) | 1.13 |
" Therapy success: systolic blood pressure ~140 mm Hg and diastolic blood pressure ~90 mm Hg, therapy failure: persistent systolic blood pressure ≥ 160 or diastolic blood pressure ≥ 110 mm Hg after maximum dosage of therapy (EL)." | ( Comparison of outcomes following intravenous magnesium compared with intravenous labetalol and oral nifedipine in 355 pregnant Han Chinese women with preeclampsia. Dong, W; Peng, Z; Xiao, Y; Zhang, J, 2023) | 1.13 |
Role | Description |
---|---|
calcium channel blocker | One of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools. |
vasodilator agent | A drug used to cause dilation of the blood vessels. |
tocolytic agent | Any compound used to suppress premature labour and immature birth by suppressing uterine contractions. |
human metabolite | Any mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens). |
[role 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] |
Class | Description |
---|---|
dihydropyridine | |
methyl ester | Any carboxylic ester resulting from the formal condensation of a carboxy group with methanol. |
C-nitro compound | A nitro compound having the nitro group (-NO2) attached to a carbon atom. |
[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 |
---|---|---|
Nifedipine Action Pathway | 47 | 8 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.1220 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 39.3099 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 0.3548 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 12.7415 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
Chain A, HADH2 protein | Homo sapiens (human) | Potency | 19.8162 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 19.8162 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 56.2341 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 21.1328 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 39.9800 | 0.0072 | 15.7588 | 89.3584 | AID1224835 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 32.5185 | 0.1000 | 20.8793 | 79.4328 | AID488773; AID588453; AID588456 |
pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 70.7946 | 0.0251 | 27.9203 | 501.1870 | AID651751 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 30.2483 | 0.1413 | 37.9142 | 100.0000 | AID1490; AID2701 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 55.0284 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 40.3464 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 12.2892 | 0.0041 | 10.8903 | 31.5287 | AID493106; AID493107; AID504467 |
Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 35.4813 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
NFKB1 protein, partial | Homo sapiens (human) | Potency | 11.2202 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
GLS protein | Homo sapiens (human) | Potency | 12.5893 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
TDP1 protein | Homo sapiens (human) | Potency | 12.2096 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 19.5062 | 0.0007 | 14.5928 | 83.7951 | AID1259368; AID1259369; AID1259392 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 11.4380 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
Thrombopoietin | Homo sapiens (human) | Potency | 1.5849 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
AR protein | Homo sapiens (human) | Potency | 52.5849 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID588515; AID743035; AID743036; AID743042; AID743054; AID743063 |
Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 20.2638 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 0.6675 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 0.1585 | 0.0013 | 18.0743 | 39.8107 | AID926 |
hypothetical protein, conserved | Trypanosoma brucei | Potency | 16.7059 | 0.2239 | 11.2451 | 35.4813 | AID624147; AID624173 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 22.2322 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839 |
progesterone receptor | Homo sapiens (human) | Potency | 24.0357 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 27.2039 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.7090 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 63.0957 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 29.7322 | 0.0002 | 14.3764 | 60.0339 | AID588533; AID720691; AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 40.8347 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 53.8132 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531; AID588544 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 41.6059 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224848; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 19.9418 | 0.3758 | 27.4851 | 61.6524 | AID588526; AID588527; AID743217 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 56.2341 | 0.0054 | 28.0263 | 1,258.9301 | AID720659 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 31.9956 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID588514; AID743069; AID743075; AID743079; AID743080; AID743091 |
G | Vesicular stomatitis virus | Potency | 4.8975 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 38.9018 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
67.9K protein | Vaccinia virus | Potency | 13.1335 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
Parkin | Homo sapiens (human) | Potency | 20.7329 | 0.8199 | 14.8306 | 44.6684 | AID720572; AID720573 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 39.8107 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 38.2776 | 0.0010 | 24.5048 | 61.6448 | AID588534; AID588535; AID743212; AID743215 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 32.9838 | 0.0010 | 19.4141 | 70.9645 | AID588536; AID588537 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 53.0336 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223; AID743241 |
IDH1 | Homo sapiens (human) | Potency | 5.1735 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 8.2015 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 58.4789 | 0.0165 | 25.3078 | 41.3999 | AID602332 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 12.2800 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 47.6313 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 54.5381 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 38.9571 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 28.8828 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
beta-2 adrenergic receptor | Homo sapiens (human) | Potency | 28.1838 | 0.0058 | 6.0263 | 32.6427 | AID492947 |
Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 3.9811 | 0.5406 | 17.6392 | 96.1227 | AID2364; AID2528 |
cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0020 | 7.5337 | 39.8107 | AID891 |
peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 75.6863 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 12.4435 | 31.6228 | AID924 |
tumor necrosis factor | Homo sapiens (human) | Potency | 10.5909 | 0.3758 | 23.4928 | 42.1632 | AID651757 |
polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 27.0050 | 1.0000 | 12.2326 | 31.6228 | AID1452 |
cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 11.8961 | 0.0025 | 5.8400 | 31.6228 | AID899 |
cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 23.7359 | 0.0063 | 6.9043 | 39.8107 | AID883 |
D(1A) dopamine receptor | Homo sapiens (human) | Potency | 17.1078 | 0.0224 | 5.9449 | 22.3872 | AID488982; AID488983 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 18.4176 | 0.0018 | 15.6638 | 39.8107 | AID894 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 11.9885 | 0.3548 | 28.0659 | 89.1251 | AID504847; AID602199; AID602200; AID602201; AID602202 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 19.1499 | 0.0060 | 26.1688 | 89.1251 | AID488953; AID540317 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 27.8707 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 49.0441 | 0.0420 | 27.3789 | 61.6448 | AID743210 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 32.4648 | 0.0398 | 16.7842 | 39.8107 | AID1454; AID995 |
atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 13.0918 | 0.0066 | 9.8094 | 18.4927 | AID1347050 |
serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 16.4816 | 0.0037 | 8.6189 | 23.2809 | AID2660 |
serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 4.7444 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
eyes absent homolog 2 isoform a | Homo sapiens (human) | Potency | 10.6928 | 1.1998 | 14.6419 | 50.1187 | AID720540 |
histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 44.9647 | 0.0103 | 23.8567 | 63.0957 | AID2662 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 59.5858 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID720636; AID743202 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 39.8107 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 1.2589 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
plasminogen precursor | Mus musculus (house mouse) | Potency | 1.2589 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 1.2589 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 16.3730 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
geminin | Homo sapiens (human) | Potency | 26.7801 | 0.0046 | 11.3741 | 33.4983 | AID463097; AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 18.1056 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 17.9199 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 12.8127 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 38.7482 | 0.1778 | 24.7352 | 79.4328 | AID488949 |
muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 0.0010 | 6.0009 | 35.4813 | AID944 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.7546 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 10.0000 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 17.2465 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 4.8975 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.8975 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 51.0755 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Integrin beta-3 | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 11.4157 | 31.6228 | AID924 |
Integrin alpha-IIb | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 11.4157 | 31.6228 | AID924 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 17.2465 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 20.3019 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 66.8242 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 10.4510 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
C-terminal-binding protein 1 | Homo sapiens (human) | Potency | 10.6928 | 0.3014 | 9.3210 | 19.0148 | AID720541 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.8975 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 24.0084 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 16.4661 | 0.0119 | 12.2221 | 68.7989 | AID588378; AID651632 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 12.8127 | 1.0000 | 12.2248 | 31.6228 | AID885 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.8975 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.8492 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
[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) |
---|---|---|---|---|---|---|---|
perilipin-5 | Homo sapiens (human) | IC50 (µMol) | 7.1330 | 0.9850 | 3.4565 | 9.4680 | AID504319 |
perilipin-1 | Homo sapiens (human) | IC50 (µMol) | 9.6190 | 0.9250 | 3.3033 | 9.6190 | AID504317 |
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform a | Homo sapiens (human) | IC50 (µMol) | 8.3760 | 0.9250 | 3.5828 | 9.6190 | AID504317; AID504319 |
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 16.6000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0429 | 0.0220 | 1.6422 | 8.9000 | AID1207670; AID1207672; AID1207673 |
Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 (µMol) | 7.3567 | 0.0003 | 2.6311 | 9.0000 | AID1207191; AID1207754; AID1581330 |
Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | Ki | 0.0147 | 0.0054 | 0.0116 | 0.0150 | AID1466481 |
Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 (µMol) | 45.4000 | 0.4000 | 2.7500 | 8.6000 | AID1209456 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 18.2730 | 0.0001 | 1.0076 | 8.7800 | AID625218 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 9.5720 | 0.0000 | 0.8871 | 10.0000 | AID625218 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 45.5875 | 0.1100 | 7.1903 | 10.0000 | AID1209455; AID1443986; AID1449628; AID1473738 |
Glutathione reductase, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 23.4000 | 1.0000 | 4.5500 | 8.1000 | AID617311 |
Glutathione reductase, mitochondrial | Homo sapiens (human) | Ki | 17.4000 | 0.8000 | 3.4500 | 6.1000 | AID617312 |
Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 0.3000 | 0.0001 | 1.7740 | 10.0000 | AID625245 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 292.5000 | 0.0002 | 2.3185 | 10.0000 | AID681153; AID681335 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 28.4947 | 0.0001 | 1.7536 | 10.0000 | AID428564; AID54753 |
Adenosine receptor A3 | Homo sapiens (human) | IC50 (µMol) | 7.2140 | 0.0000 | 1.8940 | 8.5470 | AID625196 |
Adenosine receptor A3 | Homo sapiens (human) | Ki | 7.6645 | 0.0000 | 0.9306 | 10.0000 | AID34125; AID34564; AID625196 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 3.0600 | 0.0000 | 2.8005 | 10.0000 | AID1210069 |
Polyunsaturated fatty acid lipoxygenase ALOX15 | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 15.1010 | 0.1100 | 3.2641 | 9.0330 | AID625146 |
5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0004 | 0.9086 | 10.0000 | AID54753 |
5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 0.0010 | 0.0001 | 0.6017 | 10.0000 | AID56027 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 7.2140 | 0.0002 | 1.8742 | 10.0000 | AID625196 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 4.0780 | 0.0001 | 0.9490 | 10.0000 | AID625196 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0385 | 0.0013 | 2.2495 | 6.9000 | AID1207672; AID1207673 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 0.0008 | 0.5796 | 5.4000 | AID45781; AID95580 |
Potassium voltage-gated channel subfamily A member 5 | Homo sapiens (human) | IC50 (µMol) | 6.1000 | 0.0300 | 3.7300 | 9.0000 | AID411890 |
3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.1200 | 0.0042 | 7.4680 | 21.1000 | AID2073 |
Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 18.5940 | 0.0009 | 1.2304 | 10.0000 | AID625229 |
Voltage-dependent L-type calcium channel subunit alpha-1D | Rattus norvegicus (Norway rat) | Ki | 0.0039 | 0.0008 | 0.7410 | 5.4000 | AID45781; AID95580 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 (µMol) | 18.2730 | 0.0001 | 1.0302 | 9.0000 | AID625218 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 9.5720 | 0.0001 | 0.9549 | 10.0000 | AID625218 |
Indoleamine 2,3-dioxygenase 1 | Mus musculus (house mouse) | IC50 (µMol) | 46.0000 | 0.0060 | 1.6251 | 10.0000 | AID717846 |
Adenosine receptor A2a | Homo sapiens (human) | Ki | 96.1333 | 0.0000 | 1.0609 | 9.7920 | AID34237; AID34238; AID34239 |
Adenosine receptor A1 | Homo sapiens (human) | IC50 (µMol) | 7.7010 | 0.0002 | 0.6818 | 7.7010 | AID625194 |
Adenosine receptor A1 | Homo sapiens (human) | Ki | 4.4920 | 0.0002 | 0.9316 | 10.0000 | AID625194 |
Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 14.1000 | 0.0002 | 1.4940 | 10.0000 | AID33788 |
3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.1200 | 0.0003 | 7.3294 | 21.1000 | AID2073 |
Sodium channel protein type 1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0023 | 2.8296 | 9.0000 | AID1207162 |
Sodium channel protein type 4 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0001 | 3.5075 | 10.0000 | AID1207162 |
C-C chemokine receptor type 2 | Homo sapiens (human) | IC50 (µMol) | 2.1910 | 0.0000 | 0.6736 | 6.6990 | AID625237 |
C-C chemokine receptor type 2 | Homo sapiens (human) | Ki | 0.8470 | 0.0020 | 0.8427 | 6.3096 | AID625237 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 7.2140 | 0.0000 | 1.8194 | 10.0000 | AID625196 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 4.0780 | 0.0000 | 0.9650 | 10.0000 | AID625196 |
Cytochrome P450 2J2 | Homo sapiens (human) | IC50 (µMol) | 3.0600 | 0.0120 | 2.5312 | 9.4700 | AID1210069 |
Sodium channel protein type 7 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0360 | 3.7335 | 9.0000 | AID1207162 |
Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 (µMol) | 5.8550 | 0.0003 | 2.5955 | 9.0000 | AID1141116; AID1207191; AID1207754; AID1581330 |
Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | Ki | 0.0147 | 0.0054 | 0.0288 | 0.1030 | AID1466481 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Mus musculus (house mouse) | IC50 (µMol) | 1.2000 | 1.2000 | 1.2000 | 1.2000 | AID339173 |
Voltage-dependent L-type calcium channel subunit alpha-1S | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 0.0008 | 0.6673 | 5.4000 | AID45781; AID95580 |
Voltage-dependent L-type calcium channel subunit alpha-1S | Mus musculus (house mouse) | IC50 (µMol) | 1.2000 | 1.2000 | 1.2000 | 1.2000 | AID339173 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 125.9125 | 0.0009 | 1.9014 | 10.0000 | AID1207221; AID161281; AID240820; AID243151; AID408340; AID576612 |
Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 (µMol) | 7.3567 | 0.0003 | 2.6311 | 9.0000 | AID1207191; AID1207754; AID1581330 |
Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | Ki | 0.0147 | 0.0054 | 0.0116 | 0.0150 | AID1466481 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 (µMol) | 3.6995 | 0.0003 | 2.2545 | 9.6000 | AID1207191; AID1207670; AID1207672; AID1207673; AID1207754; AID1581330 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | Ki | 0.0101 | 0.0003 | 0.0072 | 0.0150 | AID1466481; AID56027 |
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.2300 | 1.9814 | 9.0000 | AID1912032 |
Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0003 | 3.6484 | 9.2000 | AID1207162 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | IC50 (µMol) | 2.0200 | 0.0220 | 2.4133 | 10.0000 | AID1248192 |
Sodium channel protein type 9 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0060 | 2.7749 | 9.0000 | AID1207162 |
Potassium channel subfamily K member 2 | Bos taurus (cattle) | IC50 (µMol) | 8.2000 | 0.4300 | 2.5760 | 8.2000 | AID1307729 |
Indoleamine 2,3-dioxygenase 2 | Mus musculus (house mouse) | IC50 (µMol) | 1.5000 | 1.5000 | 5.0875 | 8.2000 | AID717845 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
Voltage-dependent L-type calcium channel subunit alpha-1D | Mus musculus (house mouse) | IC50 (µMol) | 1.2000 | 1.2000 | 1.2000 | 1.2000 | AID339173 |
Sodium channel protein type 2 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0000 | 3.7401 | 10.0000 | AID1207162 |
Voltage-dependent L-type calcium channel subunit alpha-1F | Mus musculus (house mouse) | IC50 (µMol) | 1.2000 | 1.2000 | 1.2000 | 1.2000 | AID339173 |
Sodium channel protein type 3 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0053 | 2.8085 | 9.0000 | AID1207162 |
Sodium channel protein type 11 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0300 | 4.3695 | 9.0000 | AID1207162 |
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 50.5000 | 0.0040 | 1.9666 | 10.0000 | AID1873207 |
Sodium channel protein type 8 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0011 | 3.4705 | 9.0000 | AID1207162 |
Sodium channel protein type 10 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 37.0000 | 0.0080 | 3.1752 | 9.0000 | AID1207162 |
[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) |
---|---|---|---|---|---|---|---|
Potassium channel subfamily K member 2 | Homo sapiens (human) | EC50 (µMol) | 8.1800 | 0.1870 | 2.7224 | 8.1800 | AID1802150 |
Transient receptor potential cation channel subfamily A member 1 | Mus musculus (house mouse) | EC50 (µMol) | 0.4000 | 0.4000 | 2.7714 | 10.0000 | AID482149 |
[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) |
---|---|---|---|---|---|---|---|
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | ID50 | 700,000.0050 | 0.0001 | 0.0051 | 0.0100 | AID76980; AID76985 |
Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | ID50 | 700,000.0050 | 0.0001 | 0.0051 | 0.0100 | AID76980; AID76985 |
Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | ID50 | 700,000.0050 | 0.0001 | 0.0051 | 0.0100 | AID76980; AID76985 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | ID50 | 700,000.0050 | 0.0001 | 0.0051 | 0.0100 | AID76980; AID76985 |
Phospholipase A2, membrane associated | Homo sapiens (human) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | ID50 | 700,000.0050 | 0.0001 | 0.0051 | 0.0100 | AID76980; AID76985 |
Platelet-activating factor receptor | Homo sapiens (human) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
Leukotriene B4 receptor 1 | Homo sapiens (human) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
Leukotriene B4 receptor 2 | Homo sapiens (human) | ID50 | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID76985 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
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. |
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. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
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. |
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. |
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. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
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. |
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. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
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. |
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. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1184074 | Solubility of the compound in pH 6.5 phosphate buffer containing 5% DMSO | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
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] | |||
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). |
AID764468 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced mortality at 30 mg/kg administered 1 hr prior to pentylenetetrazole challenge measured for 300 secs relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and evaluation of dialkyl 4-(benzo[d][1,3]dioxol-6-yl)-1,4-dihydro-2,6-dimethyl-1-substituted pyridine-3,5-dicarboxylates as potential anticonvulsants and their molecular properties prediction. |
AID78672 | Concentration required to depress contraction in the Langendorff-perfused guinea pig heart | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists. |
AID1612582 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig ileum | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
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. |
AID482865 | Inhibition of K(+)-induced intracellular Ca2+ uptake in human SH-SY5Y cells after 1 hr by Flou/AM fluorescence assay relative to control | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
AID540227 | Volume of distribution at steady state in monkey 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. |
AID550025 | Ratio of chlorpromazine IC50 to compound IC50 for human recombinant calmodulin | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
AID1248197 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 3 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID434299 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 180 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID338204 | Inhibition of adenosine A2 receptor at 10 uM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID332366 | Vasorelaxation activity in SHR rat assessed as reduction of Bay-K 8644-induced mean arterial blood pressure at 5 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
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). |
AID1070215 | Inhibition of Trichomonas vaginalis uridine nucleoside ribohydrolase using 5-fluorouridine as substrate at 0.04 to 200 uM after 40 mins by NMR spectrometric analysis | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID76669 | [Ca2+] antagonistic activity on contraction in guinea pig atria. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
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). |
AID1141131 | Neuroprotective activity against oxygen-glucose deprivation induced-oxidative stress in rat hippocampal slices assessed as maximum protection treated at 10 uM during 120 mins of reoxygenation period by MTT assay (Rvb =40%) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID1918194 | Lipophilicity, log D of the compound | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment. |
AID317289 | Chronotropic activity at L type calcium channel in guinea pig right atrium assessed as decrease in spontaneous beating | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1587142 | Inhibition of voltage-dependent L-type calcium channel in human SH-SY5Y cells assessed as protection against glutamate-induced excitotoxicity by measuring recovery of cell viability at 20 uM measured after 24 hrs by alamar blue-based fluorescence method r | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
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 |
AID32018 | Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA. | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | 6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists. |
AID165447 | Inhibition of electrically stimulated rabbit left atria contraction. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID681586 | TP_TRANSPORTER: quantitative PCR in vivo, liver of mouse | 2003 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 31, Issue:11 | Induction of ABCC3 (MRP3) by pregnane X receptor activators. |
AID1211796 | Intrinsic clearance in cryopreserved human HepaRG cells assessed per 10'6 cells 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. |
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. |
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. |
AID1193497 | Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID338207 | Inhibition of nicotinic acetylcholine receptor at 10 uM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID339173 | Antagonist activity at voltage-dependent L-type calcium channel in mouse neurobalstoma-rat glioma NG 108-15 hybrid cells assessed as inhibition of KCl-induced increase in intracellular calcium level pretreated for 3 mins before KCl challenge | 1993 | Journal of natural products, Jul, Volume: 56, Issue:7 | Polycyclic guanidine alkaloids from the marine sponge Crambe crambe and Ca++ channel blocker activity of crambescidin 816. |
AID1873207 | Inhibition of human ABCG2 expressed in human HEK293 cells mediated pheophorbide A efflux assessed as intracellular pheophorbide A accumulation for 45 mins by FACSort flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
AID78491 | Inhibitory concentration of [3H]- nitrendipine binding against guinea pig cerebral cortex membrane | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines. |
AID169102 | In vitro calcium antagonist activity was assessed against sodium induced constriction of potassium -depolarized rat aorta by 50% | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents. |
AID197526 | Concentration required to inhibit calcium-induced constriction of potassium-depolarized rat aorta by 50% | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Long acting dihydropyridine calcium antagonists. 2. 2-[2-Aminoheterocycloethoxy]methyl derivatives. |
AID747098 | Relaxant activity in potassium depolarized guinea pig aortic strips assessed as inhibition of calcium-induced contraction at 10'-6 M relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID611859 | Negative chronotropic activity against potassium-induced contraction in guinea pig right atrium assessed as decrease atrial rate at 10'-7 M relative to control | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID537132 | Antileishmanial activity against promastigotes of Leishmania amazonensis WHO/BR/00/LT0016 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID550023 | Vasorelaxant activity in Wistar rat endothelium-denuded thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction treated after noradrenaline challenge measured after 60 mins relative to control | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
AID611945 | Negative ionotropic activity against potassium-induced contraction in guinea pig left atrium assessed as decrease atrial rate | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID333049 | Antihypertensive activity in sham operated anesthetized SHR rat assessed as reduction of mean blood pressure at 5 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID1248200 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 6 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID1193495 | Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID167820 | In vitro evaluation for the inhibition of potassium-contracted rabbit aorta strips by vasorelaxant assay. | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents. |
AID234663 | Selectivity index was measured as the IC50 needed to depress the heart beat divided by IC50 needed to block [Ca2+] contractions in rabbit aortic strips | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID194645 | Compound was evaluated for antihypertensive activity in deoxy-corticosterone acetate (DOCA) treated hypertensive rats at 3 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID1587152 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension at 0.001 to 100 uM relative to control | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID333045 | Inhibition of noradrenaline release in adrenalectomized anesthetized SHR rat plasma at 5 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID89416 | Inhibition of collagen induced platelet aggregation in platelet-rich human plasma (PRP) | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
AID717839 | Cytotoxicity against HEK293T cells assessed as decrease in cell viability at 12.5 uM after 24 hrs by trypan blue exclusion assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID434147 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 480 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID332362 | Antihypertensive activity in adrenalectomized anesthetized SHR rat assessed as reduction of mean blood pressure at 15 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID167546 | Recovery of the initial contraction of rabbit aortic strips, blocked at 10e-4 M concentration. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
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. |
AID747095 | Displacement of [3H]-PN200-110 from L-type calcium channel in Hartley guinea pig atrial membrane after 90 mins | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
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). |
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. |
AID1912032 | Inhibition of PDE1C (147 to 531 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects. |
AID747093 | Displacement of [3H]-PN200-110 from L-type calcium channel in Hartley guinea pig ventricular membrane at 100 uM after 90 mins | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID1248194 | Lipophilicity, log P of the compound at pH 7.4 by shake flask method | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID234478 | Ratio between the EC30 values of aortic contracture and atrial rate | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties. |
AID1587135 | Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID764471 | Anticonvulsant activity in Wistar albino rat assessed as time of onset of subcutaneous pentylenetetrazole-induced clonic convulsion at 30 mg/kg administered 1 hr prior to pentylenetetrazole challenge measured for 300 secs (Rvb = 83 +/- 4 secs) | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and evaluation of dialkyl 4-(benzo[d][1,3]dioxol-6-yl)-1,4-dihydro-2,6-dimethyl-1-substituted pyridine-3,5-dicarboxylates as potential anticonvulsants and their molecular properties prediction. |
AID747123 | Displacement of [3H]-PN200-110 from voltage-gated calcium channel subunit alpha Cav1.2a (unknown origin) expressed in HEK293 cells at 100 uM after 90 mins by liquid scintillation counting analysis relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID612043 | Bronchodilatory activity in guinea pig trachea assessed as inhibition of carbachol-induced contraction at 10'-5 M | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID1055883 | Vasorelaxant activity in rat endothelium-denuded thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, ex vivo and in silico studies of 3-cyano-2-pyridone derivatives with vasorelaxant activity. |
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AID434146 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 360 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID45604 | Negative log antagonist concentration causing 50% displacement of [3H]nifedipine from guinea pig ileal smooth muscle membrane. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Synthesis and calcium channel antagonist activity of dialkyl 4- (dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylates. |
AID1867359 | Photostability of the compound assessed as compound degradation administered as solution irradiated with sun light and measured after 7 days by HPLC analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery. |
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AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM 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. |
AID132053 | Dose required to protect 50% of tested mice against experimental antithrombosis. | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
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AID1587139 | Inhibition of voltage-dependent L-type calcium channel in human U373MG cells assessed as protection against oxygen glucose deprivation/reperfusion-induced injury by measuring recovery of cell viability at 1 uM administered at onset of reperfusion period m | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID18875 | Half life of the compound | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists. |
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AID19424 | Partition coefficient (logD7.4) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. |
AID112426 | Effect on acute thrombic death induced by collagen in mice | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives. |
AID77612 | Intrinsic activity measured on Guinea pig tracheal spiral strips. | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Relaxant activity of 4-amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-amido-2H-1-benzopyrans on guinea pig isolated trachealis. |
AID1537627 | Antihypertensive activity in spontaneously hypertensive Wistar kyoto rat assessed as reduction in diastolic arterial pressure at 10 mg/kg, ip administered for 6 hrs and measured every 30 mins post treatment by tail-cuff method | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | Toxicities and beneficial protection of H |
AID1141125 | Neuroprotective activity against K+ induced Ca2+ overload in human SH-SY5Y cells assessed as survival at 0.3 uM after 24 hrs by MTT assay (Rvb = 52.1 +/- 3.5%) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID165725 | Vasorelaxant effect at a concentration of 10e-6 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID747097 | Relaxant activity in potassium depolarized guinea pig aortic strips assessed as inhibition of calcium-induced contraction | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID540212 | Mean residence time 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. |
AID1615136 | Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID678719 | Metabolic stability in human liver microsomes assessed as medium signal/noise ratio (S/N of 10 to 100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID611957 | Negative ionotropic activity in potassium depolarized guinea pig longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 5 X 10'-9 M | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
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. |
AID678835 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells | 1999 | Pharmaceutical research, Mar, Volume: 16, Issue:3 | Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. |
AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1577803 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as systolic left ventricular internal diameter at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiography (Rv | |||
AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
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AID332364 | Vasorelaxation activity in SHR rat assessed as reduction of methoxamine-induced mean arterial blood pressure at 10 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID717845 | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID338202 | Inhibition of T-type calcium channel at 1 nM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID1587169 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig aortic strips | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID79033 | Inhibition of carbachol-induced tonic contractile response in guinea pig ileal longitudinal smooth muscle | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and calcium channel-modulating effects of alkyl (or cycloalkyl) 1,4-dihydro-2,6-dimethyl-3-nitro-4-pyridyl-5-pyridinecarboxylate racemates and enantiomers. |
AID1612570 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension at 10'-5 M relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID1577762 | Inhibition of TGFbeta1 receptor in TGFbeta1-stimulated Sprague-Dawley rat cardiac fibroblasts assessed as reduction in alpha-SMA expression at 20 uM measured after 12 hrs by Western blot analysis | |||
AID172998 | Percent block of total Ba2+ current on L-type [Ca2+] channels in rat RIN-m5F at 3 insulinoma cells (n = 14) | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8 | Synthesis and voltage-clamp studies of methyl 1,4-dihydro-2, 6-dimethyl-5-nitro-4-(benzofurazanyl)pyridine-3-carboxylate racemates and enantiomers and of their benzofuroxanyl analogues. |
AID679183 | TP_TRANSPORTER: Northern blot in vitro, primary rat hepatocyte | 2002 | Cell biology and toxicology, , Volume: 18, Issue:4 | The drug efflux pump MRP2: regulation of expression in physiopathological situations and by endogenous and exogenous compounds. |
AID1143753 | Antioxidant activity in human SH-SY5Y cells assessed as rotenone-oligomycin-induced sequestering of mitochondrial free radicals at 0.3 uM after 120 mins using DCFH-DA by fluorescence microplate reader analysis | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases. |
AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID227125 | In vivo evaluation for the antihypertensive effect in the spontaneously hypertensive rat is % decrease in blood pressure during post drug administration at the dose of 45 umol/kg. per oral; 33/22 | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents. |
AID60702 | Cardiovascular effect upon femoral artery blood flow(FBF) in anesthetized open-chest dogs at a dose of 10 ug/ kg administered intravenously | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Novel selective hindlimb vasodilators: synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives. |
AID588218 | FDA HLAED, lactate dehydrogenase (LDH) 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. |
AID1141117 | Inhibition of rat Cav1.2 channel in rat mesenteric artery assessed as relaxation of 70 mM K+ induced contraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
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AID1466481 | Displacement of [3H]PN-200110 from voltage-dependent L-type calcium channel (unknown origin) by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Dimeric isoxazolyl-1,4-dihydropyridines have enhanced binding at the multi-drug resistance transporter. |
AID678134 | Metabolic stability in human microsomes assessed as glutathione adduct formation | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor. |
AID58963 | Duration of time taken for the compound for % decrease in coronary vasodilator activity | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Long-acting dihydropyridine calcium antagonists. 4. Synthesis and structure-activity relationships for a series of basic and nonbasic derivatives of 2-[(2-aminoethoxy)methyl]-1,4-dihydropyridine calcium antagonists. |
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AID19429 | Partition coefficient (logP) | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Inhibition of thyroid hormone uptake by calcium antagonists of the dihydropyridine class. |
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. |
AID717843 | Selectivity ratio of IC50 for mouse Ido1 to IC50 for mouse Ido2 | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID1248192 | Inhibition of MLCK (unknown origin) incubated for 15 mins using [gamma-32P]-ATP by scintillation counting method | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID165382 | The compound was tested for inhibition of potassium depolarized Rabbit aorta | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | 2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers. |
AID550021 | Vasorelaxant activity in Wistar rat endothelium-denuded thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction treated after noradrenaline challenge measured after 60 mins | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
AID536437 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po up to 360 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID614829 | Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:100 by DSC technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID747090 | Displacement of [3H]-PN200-110 from L-type calcium channel dihydropyridine binding site in Wistar rat cortex homogenate after 60 mins by liquid scintillation spectometric analysis | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID21661 | Calculated partition coefficient (clogP) (PALLAS) | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Inhibition of thyroid hormone uptake by calcium antagonists of the dihydropyridine class. |
AID185885 | Maximum fall in systolic blood pressure at interval from 1 to 6 hours at a dose of 0.3 mg/kg when administered perorally in rats | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | Synthesis and antihypertensive activity of substituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID34564 | Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. |
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. |
AID194503 | Compound was evaluated for antihypertensive activity in deoxy-corticosterone acetate (DOCA) treated hypertensive rats at 0.3 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID1216350 | AUC (0 to infinity) in healthy human assessed as fold change in presence of casopitant 120 mg, po once daily administered for 14 days | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4. |
AID1248201 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 7 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID537133 | Antileishmanial activity against promastigotes of Leishmania major MHOM/1L/80/Fredlin after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
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. |
AID667572 | Inhibition of calcium channel in pig carotid artery assessed as relaxation of KCl-induced vascular smooth muscle contraction | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Highly regioselective synthesis of N-3 organophosphorous derivatives of 3,4-dihydropyrimidin-2(1H)-ones and their calcium channel binding studies. |
AID439054 | Inhibition of calcium-induced contraction in guinea pig ileum at 0.01 uM | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID482149 | Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents. |
AID536448 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 15 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID1867357 | Photostability of the compound assessed as compound degradation administered as aqueous solution irradiated with UV and measured after 24 hrs by HPLC analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery. |
AID1867368 | Photostability of the compound assessed as half life administered as solution | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery. |
AID167552 | In vitro contraction of rabbit aorta strips. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. |
AID1612585 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig ileum at 5 x 10'-9 M relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID165732 | Vasorelaxant effect at a concentration of 10e-9 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID612046 | Bronchodilatory activity in guinea pig trachea assessed as inhibition of carbachol-induced contraction | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID681132 | TP_TRANSPORTER: ATP hydrolysis in MDR1-expressing Sf9 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. |
AID1207162 | Inhibition of Na channel (species unknown) | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID168532 | Tested for reflex tachycardia at the dose of 50 mg/kg when administered intraperitoneally in spontaneously hypertensive rats; active | 2000 | Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4 | Antihypertensive activity of substituted 2,3,8,8a-tetrahydro-7H-oxazolo[3,2-a]pyridinedicarboxylate enantiomers. |
AID536444 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 180 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID537136 | Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID577579 | Inhibition of CYP3A4 in human liver microsome | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4 | Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene. |
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. |
AID537137 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for amastigotes of Leishmania chagasi MHOM/BR/1972/LD | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID194650 | Compound was evaluated for oral antihypertensive activity in spontaneously hypertensive rats at 0.3 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID332365 | Vasorelaxation activity in SHR rat assessed as reduction of methoxamine-induced mean arterial blood pressure at 15 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID1392174 | Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells at 10 uM by Fluo-4 AM dye based fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | Substituent effect of N-benzylated gramine derivatives that prevent the PP2A inhibition and dissipate the neuronal Ca |
AID1473851 | Ratio of drug concentration at steady state in human at 30 to 60 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 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. |
AID1474164 | Ratio of drug concentration at steady state in human at 30 to 60 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells | 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. |
AID57847 | Cardiovascular effect upon blood pressure(BP) in anesthetized open-chest dogs at a dose of 10 ug/ kg administered intravenously | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Novel selective hindlimb vasodilators: synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives. |
AID670195 | Inhibition of L-type calcium channel in Sprague-Dawley rat aorta assessed as relaxation of Kcl-induced tissue contraction by aortic ring relaxation assay | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity. |
AID326586 | Inhibition of CaCl2-induced contraction in potassium-depolarized guinea pig ileal smooth muscle at 10 nM | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Synthesis and pharmacological activity of aminoindanone dimers and related compounds. |
AID194653 | Compound was evaluated for oral antihypertensive activity in spontaneously hypertensive rats at 1 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID611854 | Binding affinity to CFTR F508 deletion mutant expressed in forskolin-stimulated FRT cells assessed as increase in iodine influx measured as YFP quenching rate after 24 hrs by fluorescence assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID76393 | Inhibition of spontaneous tone in Guinea pig tracheal spiral strips. | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Relaxant activity of 4-amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-amido-2H-1-benzopyrans on guinea pig isolated trachealis. |
AID434298 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 120 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID537134 | Antileishmanial activity against promastigotes of Leishmania braziliensis MHO/BR/75/M2903 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID34239 | Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16 | Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. |
AID515314 | Octanol-water partition coefficient, log P of the compound | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Antihypertensive and antiarrhythmic properties of a para-hydroxy[bis(ortho-morpholinylmethyl)]phenyl-1,4-DHP compound: comparison with other compounds of the same kind and relationship with logP values. |
AID76370 | Tested for [Ca2+] antagonism in guinea pig atria | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
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. |
AID616228 | Antifertility effect in goat epididymis spermatozoa assessed as decrease in lactate production at 1.25 mm after 2 hrs by NMR analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID173971 | Reducing systolic blood pressure in spontaneously hypertensive rats. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID1612580 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig aortic strips | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID76358 | Compound was tested for its antagonist activity against calcium channel | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | 1,4-Dihydropyridine antagonist activities at the calcium channel: a quantitative structure-activity relationship approach. |
AID675412 | Solubility of the compound in phosphate buffer at pH 7.4 at 10 mg/mL after 30 mins by HPLC-UV-MS analysis | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Ligand-based design, in silico ADME-Tox filtering, synthesis and biological evaluation to discover new soluble 1,4-DHP-based CFTR activators. |
AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1068420 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced mortality at 30 mg/kg, po pretreated for 1 hr followed by pentylenetetrazole challenge relative to control | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1192717 | Antihypertensive activity in Sprague-Dawley rat PAH model assessed as reduction in hypoxia-induced elevated RV/(LV+S) at 10 mg/kg, po administered for 28 days measured on day 29 relative to untreated control | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity. |
AID21233 | Partition coefficient of compound in to biological membranes | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. |
AID747096 | Displacement of [3H]-PN200-110 from L-type calcium channel in Hartley guinea pig atrial membrane at 100 uM after 90 mins relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID524790 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID17662 | Equilibrium dissociation constant based on aqueous concentration in rat smooth muscle | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. |
AID317304 | Cardiovascular activity in perfused guinea pig heart assessed as change in heart rate at 10 nM by ECG | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID1248211 | Gastrointestinal toxicity in Norwegian rat assessed as ulcerative index at 50 mg/kg, po after 17 hrs | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID317313 | Displacement of (+)-[5-methyl-3H]PN200-100 from L type calcium channel in guinea pig heart ventricles | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID45614 | Displacement of [3H]nitrendipine binding to L-type calcium channel of Guinea pig cerebral cortex membranes | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines. |
AID1193498 | Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID45634 | Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle. | 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. |
AID333053 | Antihypertensive activity in adrenalectomized anesthetized SHR rat assessed as reduction of mean blood pressure at 5 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID1248209 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 3 hrs by invasive carotid artery cannulation method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID73721 | Effect on BaCl2-stimulated contraction of ileum of guinea pig | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates. |
AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
AID167364 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 10e-8 mol/L | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID617311 | Inhibition of human erythrocyte Glutathione reductase | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Design, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitors. |
AID76357 | Effective concentration required to produce mechanical response determined in muscle strips of guinea pig | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | 1,4-Dihydropyridine antagonist activities at the calcium channel: a quantitative structure-activity relationship approach. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1615134 | Vasodilating activity in Wistar rat aortic rings assessed as reduction in KCl-induced contractions relative to control | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID536447 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 30 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID77341 | Calcium channel antagonistic activity relative to 2,6-Dimethyl-4-(2-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester(=100) | 1982 | Journal of medicinal chemistry, Feb, Volume: 25, Issue:2 | Crystal structures and pharmacological activity of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-(unsubstituted, 2-methyl-, 4-methyl-, 3-nitro-, 4-nitro-, and 2,4-dinitrophenyl)-1,4-dihydropyridine. |
AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID1441978 | Inhibition of Kv1.1 (unknown origin) | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves That Improves Their Impaired Axonal Conduction. |
AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) 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. |
AID167363 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 10e-7 mol/L | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID317306 | Cardiovascular activity in perfused guinea pig heart assessed as change in atrioventricular conduction time at 1 uM by ECG | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID434300 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 240 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID524791 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID718301 | Vasorelaxant activity in Wistar rat aorta without endothelium assessed as inhibition of norepinephrine-induced contraction relative to control | 2012 | Journal of natural products, Dec-28, Volume: 75, Issue:12 | Ex vivo study of the vasorelaxant activity induced by phenanthrene derivatives isolated from Maxillaria densa. |
AID1581333 | Permeability at 100 uM by PAMPA method | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID1141119 | Neuroprotective activity against K+ induced Ca2+ overload in human SH-SY5Y cells assessed as survival at 5 uM after 24 hrs by MTT assay (Rvb = 52.1 +/- 3.5%) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID1577782 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as decrease in heart alpha-SMA level at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by immunohistochemical analysis | |||
AID592682 | Apparent permeability from apical to basolateral side of human Caco2 cells after 2 hrs by LC/MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
AID614828 | Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:5 by DSC technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID185907 | Maximum fall in blood pressure was evaluated at an oral dose of 10.0 mg/kg in (SHR) spontaneous hypertensive rats | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Synthesis and antihypertensive activity of 4-(cyclic amido)-2H-1-benzopyrans. |
AID681167 | TP_TRANSPORTER: Northern blot from LS174T cell | 2001 | The Journal of biological chemistry, May-04, Volume: 276, Issue:18 | Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. |
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. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID592683 | Apparent permeability from basolateral side to apical side of human Caco2 cells by LC/MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
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. |
AID165726 | Vasorelaxant effect at a concentration of 10e-6 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1587144 | Inhibition of voltage-dependent L-type calcium channel in Wistar rat brain slices assessed as protection against oxygen glucose deprivation/reperfusion-induced injury by measuring recovery of edema formation at 20 uM administered at onset of reperfusion p | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID1443986 | Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
AID7783 | Unbound fraction (plasma) | 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. |
AID55898 | Bmax1 from dihydropyridine receptor binding assay in guinea pig myocardial membranes | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Studies directed toward ascertaining the active conformation of 1,4-dihydropyridine calcium entry blockers. |
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. |
AID1192703 | Antihypertensive activity in Sprague-Dawley rat PAH model assessed as reduction in hypoxia-induced elevated right ventricular systolic pressure at 10 mg/kg, po administered for 28 days measured on day 29 relative to untreated control | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity. |
AID434148 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 15 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID60650 | The compound was tested for % decrease in coronary vasodilator activity in anesthetized dogs following intravenous administration | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Long-acting dihydropyridine calcium antagonists. 4. Synthesis and structure-activity relationships for a series of basic and nonbasic derivatives of 2-[(2-aminoethoxy)methyl]-1,4-dihydropyridine calcium antagonists. |
AID10375 | Hill coefficient of the compound | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate. |
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. |
AID194654 | Compound was evaluated for oral antihypertensive activity in spontaneously hypertensive rats at 3 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID195355 | Concentration required to block Ca+2-induced contraction of K+ depolarized rat aorta | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists. |
AID31706 | Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. |
AID80745 | Evaluated in vitro for its effect on spontaneous atrial contractility in isolated guinea pig atria | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties. |
AID1248205 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 0.15 hrs by invasive carotid artery cannulation method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID681335 | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells | 2002 | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Aug, Volume: 16, Issue:3 | Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. |
AID73722 | Effect on KCl-stimulated contraction of aortic strips of guinea pig | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates. |
AID333042 | Inhibition of noradrenaline release in sham operated anesthetized SHR rat plasma at 10 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID317305 | Cardiovascular activity in perfused guinea pig heart assessed as change in coronary perfusion pressure at 1 uM by ECG | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID333047 | Inhibition of noradrenaline release in adrenalectomized anesthetized SHR rat plasma at 15 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID195197 | Inhibition of [Ca2+] induced contraction of K+ depolarized rat aorta by 50% | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines. |
AID1141124 | Neuroprotective activity against rotenone-oligomycin A-induced oxidative stress in human SH-SY5Y cells assessed as protection incubated with rot/oligo for 8 hrs followed by treated with compound at 5 uM for 16 hrs by MTT assay relative to control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID28677 | Partition coefficient (logD) | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | Property-based design: optimization of drug absorption and pharmacokinetics. |
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] | |||
AID185886 | Maximum fall in systolic blood pressure at interval from 1 to 6 hours at a dose of 1 mg/kg when administered perorally in rats | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | Synthesis and antihypertensive activity of substituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID1698832 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial blood pressure at 3 mg/kg, po measured after 6 hrs | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Pharmacophore modeling, design, and synthesis of potent antihypertensives, oxazolo/thiazolo-[3,2-a]-pyrimidin-3(2H)-one, and 1,5-dihydroimidazo-[1,2-a]-pyrimidin-3(2H)-one derivatives: A pilot trial. |
AID165720 | Vasorelaxant effect at a concentration of 10e-10 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID332367 | Vasorelaxation activity in SHR rat assessed as reduction of Bay-K 8644-induced mean arterial blood pressure at 10 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID338203 | Inhibition of adenosine A1 receptor at 10 uM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID434144 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 240 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID39458 | Coronary vasodilator activity in anesthetized dogs at the dose of 150 ug/kg (iv) | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists. |
AID1184075 | Inhibition of IDO1 (unknown origin) at highest soluble concentration using L-tryptophan substrate incubated for 60 mins by HPLC | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
AID537131 | Antileishmanial activity against amastigotes of Leishmania chagasi MHOM/BR/1972/LD after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
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. |
AID1581331 | Displacement of [3H]-N-alpha-methylhistamine from human H3 receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID317303 | Cardiovascular activity in perfused guinea pig heart assessed as change in maximal rate of rise in left ventricular pressure at 10 nM by ECG | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
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. |
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. |
AID718303 | Vasorelaxant activity in Wistar rat aorta with endothelium assessed as inhibition of norepinephrine-induced contraction relative to control | 2012 | Journal of natural products, Dec-28, Volume: 75, Issue:12 | Ex vivo study of the vasorelaxant activity induced by phenanthrene derivatives isolated from Maxillaria densa. |
AID1615137 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID1577806 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as ejection fraction at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiography (Rvb = 79.59 +/- 3.13%) | |||
AID22770 | Time taken for 50% recovery of coronary vascular resistance in dogs, after administration of a dose of 150 micorg/kg intravenously | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives. |
AID721501 | Stimulation of alkaline phosphatase activity in mouse calvarial osteoblasts at 1 pM to 1 uM after 48 hrs by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
AID747099 | Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 5x10'-9 M relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID747091 | Displacement of [3H]-PN200-110 from L-type calcium channel dihydropyridine binding site in Wistar rat cortex homogenate at 100 uM after 60 mins by liquid scintillation spectometric analysis relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID166480 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 3*10e-7 mol/L; NT=Not tested | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID1628098 | Activation of AMPK/SIRT1 in human HaCaT cells assessed as nitric oxide production up to 50 uM incubated for 1 hr by DAF-2D staining-based fluorescence assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | 1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells. |
AID478846 | Antagonist activity at rat Cav1.3 expressed in HEK293 cells assessed as inhibition of voltage pulse-induced calcium current at 100 nM by FLIPR calcium 4 assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
AID1192713 | Antihypertensive activity in Sprague-Dawley rat PAH model assessed as reduction in hypoxia-induced elevated RV/BW at 10 mg/kg, po administered for 28 days measured on day 29 relative to untreated control | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity. |
AID536438 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 900 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID224185 | Evaluated in vitro for the effect on K+ induced aortic contraction in isolated aortic strips of rabbit | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties. |
AID1193500 | Thermodynamic equilibrium solubility, log S of the compound | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1473850 | Drug concentration at steady state in human at 30 to 60 mg, po QD after 24 hrs | 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. |
AID1068423 | Anticonvulsant activity in Wistar albino rat assessed as protection against maximal electroshock-induced seizures by measuring duration of limb extension at 30 mg/kg, po pretreated for 1 hr followed by maximal electroshock challenge (Rvb = 16 +/- 1 secs) | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
AID333046 | Inhibition of noradrenaline release in adrenalectomized anesthetized SHR rat plasma at 10 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID1577761 | Inhibition of TGFbeta1 receptor in TGFbeta1-stimulated Sprague-Dawley rat cardiac fibroblasts assessed as reduction in fibronectin expression at 20 uM measured after 12 hrs by Western blot analysis | |||
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. |
AID332369 | Antihypertensive activity in SHR rat assessed as changes in tail arterial mean blood pressure at 1 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID679779 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5uM, Nifedipine:125uM) 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. |
AID76581 | Maximum inhibition of KCl-stimulated contraction of aortic strips of guinea pig | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates. |
AID411890 | Inhibition of human Kv1.5 channel expressed in mouse L929 cells by EP voltage clamp technique | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)). |
AID1367795 | Unbound intrinsic clearance in human at 10 mg, tid | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Relevance of Half-Life in Drug Design. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID536439 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 720 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID1615131 | Vasodilating activity in Wistar rat aortic rings assessed as reduction in phenylephrine-induced contractions | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID540226 | Clearance in monkey 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. |
AID76978 | Inhibition of muscarinic receptor mediated [Ca2+] dependent contraction of guinea pig ileal longitudinal smooth muscle | 1982 | Journal of medicinal chemistry, Feb, Volume: 25, Issue:2 | Crystal structures and pharmacological activity of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-(unsubstituted, 2-methyl-, 4-methyl-, 3-nitro-, 4-nitro-, and 2,4-dinitrophenyl)-1,4-dihydropyridine. |
AID478856 | Selectivity ratio of antagonist activity at rat Cav1.3 to antagonist activity at rabbit Cav1.2 at 100 nM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
AID444053 | Renal 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. |
AID34125 | Inhibition of [125I]- AB-MECA binding to human Adenosine A3 receptors expressed in HEK cells | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | 6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists. |
AID333040 | Inhibition of noradrenaline release in sham operated anesthetized SHR rat plasma at 1 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID317315 | Displacement of (+)-[5-methyl-3H]PN200-100 from L type calcium channel Cav1.2b in rabbit expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID165727 | Vasorelaxant effect at a concentration of 10e-7 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1207674 | 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. |
AID1577764 | Inhibition of TGFbeta1 receptor in TGFbeta1-stimulated Sprague-Dawley rat cardiac fibroblasts assessed as reduction in collagen 3 expression at 20 uM measured after 12 hrs by Western blot analysis | |||
AID1207191 | Inhibition of voltage-gated L-type Ca channel (species unknown) | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID79827 | In vitro assessment of negative inotropy in the isolated Langendorff perfused guinea pig heart | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Long acting dihydropyridine calcium antagonists. 2. 2-[2-Aminoheterocycloethoxy]methyl derivatives. |
AID47566 | Binding affinity for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities. |
AID165719 | Vasorelaxant effect at a concentration of 10e-10 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID681153 | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | 2001 | Chemical research in toxicology, Dec, Volume: 14, Issue:12 | Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. |
AID165587 | The vascular smooth muscle relaxant activity was expressed as percent relaxation of the developed isometric tension in potassium depolarized rabbit aortic smooth muscle | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Tetrahydropyrrolo[1,2-a]quinoxalines and tetrahydropyrrolo[1,2-a]pyrido[3,2-a]pyrazines: vascular smooth muscle relaxants and antihypertensive agents. |
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. |
AID9718 | Half-recovery time (T1/2) of the vascular resistance decrease at ED30 in anesthetized dogs | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity. |
AID524796 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID234388 | Vasorelaxant effect on KCl-Induced contraction of porcine coronary artery vs rat aorta | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | Synthesis and selective coronary vasodilatory activity of 3,4-dihydro-2,2-bis(methoxymethyl)-2H-1-benzopyran-3-ol derivatives: novel potassium channel openers. |
AID1443991 | Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
AID537139 | Cytotoxicity in BALB/c mouse erythrocytes assessed as hemolysis at 50 uM after 3 hrs | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID73832 | Negative inotropy measured as the concentration required to depress contraction in the isolated Langendorff-perfused guinea pig heart by 25% | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents. |
AID611853 | Activity at CFTR F508 deletion mutant expressed in forskolin-stimulated FRT cells assessed as maximal increase in iodine influx measured as YFP quenching rate after 24 hrs by fluorescence assay | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID1216347 | AUC (0 to infinity) in healthy human assessed as fold change in presence of casopitant 30 mg, po once daily administered for 3 days | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4. |
AID717846 | Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID764465 | Anticonvulsant activity in Wistar albino rat assessed as protection against maximum electric shock-induced hind limb tonic extension at 30 mg/kg administered 1 hr followed by maximum electric shock induction relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and evaluation of dialkyl 4-(benzo[d][1,3]dioxol-6-yl)-1,4-dihydro-2,6-dimethyl-1-substituted pyridine-3,5-dicarboxylates as potential anticonvulsants and their molecular properties prediction. |
AID333052 | Antihypertensive activity in adrenalectomized anesthetized SHR rat assessed as reduction of mean blood pressure at 1 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID333048 | Antihypertensive activity in sham operated anesthetized SHR rat assessed as reduction of mean blood pressure at 1 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
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. |
AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
AID91705 | Percent decrease in tonic contractile response in guinea pig ileal longitudinal smooth muscle. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Synthesis, rotamer orientation, and calcium channel modulation activities of alkyl and 2-phenethyl 1,4-dihydro-2,6-dimethyl-3-nitro-4-(3- or 6-substituted-2-pyridyl)-5-pyridinecarboxylates. |
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AID1207252 | 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. |
AID1581347 | Vasodilating activity in Wistar rat endothelium-denuded aortic rings preconstricted with 100 mM KCl assessed as vasorelaxation at 0.1 nM relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
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. |
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. |
AID167367 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 3*10e-9 mol/L | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID173970 | Compound evaluated for reducing diastolic blood pressure spontaneously hypertensive rats. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID167366 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 3*10e-8 mol/L | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID332363 | Vasorelaxation activity in SHR rat assessed as reduction of methoxamine-induced mean arterial blood pressure at 5 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID29851 | Half life was measured as time taken to decrease half of its initial concentration | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | Property-based design: optimization of drug absorption and pharmacokinetics. |
AID76985 | Inhibition of the muscarinic receptor mediated [Ca(2+)]-dependent contraction of guinea pig ileal longitudinal smooth muscle. | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | Synthesis and calcium channel antagonist activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pyridinyl)-3,5-pyridinedicarboxylates. |
AID77874 | Intrinsic activity value in comparison with nifedipine. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates. |
AID1068421 | Anticonvulsant activity in Wistar albino rat assessed as protection against maximal electroshock-induced electroconvulsive seizures at 30 mg/kg, po pretreated for 1 hr followed by maximal electroshock challenge relative to control | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
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AID79826 | Evaluated for the negative ionotropy logarithm of the molar concentration required to depress contraction in the Langendorff-perfused guinea pig heart by 25% | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5 -(methoxycarbonyl)-6-methyl-1,4-dihydropyridine. |
AID167351 | Blockade of calcium-evoked contractions in depolarized aortic strips | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
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. |
AID28233 | Fraction ionized (pH 7.4) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1581348 | Vasodilating activity in Wistar rat endothelium-denuded aortic rings preconstricted with 100 mM KCl assessed as vasorelaxation at 1 nM relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID444058 | Volume of distribution at steady state 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. |
AID1698831 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial blood pressure at 1.5 mg/kg, po measured after 12 hrs | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Pharmacophore modeling, design, and synthesis of potent antihypertensives, oxazolo/thiazolo-[3,2-a]-pyrimidin-3(2H)-one, and 1,5-dihydroimidazo-[1,2-a]-pyrimidin-3(2H)-one derivatives: A pilot trial. |
AID747112 | Negative chronotropic activity in guinea pig right atrium assessed as decrease in atrial rate at 10'-7 M relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
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AID1210073 | Inhibition of CYP2C19 in human liver microsomes using omeprazole 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. |
AID317288 | Inotropic activity at L type calcium channel in guinea pig left atrium assessed as decrease in tension | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID1193496 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
AID1193493 | Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1577801 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as systolic left ventricular anterior wall thickness at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiograp | |||
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
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AID1443992 | Total Cmax in human administered as single dose | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
AID45618 | Dissociation constant for inhibition of [3H]nitrendipine binding to guinea pig myocardial membranes | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Studies directed toward ascertaining the active conformation of 1,4-dihydropyridine calcium entry blockers. |
AID75198 | Concentration needed to elicit a 75% increase beyond control in coronary flow in ''Langendorff'', guinea pig heart (in vitro) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
AID721506 | Induction of mineralization in mouse calvarial osteoblasts assessed as increase of mineralized nodules formation measuring concentration required for maximum activity after 21 days by alizarin red-S staining based spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
AID536440 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 600 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID228679 | Solvation energy | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Stereoselective characterization of the 1,4-dihydropyridine binding site at L-type calcium channels in the resting state and the opened/inactivated state. |
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AID227268 | In vivo evaluation for the antihypertensive effect in the spontaneously hypertensive rat is % decrease in blood pressure during post drug administration at the dose of 5 umol/kg. per oral; 12/10 | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents. |
AID95743 | Free energies of binding (delta G) in the Resting state (rs) of voltage-gated L-type [Ca2+] channel(VGCCs) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Stereoselective characterization of the 1,4-dihydropyridine binding site at L-type calcium channels in the resting state and the opened/inactivated state. |
AID1574948 | Cytotoxicity against human HepG2 cells after 24 hrs by LDH release assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
AID611864 | Negative chronotropic activity against potassium-induced contraction in guinea pig right atrium assessed as decrease atrial rate | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID1867358 | Photostability of the compound assessed as compound degradation administered as solid irradiated with sun light and measured after 7 days by HPLC analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery. |
AID617312 | Competitive inhibition of human erythrocyte Glutathione reductase using GSSG substrate by Lineweaver-Burk plot analysis | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Design, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitors. |
AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) 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. |
AID624622 | Apparent permeability (Papp) from 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. |
AID536441 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 360 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID1577807 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as fractional shortening at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiography (Rvb = 48.17 +/- 4.69%) | |||
AID540229 | Volume of distribution at steady state in human 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. |
AID80746 | Evaluated in vitro for the effect on spontaneous atrial rate in isolated guinea pig atria | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties. |
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. |
AID167365 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 10e-9 mol/L | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID616223 | Binding affinity to multilamellar vesicles assessed as apparent binding constant after 2 hrs by double reciprocal plot | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID718304 | Vasorelaxant activity in Wistar rat aorta with endothelium assessed as inhibition of norepinephrine-induced contraction | 2012 | Journal of natural products, Dec-28, Volume: 75, Issue:12 | Ex vivo study of the vasorelaxant activity induced by phenanthrene derivatives isolated from Maxillaria densa. |
AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
AID1248210 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 4 hrs by invasive carotid artery cannulation method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID420011 | Inhibition of calcium channel in pig carotid artery assessed as relaxation of KCl-induced tissue contraction | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity. |
AID75504 | Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro negative inotropic activity) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
AID1143754 | Inhibition of calcium channel in human SH-SY5Y cells assessed as blockade of K+-evoked cytosolic calcium increase at 3 uM after 15 mins using Fluo-4/AM by fluorescence microplate reader analysis | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases. |
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] | |||
AID338206 | Inhibition of low conductance potassium channel at 10 uM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID536446 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 60 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID747092 | Displacement of [3H]-PN200-110 from voltage-gated calcium channel subunit alpha Cav1.2a (unknown origin) expressed in HEK293 cells after 90 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID1612572 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID366631 | Displacement of [3H]nitrendipine from voltage-dependent calcium channel in rat brain cortex by scintillation counting | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID165730 | Vasorelaxant effect at a concentration of 10e-8 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID185889 | Maximum fall in systolic blood pressure at interval from 1 to 6 hours at a dose of 3 mg/kg when administered perorally in rats | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | Synthesis and antihypertensive activity of substituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID721508 | Stimulation of alkaline phosphatase activity in mouse calvarial osteoblasts assessed as concentration required for maximum activity after 48 hrs by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
AID354897 | Vasorelaxant activity against high potassium-induced contraction in Wistar rat thoracic aorta at 1 ug/ml | 1996 | Journal of natural products, May, Volume: 59, Issue:5 | Antiplatelet of vasorelaxing actions of some benzylisoquinoline and phenanthrene alkaloids. |
AID179416 | Dose-dependent inhibition of calcium contraction in depolarized rat aortic strips | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation |
AID540228 | Clearance in human 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. |
AID1872383 | Binding affinity to EZH2-EED (unknown origin) protein interaction assessed as inhibition constant by FP binding assay | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
AID434140 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 30 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID428564 | Inhibition of CYP3A4 | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques. |
AID747122 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID679600 | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM, Nifedipine: 100 uM) in Caco-2 cells | 1999 | Pharmaceutical research, Mar, Volume: 16, Issue:3 | Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. |
AID44639 | IKCa channel inhibition was determined measuring ionomycin-induced Rb+ efflux of pre loaded rat C6BU1 glioma cell in comparison with Nifedipine | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | 4-Phenyl-4H-pyrans as IK(Ca) channel blockers. |
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AID1367790 | Inhibition of human calcium channel | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Relevance of Half-Life in Drug Design. |
AID1577780 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as decrease in heart fibronectin level at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by immunohistochemical analysis | |||
AID180478 | Molar concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50% | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines. |
AID540213 | Half life 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. |
AID747111 | Negative chronotropic activity in guinea pig right atrium assessed as decrease in atrial rate | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID524795 | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
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. |
AID1577800 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as diastolic left ventricular anterior wall thickness at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiogra | |||
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 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). |
AID79829 | Negative logarithm of the concentration required to depress contraction in the Langendorff perfused guinea pig heart by 25% | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Long-acting dihydropyridine calcium antagonists. 4. Synthesis and structure-activity relationships for a series of basic and nonbasic derivatives of 2-[(2-aminoethoxy)methyl]-1,4-dihydropyridine calcium antagonists. |
AID337900 | Displacement of [3H]nitrendipine from T-type calcium channel | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID1587162 | Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate at 10'-7 M relative to control | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
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 |
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. |
AID1216349 | AUC (0 to infinity) in healthy human assessed as fold change in presence of casopitant 120 mg, po once daily administered for 3 days | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4. |
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. |
AID333041 | Inhibition of noradrenaline release in sham operated anesthetized SHR rat plasma at 5 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
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. |
AID747118 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension at 10'-5 M relative to control | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport 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. |
AID1141116 | Inhibition of human Cav1.3 channel in human SH-SY5Y cells assessed as 70 mM K+ induced calcium elevation compound treated 15 mins before stimulus by Fluo-4/AM assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
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 |
AID34237 | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16 | Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. |
AID536443 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 240 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID1192707 | Antihypertensive activity in Sprague-Dawley rat PAH model assessed as reduction in hypoxia-induced central vein pressure at 10 mg/kg, po administered for 28 days measured on day 29 relative to untreated control | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity. |
AID434142 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 120 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
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). |
AID1156817 | Inhibition of voltage-dependent calcium channel in Sprague-Dawley rat thoracic aorta assessed as inhibition of CaCl2-induced contraction at 0.001 to 100 mM by isometric force transducer | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers. |
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. |
AID540223 | Volume of distribution at steady state in rat 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. |
AID444055 | Fraction absorbed 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. |
AID95580 | Inhibition of [3H](+)-PN200-110 binding to L-type calcium channel 1,4-DHP binding site of rat ventricular myocytes | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels. |
AID612042 | Negative ionotropic activity in potassium depolarized guinea pig longitudinal smooth muscle assessed as inhibition of calcium-induced contraction | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID537130 | Antileishmanial activity against promastigotes of Leishmania chagasi MHOM/BR/1972/LD after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID1141121 | Neuroprotective activity against rotenone-oligomycin A-induced oxidative stress in human SH-SY5Y cells assessed as survival at 5 uM co-incubated rot/oligo for 24 hrs by MTT assay (Rvb =65.6 +/- 1.3%) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID95589 | Effect on L-type [Ca2+] channels of rat RIN-m5F insulinoma cells in 10 mM Ba2+, -60 mV holding potential at 3uM, -20 mV | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | New 1,4-dihydropyridines endowed with NO-donor and calcium channel agonist properties. |
AID780994 | Antagonist activity at calcium channel albino guinea pig ileal longitudinal smooth muscle assessed as inhibition of KCl-induced contraction | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Design and synthesis of novel 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridines as small molecule BACE-1 inhibitors. |
AID333051 | Antihypertensive activity in sham operated anesthetized SHR rat assessed as reduction of mean blood pressure at 15 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID19427 | HPLC capacity factor (k) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | ElogPoct: a tool for lipophilicity determination in drug discovery. |
AID540209 | Volume of distribution at steady state 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. |
AID540222 | Clearance in rat 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. |
AID1207221 | 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. |
AID420017 | Antagonist activity at voltage dependent L-type calcium channel in New Zealand white rabbit sigmoid colon circular smooth muscle strip assessed as relaxation response | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Condensed 1,4-dihydropyridines with various esters and their calcium channel antagonist activities. |
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. |
AID373867 | Hepatic clearance in human hepatocytes in absence of fetal calf serum | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | First-principle, structure-based prediction of hepatic metabolic clearance values in human. |
AID1380098 | Inhibition of Cch1 in Candida albicans isolate 16 assessed as potentiation of fluconazole-induced antifungal activity by measuring fractional inhibitory concentration index after 24 hrs by checkerboard assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Emerging New Targets for the Treatment of Resistant Fungal Infections. |
AID420013 | Antagonist activity at voltage dependent L-type calcium channel in New Zealand white rabbit sigmoid colon circular smooth muscle strip assessed as relaxation response relative to papaverine | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Condensed 1,4-dihydropyridines with various esters and their calcium channel antagonist activities. |
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. |
AID337899 | Displacement of [3H]nitrendipine from L-type calcium channel | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID1577763 | Inhibition of TGFbeta1 receptor in TGFbeta1-stimulated Sprague-Dawley rat cardiac fibroblasts assessed as reduction in collagen 1 expression at 20 uM measured after 12 hrs by Western blot analysis | |||
AID30135 | Volume of distribution of the compound | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | Property-based design: optimization of drug absorption and pharmacokinetics. |
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. |
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. |
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. |
AID1193492 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID537138 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for trypomastigotes of Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID1212314 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID165731 | Vasorelaxant effect at a concentration of 10e-9 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID332368 | Vasorelaxation activity in SHR rat assessed as reduction of Bay-K 8644-induced mean arterial blood pressure at 15 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID333044 | Inhibition of noradrenaline release in adrenalectomized anesthetized SHR rat plasma at 1 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID56033 | Inhibition of [3H]nitrendipine binding to calcium channels in the rat brain. | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | 2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers. |
AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
AID537736 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p 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. |
AID165728 | Vasorelaxant effect at a concentration of 10e-7 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1307816 | Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 10'-6 M | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
AID1635444 | Aqueous solubility of compound after 48 hrs by HPLC analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents. |
AID192055 | Systolic blood pressure after administration of a single oral dose (20 mg/kg) | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
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. |
AID317294 | Activity at L type calcium channel in K+ depolarized guinea pig aortic strip assessed as inhibition of calcium induced contraction at 1 uM | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID317307 | Cardiovascular activity in perfused guinea pig heart assessed as change in ventricular repolarization time at 10 nM by ECG | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1307729 | Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target? |
AID1207673 | 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. |
AID1248203 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 9 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
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). |
AID614827 | Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:1 by DSC technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID48347 | [Ca2+] antagonistic activity on [Ca2+] current in cat papillary. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID1216348 | AUC (0 to infinity) in healthy human assessed as fold change in presence of casopitant 30 mg, po once daily administered for 14 days | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4. |
AID1248196 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 2 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID398840 | Vasorelaxant activity against 80 mM potassium-induced contractions in rat thoracic aorta assessed as muscle contractions at 1 uM pretreated for 15 mins before potassium administration relative to control | 1997 | Journal of natural products, Jun, Volume: 60, Issue:6 | Bioactive alkaloids from Illigera luzonensis. |
AID95740 | Evaluated for the free energies of binding (delta G) (in the resting state (rs) of voltage-gated L-type [Ca2+] channel (VGCCs)) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Stereoselective characterization of the 1,4-dihydropyridine binding site at L-type calcium channels in the resting state and the opened/inactivated state. |
AID1577781 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as decrease in heart collagen level at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by Masson's trichrome staining-bas | |||
AID28235 | Unbound fraction (plasma) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1248202 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 8 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID524794 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID1211791 | Fraction unbound in human hepatocytes | 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. |
AID19262 | Aqueous solubility | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Prediction of drug solubility from Monte Carlo simulations. |
AID1628097 | Antagonist activity at calcium channel in guinea pig smooth muscle assessed as inhibition of calcium-induced contraction in K+-depolarized aortic strips | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | 1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells. |
AID180311 | Inhibition of [3H]nitrendipine binding to L-type calcium channels of rat cerebral cortex | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity. |
AID444056 | Fraction escaping gut-wall 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. |
AID56027 | Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation |
AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
AID166473 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 10E-6 mol/L; NT=Not tested | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID28236 | Unbound fraction (tissues) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1211797 | Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells 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. |
AID19006 | Calculated membrane partition coefficient (Kmemb) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability. |
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID185729 | Antihypertensive effects in conscious, unrestrained, spontaneously hypertensive rats after 30 mg/kg i.p. administration. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Antihypertensive dihydropyridines with 1,4,4-trisubstitution. |
AID536442 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 300 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID76980 | Inhibition of muscarinic receptor mediated [Ca2+] dependent contraction of guinea pig ileal longitudinal smooth muscle. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Synthesis and calcium channel antagonist activity of dialkyl 4- (dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylates. |
AID1212341 | Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID227124 | In vivo evaluation for the antihypertensive effect in the spontaneously hypertensive rat is % decrease in blood pressure during post drug administration at the dose of 15 umol/kg. per oral; 26/15 | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents. |
AID420019 | Antagonist activity at voltage dependent L-type calcium channel in New Zealand white rabbit sigmoid colon circular smooth muscle strip assessed as induction of relaxation response in absence of Ca2+-activated potassium channel blocker tetraethylammonium | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Condensed 1,4-dihydropyridines with various esters and their calcium channel antagonist activities. |
AID709633 | Inhibition of calcium transients in mouse HL-1 cells after 10 mins using Fluo-4 by fluorescene assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling. |
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). |
AID197533 | Negative logarithm of molar concentration required to block calcium-induced contraction of potassium depolarized rat aorta by 50% | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives. |
AID537135 | Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID1248206 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 0.3 hrs by invasive carotid artery cannulation method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID76373 | Tested for [Ca2+] antagonism in guinea pig right ventricle | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
AID29360 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1537623 | Antihypertensive activity in spontaneously hypertensive Wistar kyoto rat assessed as reduction in systolic arterial pressure at 10 mg/kg, ip administered for 6 hrs and measured every 30 mins post treatment by tail-cuff method | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | Toxicities and beneficial protection of H |
AID1248198 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 4 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
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 | |||
AID54753 | Binding affinity for Cytochrome P450 3A4; Range = 1-10 uM | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4). |
AID173542 | Percent decrease in blood pressure in hypertensive rat at 16 mg/kg po | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport 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. |
AID377019 | Antispasmodic activity in guinea pig ileum assessed as inhibition of acetylcholine-induced contraction at 1 uM | 2006 | Journal of natural products, Jun, Volume: 69, Issue:6 | Spasmolytic effects of nonprenylated rotenoid constituents of Boerhaavia diffusa roots. |
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. |
AID467613 | Volume of distribution at steady state in human | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID195182 | Vasodilator activity was measured on rat aorta in the presence of guanylate cyclase methylene blue(MB). | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities. |
AID1615139 | Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID45635 | Calcium channel blocking activity in rabbit | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters. |
AID165364 | Tested for [Ca2+] antagonism in rabbit renal artery | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
AID33788 | Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. |
AID47565 | Inhibitory concentration for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities. |
AID76580 | Maximum inhibition of BaCl2-stimulated contraction of ileum of guinea pig | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates. |
AID1612576 | Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate at 10'-7 M | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID536445 | Antihypertensive activity against DOCA-salt induced hypertension in albino rat assessed as reduction in systolic blood pressure at 10 mg/kg, po after 120 mins by tail-cuff method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation. |
AID317302 | Activity at L type calcium channel in K+ depolarized guinea pig longitudinal smooth muscle assessed as inhibition of calcium induced contraction | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID1443995 | Hepatotoxicity in human assessed as drug-induced liver injury | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
AID1581330 | Inhibition of voltage-dependent L-type calcium channel in 70 mM K+-induced human SH-SY5Y cells assessed as blocking of depolarization-induced Ca2+ uptake by Fluo-4/AM dye based fluorescence microplate reader assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID355712 | Antihypertensive activity in adrenalectomized anesthetized SHR rat assessed as reduction of mean blood pressure at 10 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID165724 | Vasorelaxant effect at a concentration of 10e-5 M on rabbit aortic rings previously contracted with 50 mM KCl. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1061889 | Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands. |
AID550020 | Vasorelaxant activity in Wistar rat endothelium-intact thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction treated after noradrenaline challenge measured after 60 mins | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
AID721696 | Stimulation of alkaline phosphatase activity in mouse calvarial osteoblasts after 48 hrs by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
AID1248204 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 10 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID550022 | Vasorelaxant activity in Wistar rat endothelium-intact thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction treated after noradrenaline challenge measured after 60 mins relative to control | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
AID1232307 | Lipophilicity, log P of the compound | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID29423 | HPLC capacity factor (k') | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1207672 | 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. |
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. |
AID1207754 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits | 2013 | Scientific reports, , Volume: 3 | MICE models: superior to the HERG model in predicting Torsade de Pointes. |
AID1473849 | AUC in human at 30 to 60 mg, po QD after 24 hrs | 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. |
AID175301 | Concentration required to produce 25% increase in coronary flow | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | 2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers. |
AID1248207 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 1 hr by invasive carotid artery cannulation method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID215770 | In vitro inhibition of thromboxane B2 production in rat whole blood. | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
AID61754 | Percent decrease in coronary vascular resistance in dogs at 150 u/kg intravenous dose | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Long acting dihydropyridine calcium antagonists. 2. 2-[2-Aminoheterocycloethoxy]methyl derivatives. |
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. |
AID194466 | Antihypertensive activity expressed as maximal change in systolic blood pressure (SBP) from pretreatment levels at either 1.5 or 4 hr after dosing | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Tetrahydropyrrolo[1,2-a]quinoxalines and tetrahydropyrrolo[1,2-a]pyrido[3,2-a]pyrazines: vascular smooth muscle relaxants and antihypertensive agents. |
AID680053 | TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM, Nifedipine: 50 uM) in MDR1-expressing LLC-PK1 cells | 2001 | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb, Volume: 12, Issue:4 | Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. |
AID171866 | Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR), at 3-6h after 30 mg/kg oral administration | 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. |
AID411889 | Inhibition of L-type calcium channel expressed in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)). |
AID1581329 | Inhibition of voltage-dependent L-type calcium channel in 70 mM K+-induced human SH-SY5Y cells assessed as blocking of depolarization-induced Ca2+ uptake at 10 uM by Fluo-4/AM dye based fluorescence microplate reader assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID338183 | Displacement of [3H]nitrendipine from L-type calcium channel assessed as specific binding relative to total binding | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID338201 | Inhibition of L-type calcium channel at 1 nM | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID1407635 | Inhibition of voltage gated calcium channel in human SH-SY5Y cells assessed as blockade of K+-evoked calcium uptake at 3 uM pretreated for 10 mins followed by 70 mM K+ addition by Fluo-4AM dye based fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design and synthesis of multipotent 3-aminomethylindoles and 7-azaindoles with enhanced protein phosphatase 2A-activating profile and neuroprotection. |
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. |
AID1698833 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial blood pressure at 3 mg/kg, po measured after 12 hrs | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Pharmacophore modeling, design, and synthesis of potent antihypertensives, oxazolo/thiazolo-[3,2-a]-pyrimidin-3(2H)-one, and 1,5-dihydroimidazo-[1,2-a]-pyrimidin-3(2H)-one derivatives: A pilot trial. |
AID434149 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 30 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID1207675 | 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. |
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). |
AID22772 | Time taken for 50% recovery of coronary vascular resistance, expressed in hours was determined in dogs | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Long acting dihydropyridine calcium antagonists. 2. 2-[2-Aminoheterocycloethoxy]methyl derivatives. |
AID76371 | Tested for [Ca2+] antagonism in guinea pig ileum | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
AID27900 | Plasma clearance of the compound | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | Property-based design: optimization of drug absorption and pharmacokinetics. |
AID160680 | Vasorelaxant effect on KCl-Induced contraction of porcine coronary artery | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | Synthesis and selective coronary vasodilatory activity of 3,4-dihydro-2,2-bis(methoxymethyl)-2H-1-benzopyran-3-ol derivatives: novel potassium channel openers. |
AID721507 | Induction of proliferation of mouse calvarial osteoblasts at 1 pM to 1 uM after 48 hrs | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
AID611949 | Vasorelaxant activity in potassium depolarized guinea pig aortic strip assessed as inhibition of calcium-induced contraction | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
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. |
AID185878 | Ability to lower blood pressure in the spontaneously hypertensive rat (SHR) at 10 mg/kg (p.o.) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | 2-Ethynylbenzenealkanamines. A new class of calcium entry blockers. |
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. |
AID1615132 | Vasodilating activity in Wistar rat aortic rings assessed as reduction in phenylephrine-induced contractions relative to control | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
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. |
AID171865 | Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR),at 0.5-2h after 30 mg/kg oral administration | 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. |
AID1587141 | Inhibition of voltage-dependent L-type calcium channel in human SH-SY5Y cells assessed as protection against glutamate-induced excitotoxicity by measuring recovery of cell viability at 1 uM measured after 24 hrs by alamar blue-based fluorescence method re | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
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. |
AID1587143 | Inhibition of voltage-dependent L-type calcium channel in Wistar rat brain slices assessed as protection against oxygen glucose deprivation/reperfusion-induced injury by measuring recovery of LDH release at 20 uM administered at onset of reperfusion perio | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID61748 | Coronary vasodilator activity in dogs, after administration of a dose of 150 micorg/kg intravenously | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives. |
AID185906 | Maximum fall in blood pressure was evaluated at an oral dose of 1.0 mg/kg in (SHR) spontaneous hypertensive rats | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Synthesis and antihypertensive activity of 4-(cyclic amido)-2H-1-benzopyrans. |
AID1615138 | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1918192 | Inhibition of human OAT2 tv.1 variant expressed in HEK293 cells assessed as inhibition of [3H]cGMP uptake by scintillation analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment. |
AID694787 | Inhibition of KCl-induced Ca2+ overload in Sprague-Dawley rat primary cortical neurons assessed as reduction in F340/F380 fluorescence ratio at 1 uM by Fura-2/AM-based fluorescence assay (Rvb = 1.31 +/- 0.24) | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca²⁺ overload. |
AID1612579 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig aortic strips at 10'-6 M relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
AID174616 | Duration of action in spontaneously hypertensive rats. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID1232310 | Volume of distribution at steady state in human | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID1210074 | Inhibition of CYP1A2 in human liver microsomes using phenacetin 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. |
AID235556 | Ratio of pIC50 of rat aorta to pIC25 of guinea pig | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists. |
AID1698830 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial blood pressure at 1.5 mg/kg, po measured after 6 hrs | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Pharmacophore modeling, design, and synthesis of potent antihypertensives, oxazolo/thiazolo-[3,2-a]-pyrimidin-3(2H)-one, and 1,5-dihydroimidazo-[1,2-a]-pyrimidin-3(2H)-one derivatives: A pilot trial. |
AID165729 | Vasorelaxant effect at a concentration of 10e-8 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID550024 | Inhibition of human recombinant calmodulin assessed as inhibition of calmodulin-sensitive cAMP phosphodiesterase activation after 15 mins by spectrophotometric analysis | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. |
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. |
AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID439058 | Inhibition of calcium-induced contraction in guinea pig ileum | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties. |
AID234479 | Ratio between the EC30 values of atrial contractility and atrial rate | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties. |
AID1587170 | Inhibition of calcium-induced contraction in K+-depolarized guinea pig aortic strips at 10'-6 M relative to control | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 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). |
AID1872390 | Inhibition of EZH2-EED (unknown origin) protein interaction by FP binding assay | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
AID1277327 | Neuroprotective activity against potassium ion-induced cytotoxicity in human SH-SY5Y cells assessed as cell viability at 3 uM pretreated for 24 hrs measured 24 hrs post potassium ion challenge by MTT assay relative to control | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Neuroprotective profile of pyridothiazepines with blocking activity of the mitochondrial Na(+)/Ca(2+) exchanger. |
AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID167373 | Rate of reversal by Bay K 8644 of the blockade of K+ - stimulated rabbit aortic strips produced by the compound | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID1193499 | Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID95741 | Free energy of binding (delta G) for inactivated state (is) of voltage-gated L-type [Ca2+] channel(VGCCs) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Stereoselective characterization of the 1,4-dihydropyridine binding site at L-type calcium channels in the resting state and the opened/inactivated state. |
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] | |||
AID195196 | Inhibitory effect of compound on contraction induced by high potassium in isolated rat aorta | 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. |
AID1587145 | Negative inotropic activity in guinea pig left atrium assessed as decrease in developed tension at 10'-5 M relative to control | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID167659 | Compound was tested for ability to relax potassium-contracted rabbit aorta smooth muscle | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Studies directed toward ascertaining the active conformation of 1,4-dihydropyridine calcium entry blockers. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-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. |
AID76659 | Antagonistic activity against ACh in guinea pig ileum. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 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). |
AID1141123 | Neuroprotective activity against rotenone-oligomycin A-induced oxidative stress in human SH-SY5Y cells assessed as survival incubated with rot/oligo for 8 hrs followed by treated with compound at 5 uM for 16 hrs by MTT assay (Rvb =70.6 +/- 1.8%) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID317287 | Chronotropic activity at L type calcium channel in guinea pig right atrium assessed as decrease in spontaneous beating at 0.1 uM relative to control | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID434150 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced diastolic blood pressure at 10 mg/kg, po after 60 mins by invasive carotid artery cannulation method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID195195 | Inhibitory effect of compound on calcium influx by high potassium in isolated rat aorta | 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. |
AID101854 | Compound was tested for percent of fraction inhibition by anti-P-450 NF. | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Oxidation of 4-aryl- and 4-alkyl-substituted 2,6-dimethyl-3,5-bis(alkoxycarbonyl)-1,4-dihydropyridines by human liver microsomes and immunochemical evidence for the involvement of a form of cytochrome P-450. |
AID1615140 | Cytotoxicity against human MSC assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID717844 | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID434145 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 300 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID86389 | Inhibitory effect on L-triiodothyronine (L-T3) uptake by human HepG2 hepatoma cells at an application dose 10E-5 M | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Inhibition of thyroid hormone uptake by calcium antagonists of the dihydropyridine class. |
AID1141120 | Neuroprotective activity against K+ induced Ca2+ overload in human SH-SY5Y cells assessed as protection at 5 uM after 24 hrs by MTT assay relative to control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID1248193 | Inhibition of porcine kidney ACE assessed as reduction in hippuryl-histidyl-leucine hydrolysis to hippuric acid release incubated for 30 mins high-throughput colorimetric method | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID478851 | Antagonist activity at rabbit Cav1.2 expressed in HEK293 cells assessed as inhibition of voltage pulse-induced calcium current at 100 nM by FLIPR calcium 4 assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
AID1248195 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 1 hr by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID175303 | Concentration required to produce 25% increase in intraventricular pressure(LV dp/dt) | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | 2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers. |
AID77008 | The compound was tested for inhibition of muscarinic responses in guinea pig ileal longitudinal smooth muscle | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12 | Crystal structures of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-[2-nitro-, 3-cyano-, 4-(dimethylamino)-, and 2,3,4,5,6-pentafluorophenyl]-1,4-dihydropyridine. |
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. |
AID167553 | In vitro inhibition of potassium-induced contractions in rabbit aorta strips. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. |
AID197527 | Concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50% | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Long-acting dihydropyridine calcium antagonists. 4. Synthesis and structure-activity relationships for a series of basic and nonbasic derivatives of 2-[(2-aminoethoxy)methyl]-1,4-dihydropyridine calcium antagonists. |
AID1184068 | Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins by HPLC | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
AID616225 | Antifertility activity against goat epididymis sperm cells assessed as inhibition of sperm motility at 1.25 mM after 2 hrs by Sander-Cramer test | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 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). |
AID1141122 | Neuroprotective activity against rotenone-oligomycin A-induced oxidative stress in human SH-SY5Y cells assessed as protection at 5 uM co-incubated rot/oligo for 24 hrs by MTT assay relative to control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID197523 | Evaluated for the negative logarithm of the molar concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50%. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5 -(methoxycarbonyl)-6-methyl-1,4-dihydropyridine. |
AID1291202 | Inhibition of Ach-induced contraction in Sprague-Dawley rat trachea at 1 to 100 umol/L | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | New isosteroidal alkaloids with tracheal relaxant effect from the bulbs of Fritillaria pallidiflora Schrenk. |
AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
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. |
AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID624623 | Apparent permeability (Papp) from basolateral to apical 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. |
AID22293 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID9879 | Time to peak response on lowering of vascular resistance, in dogs when administered intravenously | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity. |
AID640615 | Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Capture hydrolysis signals in the microsomal stability assay: molecular mechanisms of the alkyl ester drug and prodrug metabolism. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID181533 | Antihypertensive activity when administered orally to spontaneously hypertensive rats | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Dihydropyrimidine calcium channel blockers. 3. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic acid esters as orally effective antihypertensive agents. |
AID1248199 | Antihypertensive activity in Norwegian albino rat model of DOCA-salt-induced hypertension assessed as inhibition of systolic blood pressure at 10 mg/kg, po after 5 hrs by non-invasive tail cuff method relative to control | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers. |
AID1612574 | Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment. |
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. |
AID1587140 | Inhibition of voltage-dependent L-type calcium channel in human U373MG cells assessed as protection against oxygen glucose deprivation/reperfusion-induced injury by measuring recovery of cell viability at 20 uM administered at onset of reperfusion period | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. |
AID34238 | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16 | Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. |
AID59297 | Effective dose that lowers vascular resistance by, 30% in dogs when administered intravenously | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID233859 | Selectivity between calcium antagonist activity vs negative inotropy in guinea pig | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Long acting dihydropyridine calcium antagonists. 2. 2-[2-Aminoheterocycloethoxy]methyl derivatives. |
AID333050 | Antihypertensive activity in sham operated anesthetized SHR rat assessed as reduction of mean blood pressure at 10 mg/kg, iv | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID317278 | Inotropic activity at L type calcium channel in guinea pig left atrium assessed as decrease in tension at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID1068426 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced seizures by measuring latency period at 30 mg/kg, po pretreated for 1 hr followed by pentylenetetrazole challenge measured over 300 secs (R | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
AID721504 | Induction of mineralization in mouse calvarial osteoblasts assessed as increase of mineralized nodules formation after 21 days by alizarin red-S staining based spectrophotometric analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Discovery of coumarin-dihydropyridine hybrids as bone anabolic agents. |
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). |
AID1232313 | Elimination half life in human | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID311367 | Permeability coefficient in human skin | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds. |
AID195183 | Vasodilator activity was measured on rat aorta in the presence of ODQ. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities. |
AID1577804 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as diastolic left ventricular posterior wall thickness at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiogr | |||
AID717840 | Inhibition of mouse Tdo2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 100 uM after 45 mins by spectrophotometric analysis relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
AID167549 | Relative potency was evaluated. (relative potency = IC50 of compound / IC50 of nifedipine) | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. |
AID439056 | Inhibition of calcium-induced contraction in guinea pig ileum at 0.001 to 0.1 uM | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties. |
AID1211793 | Lipophilicity, log P 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. |
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. |
AID45781 | Inhibition of [3H]nitrendipine binding to L-type calcium channel from rat brain cortex homogenate | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate. |
AID29421 | Partition coefficient (logP) (HPLC) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | ElogPoct: a tool for lipophilicity determination in drug discovery. |
AID434138 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 420 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
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. |
AID79830 | Negative logarithm of the molar concentration required to depress contraction in the Langendorff-perfused guinea pig heart by 25%. | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives. |
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. |
AID56025 | Displacement of [3H]nitrendipine from dihydropyridine receptor of guinea pig myocardial membranes | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. |
AID227627 | Vasorelaxant effect on KCl-Induced contraction of rat aorta | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | Synthesis and selective coronary vasodilatory activity of 3,4-dihydro-2,2-bis(methoxymethyl)-2H-1-benzopyran-3-ol derivatives: novel potassium channel openers. |
AID434141 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 60 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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. |
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). |
AID1207671 | 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. |
AID1055886 | Vasorelaxant activity in rat endothelium-intact thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, ex vivo and in silico studies of 3-cyano-2-pyridone derivatives with vasorelaxant activity. |
AID166478 | Effect on 35 mM K+-induced contraction on rabbit aorta at a dose of 3*10e-6 mol/L; NT=Not tested | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines. |
AID227699 | Virtual screen for compounds with anticonvulsant activity | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity. |
AID235901 | Selectivity index calculated as the ratio of Calcium pIC50 to that of negative inotropy IC25 | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5 -(methoxycarbonyl)-6-methyl-1,4-dihydropyridine. |
AID55902 | Cardiovascular effect upon coronary artery blood flow(CBF) in anesthetized open-chest dogs at a dose of 10 ug/ kg administered intravenously | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Novel selective hindlimb vasodilators: synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives. |
AID194644 | Compound was evaluated for antihypertensive activity in deoxy-corticosterone acetate (DOCA) treated hypertensive rats at 1 mg/kg peroral administration | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols. |
AID165723 | Vasorelaxant effect at a concentration of 10e-5 M on rabbit aortic rings previously contracted with 1.0 uM Norepinephrine. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport 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. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID76660 | Antagonistic activity against K+ induced responses in guinea pig ileum. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | New developments in Ca2+ channel antagonists. |
AID76372 | Inhibition of K+ induced contractions of the isolated guinea pig ileum. | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. |
AID1367793 | Half life in human at 10 mg, tid | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Relevance of Half-Life in Drug Design. |
AID317314 | Displacement of (+)-[5-methyl-3H]PN200-100 from L type calcium channel Cav1.2a in rabbit expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity. |
AID127918 | Concentration causing local anesthetic activity in mice | 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. |
AID78157 | Calcium channel antagonist activity causing 50% inhibition of carbachol (1.6 x 10-7 M) induced Ca++ dependent contraction (tonic response) in guinea pig ileum longitudinal smooth muscle | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Syntheses, calcium channel agonist-antagonist modulation activities, and nitric oxide release studies of nitrooxyalkyl 1,4-dihydro-2,6-dimethyl-3-nitro-4-(2,1,3-benzoxadiazol-4-yl)pyridine-5-carboxylate racemates, enantiomers, and diastereomers. |
AID185909 | Maximum fall in blood pressure was evaluated at an oral dose of 3.0 mg/kg in (SHR) spontaneous hypertensive rats | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Synthesis and antihypertensive activity of 4-(cyclic amido)-2H-1-benzopyrans. |
AID1615133 | Vasodilating activity in Wistar rat aortic rings assessed as reduction in KCl-induced contractions | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. |
AID611867 | Negative ionotropic activity against potassium-induced contraction in guinea pig left atrium assessed as decrease atrial rate at 10'-5 M relative to control | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines. |
AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID101858 | Rate of Oxidation in human liver microsomes is measured as mean (nmol product) formed / min per nmol cytochrome P-450 | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Oxidation of 4-aryl- and 4-alkyl-substituted 2,6-dimethyl-3,5-bis(alkoxycarbonyl)-1,4-dihydropyridines by human liver microsomes and immunochemical evidence for the involvement of a form of cytochrome P-450. |
AID1193494 | Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID747100 | Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity. |
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. |
AID1232312 | Clearance in human | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID1581349 | Vasodilating activity in Wistar rat endothelium-denuded aortic rings preconstricted with 100 mM KCl assessed as vasorelaxation at 10 nM relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
AID1055885 | Vasorelaxant activity in rat endothelium-intact thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, ex vivo and in silico studies of 3-cyano-2-pyridone derivatives with vasorelaxant activity. |
AID1577805 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as systolic left ventricular posterior wall thickness at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiogra | |||
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AID1581332 | Antioxidant activity assessed as Trolox equivalents incubated for 15 mins by fluorescein based ORAC-FL assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
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AID1380097 | Inhibition of Cch1 in Candida albicans isolate 10 assessed as potentiation of fluconazole-induced antifungal activity by measuring fractional inhibitory concentration index after 24 hrs by checkerboard assay | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Emerging New Targets for the Treatment of Resistant Fungal Infections. |
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AID1577802 | Antifibrotic activity in abdominal aortic constriction Sprague-Dawley rat model of cardiac fibrosis assessed as diastolic left ventricular internal diameter at 10 mg/kg, ip administered once daily for 4 weeks measured post-last dose by echocardiography (R | |||
AID235709 | Selectivity for vascular (Ca pIC50) over cardiac (negative inotropy IC25) calcium channels | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID1055884 | Vasorelaxant activity in rat endothelium-denuded thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, ex vivo and in silico studies of 3-cyano-2-pyridone derivatives with vasorelaxant activity. |
AID1141118 | Selectivity ratio of IC50 for human Cav1.3 channel to IC50 for rat Cav1.2 channel | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury. |
AID333043 | Inhibition of noradrenaline release in sham operated anesthetized SHR rat plasma at 15 mg/kg, iv after 20 mins | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2 | Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum. |
AID434143 | Antihypertensive activity in Norwegian albino rat assessed as inhibition of DOCA salt-induced systolic blood pressure at 10 mg/kg, po after 180 mins by non-invasive tail-cuff method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID392820 | Antagonist activity at calcium channel in guinea pig ileum assessed as inhibition of KCl-induced contraction of ileal longitudinal smooth muscle pretreated 15 mins before KCl challenge | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Synthesis and biological evaluation of some new 1,4-dihydropyridines containing different ester substitute and diethyl carbamoyl group as anti-tubercular agents. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1346690 | Mouse Kv1.1 (Voltage-gated potassium channels) | 1994 | Molecular pharmacology, Jun, Volume: 45, Issue:6 | Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. |
AID1346684 | Human Kv1.5 (Voltage-gated potassium channels) | 1994 | Molecular pharmacology, Jun, Volume: 45, Issue:6 | Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. |
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AID1346741 | Human Pregnane X receptor (1I. Vitamin D receptor-like receptors) | 1998 | Proceedings of the National Academy of Sciences of the United States of America, Oct-13, Volume: 95, Issue:21 | Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. |
AID1346704 | Rat Kv1.2 (Voltage-gated potassium channels) | 1994 | Molecular pharmacology, Jun, Volume: 45, Issue:6 | Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. |
AID1346681 | Mouse Kv3.1 (Voltage-gated potassium channels) | 1994 | Molecular pharmacology, Jun, Volume: 45, Issue:6 | Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. |
AID1346659 | Mouse Kv1.7 (Voltage-gated potassium channels) | 1998 | The Journal of biological chemistry, Mar-06, Volume: 273, Issue:10 | Genomic organization, chromosomal localization, tissue distribution, and biophysical characterization of a novel mammalian Shaker-related voltage-gated potassium channel, Kv1.7. |
AID1346650 | Human Cav1.3 (Voltage-gated calcium channels) | 2009 | Molecular pharmacology, Feb, Volume: 75, Issue:2 | Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
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AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 5659 (37.75) | 18.7374 |
1990's | 5077 (33.87) | 18.2507 |
2000's | 2532 (16.89) | 29.6817 |
2010's | 1432 (9.55) | 24.3611 |
2020's | 291 (1.94) | 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 (112.43) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 2,496 (15.58%) | 5.53% |
Trials | 0 (0.00%) | 5.53% |
Reviews | 776 (4.84%) | 6.00% |
Reviews | 2 (6.67%) | 6.00% |
Case Studies | 958 (5.98%) | 4.05% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 15 (0.09%) | 0.25% |
Observational | 0 (0.00%) | 0.25% |
Other | 11,779 (73.51%) | 84.16% |
Other | 28 (93.33%) | 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 | ||
---|---|---|---|---|---|---|---|
Blood Pressure Control of Nifedipine GITS 60mg Treatment in Chinese Hypertensive Subjects Uncontrolled on Starting-dose Mono-therapy: A Prospective, Open-label, Multicenter, Single-arm, 8-week Study. [NCT02413515] | Phase 4 | 278 participants (Actual) | Interventional | 2015-03-26 | Completed | ||
A Multicenter, Double-blind, Parallel-group Comparative Study Between Oral BAYA1040_CR 80 mg and 40 mg for 8 Weeks in Patients With Essential Hypertension for Whom Oral BAYA1040_CR 40 mg is Insufficient [NCT01287260] | Phase 3 | 352 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
Post-marketing Surveillance for Hypertensive Patients With Diabetes and/or Chronic Kidney Disease [NCT01363336] | 1,882 participants (Actual) | Observational | 2009-11-30 | Completed | |||
AdADOSE - Antihypertensive Treatment With Adalat® in Different Doses and Combination Therapy [NCT01118286] | 4,497 participants (Actual) | Observational | 2010-01-31 | Completed | |||
Pilot Treatment of Persistent Non-Severe Postpartum Hypertension [NCT04349124] | Phase 4 | 12 participants (Actual) | Interventional | 2020-08-25 | Terminated(stopped due to Unable to continue recruiting) | ||
Does Adjunctive Treatment With Vaginal Nifedipine Result in Symptomatic Improvement in Patients With Levator Myalgia and Pelvic Floor Pain Who Are Undergoing Pelvic Floor Physical Therapy? [NCT01586286] | 0 participants (Actual) | Interventional | 2012-07-31 | Withdrawn(stopped due to No patients were recruited over a 12 month period) | |||
A Randomized Controlled Trial Comparing Nifedipine and Enalapril in Medical Resources Used in the Postpartum Period [NCT04236258] | Phase 4 | 94 participants (Actual) | Interventional | 2020-01-24 | Completed | ||
Single Dose Study to Compare the Pharmacokinetics as Well as Safety and Tolerability of a Novel Fixed Dose Combination of Nifedipine GITS and Candesartan, the Loose Combination of Both and the Single Components Alone and to Investigate the Bioequivalence [NCT01227603] | Phase 1 | 49 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
Diastolic Heart Failure Management by Nifedipine [NCT01157481] | 226 participants (Actual) | Interventional | 2010-07-31 | Active, not recruiting | |||
A Multicenter, Open Label, Long Term Study of Oral BAYA1040_CR 80 mg (40 mg Bid) in Combination With Other Antihypertensives for 52 Weeks in Patients With Essential Hypertension [NCT01294215] | Phase 3 | 72 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
Non-invasive Hemodynamic Monitoring and Goal-Directed Therapy in Pregnant Women at High Risk of Developing Preeclampsia [NCT01351428] | 20 participants (Actual) | Interventional | 2010-12-31 | Completed | |||
Single Dose Study to Compare the Pharmacokinetics as Well as Safety and Tolerability of a Novel Fixed Dose Combination of Nifedipine GITS and Candesartan and the Loose Combination of Both Components and to Investigate the Bioequivalence Between the Fixed [NCT01350609] | Phase 1 | 49 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
A Multicenter, Open Label, Long Term Extension Study of Oral BAYA1040 CR 80 mg (40 mg Bid) for 44 Weeks in Patients With Essential Hypertension (Extension From Study 13176) [NCT01355367] | Phase 3 | 120 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
Influence of Genetic Polymorphisms of ABCG2/BCRP on the Transport of Nifedipine to Breast Milk in Hypertensive Breastfeeding Women. [NCT03710395] | Phase 4 | 19 participants (Anticipated) | Interventional | 2015-12-14 | Active, not recruiting | ||
Randomized Controlled Trial for Postpartum Antihypertensive Treatment of Women With Preeclampsia [NCT04298034] | Phase 3 | 300 participants (Anticipated) | Interventional | 2020-07-17 | Recruiting | ||
Individualized Dosing of Nifedipine for Tocolysis in Preterm Labor [NCT02090920] | 20 participants (Actual) | Observational | 2011-07-31 | Completed | |||
A Comparative Study for the Effects of Nifedipine GITS and Amlodipine Besylate on Recovery of Blood Pressure Rhythm and Arterial Stiffness in the Young and Middle-aged Subjects With Non-dipper Hypertension [NCT02940548] | Phase 4 | 99 participants (Actual) | Interventional | 2016-12-31 | Terminated(stopped due to The patient recruitment and follow-ups were influenced with the pandemic of COVID-19) | ||
Single Dose Escalation Study to Investigate the Pharmacokinetics as Well as Safety and Tolerability of a Concomitant Administration of Nifedipne GITS and Candesartan Tablets Under Fasting Conditions in Healthy Male Subjects in an Open Label, Non-randomize [NCT03136666] | Phase 1 | 12 participants (Actual) | Interventional | 2010-04-19 | Completed | ||
Oral Nifedipine Versus Intravenous Magnesium Sulfate for Prevention of Preterm Labor in Symptomatic Placenta Previa: Randomized Controlled Trial. [NCT03542552] | Phase 3 | 176 participants (Actual) | Interventional | 2018-06-01 | Completed | ||
Personalized Hemodynamically Guided Antihypertensive Treatment in Pregnant Women With Mild to Moderate Hypertension: a Randomized Controlled Trial [NCT02531490] | Phase 4 | 368 participants (Anticipated) | Interventional | 2015-01-01 | Recruiting | ||
A Relative Bioavailability Study of 60 mg Nifedipine Extended Release Tablets Under Non-Fasting Conditions [NCT00864617] | Phase 1 | 84 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
THE EFFECTS OF SITAXSENTAN ONCE DAILY DOSING ON PROTEINURIA, 24-HOUR BLOOD PRESSURE, AND ARTERIAL STIFFNESS IN SUBJECTS WITH CHRONIC KIDNEY DISEASE [NCT00810732] | Phase 2 | 27 participants (Actual) | Interventional | 2007-05-09 | Completed | ||
Pharmacokinetics and Safety of Commonly Used Drugs in Lactating Women and Breastfed Infants [NCT03511118] | 1,600 participants (Anticipated) | Observational | 2018-10-04 | Recruiting | |||
Nifedipine Pharmacokinetics and Pharmacodynamics When Used as a Tocolytic in Patients Hospitalized for Acute Threatened Preterm Labour [NCT02068404] | Phase 4 | 75 participants (Anticipated) | Interventional | 2014-04-30 | Recruiting | ||
Treatment of Elevated Blood Pressures in Early Pregnancy [NCT05955040] | Phase 2 | 234 participants (Anticipated) | Interventional | 2023-07-11 | Recruiting | ||
Efficacy of Nifedipine Versus Hydralazine in Management of Severe Hypertension in Pregnancy - A Randomised Controlled Trial [NCT04435210] | 69 participants (Actual) | Interventional | 2018-08-13 | Completed | |||
Random, Open Label, Active Comparator-controlled Parallel Study to Evaluate the Efficacy of Nifedipine Controlled-released Tablets (Xin Ran) in Patients With Mild to Moderate Essential Hypertension [NCT02031861] | Phase 4 | 38 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
Prospective Multicenter Randomized Parallel Controlled Clinical Trial to Evaluate the Safety and Effectiveness of a Radiofrequency Renal Denervation System for the Treatment of Essential Hypertension [NCT03261375] | 205 participants (Actual) | Interventional | 2021-01-19 | Completed | |||
Clinical Study on the Effect of PTH on CYP3A4 Activity [NCT03695107] | 200 participants (Anticipated) | Observational | 2019-10-02 | Recruiting | |||
Is Procardia XL 60 mg Q Daily Equivalent to 30 mg XL Given Twice Daily? [NCT03595982] | Phase 4 | 5 participants (Actual) | Interventional | 2018-09-15 | Terminated(stopped due to Low enrollment) | ||
Regional Grafting of Autologous Adipose Tissue in the Treatment of Systemic Sclerosis Digital Ulcers: a Prospective Randomized Controlled Study [NCT03406988] | 46 participants (Anticipated) | Interventional | 2017-07-18 | Recruiting | |||
Randomized Open-label 2-arm Parallel Design Comparator Study of the Effect of Adalat® XL® Compared to Diltiazem on Proteinuria and Blood Pressure in Patients With Diabetes and Mild to Moderate Hypertension When Used as an Add on to Avalide® [NCT00713011] | Phase 3 | 0 participants (Actual) | Interventional | 2008-11-30 | Withdrawn(stopped due to Study was stopped by sponsor prior to first patient assignment to groups due to operational reasons.) | ||
Bioequivalence of Extended Release Nifedipine Tablets in Healthy Chinese Subjects: A Single-dose and Two-period Crossover Study [NCT04438720] | Phase 1 | 60 participants (Anticipated) | Interventional | 2020-06-25 | Recruiting | ||
Nifedipine vs. Indomethacin in the Treatment of Preterm Labour and Short Cervix. A Randomized, Controlled Trial. [NCT01360034] | Phase 3 | 216 participants (Anticipated) | Interventional | 2015-12-31 | Not yet recruiting | ||
A Single-Dose, Open-label, Randomized, Crossover, Drug-Drug Interaction Study of Nifedipine Extended-release Tablets With or Without Multiple-dose Administration of Proton-Pump Inhibitor Omeprazole/Sodium Bicarbonate in Healthy Volunteers [NCT03100838] | Phase 1 | 64 participants (Actual) | Interventional | 2017-03-20 | Completed | ||
ADMINISTRATION OF NIFIDEPINE VERSUS ATOSIBAN IN PREGNANT WOMEN WITH A THREAT OF PREMATURE LABOR [NCT01314859] | Phase 3 | 0 participants (Actual) | Interventional | 2011-07-31 | Withdrawn | ||
The Effect of Intra-anal Nifedipine, Used As Add-on to Conservative Therapy, on Pain in Patients With Anal Fissure [NCT02527109] | Phase 2/Phase 3 | 339 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
Oral Nifedipine Versus IV Labetalol in Treatment of Severe Pre Eclampsia in Pregnancy [NCT03325348] | Phase 2/Phase 3 | 194 participants (Anticipated) | Interventional | 2017-02-23 | Recruiting | ||
Tocolytic Therapy for Preterm Labor in Multiple Gestation [NCT02725736] | Phase 3 | 140 participants (Anticipated) | Interventional | 2016-03-31 | Not yet recruiting | ||
[NCT00000530] | Phase 3 | 0 participants | Interventional | 1992-09-30 | Completed | ||
Non-Invasive Positive Pressure Ventilation Management of High Altitude Pulmonary Edema [NCT04288219] | 16 participants (Anticipated) | Interventional | 2020-03-01 | Recruiting | |||
The Systemic & Renal Effects of Endothelin Receptor Antagonism in Proteinuric Nephropathy [NCT00722215] | Phase 1 | 22 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
A Randomized Controlled Study of Nifecardia SRFC (Nifedipine) and Adalat OROS (Nifedipine) in the Treatment of Patients With Essential Hypertension [NCT00173667] | Phase 4 | 60 participants | Interventional | Not yet recruiting | |||
The Effects of Doxazosin and Nifedipine on Blood Pressure Variability and Uric Acid in Plasma in Hypertensive Patients [NCT02563405] | Phase 2/Phase 3 | 30 participants (Anticipated) | Interventional | 2015-09-30 | Recruiting | ||
Tocolysis in the Management of Preterm Premature Rupture of Membranes Before 34 Weeks of Gestation: a Double-blinded Randomized Controlled Trial [NCT03976063] | Phase 3 | 850 participants (Anticipated) | Interventional | 2019-10-07 | Recruiting | ||
An Open Label Study to Examine the Effect of Coated Nifedipine Suppositories on Anal Pressure in Healthy Subjects [NCT00816205] | Phase 1/Phase 2 | 0 participants | Interventional | Completed | |||
A Relative Bioavailability Study of 60 mg Nifedipine Extended Release Tablets Under Fasting Conditions [NCT00865891] | Phase 1 | 96 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
A Multicenter, Multifactorial, Randomized, Double-Blind, Placebo-Controlled Dose-Finding Study of Nifedipine GITS and Candesartan in Combination Compared to Monotherapy in Adult Patients With Essential Hypertension [NCT01303783] | Phase 2 | 1,381 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
An Initial Clinical Study to Treat Postictal Symptoms [NCT03949478] | Phase 2 | 90 participants (Anticipated) | Interventional | 2021-02-01 | Recruiting | ||
A Single-center, Open-Label, Drug Interaction Study to Determine the Effects of Apatinib on the Metabolism of CYP3A4/5 and CYP2C9 Probe Drugs in Patients With Solid Tumors [NCT03245307] | Phase 1 | 20 participants (Anticipated) | Interventional | 2017-08-22 | Recruiting | ||
The Influence of Nifedipine Treatment on Uterine Contractility During Frozen Embryo Transfer [NCT02072291] | Phase 2 | 90 participants (Anticipated) | Interventional | 2014-03-31 | Recruiting | ||
Crossover Randomised Bioavailability Clinical Study Of A Single Dose Of Nifedipine Oral Solution From Laboratorio Reig Jofre S.A. Compared To Adalat(R) Capsules In Healthy Female Volunteers [NCT02071589] | Phase 1 | 36 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
Assessment of Efficacy and Side Effects of Dlitiazem Ointment With Lidocaine vs. Diltiazem Ointment With Lidocaine for Treatment of Chronic Anal Fissure: Randomized Clinical Trial [NCT04887818] | Phase 2/Phase 3 | 430 participants (Anticipated) | Interventional | 2021-06-30 | Not yet recruiting | ||
Intensive Postpartum Antihypertensive Treatment to Improve Women's Cardiovascular Health (IPAT Study) [NCT05687344] | Phase 3 | 60 participants (Anticipated) | Interventional | 2023-09-01 | Recruiting | ||
A Multicenter Study Evaluating the Efficacy of Nifedipine GITS - Telmisartan Combination in Blood Pressure Control and Beyond: Comparison of Two Treatment Strategies. [NCT00750113] | Phase 4 | 405 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
"Cardiac Transfer of SARS-CoV-2 Spike Protein Circulation Techniques - Medicine Induced Hemodialysis on Vaccinated Immune Attacks" [NCT05711810] | Phase 4 | 1 participants (Actual) | Interventional | 2023-01-02 | Completed | ||
The Effect of Sitaxsentan Once Daily Dosing on Proteinuria, 24-Hour Systemic Blood Pressure, and Arterial Stiffness in Subjects With Chronic Kidney Disease [NCT00817037] | Phase 2 | 27 participants (Actual) | Interventional | 2007-05-31 | Active, not recruiting | ||
A Prospective, Open-label, Active-controlled, Randomized Study Comparing Nifedipine GITS Versus Valsartan Versus a Combination of Both on Central Blood Pressure in Inadequately Controlled Essential Hypertension. [NCT01071122] | Phase 4 | 365 participants (Actual) | Interventional | 2010-01-31 | 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 | |||
Effect of Nifedipine GITS in Patients With Mild-to-moderate Primary Hypertension: a Multi-center, Open-label, Observational Study [NCT02641821] | Phase 4 | 700 participants (Anticipated) | Interventional | 2015-10-31 | Recruiting | ||
Maintenance Oral Nifedipine for Management of Symptomatic Placenta Previa : A Randomized Clinical Trial [NCT00620724] | Phase 2 | 109 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
Extended Release Nifedipine Treatment as Maintenance Tocolysis to Prevent Preterm Delivery:A Prospective Interventional Study [NCT00525486] | 0 participants | Interventional | 2007-12-31 | Terminated | |||
An Open Label Study to Examine the Effect of Coated Nifedipine Suppository on Anal Fissure Pain and Healing in Human Subjects [NCT00972907] | Phase 1/Phase 2 | 20 participants (Anticipated) | Interventional | 2009-12-31 | Completed | ||
Frequency and Dosing of Long Acting Anti-Hypertensive Agent in Women With Pre-eclampsia With Severe Features Undergoing Expectant Management: A Randomized Controlled Trial [NCT05096728] | 56 participants (Actual) | Observational | 2021-12-01 | Completed | |||
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404] | 5,000 participants (Anticipated) | Observational | 2020-03-05 | Recruiting | |||
the Therapeutic Effect Treated With Tamsulosin After ESWL in Urinary Calculus [NCT01010048] | Phase 4 | 120 participants (Anticipated) | Interventional | 2009-10-31 | Recruiting | ||
The Tocolytic Efficacy of Nifedipine in the Management of Threatened and Advanced Preterm Labor: A Study on 444 Singleton Pregnant Women With Intact Membranes [NCT04644354] | 444 participants (Anticipated) | Observational | 2020-12-15 | Not yet recruiting | |||
Effects of Adalat LA 30 mg and Coracten 30 mg on Nifedipine Plasma Concentration , Plasma Catecholamines, Blood Pressure Response and Heart Rate in Fed Mild to Moderate Hypertensive Patients. [NCT00672113] | Phase 4 | 43 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
Efficacy and Safety of Mexartan Potassium Tablets (AZL-M) and Calcium Channel Blockers (CCB) in the Treatment of Adults With Essential Hypertension in Chinese Population: a National Multicenter, Prospective, Observational Study [NCT05947448] | 1,215 participants (Anticipated) | Observational [Patient Registry] | 2023-09-25 | Not yet recruiting | |||
Nifedipine XL Versus Placebo for the Treatment of Preeclampsia With Severe Features During Induction of Labor [NCT04392375] | Phase 4 | 110 participants (Actual) | Interventional | 2020-06-09 | Completed | ||
Transdermal Nitroglycerin and Nifedipine for Managing Preterm Labor: a Randomized Clinical Trial [NCT02583633] | Phase 4 | 112 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
the Effect of Nifedipine Controlled Release Tablets in Hypertensive Patients on Chronic Maintenance Hemodialysis and the Influence of Hemodialysis on the Plasma Concentration of Nifedipine [NCT01021501] | Phase 4 | 20 participants (Anticipated) | Interventional | 2009-12-31 | Not yet recruiting | ||
Evaluation of the Efficacy, Safety, and Pharmacokinetics/Pharmacodynamics of BAY A1040 CR Tablet on High Dose Administration in Patients With Essential Hypertension. [NCT00768560] | Phase 2 | 35 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
Comparing Fetal Cerebral Blood Flow Between Magnesium Sulfate & Calcium Channel Blockers in Patients With Preterm Labor; a Randomized Controlled Trial. [NCT02591004] | Phase 2/Phase 3 | 130 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
Evaluation of Alfuzosin as Medical Expulsion Therapy for Ureteral Stones [NCT00713739] | Phase 3 | 240 participants (Anticipated) | Interventional | 2008-01-31 | Recruiting | ||
Drug Discrimination in Methadone-Maintained Humans Study 2 [NCT00733239] | Phase 1 | 15 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
A Randomized Controlled Phase Ⅳ Trial With Two Equally Sized Treatment Groups: Amlodipine And Nifedipine GITS [NCT01030081] | Phase 4 | 510 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Safest Choice of Antihypertensive Regimen for Postpartum Hypertension: A Randomized Control Trial (SCARPH) [NCT05551104] | 500 participants (Anticipated) | Interventional | 2023-12-31 | Recruiting | |||
Phase 2 Study of Clinical Utility of Combination Tocolysis in Preterm Labor [NCT01429545] | Phase 2 | 110 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Drug Discrimination in Methadone-Maintained Humans Study 3 [NCT01068847] | Phase 1 | 9 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
A Multicenter, Randomized, Double-Blind, Monotherapy-Controlled Study of Nifedipine Gastrointestinal Therapeutic System and Candesartan Cilexetil in Combination Taken Orally for 8 Weeks in Adult Subjects With Essential Hypertension Who Are Inadequately Co [NCT02047019] | Phase 3 | 0 participants (Actual) | Interventional | 2017-12-01 | Withdrawn(stopped due to GPDC decided to terminate the study) | ||
[NCT00000478] | Phase 3 | 0 participants | Interventional | 1990-11-30 | Completed | ||
Randomized, Non-blind, 4-fold Crossover Study on Safety, Tolerability and Pharmacokinetics of Nifedipine After Single Oral Doses of Adalat® LA 60 mg or of a Marketed Generic Version of Nifedipine Retard 60 mg After an Overnight Fasting or Immediately Afte [NCT00884442] | Phase 1 | 28 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
Oral Antihypertensive Regimens for Management of Hypertension in Pregnancy [NCT01912677] | Phase 4 | 894 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
STUDY ON EFFICACY OF UTROGESTAN AS TOCOLYSIS FOR PRETERM LABOR [NCT01985594] | Phase 2 | 32 participants (Anticipated) | Interventional | 2013-11-30 | Not yet recruiting | ||
A 12 Weeks, Multi-center, Open Label, Randomized, Active Drug Parallel Control Trial to Compare the Effectiveness of Valsartan/Amlodipine and Nifedipine in Treating Chinese Hypertensive Patients Not Respond to Mono Antihypertensive Treatment [NCT01167153] | Phase 4 | 564 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
An Open Label Multi-Dose Study to Examine the Effect of Coated Nifedipine Suppository on Anal Fissure Pain and Healing [NCT02023047] | Phase 1/Phase 2 | 33 participants (Actual) | Interventional | 2014-03-31 | Terminated(stopped due to Met primary endpoint) | ||
Postoperative Renal Function After Open-Heart Surgery in Patients With Impaired Renal Function Preoperatively. A Study of the Calcium Channel Blocker Nifedipine's Prophylactic Effect on Further Decline in Renal Function. [NCT00244530] | Phase 4 | 20 participants | Interventional | 2001-06-30 | Completed | ||
Drug Discrimination in Methadone-Maintained Humans Study 1 [NCT00593463] | Phase 1 | 40 participants (Anticipated) | Interventional | 2006-09-30 | Completed | ||
Nifedipine Compared to Atosiban for Treating Preterm Labor. A Randomized Controlled Trial. [NCT00599898] | Phase 4 | 145 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
A Trial of Oral Nifedipine for the Treatment of Iron Overload [NCT00712738] | Phase 1 | 6 participants (Actual) | Interventional | 2008-06-20 | Completed | ||
Randomized,Open-label,Parallel Design Comparator Study of Effect of Nifedipine GITS/OROS (Adalat) 30 mg in Combination With Valsartan (Diovan) 80 mg Compared to Valsartan (Diovan) 160 mg Monotherapy in Patients Whose Blood Pressure is Not Well Controlled [NCT00993109] | Phase 4 | 360 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
A Pragmatic Multicenter Randomized Clinical Trial (RCT) of Antihypertensive Therapy for Mild Chronic Hypertension During Pregnancy: Chronic Hypertension and Pregnancy (CHAP) Project [NCT02299414] | Phase 4 | 2,408 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
Role of T-type Calcium Channels in Vascular Function [NCT02885558] | 12 participants (Actual) | Interventional | 2017-11-01 | Completed | |||
Tocolysis for Preterm Labor [NCT00811057] | 301 participants (Actual) | Interventional | 2004-06-30 | Completed | |||
The Effect of Nifedipine Versus Telmisartan on Prevention of Atrial Fibrillation Recurrence in Hypertensive Patients With Paroxysmal Atrial Fibrillation by Intensive Lower Blood Pressure [NCT01435161] | Phase 4 | 160 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
Ethnic Differences in Anti-Hypertensive Medication Response Among Pregnant and Postpartum Patients [NCT03506724] | Phase 4 | 109 participants (Actual) | Interventional | 2017-09-11 | Completed | ||
Randomized Study of Antihypertensives and Antilipemics in American Indians With Non-Insulin-Dependent Diabetes Mellitus at High Risk of Developing Nephropathy and Cardiovascular Disease [NCT00004266] | Phase 3 | 160 participants (Actual) | Interventional | 1993-08-31 | Completed | ||
Losartan Decreases Pulmonary Artery Pressure and Improves Exercise Capacity in Patients With Pulmonary Hypertension [NCT00519870] | Phase 3 | 0 participants | Interventional | 2005-01-31 | Completed | ||
Pharmacokinetics of Understudied Drugs Administered to Children Per Standard of Care [NCT01431326] | 3,520 participants (Actual) | Observational | 2011-11-30 | Completed | |||
Changes in Central Arterial Pressure When Comparing Nifedipine and Labetalol for Routine Hypertension Control in Pregnancy [NCT02912910] | 0 participants (Actual) | Observational | 2016-09-30 | Withdrawn(stopped due to PI withdrew protocol) | |||
Utility of Tocolytic Therapy for Maintenance Tocolysis in the Management of Threatened Preterm Delivery [NCT01796522] | Phase 3 | 0 participants (Actual) | Interventional | 2013-03-31 | Withdrawn(stopped due to have been published new studies that it showed the ineffectiveness of the treatments proposed in this study.) | ||
Choroidal Blood Flow Regulation During Isometric Exercise: Effects of Ca2+-Channel Blockade [NCT00280462] | 21 participants (Actual) | Interventional | 2005-08-31 | Completed | |||
Study of Different Doses of Nifedipine to Treat Preterm Labor [NCT00137501] | Phase 3 | 102 participants (Actual) | Interventional | 2003-05-31 | Terminated(stopped due to The trial was terminated because of difficulties in recruitement.) | ||
Comparative Study Between Nifedipine and Ritodrine as Maintenance Tocolytic Therapy in Preterm Labor: A Randomized Controlled Trial [NCT03040752] | Phase 4 | 200 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
The Effect of Zinc, Beta-carotene, and Vitamin D3 Supplementation as Pro-inflammation Mediated Regulator in Preterm Delivery Through Placental Protein Adaptor MyD88 and TRIF, Transcription Factor NFkB, and Pro-inflammatory Cytokine IL-1β [NCT03005496] | Phase 4 | 56 participants (Actual) | Interventional | 2017-01-31 | Completed | ||
[NCT00000102] | Phase 1/Phase 2 | 0 participants | Interventional | Completed | |||
Changes in Central Arterial Pressure When Comparing ACOG Hypertensive Urgency Protocols [NCT02933593] | 0 participants (Actual) | Interventional | 2016-08-31 | Withdrawn(stopped due to PI withdrew the protocol) | |||
Nifedipine for the Maintenance Tocolysis of Preterm Labor: Comparison to Placebo in a Prospective, Randomized Double Blind Trial [NCT00185952] | 70 participants (Actual) | Interventional | 2001-11-30 | Completed | |||
Changes in Central Arterial Pressure of Normotensive Women Taking Nifedipine for Tocolysis [NCT02902354] | 0 participants (Actual) | Interventional | 2016-09-30 | Withdrawn | |||
Topical Application of Nifedipine Cream for the Treatment of Vulvar Vestibulitis Syndrome [NCT00496184] | Phase 3 | 30 participants (Anticipated) | Interventional | 2006-04-30 | Completed | ||
Clinical Effect and Cost Effectiveness of Ca Antagonist in Combination With AII Receptor Antagonist in Patient With Essential Hypertension (PMS Study) [NCT01518855] | Phase 4 | 514 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
Treatment Targets for Chronic Hypertension in Pregnancy [NCT00194974] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2004-07-31 | Withdrawn(stopped due to Lack of funding) | ||
The Pathophysiology and Treatment of Supine Hypertension in Patients With Autonomic Failure [NCT00223717] | Phase 1 | 152 participants (Actual) | Interventional | 2001-01-31 | Completed | ||
Nifedipine for Acute Tocolysis of Preterm Labor [NCT02132533] | Phase 3 | 88 participants (Actual) | Interventional | 2014-05-05 | Completed | ||
Vaginal Indomethacin Versus Oral Nifedipine for Preterm Labor; a Randomized Controlled Trial [NCT04404686] | Phase 2/Phase 3 | 300 participants (Anticipated) | Interventional | 2020-10-31 | Not yet recruiting | ||
Black Education and Treatment of Hypertension (BEAT HTN) [NCT00661895] | Phase 4 | 99 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Indocin Versus Nifedipine for Preterm Labor Tocolysis - A Randomized Double-Blinded Clinical Trial [NCT00486824] | Phase 1/Phase 2 | 29 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Randomized Double-Blinded Trial of Magnesium Sulfate Tocolysis Versus Nifedipine Tocolysis in Women With Preterm Labor Between 24 to 32 6/7 Weeks' Gestation [NCT00306462] | 33 participants (Actual) | Interventional | 2006-03-31 | Terminated(stopped due to No enrollment in past year, lack of interest) | |||
[NCT02357615] | Phase 4 | 244 participants (Anticipated) | Interventional | 2014-12-31 | Recruiting | ||
HIGH Altitude CArdiovascular REsearch in the ANDES [NCT01830530] | Phase 4 | 100 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Comparison of the Effects of Nifedipine and Magnesium Sulfate on Maternal and Fetal Doppler Blood Flow Patterns in Women With Preterm Labor [NCT05520021] | 30 participants (Anticipated) | Interventional | 2022-09-01 | Recruiting | |||
Multicenter, Open-Label, Long-Term Safety and Efficacy Study of the Fixed Dose Combination of Nifedipine Gastrointestinal Therapeutic System and Candesartan Cilexetil in Adult Subjects With Moderate to Severe Essential Hypertension [NCT01788358] | Phase 3 | 508 participants (Actual) | Interventional | 2013-02-14 | Completed | ||
Comparison of Nifedipine Versus Indomethacin for Acute Preterm Labor [NCT03129945] | 36 participants (Actual) | Interventional | 2017-01-17 | Completed | |||
Comparison of Oral Nifedipine to Oral Labetolol for the Management of Severe Postpartum Hypertension [NCT02168309] | 50 participants (Actual) | Interventional | 2014-06-30 | 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) | ||
Effect of a Proposed Cav1.3 Inhibitor in Primary Aldosteronism - a Pilot Study [NCT05686993] | 15 participants (Anticipated) | Interventional | 2023-05-05 | Recruiting | |||
Three New Ideas to Protect Special Forces From the Stress of High Altitude [NCT02463357] | Phase 4 | 148 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
Labetalol or Nifedipine for Control of Postpartum Hypertension: A Randomized Controlled Trial [NCT05309460] | Phase 4 | 600 participants (Anticipated) | Interventional | 2022-06-06 | Not yet recruiting | ||
The Effect of Labetalol, Atenolol, and Nifedipine on Maternal Hemodynamics Measured by Impedance Cardiography in Early Pregnancy [NCT04755764] | 60 participants (Anticipated) | Observational | 2021-03-03 | Recruiting | |||
Oral Combined Hydrochlorothiazide/Lisinopril Versus Oral Nifedipine for Postpartum Hypertension: A Comparative Effectiveness Pilot Randomized Controlled Trial [NCT05049616] | Phase 4 | 70 participants (Actual) | Interventional | 2021-10-18 | Active, not recruiting | ||
Oral Nifedipine Versus Intravenous Labetalol for Postpartum (PP) Hypertensive Emergency: A Randomized Clinical Trial (RCT) [NCT05139238] | Phase 4 | 104 participants (Anticipated) | Interventional | 2023-08-01 | Not yet recruiting | ||
Effectiveness and Tolerability of Long-Acting Nifedipine Gastrointestinal Therapeutic System in Chronic Kidney Disease With Uncontrolled Hypertension Patients, a Prospective, Multicenter, Observational Study [NCT03194633] | 871 participants (Actual) | Observational | 2017-07-10 | Completed | |||
Comparison of Oral Labetalol and Oral Nifedipine for Postpartum Hypertension Management [NCT02426177] | Phase 3 | 98 participants (Anticipated) | Interventional | 2015-05-31 | Not yet recruiting | ||
Use of Impedance Cardiography to Decrease the Risk of Preeclampsia in Obese Patients [NCT03105661] | Early Phase 1 | 400 participants (Anticipated) | Interventional | 2017-04-04 | Recruiting | ||
Magnesium Sulfate Versus Nifedipine for the Acute Tocolysis of Preterm Labor: A Prospective, Randomized Trial [NCT00185900] | 192 participants (Actual) | Interventional | 1999-04-30 | Completed | |||
Nifedipine Alone or Nifedipine Plus Indomethacin for Treatment of Acute Preterm Labor: An Open Label, Randomized Comparative Effectiveness Controlled Trial [NCT02438371] | Phase 4 | 49 participants (Actual) | Interventional | 2015-05-31 | Terminated(stopped due to Study halted due to slow recruitment) | ||
Multicenter Randomized Double-Blind Control Trial Evaluating the Utility of Continuous Positive Airway Pressure (CPAP) in the Treatment of High Altitude Pulmonary Edema (HAPE) [NCT04186598] | 264 participants (Anticipated) | Interventional | 2020-01-20 | Recruiting | |||
Nifedipine Plus Magnesium Sulfate Versus Magnesium Sulfate Alone for Tocolysis in Pregnant Women at 28 - 31 Weeks Gestation With Threatened Preterm Labor [NCT05345132] | 264 participants (Anticipated) | Interventional | 2022-04-10 | Recruiting | |||
The Antihypertensives and Vascular, Endothelial and Cognitive Function Trial (AVEC Trial) [NCT00605072] | Phase 2 | 53 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
Nifedipine Versus Magnesium Sulfate for Tocolysis in Pregnant Women at 32 - 36 Weeks Gestation With Threatened Preterm Labor [NCT05343806] | 264 participants (Anticipated) | Interventional | 2023-03-01 | Recruiting | |||
Short - Medium and Long Term Blood Pressure Variability in Essential Hypertensive Patients Treated With Nifedipine GITS or Ramipril - a Randomized Trial [NCT02499822] | Phase 4 | 168 participants (Actual) | Interventional | 2015-10-31 | Completed | ||
Use of Impedance Cardiography to Decrease the Risk of Preeclampsia [NCT03245970] | Early Phase 1 | 0 participants (Actual) | Interventional | 2017-04-24 | Withdrawn(stopped due to Investigator retired. Other investigators did not want to continue study.) | ||
"Color Doppler Ultrasound Comparison of Topical 10 % Nifedipine Versus 5% Sildenafil in Secondary Raynaud: A Randomized, Double-blind, Placebo-controlled Pilot Study" [NCT03027674] | Early Phase 1 | 10 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
The Effects of Nifedipine and Metoprolol on Blood Pressure Variability in Northern Chinese: a Randomized Crossover Study [NCT02513927] | Phase 2/Phase 3 | 40 participants (Anticipated) | Interventional | 2015-08-31 | Recruiting | ||
Amlodipine Versus Nifedipine ER for the Management of Postpartum Hypertension: A Randomized Controlled Noninferiority Trial [NCT04790279] | Phase 4 | 132 participants (Actual) | Interventional | 2021-04-09 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |