Page last updated: 2024-11-04

nicardipine

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Description

Nicardipine is a dihydropyridine calcium channel blocker used to treat hypertension and angina. It is synthesized through a multi-step process involving various organic reactions. Nicardipine acts by blocking the influx of calcium ions into smooth muscle cells, leading to vasodilation and a reduction in blood pressure. Its importance lies in its effectiveness in managing cardiovascular diseases. Research on nicardipine focuses on its mechanism of action, potential side effects, and its role in various clinical scenarios. The study of nicardipine aims to optimize its therapeutic use and explore its potential for new applications in cardiovascular medicine.'

Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID4474
CHEMBL ID1484
CHEMBL ID3302409
CHEBI ID180905
CHEBI ID7550
SCHEMBL ID34277
MeSH IDM0014820

Synonyms (156)

Synonym
BIDD:GT0621
AC-19947
CBIOL_001802
OPREA1_436998
AB00053604-03
2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CHEBI:180905
BRD-A26711594-001-02-7
BRD-A26711594-003-05-6
o5-methyl o3-[2-(methyl-(phenylmethyl)amino)ethyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
gtpl2559
(r,s)-nicardipine
DIVK1C_000540
KBIO1_000540
perpidine
methyl 2-[methyl(phenylmethyl)amino]ethyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SPECTRUM_001372
BSPBIO_002943
nicardipino [inn-spanish]
einecs 259-932-3
2-(benzylmethylamino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)pyridine-3,5-dicarboxylate
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-(benzylmethylamino)ethyl methyl ester
nicardipinum [inn-latin]
brn 0504321
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 2-(methyl(phenylmethyl)amino)ethyl ester
nicardipine [inn:ban]
BIO1_000088
BIO2_000589
BIO1_001066
BIO1_000577
BIO2_000109
BSPBIO_000565
LOPAC0_000809
BSPBIO_001389
IDI1_000540
PRESTWICK3_000383
IDI1_033859
SPECTRUM5_001320
BPBIO1_000623
AB00514658
C07264
55985-32-5
nicardipine
DB00622
NCGC00162262-03
NCGC00162262-02
KBIO2_000109
KBIO2_004420
KBIO2_006988
KBIO2_001852
KBIOGR_000744
KBIO3_000218
KBIOSS_001852
KBIOGR_000109
KBIO2_002677
KBIO2_005245
KBIO3_000217
KBIO3_002443
KBIOSS_000109
SPECTRUM2_001415
SPBIO_002486
SPBIO_001490
SPECTRUM3_001452
SPECTRUM4_000422
NINDS_000540
PRESTWICK1_000383
PRESTWICK0_000383
PRESTWICK2_000383
NCGC00162262-04
NCGC00162262-01
flusemide
HMS2089C09
HMS1989F11
NCGC00015747-06
nicardipine (stn)
chebi:7550 ,
CHEMBL1484
L000715
D08270
nicardipine (inn)
HMS1791F11
5-o-[2-[benzyl(methyl)amino]ethyl] 3-o-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
AKOS001637090
NCGC00015747-03
tox21_110211
dtxcid903363
cas-55985-32-5
dtxsid6023363 ,
CCG-204893
NCGC00015747-07
NCGC00015747-04
NCGC00015747-02
NCGC00015747-05
cz5312222s ,
nicardipino
unii-cz5312222s
nicardipinum
FT-0630688
NCGC00015747-11
S5255
2,6-dimethyl-3-methoxycarbonyl-4-(3-nitrophenyl)-5-[ 2-(n-benzyl-n-methylamino)ethoxycarbonyl]-1,4-dihydropyridine
2-(n-benzyl-n-methylamino)ethyl methyl 2,6-dimethyl-4(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CHEMBL3302409
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-methyl 5-(2-(methyl(phenylmethyl)amino)ethyl) ester
nicardipine [who-dd]
nicardipine [mi]
nicardipine [vandf]
nicardipine [inn]
(+/-)-nicardipine
2-(benzylmethylamino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
SCHEMBL34277
NCGC00015747-09
tox21_110211_1
CS-3685
3-(2-[benzyl(methyl)amino]ethyl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate #
2-(benzylmethylamino) ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 2-[methyl(phenylmethyl)amino]ethyl ester
HY-12515
AB00053604_04
AB00053604_05
3-{2-[benzyl(methyl)amino]ethyl} 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
bdbm50101815
SBI-0050786.P003
methyl 2-(benzyl-methyl-amino)ethyl2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
3-(2-(benzyl(methyl)amino)ethyl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
BCP21397
106664-28-2
Q729213
BRD-A26711594-003-06-4
SDCCGSBI-0050786.P004
HMS3886G17
NCGC00015747-18
EX-A4680
yc-93 (free base)
l-glutamicacid,n-(1-deoxy-d-fructos-1-yl)-
1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 2-[methy(phenyl-methyl)amino]ethyl ester
A924111
AS-56335
flusemidenicardipine
BN166182
EN300-708781
AC-36578
AKOS040744847
PD156023
PD033077
yc-93 free base
2-(benzyl(methyl)amino)ethyl methyl (4rs)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
nicardipineum
nicardipino (inn-spanish)
nicardipinum (inn-latin)
rac-nicardipine
racemic nicardipine
(rs)-nicardipine
nicardipina
c08ca04
(+-)-nicardipine

Research Excerpts

Overview

Nicardipine is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage. It is a potent drug to control hypertension during pregnancy with side effects including maternal headaches, nausea and tachycardia.

ExcerptReferenceRelevance
"Nicardipine is a strong coronary vasodilator but its efficacy and safety for assessing FFR is not established."( Comparison of efficacy and safety of intracoronary nicardipine and adenosine for fractional flow reserve assessment of coronary stenosis.
Angkananard, T; Jirapattrathamrong, S; Rattanajaruskul, N; Roongsangmanoon, W; Wongsoasup, A, 2022
)
1.69
"Nicardipine proved to be a safe and effective option in the management of complications such as no reflow in patients receiving therapies to restore blood flow following CAD."( Therapeutic and safety outcomes of intracoronary nicardipine in coronary artery disease patients: a systematic review.
Ahmed, J; Asghar, MS; Hussain, HU; Imran, L; Islam, MS; Javed, SO; Rehan, ST; Salim, A; Sohail, A; Yasmin, F, 2023
)
1.89
"Nicardipine is a safe and effective alternative of verapamil in preventing spasm of radial artery conduit."( Preventing spasm of the radial artery conduit during coronary artery bypass grafting: Nicardipine versus verapamil.
Haanschoten, M; Özdemir, AB; Özdemir, HI; Soliman-Hamad, MA; van Dijk, CHB; van Straten, BHM, 2019
)
1.46
"Nicardipine is an antihypertensive drug that may be used off-label by oral route to treat hypertension in children. "( Stability study of a compounded oral solution of nicardipine for the treatment of hypertension in children.
Buchbinder, N; Colnot, M; Coquard, A; Fuss, D; Gondé, H; Hervouët, C; Lamoureux, F; Pereira, T; Varin, R, 2021
)
2.32
"Nicardipine is a desirable option because of its rapid and titratable antihypertensive properties and low incidence of adverse effects."( Nicardipine for the Treatment of Neonatal Hypertension During Extracorporeal Membrane Oxygenation.
DeAvilla, KM; Liviskie, CJ; McPherson, CC; Najaf, T; Zeller, BN, 2019
)
2.68
"Nicardipine is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage. "( Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection.
Chang, PC; Hsu, HC; Huang, BR; Huang, SS; Ko, PY; Lee, CH; Lin, C; Lin, HY; Liu, YS; Lu, DY; Tsai, CF; Wu, CY; Yeh, WL, 2014
)
2.09
"Nicardipine is a potent drug to control hypertension during pregnancy with side effects including maternal headaches, nausea and tachycardia. "( The optimal treatment of severe hypertension in pregnancy: update of the role of nicardipine.
de Groot, CJ; Meuleman, T; Nooij, LS; Roelofs, R; Visser, S; Vos, P, 2014
)
2.07
"Nicardipine is a dihydropyridine calcium-channel blocker that is frequently used in the acute treatment of hypertension in the emergency department (ED). "( Bradycardia caused by intravenous nicardipine in an elderly patient with acute ischemic infarct.
Abboud, ME; Frasure, SE, 2016
)
2.16
"Nicardipine is a dihydropyridine-type calcium channel blocker (CCB) with a peculiar cerebrovascular profile developed approximately 30 years ago."( Nicardipine: a hypotensive dihydropyridine-type calcium antagonist with a peculiar cerebrovascular profile.
Amenta, F; Mignini, F; Tomassoni, D; Traini, E; Veglio, F, 2008
)
2.51
"Nicardipine is a dihydropyridine-type Ca(2+) channel blocker (CCB) with strong antihypertensive activity and with a peculiar cerebrovascular profile. "( Nicardipine use in cerebrovascular disease: a review of controlled clinical studies.
Amenta, F; Lanari, A; Mignini, F; Silvestrelli, G; Tomassoni, D; Traini, E, 2009
)
3.24
"Nicardipine is a calcium antagonist alternative to verapamil and is reportedly more effective in vitro."( Nicardipine vs. saline injection as treatment for Peyronie's disease: a prospective, randomized, single-blind trial.
Fujiwara, T; Kamoi, K; Kanemitsu, N; Kawauchi, A; Miki, T; Naitoh, Y; Naya, Y; Ochiai, A; Soh, J, 2010
)
2.52
"Nicardipine is a very effective therapy for treatment of severe hypertension in pregnancy and may be a better alternative to other available treatment options."( Nicardipine for the treatment of severe hypertension in pregnancy: a review of the literature.
Duvekot, JJ; Nij Bijvank, SW, 2010
)
2.52
"Nicardipine is a commonly used anti-hypertensive drug for acute situations. "( [Nicardipine induced hypoxia: role of hypoxic pulmonary vasoconstriction].
Bordes, J; Cotte, J; D'Aranda, E; Esnault, P; Meaudre, E, 2012
)
2.73
"Nicardipine is a dihydropyridine-type Ca(2+) channel blocker with a powerful antihypertensive activity and a unique cerebrovascular profile. "( Nicardipine in the treatment of aneurysmal subarachnoid haemorrhage: a meta-analysis of published data.
Feng, ZM; Huang, RQ; Jiang, FG; Wang, TY, 2013
)
3.28
"Nicardipine is a potent coronary and systemic vasodilator without depression of ventricular function. "( Nicardipine augments local myocardial perfusion after coronary artery reperfusion in dogs.
Jang, YH; Kim, JM, 2003
)
3.2
"Nicardipine is an effective antihypertensive agent for neonates receiving ECMO therapy. "( Nicardipine to control neonatal hypertension during extracorporeal membrane oxygen support.
Campbell, M; Frey, BM; McBride, BF; White, CM, 2003
)
3.2
"Nicardipine is an effective agent for treatment of postcoarctectomy hypertension in children with coarctation of the aorta."( Intravenous nicardipine for treatment of postcoarctectomy hypertension in children.
Morris, A; Nakagawa, TA; Sartori, SC; Schneider, DS,
)
1.23
"Nicardipine is a water soluble calcium channel antagonist, with predominantly vasodilatory actions. "( Intravenous nicardipine: its use in the short-term treatment of hypertension and various other indications.
Curran, MP; Keating, GM; Robinson, DM, 2006
)
2.16
"Nicardipine is an effective antianginal agent with an optimal dose of 90 to 120 mg/day."( Short- and long-term efficacy of nicardipine, assessed by placebo-controlled single- and double-blind crossover trials in patients with chronic stable angina.
Bala Subramanian, V; Bowles, MJ; Khurmi, NS; Raftery, EB, 1984
)
1.27
"Nicardipine is a potent vasodilator, which produced a marked reduction of systemic vascular resistance and left ventricular end-diastolic pressure during exercise."( Immediate and longer-term effects of nicardipine, at rest and during exercise, in patients with coronary artery disease.
Jaarsma, W; Kan, G; Lie, KI; Visser, CA, 1984
)
1.26
"Nicardipine is a second generation dihydropyridine-type Ca2+ antagonist with high vascular selectivity and strong cerebral and coronary vasodilatory activity. "( Nicardipine and treatment of cerebrovascular diseases with particular reference to hypertension-related disorders.
Amenta, F; Sabbatini, M; Strocchi, P, 1995
)
3.18
"Nicardipine is a relatively new calcium channel blocker with important properties that could result in attenuation of the adverse proliferative changes in autogenous vein bypass grafts. "( Preventive effect of nicardipine on hyperplastic changes in venous bypass grafts.
Gökçe, C; Gökçe, O; Günel, S; Güngen, Y; Hüseyinoğlu, K; Ozden, A; Uçar, O,
)
1.89
"Nicardipine is a second generation dihydropyridine calcium antagonist which selectively inhibits vascular smooth muscle contraction. "( Nicardipine. A review of its pharmacology and therapeutic efficacy in older patients.
Faulds, D; Frampton, JE,
)
3.02
"Nicardipine is a potent arteriolar vasodilator without a significant direct depressant effect on myocardium."( Management of hypertensive urgencies and emergencies.
Abdelwahab, W; Frishman, W; Landau, A, 1995
)
1.01
"Nicardipine appears to be an effective agent for controlled hypotension in children."( Nicardipine for controlled hypotension during spinal surgery.
Green, NE; Hersey, S; Mencio, GA; Tobias, JD,
)
2.3
"Nicardipine is an intravenously administered dihydropyridine calcium channel antagonist whose primary physiological action includes vasodilatation."( Nicardipine to control mean arterial pressure during extracorporeal membrane oxygenation.
Lynch, A; Pietsch, JB; Tobias, JD, 1996
)
2.46
"Nicardipine is a calcium channel blocker (CCB) that has been shown to be efficient in controlling postoperative hypertension."( Nicardipine as antihypertensive therapy in liver transplant recipients: results of long-term use.
Cherqui, D; Dhumeaux, D; Di Martino, V; Duvoux, C; Fagniez, PL; Lauzet, JY; Métreau, JM; Salvat, A, 1997
)
2.46
"Nicardipine is a tocolytic agent as effective as salbutamol in the treatment of premature labor. "( Nicardipine versus salbutamol in the treatment of premature labor. A prospective randomized study.
Abankwa, A; Carbonne, B; Guyard, B; Jannet, D; Marpeau, L; Milliez, J, 1997
)
3.18
"Nicardipine is a potent arteriolar vasodilator with a negligible negative inotropic effect. "( Determining the optimum dose for the intravenous administration of nicardipine in the treatment of acute heart failure--a multicenter study. The Nicardipine Heart Failure Study Group.
Hirota, Y; Hori, R; Kawai, C; Kawamura, K; Kinoshita, M; Kumada, T; Kusukawa, R; Ogawa, H; Okumura, K, 1997
)
1.98
"Nicardipine is an antihypertensive drug of the dihydropyridine series. "( Formulation of controlled release microspheres containing nicardipine: the role of pharmacokinetic modeling and computer simulation.
Bogataj, M; Grabnar, I; Karba, R; Mrhar, A,
)
1.82
"Nicardipine was found to be an effective inducer of CYP3A; in particular, CYP3A23 was increased approximately 36-fold following treatment with 100 mg of nicardipine/kg/day."( Effect of calcium channel antagonists nifedipine and nicardipine on rat cytochrome P-450 2B and 3A forms.
Anderson, A; Edwards, RJ; Kim, H; Okita, JR; Okita, RT; Springer, DL; Thomas, PE; Zangar, RC, 1999
)
1.27
"Oral nicardipine is an effective, safe, and well-tolerated tocolytic agent. "( Oral nicardipine versus intravenous magnesium sulfate for the treatment of preterm labor.
Dickerson, GA; Fischer, RG; Larmon, JE; May, WL; Morrison, JC; Ross, BS, 1999
)
1.33
"Nicardipine is a calcium antagonist which in previous trials has been shown to be effective in the prevention of stroke and the treatment of its sequelae, such as cognitive deterioration of vascular origin. "( [A study of the tolerability and effectiveness of nicardipine retard in cognitive deterioration of vascular origin].
González-González, JA; Lozano, R,
)
1.83
"Nicardipine retard is a drug which is safe and effective when used for the treatment of mental deterioration of vascular origin."( [A study of the tolerability and effectiveness of nicardipine retard in cognitive deterioration of vascular origin].
González-González, JA; Lozano, R,
)
1.83
"Nicardipine is a calcium antagonist belonging to the dihydropyridine group of molecules. "( [Intravenous nicardipine: a new calcium antagonist for perioperative use].
Barcina Sánchez, M; Muñoz Alameda, LE, 2001
)
2.12
"Nicardipine is an effective agent for controlling MAP after cardiothoracic surgical procedures in infants and children."( Nicardipine to control mean arterial pressure after cardiothoracic surgery in infants and children.
Tobias, JD,
)
2.3
"Nicardipine acts as an inhibitor of angiogenesis in vitro by inhibiting the migration of endothelial cells. "( Effects of nicardipine on tube formation of bovine vascular endothelial cells in vitro.
Fujisato, T; Ikada, Y; Kaneko, T; Kikuchi, H; Kubo, H; Miyamoto, S; Nagata, I, 1992
)
2.12
"Nicardipine hydrochloride is a newer agent that has undergone extensive evaluation in recent years."( Clinical pharmacology, pharmacokinetics, and hemodynamic effects of nicardipine.
Josephson, MA; Singh, BN, 1990
)
1.24
"Nicardipine is a light-stable, water-soluble calcium antagonist with minimal myocardial depressant effects."( Pretreatment with nicardipine preserves ventricular function after hypothermic ischemic arrest.
Brown, PS; Clark, RE; Holland, FW; Parenteau, GL, 1991
)
1.34
"Nicardipine is a second-generation dihydropyridine calcium antagonist with relative coronary and cerebrovascular selectivity. "( Effects of nicardipine on myocardial function in vitro and in vivo.
Buss, DD; Lambert, CR; Pepine, CJ, 1990
)
2.11
"Nicardipine is an investigational dihydropyridine calcium-channel blocker. "( Nicardipine in severe hypertension: oral therapy following intravenous treatment.
Bienvenu, GS; Clifton, GG; Cook, E; Laddu, A; Turlapaty, P; Wallin, JD, 1990
)
3.16
"Nicardipine is an investigational dihydropyridine calcium channel blocking agent. "( Nicardipine and hydrochlorothiazide in essential hypertension.
Brown, R; Conrad, KA; Fagan, TC; Freedman, D; Lessem, J; Michelson, E; Montijo, M; Schnaper, H; Smolens, P, 1989
)
3.16
"Nicardipine hydrochloride is a short-acting dihydropyridine calcium antagonist with a unique configuration and characteristics that make it attractive for intraoperative and postoperative use."( The role of nicardipine during anesthesia and surgery.
Kaplan, JA, 1989
)
1.38
"Nicardipine hydrochloride is an effective, well-tolerated medication for the treatment of stable exertional angina, and is a good alternative to currently available calcium antagonists."( Usefulness of nicardipine as monotherapy for chronic, stable angina.
Buhite, SG; Dennish, GW; Freedman, D; Giles, T; Glode, J; Koretz, SH; Roe, RL; Sklar, J; Wyskoarko, NP, 1989
)
1.36
"Nicardipine is a powerful arteriodilator without detectable negative inotropic effects and prolongs the time to pacing induced angina."( Effect of nicardipine on left ventricular function and on angina induced by atrial pacing in patients with coronary artery disease.
Lipkin, DP; Poole-Wilson, PA, 1985
)
1.39
"Nicardipine is a new dihydropyridine calcium channel blocking drug with actions that suggest considerable usefulness as an agent for chronic stable angina. "( Therapy for angina pectoris: comparison of nicardipine with other antianginal agents.
Scheidt, S, 1988
)
1.98
"Nicardipine is an antagonist of calcium influx through the slow channel of the cell membrane and has been shown to be an effective and relatively well-tolerated treatment for stable effort angina and rest angina due to coronary artery spasm, and mild to moderate hypertension. "( Nicardipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in the treatment of angina pectoris, hypertension and related cardiovascular disorders.
Clissold, SP; Sorkin, EM, 1987
)
3.16
"Nicardipine is a powerful systemic vasodilator with minimal effects on myocardial inotropic state, even in patients with compromised left ventricular function and patients receiving beta blocker therapy."( Hemodynamics of nicardipine in coronary artery disease.
Dunning, AJ; Koolen, JJ; van Wezel, H; Visser, CA, 1987
)
1.34
"Nicardipine appears to be an effective single drug treatment for mild to moderate hypertension."( Nicardipine in the treatment of essential hypertension controlled 6-month-study comparing nicardipine with propranolol at rest and during exercise.
Bjerle, P; Danielsson, A; Ek, B; Steen, L; Suhr, O, 1987
)
2.44
"Nicardipine appears to be a safe and effective drug for intravenous use in the treatment of severe hypertension."( Intravenous nicardipine for the treatment of severe hypertension.
Bienvenu, GS; Blanski, L; Clifton, GG; Cook, ME; Laddu, A; Langford, H; Turlapaty, P; Wallin, JD, 1988
)
2.1
"Nicardipine is a potent coronary and systemic vasodilating drug that improves exercise tolerance and myocardial metabolic response to pacing stress, the mechanism for which appears to be partially mediated through increased coronary blood flow."( Effects of nicardipine on exercise- and pacing-induced myocardial ischemia in angina pectoris.
Feldman, RL; Hill, JA; Lambert, CR; Pepine, CJ, 1987
)
1.38
"Nicardipine is a new calcium ion antagonist with vasodilating properties which has been shown to be effective in the treatment of hypertension and angina. "( Acute and chronic effects of nicardipine on systolic and diastolic left ventricular performance in patients with heart failure: a pilot study.
Caruana, MP; Kohli, RS; Lahiri, A; Raftery, EB; Robinson, CW, 1986
)
2
"Nicardipine is a new slow channel calcium blocker. "( The acute haemodynamic effects of nicardipine in patients with chronic left ventricular failure.
Evans, TR; Greenbaum, RA; Wan, S, 1986
)
1.99
"Nicardipine hydrochloride is an investigational antianginal calcium channel blocking agent with potent vasodilating properties. "( The electrophysiologic effects of nicardipine hydrochloride in man.
Klausner, SC; Moskowitz, RM; Schwartz, AB,
)
1.85
"Nicardipine is a dihydropyridine derivative with enhanced selectivity for vascular smooth muscle."( Noninvasive assessment of the haemodynamic effects of nicardipine in normotensive subjects.
Campbell, BC; Hillis, WS; Kelman, AW, 1985
)
1.24

Effects

Nicardipine hydrochloride has a mean residence time in the body of 1.27 h, of which 0.324 h were spent in the systemic circulation and the remainder in the periphery. It is as effective as nitroglycerin or nitroprusside in the control of hypertension.

Nicardipine has been used to treat cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage. It has been studied or recommended for management of hypertension in many neurovascular settings (ischemic stroke, intracerebral hemorrhage, craniotomy and spinal surgery)

ExcerptReferenceRelevance
"Nicardipine hydrochloride has a mean residence time in the body of 1.27 h, of which 0.324 h were spent in the systemic circulation and the remainder in the periphery."( Application of a system analysis approach to population pharmacokinetics and pharmacodynamics of nicardipine hydrochloride in healthy males.
Dow, RJ; Graham, DJ; Modi, NB; Veng-Pedersen, P, 1993
)
1.22
"Nicardipine has a prolonged duration of action in the presence of isoflurane and produces greater initial hypotension with sevoflurane."( Interactions between nicardipine and enflurane, isoflurane, and sevoflurane.
Conway, CM; Hanaoka, K; Matsukawa, T; Nishiyama, T, 1997
)
1.34
"Nicardipine has a short duration factor, is easily titratable and is as effective as nitroglycerin or nitroprusside in the control of hypertension."( Clinical considerations for the use of intravenous nicardipine in the treatment of postoperative hypertension.
Kaplan, JA, 1990
)
1.25
"Nicardipine also has a favorable effect on peripheral and cerebral blood flow."( Nicardipine for systemic hypertension: effects on blood pressure and target organ function.
Ram, CV, 1987
)
2.44
"Nicardipine has strong, rapidly acting antihypertensive activity. "( Intensive blood pressure lowering with nicardipine and outcomes after intracerebral hemorrhage: An individual participant data systematic review.
Fukuda-Doi, M; Hsu, CY; Ihara, M; Inoue, M; Itabashi, R; Koga, M; Martin, RH; Minematsu, K; Okada, Y; Palesch, YY; Qureshi, AI; Sakai, N; Steiner, T; Suarez, JI; Toyoda, K; Wang, Y; Yamagami, H; Yamamoto, H; Yoon, BW; Yoshimura, S, 2022
)
2.43
"Nicardipine has long been recognized as a potent cerebrovascular vasodilator with a history off-label use to prevent vasospasm and DCI."( Nicardipine Prolonged Release Implants for Prevention of Delayed Cerebral Ischemia after Aneurysmal Subarachnoid Hemorrhage: A Meta-Analysis.
Akbik, F; Jaja, BNR; Macdonald, RL; Moore, R; Sadan, O; Samuels, OB; Waddel, H, 2021
)
2.79
"Nicardipine has been used to treat cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage. "( Angiographic and hemodynamic effect of high concentration of intra-arterial nicardipine in cerebral vasospasm.
Andreone, V; Delgado-Mederos, R; Gounis, M; Hendricks, L; Linfante, I; Wakhloo, AK, 2008
)
2.02
"Nicardipine has been studied or recommended for management of hypertension in many neurovascular settings (ischemic stroke, intracerebral hemorrhage, craniotomy, and spinal surgery), for vasospasm in aneurysmal subarachnoid hemorrhage, and in acute traumatic brain injury."( Use of injectable nicardipine for neurovascular indications.
Reddy, P; Yeh, YC, 2009
)
1.41
"Nicardipine has been used extensively in different clinical settings including neurosurgery, cardiothoracic surgery, transplant medicine, and internal medicine patients."( Acute antihypertensive therapy in pregnancy-induced hypertension: is nicardipine the answer?
Hankins, GD; Pacheco, LD; Vadhera, RB, 2009
)
1.31
"Nicardipine hydrochloride has been used widely for the treatment of angina pectoris and hypertension. "( The effect of component of microemulsion for transdermal delivery of nicardipine hydrochloride.
Chang, JS; Huang, YB; Lin, YH; Tsai, YH; Wu, PC, 2010
)
2.04
"Nicardipine has previously been used to treat vasospasm through superselective intracranial microcatheter injections."( A simplified method for administration of intra-arterial nicardipine for vasospasm with cervical catheter infusion.
Do, HM; Dodd, R; Marks, MP; Pandey, P; Steinberg, GK, 2012
)
1.35
"Nicardipine hydrochloride has a mean residence time in the body of 1.27 h, of which 0.324 h were spent in the systemic circulation and the remainder in the periphery."( Application of a system analysis approach to population pharmacokinetics and pharmacodynamics of nicardipine hydrochloride in healthy males.
Dow, RJ; Graham, DJ; Modi, NB; Veng-Pedersen, P, 1993
)
1.22
"Nicardipine monotherapy has also demonstrated efficacy in angina pectoris and shown promise in the management of ischaemia-related cerebrovascular diseases, notably subarachnoid haemorrhage."( Nicardipine. A review of its pharmacology and therapeutic efficacy in older patients.
Faulds, D; Frampton, JE,
)
2.3
"Nicardipine has been shown to have an anti-atherogenic effect in rabbits given a 2% cholesterol diet. "( Effects of nicardipine on lipid peroxidation in rabbits given 2% cholesterol diet.
Hashim, S; Ismail, NM; Jaarin, K; Vasudevan, SK, 1995
)
2.12
"Nicardipine has been used to control blood pressure intraoperatively in response to tracheal intubation and in the postoperative period."( Nicardipine: applications in anesthesia practice.
Tobias, JD, 1995
)
2.46
"Nicardipine has no clinically significant negative inotropic effect."( Concomitant diseases in elderly hypertensives: the position of nicardipine.
Zannad, F, 1996
)
1.25
"Nicardipine has a prolonged duration of action in the presence of isoflurane and produces greater initial hypotension with sevoflurane."( Interactions between nicardipine and enflurane, isoflurane, and sevoflurane.
Conway, CM; Hanaoka, K; Matsukawa, T; Nishiyama, T, 1997
)
1.34
"nicardipine has urged us to prove this drug in the treatment of hypertensive attacks (SAP greater than or equal to 210 mmHg and/or DAP greater than or equal to 110 mmHg)."( [Effects of i.v. nicardipine in the treatment of hypertensive crisis].
Bolognesi, R; Conti, M; Manca, C; Straneo, U; Tsialtas, D, 1990
)
1.34
"Nicardipine has a short duration factor, is easily titratable and is as effective as nitroglycerin or nitroprusside in the control of hypertension."( Clinical considerations for the use of intravenous nicardipine in the treatment of postoperative hypertension.
Kaplan, JA, 1990
)
1.25
"Nicardipine has high affinity for the dihydropyridine-binding site and has been shown to inhibit the influx of extracellular calcium through membrane slow channels. "( Animal pharmacology of nicardipine and its clinical relevance.
Whiting, RL, 1987
)
2.03
"Nicardipine has highly specific modes of action, producing coronary and systemic vasodilation, a reduction in coronary spasm, and cardioprotection not consistently seen with other calcium antagonists."( The role of nicardipine during anesthesia and surgery.
Kaplan, JA, 1989
)
1.38
"Nicardipine has been shown to be effective in the treatment of mild to moderate hypertension both as monotherapy and in combination with other antihypertensive agents."( Intravenous nicardipine: cardiovascular effects and clinical relevance.
Pepine, CJ, 1988
)
1.38
"Nicardipine treatment has been evaluated in patients with chronic stable effort angina or with angina at rest due to coronary spasm. "( Usefulness of nicardipine for angina pectoris.
Lambert, CR; Pepine, CJ, 1987
)
2.08
"Nicardipine has been shown to lower blood pressure in patients with uncomplicated hypertension as well as in patients with concomitant renal impairment, coronary artery disease or congestive heart failure. "( Nicardipine for systemic hypertension: effects on blood pressure and target organ function.
Ram, CV, 1987
)
3.16

Actions

Nicardipine can inhibit autophagy by activating expression of mTOR, thus play tumor inhibition roles. It does not cause any chronic activation of the sympathetic nervous system or the renin-angiotensin system.

ExcerptReferenceRelevance
"Nicardipine can inhibit autophagy by activating expression of mTOR, thus play tumor inhibition roles both"( Nicardipine sensitizes temozolomide by inhibiting autophagy and promoting cell apoptosis in glioma stem cells.
Dong, J; Dong, X; Jiang, Q; Li, H; Liu, L; Shi, J; Wang, H; Wang, L, 2021
)
2.79
"Nicardipine did not cause an increase in ICP."( Combined effects of nicardipine and hypocapnic alkalosis on cerebral vasomotor activity and intracranial pressure in man.
Combes, P; Durand, M, 1991
)
1.33
"Nicardipine did not produce any significant alteration in plasma renin activity and plasma aldosterone after acute or chronic administration."( Acute and chronic effects of a new calcium inhibitor, nicardipine, on renal hemodynamics in hypertension.
Bellet, M; Chaignon, M; Guedon, J; Lucsko, M; Rapoud, C,
)
1.1
"Nicardipine does not cause any chronic activation of the sympathetic nervous system or the renin-angiotensin system."( Nicardipine in the elderly hypertensive: a review of experience in the United Kingdom.
Littler, WA, 1989
)
2.44
"Nicardipine was found to produce a concentration-dependent depression of the isometric contraction of the isolated, spontaneously beating atria of the guinea-pig. "( [Effects of nicardipine on the spontaneous beat of isolated atria of guinea pigs].
Prostran, M; Varagic, VM, 1987
)
2.09
"Nicardipine did not inhibit the aldosterone response to angiotensin."( Effects of nicardipine on aldosterone release and pressor mechanisms.
Elliott, HL; Pasanisi, F; Reid, JL, 1985
)
1.38
"Nicardipine may increase CSFP to undesirable levels in patients with intracranial hypertension."( The effects of nicardipine on cerebrospinal fluid pressure in humans.
Namiki, A; Nishikawa, T; Omote, K; Takahashi, T, 1986
)
1.35
"Nicardipine appears to blunt the secretion of aldosterone responding to an increased PRA possibly through its calcium-antagonizing action."( Multiple oral doses of nicardipine, a calcium-entry blocker: effects on renal function, plasma renin activity, and aldosterone concentration in mild-to-moderate essential hypertension.
Aoyagi, K; Baba, T; Ishizaki, T; Murabayashi, S; Takebe, K; Tamasawa, N, 1987
)
1.3
"Nicardipine did not produce any ECG changes at rest or during exercise."( Nicardipine in the treatment of essential hypertension controlled 6-month-study comparing nicardipine with propranolol at rest and during exercise.
Bjerle, P; Danielsson, A; Ek, B; Steen, L; Suhr, O, 1987
)
2.44
"Nicardipine inhibited the increase in blood pressure with cholesterol and normal diets."( [Effect of nicardipine on cholesterol-fed S.H.R].
Kawashima, I; Nakayama, S; Ohba, T; Sakamoto, K; Tonooka, M; Yasuhara, H, 1985
)
1.38

Treatment

Treatment with nicardipine (3 micrograms kg-1 i.v.) or trichlormethiazide did not affect relaxant effect of tamsulosin on prostatic pressure in UPP, or potentiate its hypotensive effect. Treatment with nicardedipine increased the number of neurones in the frontal cortex and in the occipital cortex of SHR.

ExcerptReferenceRelevance
"Nicardipine treatment (10 mg/kg/d) was applied to block L-type VGCCs for 10 d."( Blocking of L-type calcium channels protects hippocampal and nigral neurons against iron neurotoxicity. The role of L-type calcium channels in iron-induced neurotoxicity.
Bagirici, F; Bostanci, MÖ, 2013
)
1.11
"Nicardipine treatment resulted in the reduction of MAP (12.3 mmHg, standard error [SE] 1.34, P-value <0.0001) without any significant change in ICP."( Super-selective intra-arterial magnesium sulfate in combination with nicardipine for the treatment of cerebral vasospasm in patients with subarachnoid hemorrhage.
Georgiadis, AL; Kozak, OS; Memon, MZ; Qureshi, AI; Rodriguez, GJ; Shah, QA; Suri, MF; Taylor, RA; Tummala, RP; Vazquez, G, 2009
)
1.31
"In nicardipine pretreated condition, the concentration-response curves for the negative inotropic effect of potassium channel blockers were shifted to the right by the increasing concentration of carbachol from 0.5 microM to 5 microM."( Inhibitory effects of potassium channel blockers on carbachol-induced contraction in rat detrusor muscle.
Ahn, SC; Oh, SJ, 2003
)
0.83
"Nicardipine treatment was continued for as long as the maternal and foetal conditions allowed."( Intravenous use of the calcium-channel blocker nicardipine as second-line treatment in severe, early-onset pre-eclamptic patients.
Bartels, PA; Bijvank, BN; Hanff, LM; Roofthooft, DW; Steegers, EA; Visser, W; Vulto, AG, 2005
)
1.31
"Nicardipine treatment significantly modified the general haemodynamic responses to LAD ligation particularly in maintaining a low LV systolic pressure and inhibiting elevation of LV end diastolic pressure.(ABSTRACT TRUNCATED AT 250 WORDS)"( The beneficial effect of nicardipine on the healing of myocardial infarcts in dogs.
Alps, BJ; Calder, C; Scott-Park, FM; Wilson, A, 1983
)
1.29
"Nicardipine treatment significantly decreased systolic and diastolic blood pressure and increased plasma noradrenaline levels measured at supine rest."( [Nicardipine attenuates the sympathetic reflex of orthostatism: do dihydropyridine-sensitive calcium channels regulate noradrenaline release?].
Cherchi, A; Lai, L; Longu, G; Manca, MR; Mercuro, G; Rossetti, ZL; Ruscazio, M, 1992
)
1.92
"Nicardipine treatment normalized PDH activity quickly and improved energy metabolism after reperfusion."( Effect of nicardipine, a Ca2+ channel blocker, on pyruvate dehydrogenase activity and energy metabolites during cerebral ischemia and reperfusion in gerbil brain.
Fukuchi, T; Katayama, Y; McKee, A; Terashi, A, 1998
)
1.42
"Nicardipine treatment produced a 16% reduction in systolic blood pressure, a 23% reduction in diastolic blood pressure, and a 7% increase in heart rate."( Intravenous nicardipine for treatment of severe hypertension in children.
Brophy, PD; Bunchman, TE; Flynn, JT; Kershaw, DB; Mottes, TA; Smoyer, WE, 2001
)
1.41
"nicardipine-treated patients (i.v."( Postoperative hypertension: a multicenter, prospective, randomized comparison between intravenous nicardipine and sodium nitroprusside.
Floyd, J; Gabrielson, G; Goldberg, JS; Goldberg, M; Greenstein, RJ; Halpern, NA; Neely, C; Sladen, RN, 1992
)
1.22
"Nicardipine treatment significantly reduced blood pressures both in the supine and standing positions (p < 0.0004) when compared with placebo treatment."( Dose requirement and effect of nicardipine on lipid profile in mild to moderate essential hypertensives.
Christina, P; Kamsiah, J; Maheendran, K; Tariq, AR, 1992
)
1.29
"Nicardipine pretreatment attenuated the increase in LDH level, perfusion pressure and intrahepatic volumes after reoxygenation, but there were no difference in liver microcirculation during 120-min hypoxia."( Influence of nicardipine on post-hypoxic injury in the isolated perfused rat liver.
Fujita, Y; Kimura, K; Takaori, M, 1991
)
1.37
"Nicardipine treatment allowed blood pressure control, reduction of left ventricular mass, and improvement in mechanical performance, but was unable to restore minimal coronary vascular resistance. "( Nicardipine and cardiac hypertrophy: effects on left ventricular mass. Haemodynamics and mechanical performance in renovascular hypertensive rats.
Besse, P; Bonoron-Adèle, S; Grellet, J; Stuyvers, B; Tariosse, L, 1991
)
3.17
"Nicardipine treatment was well tolerated and no significant changes of heart rate, creatinine clearance and urinary excretion of Na, K, Ca and aldosterone were observed after 12 weeks' treatment."( [Effects of slow-release nicardipine on blood pressure, renal function and the renin-angiotensin-aldosterone system in patients with mild-to-moderate essential arterial hypertension].
Colivicchi, F; Guerrera, C; Guerrera, G; Melina, D; Melina, G; Musumeci, V; Santoliquido, A,
)
1.16
"Nicardipine-treated and control groups had similar jeopardy area values (41.2 +/- 1.6% versus 47.4 +/- 3.1% of the left ventricle), but infarct area was significantly reduced in the nicardipine-treated group (3.2 +/- 1.1% versus 24.9 +/- 7.5% of jeopardy area, p less than 0.01)."( Effects of nicardipine, a calcium antagonist, on myocardial salvage and high energy phosphate stores in reperfused myocardial injury.
Derugin, N; Higgins, CB; Holt, WW; Saeed, M; Wendland, MF; Wolfe, C, 1990
)
1.39
"Nicardipine-treated animals had significantly less calcium-calmodulin binding in CA1 and in the dentate after 2 hours of reperfusion."( Calcium-calmodulin binding in ischemic rat neurons after calcium channel blocker therapy.
Dedman, JR; Earls, R; Grotta, JC; Picone, CM; Strong, R; Yao, L, 1990
)
1
"Nicardipine-treated patients had a lower incidence of each of the symptoms than did the nifedipine-treated patients."( Randomized double-blind comparison of side effects of nicardipine and nifedipine in angina pectoris. The Nicardipine Investigators Group.
DeWood, MA; Wolbach, RA, 1990
)
1.25
"Nicardipine-treated patients required more intravenous fluids during the operative procedure (2.4 +/- 0.3 L vs 1.5 +/- 0.4 L, P less than 0.05) and were less likely to require isoflurane supplementation to morphine sulphate/nitrous oxide anaesthesia (P less than 0.01)."( Nicardipine HCl: clinical experience in patients undergoing anaesthesia for intracranial aneurysm clipping.
Adams, HP; Godersky, JC; Maktabi, M; Sokoll, MD; Warner, DS, 1989
)
2.44
"Nicardipine-based treatment is therefore effective, safe, and well tolerated in elderly hypertensive patients with concomitant disease."( The clinical performance of nicardipine in elderly hypertensive patients with concomitant diseases.
Leonetti, G, 1989
)
1.29
"Nicardipine treatment (10 to 15 mg intraperitoneal dosage during 8 weeks), led to: an efficient but incomplete control of hypertension."( [Effects of nicardipine on left ventricular hypertrophy of the rat with renovascular arterial hypertension].
Besse, P; Bonoron-Adèle, S; Grellet, J; Stuyvers, B; Tariosse, L, 1988
)
1.38
"Nicardipine-based treatment reduced systolic and diastolic blood pressures to similar levels independently of the age of the patients."( Antihypertensive efficacy of nicardipine-based treatment in patients of different age and in patients with isolated systolic hypertension.
Leonetti, G; Zanchetti, A, 1988
)
1.29
"Nicardipine treatment has been evaluated in patients with chronic stable effort angina or with angina at rest due to coronary spasm. "( Usefulness of nicardipine for angina pectoris.
Lambert, CR; Pepine, CJ, 1987
)
2.08
"Nicardipine treatment significantly reduced Ca2+ accumulation in the middle cerebral artery territory by 60% compared with six untreated rats 6 hours after arterial occlusion."( Nicardipine reduces calcium accumulation and electrolyte derangements in regional cerebral ischemia in rats.
Flamm, ES; Hadani, M; Young, W, 1988
)
2.44
"Nicardipine-treated patients commenced therapy with a significantly higher mean supine diastolic blood pressure than the nifedipine-treated patients."( Comparison of the efficacy of nicardipine, a new calcium channel blocker, with nifedipine in the treatment of mild to moderate essential hypertension.
Armstrong, C; Blackwood, R; Garnham, J, 1987
)
1.28
"Nicardipine treatment initiated either before or after ischemia failed to improve neurologic outcome at 48 h postischemia."( Nicardipine increases cerebral blood flow but does not improve neurologic recovery in a canine model of complete cerebral ischemia.
Ishikawa, T; Masuda, T; Matsumoto, M; Nagai, I; Sakabe, T; Takeshita, H; Tateishi, A, 1986
)
2.44
"Nicardipine HCl treatment was associated with a rise in pulse rate and concomitant fall in mean arterial pressure."( Cardiovascular and uterine blood flow changes during nicardipine HCl tocolysis in the rabbit.
Holbrook, RH; Katz, M; Lirette, M, 1987
)
1.24
"Treatment with nicardipine inhibited microglial cell migration."( Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection.
Chang, PC; Hsu, HC; Huang, BR; Huang, SS; Ko, PY; Lee, CH; Lin, C; Lin, HY; Liu, YS; Lu, DY; Tsai, CF; Wu, CY; Yeh, WL, 2014
)
0.98
"Pretreatment with nicardipine for RSI improved intubation conditions and shortened the onset time of rocuronium and attenuated changes in MAP after intubation. "( The effects of nicardipine or esmolol on the onset time of rocuronium and intubation conditions during rapid sequence induction: a randomized double-blind trial.
Kim, Y; Lee, C; Lee, JH; Lee, JY; Lee, KH; Rim, SK, 2015
)
1.1
"Treatment with nicardipine, nitroprusside, and verapamil are equally effective in improving flow."( No-reflow phenomenon following percutaneous coronary intervention for acute myocardial infarction: incidence, outcome, and effect of pharmacologic therapy.
Abdalrahman, IB; Dharmashankar, KC; Kloner, RA; Rezkalla, SH, 2010
)
0.7
"Treatment with nicardipine and to a lesser extent with hydralazine countered ophthalmoscopic changes noticeable in SHR."( Quantitative image analysis of choroid and retinal vasculature in SHR: a model of cerebrovascular hypertensive changes?
Amenta, F; Mancinelli, G; Mignini, F; Sabbatini, M; Tomassoni, D,
)
0.47
"Pretreatment with nicardipine (1 microM) and Ca2+ -free conditions inhibited the NC-1900-induced [Ca2+](i) response in the VH."( Ameliorative effect of NC-1900, a new AVP4-9 analog, through vasopressin V1A receptor on scopolamine-induced impairments of spatial memory in the eight-arm radial maze.
Abe, K; Egashira, N; Fujiwara, M; Inada, K; Iwasaki, K; Matsumoto, Y; Mishima, K; Miura, I; Tsukikawa, H, 2003
)
0.64
"Treatment with nicardipine countered microanatomical changes occurring in SHR, whereas hydralazine displayed a less pronounced effect."( Treatment with nicardipine protects brain in an animal model of hypertension-induced damage.
Amenta, F; Tomassoni, D, 2004
)
1.02
"Treatment with nicardipine significantly reduced blood pressure and albuminuria and increased urinary sodium excretion."( Protective effect of nicardipine treatment on renal microanatomical changes in spontaneously hypertensive rats.
Abbate, F; Amenta, F; Ciriaco, E; Ferrante, F; Polidori, C, 1994
)
0.95
"Pretreatment with nicardipine, a Ca(2+)-channel blocker (1 mg/kg iv), significantly attenuated the ET-1-induced mucosal damage as well as the decrease in mucosal blood flow."( Gastric ulcer induced by submucosal injection of ET-1: role of potent vasoconstriction and intraluminal acid.
Fukutomi, H; Goto, K; Kashimura, H; Lazaratos, S; Miyauchi, T; Nakahara, A; Osuga, T; Urushidani, T, 1993
)
0.61
"Pretreatment with nicardipine prevented the inhibitory effect of exogenous calcium on the testicular CR activity in 3-week-old rats, indicating that the suppressing action of calcium on the enzyme activity was mediated by the entry of extracellular calcium via calcium channels."( Effects of age and calcium ion on testis carbonyl reductase in rats.
Fujii, T; Inazu, N, 1993
)
0.61
"Treatment with nicardipine (3 micrograms kg-1 i.v.), captopril (100 micrograms kg-1 i.v.) or trichlormethiazide (100 micrograms kg-1 i.v.) did not affect relaxant effect of tamsulosin on prostatic pressure in UPP, or potentiate its hypotensive effect."( Effect of tamsulosin, a novel alpha 1-adrenoceptor antagonist, on urethral pressure profile in anaesthetized dogs.
Asano, M; Inagaki, O; Sudoh, K; Takenaka, T; Tanaka, H, 1996
)
0.63
"Treatment with nicardipine significantly reduced systolic pressure in the SHR."( Vascular and neuronal hypertensive brain damage: protective effect of treatment with nicardipine.
Amenta, F; Sabbatini, M; Strocchi, P, 1996
)
0.86
"Treatment with nicardipine increased the number of neurones in the frontal cortex and in the occipital cortex of SHR and countered hyperplasia and hypertrophy of GFAP-immunoreactive astrocytes."( Vascular and neuronal hypertensive brain damage: protective effect of treatment with nicardipine.
Amenta, F; Sabbatini, M; Strocchi, P, 1996
)
0.86
"Pretreatment with nicardipine (2.5 mg/kg) only partially antagonised the training dose of (+/-)-Bay K 8644 whereas nimodipine (0.6-10 mg/kg) did not affect the (+/-)-Bay K 8644 discriminative stimulus."( 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
"The treatment with nicardipine at any period of time did not reduce infarct size."( [Comparison of effects of verapamil and those of nicardipine on myocardial ischemia and reperfusion injury: a study in an in situ rabbit model].
Furuya, M; Yoshida, K, 1999
)
0.88
"Treatment with nicardipine (20 mg/kg/day, s.c.) prevented enhanced nitric oxide degradation without affecting superoxide dismutase and catalase activities."( Antioxidant enzyme activities and total nitrite/nitrate levels in the collar model. Effect of nicardipine.
Kerry, Z; Onat, T; Sözmen, EY; Ustünes, L; Uysal, F; Yasa, M; Yetik, G, 2000
)
0.87
"Treatment with nicardipine significantly reduced SBP, the thickness of tunica media, media-to-lumen ratio and increased luminal area of medium- and small-sized pial arteries and of intracerebral arteries."( Protective effect of treatment with nicardipine on cerebrovascular tree of spontaneously hypertensive rats.
Amenta, F; Bellagamba, G; Casado, A; Sabbatini, M; Tayebati, SK; Venarucci, D,
)
0.75
"Pretreatment with nicardipine significantly improved postischemic myocardial performance under hypothermic conditions and should be administered or at least not discontinued before cardiac operations."( Pretreatment with nicardipine preserves ventricular function after hypothermic ischemic arrest.
Brown, PS; Clark, RE; Holland, FW; Parenteau, GL, 1991
)
0.94
"Pretreatment with nicardipine (10(-6)M), a calcium channel blocker, significantly suppressed these effects of endothelin."( Endothelin activates the vascular renin-angiotensin system in rat mesenteric arteries.
Higashimori, K; Mikami, H; Nagano, M; Nakamaru, M; Ogihara, T; Rakugi, H; Tabuchi, Y, 1990
)
0.6

Toxicity

Nicardipine proved to be a safe and effective option in the management of complications such as no reflow in patients receiving therapies to restore blood flow following CAD. Adverse experiences reported with IV nicardipines included hypotension (4.IC bolus injection)

ExcerptReferenceRelevance
" Adverse experiences reported with IV nicardipine included hypotension (4."( Efficacy and safety of intravenous nicardipine in the control of postoperative hypertension. IV Nicardipine Study Group.
, 1991
)
0.83
" Most adverse reactions were transient and were related to vasodilation, and included peripheral edema in 7% of the patients, flushing in 7%, and headache in 4%."( Efficacy and safety of nicardipine in 29,104 patients with hypertension.
Blanchard, D; Dubois, C,
)
0.44
" No deaths or serious adverse reactions were attributed to nicardipine during clinical trials."( An overview of the safety and efficacy of nicardipine in clinical trials.
Agre, K, 1987
)
0.78
" A clear species difference in LD50 values was found in acute toxicity of PP-1466, and rabbits were the most sensitive between animal species used, then dogs, mice and rats in order."( Acute and subacute toxicity of 2,6-dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1 ,4-dihydropyridine (PP-1466).
Aikawa, K; Fujikura, M; Gomi, T; Hirao, A; Kobayashi, M; Okumura, M; Ozeki, M; Tateishi, T; Yamamoto, H; Yumoto, S, 1985
)
0.27
" The drug was well tolerated, and no significant adverse events occurred."( Evaluation of the efficacy and safety of oral nicardipine in treatment of urgent hypertension: a multicenter, randomized, double-blind, parallel, placebo-controlled clinical trial.
Dunbar, LM; Friday, KJ; Habib, GB; Neale, AC; Rodrigues, R, 1995
)
0.55
" These results indicate that nicardipine is at least as safe and effective as nifedipine in the treatment of unstable angina."( [The efficacy and safety of slow-release nicardipine vs nifedipine in angina].
Maddalena, F; Rocco, CG; Villanova, C, 1994
)
0.85
" Nicardipine appeared to be safe and effective in controlling hypertension in these patients."( Nicardipine is a safe and effective agent in pediatric hypertensive emergencies.
Sakarcan, A; Tenney, F, 2000
)
2.66
" These results suggested that nicardipine-prolonged release preparation is safe as well as effective for cerebral vasospasm."( [The efficacy and safety of the nicardipine prolonged-release implant in a canine double hemorrhage model].
Aihara, Y; Hori, T; Izawa, M; Kasuya, H; Kawashima, A; Sasahara, A, 2000
)
0.88
" However, the total incidence of adverse reactions, including non-CV events and unfavorable BP changes, was 31 cases (15."( Tolerability and safety of a calcium channel blocker in comparison with a diuretic in the treatment of elderly patients with hypertension: secondary analysis of the NICS-EH.
Abe, K; Fujishima, M; Fukiyama, K; Hiwada, K; Iimura, O; Ishii, M; Kuramoto, K; Kuwajima, I; Ogihara, T; Saruta, T, 2001
)
0.31
" Blood pressures after discontinuation of the infusion were not significantly different from those measured on the third day of infusion and no definite adverse effects attributable to the treatment were observed."( Nicardipine hydrochloride injectable phase IV open-label clinical trial: study on the anti-hypertensive effect and safety of nicardipine for acute aortic dissection.
Ahn, H; Kim, KH; Koh, YB; Moon, IS; Park, JS,
)
1.57
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"In this small series, high-dose intra-arterial nicardipine infusion to treat SAH-associated vasospasm seems to be safe and effective."( Safety and feasibility of intra-arterial nicardipine for the treatment of subarachnoid hemorrhage-associated vasospasm: initial clinical experience with high-dose infusions.
Chaloupka, JC; Hayakawa, M; Lee, SK; Taylor, RA; Tejada, JG; Ugurel, MS, 2007
)
0.86
"When used for control of hypertension in patients with subarachnoid or intracerebral hemorrhage, NC and SNP were both safe and effective, but patients on an NC drip required fewer dose adjustments and fewer additional medications."( Prospective randomized comparison of safety and efficacy of nicardipine and nitroprusside drip for control of hypertension in the neurosurgical intensive care unit.
Alaraj, A; Hardman, J; Mangubat, EZ; Merchant, A; Mlinarevich, N; Roitberg, BZ; Ruland, S; Urbaniak, K; Watson, KS, 2008
)
0.59
" Adverse effects linked to tocolysis were recorded."( Nicardipine versus salbutamol in the treatment of premature labor: comparison of their efficacy and side effects.
Abdennadheur, W; Amouri, H; Ben Amar, H; Gargouri, A; Guermazi, M; Hadj Taib, H; Kallel, W; Trabelsi, K; Zribi, A, 2008
)
1.79
" Aside from patients presenting with ischemic or traumatic brain injury, labetalol was safe to use in this population for hypertensive emergencies and had a satisfactory adverse effect profile."( Safety and efficacy of intravenous labetalol for hypertensive crisis in infants and small children.
Feig, DI; Moffett, BS; Mott, AR; Thomas, CA; Wagner, JL, 2011
)
0.37
" Six of eight (75%) CYP3A5*3/*3 cases had potentially toxic MaxC0 (>20 ng/mL) compared with none of four CYP3A5*1/*1 cases and 3 of 26 (11."( Risk of tacrolimus toxicity in CYP3A5 nonexpressors treated with intravenous nicardipine after kidney transplantation.
Fukuda, T; Gardiner, R; Goebel, J; Hooper, DK; Kirby, CL; Logan, B; Roy-Chaudhury, A; Vinks, AA, 2012
)
0.61
"Both agents appear equally effective and safe for blood pressure control in SAH and ICH during the initial admission hours."( Effectiveness and safety of nicardipine and labetalol infusion for blood pressure management in patients with intracerebral and subarachnoid hemorrhage.
Agarwal, S; Badjatia, N; Carpenter, AM; Claassen, J; Lantigua, H; Lee, K; Lesch, C; Li, M; Mayer, SA; Ortega-Gutierrez, S; Reccius, A; Schmidt, JM; Thomas, J, 2013
)
0.68
" Demographic, operative, laboratory, and postoperative data were collected for adverse effect analysis and outcomes comparisons between infants aged younger than 6 months (group 1) and older than 6 months (group 2)."( Use of Nicardipine After Cardiac Operations Is Safe in Children Regardless of Age.
Buck, M; Gangemi, J; Kelly, J; Mistry, M; Stone, ML; Vergales, J, 2018
)
0.94
" Thus, nicardipine should be considered as safe and effective in children of all ages for control of hypertension after cardiac operations."( Use of Nicardipine After Cardiac Operations Is Safe in Children Regardless of Age.
Buck, M; Gangemi, J; Kelly, J; Mistry, M; Stone, ML; Vergales, J, 2018
)
1.39
"IC bolus injection of nicardipine could be introduced as a safe and practical alternative method of inducing hyperemia during FFR measurements."( Comparison of efficacy and safety of intracoronary nicardipine and adenosine for fractional flow reserve assessment of coronary stenosis.
Angkananard, T; Jirapattrathamrong, S; Rattanajaruskul, N; Roongsangmanoon, W; Wongsoasup, A, 2022
)
1.29
" Nicardipine proved to be a safe and effective option in the management of complications such as no reflow in patients receiving therapies to restore blood flow following CAD."( Therapeutic and safety outcomes of intracoronary nicardipine in coronary artery disease patients: a systematic review.
Ahmed, J; Asghar, MS; Hussain, HU; Imran, L; Islam, MS; Javed, SO; Rehan, ST; Salim, A; Sohail, A; Yasmin, F, 2023
)
2.07

Pharmacokinetics

The myocardial pharmacodynamic effects of the two dihydropyridine calcium-antagonists nicardipine and nitrendipine were comparatively studied in the isolated, spontaneously beating and retrogradely perfused rabbit heart at stepwise increased drug concentrations.

ExcerptReferenceRelevance
" We evaluated the pharmacodynamic effect of the calcium channel blocker nicardipine on left ventricular function assessed by radionuclide ventriculography in 20 patients with systemic sclerosis."( Pharmacodynamic effect of nicardipine on left ventricular function in systemic sclerosis.
Amor, B; Devaux, JY; Guérin, F; Kahan, A; Menkès, CJ; Strauch, G; Venot, A; Weber, S, 1990
)
0.81
" In comparison to the patients with normal renal function, there were significant increases in AUC and Cmax in the patients with renal impairment."( Inhibitory effect of uraemia on the hepatic clearance and metabolism of nicardipine.
Ahmed, JH; Elliott, HL; Grant, AC; Murray, GR; Rodger, RS, 1991
)
0.51
"The present study was designed to compare the pharmacokinetic handling of a single oral dose of nicardipine in normal subjects and in patients with hepatic cirrhosis and to compare the sensitivity of the two groups to its hypotensive effect."( The effect of hepatic cirrhosis on the pharmacokinetics and blood pressure response to nicardipine.
Conway, EL; Drummer, OH; Louis, WJ; McNeil, JJ; Razak, TA; Sewell, RB; Smallwood, RA, 1990
)
0.72
" Co-administration of nicardipine significantly increased the AUC and the mean Cmax of propranolol."( Influence of nicardipine on the pharmacokinetics and pharmacodynamics of propranolol in healthy volunteers.
Dupont, AG; Massart, DL; Musch, G; Schoors, DF; Vercruysse, I, 1990
)
0.96
" The dual purpose of the present study was to evaluate the influence of orally administered nicardipine on plasma digoxin concentrations over 24 hours and to measure possible variations in the pharmacodynamic effects of digoxin in 9 patients with chronic congestive heart failure."( [Pharmacokinetics and pharmacodynamic effects of digoxin in dilated cardiomyopathies. Influence of nicardipine].
Commeau, P; Debruyne, D; Dorey, H; Gérard, JL; Grollier, G; Huret, B; Lamy, E; Moore, N; Potier, JC; Scanu, P, 1987
)
0.71
" 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
"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
)
0.72
" 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
)
0.48
" 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
)
1.94
" 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
)
1.47
" Coadministration of nicardipine significantly increased the AUC and Cmax and significantly decreased the Cl(o) and Cl'intr for unbound drug of (R)- and (S)-propranolol."( Enantioselective inhibitory effect of nicardipine on the hepatic clearance of propranolol in man.
Belpaire, F; Dupont, AG; Massart, DL; Vercruysse, I; Wynant, P, 1994
)
0.88
" After 30 mg kg-1 oral dose, maximum plasma concentration, tmax and AUC of YM-21095 were 28."( Pharmacokinetics and cardiovascular effects of YM-21095, a novel renin inhibitor, in dogs and monkeys.
Asano, M; Inagaki, O; Shibasaki, M; Takenaka, T; Usui, T, 1994
)
0.29
" The determined pharmacokinetic model was linked to a pharmacodynamic model that allowed the change in the mean arterial blood pressure and heart rate to be described and predicted."( Application of a system analysis approach to population pharmacokinetics and pharmacodynamics of nicardipine hydrochloride in healthy males.
Dow, RJ; Graham, DJ; Modi, NB; Veng-Pedersen, P, 1993
)
0.5
"The present study was conducted to compare pharmacokinetic behaviors of nicardipine enantiomers given in different doses with different formulations of racemic nicardipine in healthy volunteers."( Pharmacokinetics of nicardipine enantiomers in healthy young volunteers.
Higuchi, S; Honda, M; Inotsume, N; Iwaoka, T; Nakano, M; Naomi, S; Okamoto, Y; Teramura, T; Tomita, K, 1997
)
0.85
"One or two 20-mg racemic nicardipine tablets, and a 40-mg sustained-release capsule of nicardipine were administered to eight healthy volunteers in a crossover fashion and pharmacokinetic parameters were evaluated."( Pharmacokinetics of nicardipine enantiomers in healthy young volunteers.
Higuchi, S; Honda, M; Inotsume, N; Iwaoka, T; Nakano, M; Naomi, S; Okamoto, Y; Teramura, T; Tomita, K, 1997
)
0.92
" The results inferred that nicardipine is absorbed rapidly and has a relatively short half-life in healthy individuals."( A high-performance liquid chromatographic method for the determination of nicardipine in plasma and its application to pharmacokinetics in humans.
Li, K; Yuan, YS; Zhang, X; Zhao, FL,
)
0.66
" The time course for nicardipine bolus was consistent with a two-compartment pharmacokinetic model with rapid redistribution from a small central compartment."( Nicardipine intravenous bolus dosing for acutely decreasing arterial blood pressure during general anesthesia for cardiac operations: pharmacokinetics, pharmacodynamics, and associated effects on left ventricular function.
Cheung, AT; Guvakov, DV; Meng, QC; Salgo, IS; Savino, JS; Weiss, SJ, 1999
)
2.07
"Several statistical regression models and artificial neural networks were used to predict the hepatic drug clearance in humans from in vitro (hepatocyte) and in vivo pharmacokinetic data and to identify the most predictive models for this purpose."( Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
Coassolo, P; Lavé, T; Schneider, G, 1999
)
0.3
" 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
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
" In the presence of morin, the pharmacokinetic parameters of nicardipine were significantly altered in the oral group but not in the intravenous group, suggesting that CYP3A-mediated metabolism of nicardipine in the liver is not significantly inhibited by morin."( Effects of morin on the pharmacokinetics of nicardipine after oral and intravenous administration of nicardipine in rats.
Choi, JS; Piao, YJ, 2008
)
0.85
" 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 two-compartment pharmacokinetic model described the mechanisms of how the human body handles with ingestion of NC-cyclodextrin complexes in gastrointestinal tract (GI), distribution in plasma, and their metabolism in the liver."( Pharmacokinetic delivery and metabolizing rate of nicardipine incorporated in hydrophilic and hydrophobic cyclodextrins using two-compartment mathematical model.
Förster, C; Shityakov, S, 2013
)
0.64
"This study aimed to quantify the pharmacokinetic drug-drug interaction between CsA and nicardipine, amlodipine, and lacidipine."( Pharmacokinetic drug-drug interaction of calcium channel blockers with cyclosporine in hematopoietic stem cell transplant children.
Bernard, E; Bertrand, Y; Bleyzac, N; Goutelle, S, 2014
)
0.63

Compound-Compound Interactions

Nicardipine and two new cardiotonic agents, APP 201-533 and DPI 201-106, interact with the N-terminal domain of troponin C, and either do not affect or slightly increase the affinity of the Ca(2+)-specific site.

ExcerptReferenceRelevance
" Nicardipine and two new cardiotonic agents, APP 201-533 and DPI 201-106, interact with the N-terminal domain of troponin C, and either do not affect or, in the case of DPI 201-106, slightly increase the affinity of the Ca(2+)-specific site of troponin C for Ca2+ ion."( Drug interaction with cardiac and skeletal muscle troponin C.
Geguchadze, RN; Gusev, NB; Krylatov, AV, 1990
)
1.19
" Nicardipine in combination with atenolol or clonidine most effectively lowered blood pressure."( Nicardipine in combination with other antihypertensive drugs: calcium antagonist and prazosin have no additive antihypertensive effect?
Jounela, AJ; Juustila, H; Kanniainen, E; Lilja, M; Pasanen, A, 1990
)
2.63
" In conclusion, nicardipine, alone or in combination with enalapril, is an effective and well tolerated drug for use in treatment of hypertension secondary to chronic renal disease."( [Nicardipine, alone or in combination with enalapril, in the therapy of arterial hypertension secondary to chronic nephropathy].
Feriozzi, S; Mavrikakis, G; Morabito, S; Pecci, G; Pierucci, A; Roscia, E; Simonetti, BM, 1989
)
1.53
"We studied the safety and efficacy of intravenous nicardipine alone and in combination with oral captopril."( Antihypertensive effects of parenteral nicardipine alone and in combination with captopril.
Conrad, KA; Davis, TP; Fagan, TC; Johnson, DG; Mayshar, P, 1987
)
0.8
"Cancer chemotherapy combined with calcium-channel blockers was administered to seventeen evaluable patients with hematologic malignancy and solid tumor who became resistant to standard chemotherapies between November 1981 and June 1986 in Saitama Cancer Center."( [Cancer chemotherapy combined with a calcium antagonist in patients with hematologic malignancies and solid tumors resistant to standard chemotherapy].
Sampi, K, 1987
)
0.27
"2 Gy) combined with radiosensitizing agents."( Radiation therapy combined with radiosensitizing agents for cerebral glioblastoma in adults.
Asai, A; Fujimaki, T; Matsutani, M; Nagashima, T; Nakamura, M; Nakamura, O; Tanaka, H; Tanaka, Y; Ueki, K, 1994
)
0.29
" The purpose of the present study was to investigate whether the use of nicardipine (Nc) and phentolamine (Ph) in combination with NE could ameliorate the adverse vasoconstrictive action of NE."( Hemodynamic effects of nicardipine and phentolamine in combination with norepinephrine in a canine low-output-state model.
Hashiyada, H; Kugimiya, T; Miyagawa, N; Shibata, R; Takagi, M; Yamada, T; Yamauchi, H, 1997
)
0.84
" Rofecoxib combined with ritodrine had a synergic effect."( In vitro study of tocolytic effect of rofecoxib, a specific cyclo-oxygenase 2 inhibitor. Comparison and combination with other tocolytic agents.
Benchaib, M; Doret, M; Gharib, C; Mellier, G; Pasquier, JC; Piacenza, JM, 2002
)
0.31
" This study aimed at investigating whether or not nicardipine combined with esmolol (1:10) can maintain systemic and tissue oxygenation during OPCABG."( Effect of nicardipine combined with esmolol on systemic and tissue oxygenation during off-pump coronary artery bypass grafting surgery.
Jiang, Y; Wang, TL; Yang, BX, 2005
)
0.98
"Twenty patients scheduled for OPCABG were divided ramdomly into Group nicardipine (N) and Group nitroglycerine (X) respectively combined with esmolol (E) (Dosage ratio: 1 to 10) (Group N + E and Group X + E) with 10 patients in each group."( Effect of nicardipine combined with esmolol on systemic and tissue oxygenation during off-pump coronary artery bypass grafting surgery.
Jiang, Y; Wang, TL; Yang, BX, 2005
)
0.96
"Nicardipine combined with esmolol (1:10) regimen may maintain systemic and tissue oxygenation during OPCABG."( Effect of nicardipine combined with esmolol on systemic and tissue oxygenation during off-pump coronary artery bypass grafting surgery.
Jiang, Y; Wang, TL; Yang, BX, 2005
)
2.17
"To determine the safety and tolerability of super-selective intra-arterial magnesium sulfate in combination with intra-arterial nicardipine in patients with cerebral vasospasm after subarachnoid hemorrhage."( Super-selective intra-arterial magnesium sulfate in combination with nicardipine for the treatment of cerebral vasospasm in patients with subarachnoid hemorrhage.
Georgiadis, AL; Kozak, OS; Memon, MZ; Qureshi, AI; Rodriguez, GJ; Shah, QA; Suri, MF; Taylor, RA; Tummala, RP; Vazquez, G, 2009
)
0.79
"25-1 g) was administered via a microcatheter in the affected vessels in combination with nicardipine (2."( Super-selective intra-arterial magnesium sulfate in combination with nicardipine for the treatment of cerebral vasospasm in patients with subarachnoid hemorrhage.
Georgiadis, AL; Kozak, OS; Memon, MZ; Qureshi, AI; Rodriguez, GJ; Shah, QA; Suri, MF; Taylor, RA; Tummala, RP; Vazquez, G, 2009
)
0.81
"Administration of intra-arterial magnesium sulfate in combination with nicardipine was well tolerated in patients with subarachnoid hemorrhage and cerebral vasospasm without a significant change in MAP and ICP."( Super-selective intra-arterial magnesium sulfate in combination with nicardipine for the treatment of cerebral vasospasm in patients with subarachnoid hemorrhage.
Georgiadis, AL; Kozak, OS; Memon, MZ; Qureshi, AI; Rodriguez, GJ; Shah, QA; Suri, MF; Taylor, RA; Tummala, RP; Vazquez, G, 2009
)
0.82
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"This study aimed to quantify the pharmacokinetic drug-drug interaction between CsA and nicardipine, amlodipine, and lacidipine."( Pharmacokinetic drug-drug interaction of calcium channel blockers with cyclosporine in hematopoietic stem cell transplant children.
Bernard, E; Bertrand, Y; Bleyzac, N; Goutelle, S, 2014
)
0.63

Bioavailability

The nasal bioavailability of nicardipine from plain buffered solution was 44%, and increased steadily to 56-79% in direct proportion to the amount of PEG 400 added. The steady-state bioavailability was shown to be dose-dependent and averaged 19% (10 mg), 22% (20 mg), 28% (30 mg), and 38% (40 mg)

ExcerptReferenceRelevance
" These increases were particularly marked during chronic dosing - AUC was increased by 163%, Cmax by 127% and apparent oral bioavailability by 90%."( Inhibitory effect of uraemia on the hepatic clearance and metabolism of nicardipine.
Ahmed, JH; Elliott, HL; Grant, AC; Murray, GR; Rodger, RS, 1991
)
0.51
" 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
" Results of a pharmacokinetic study performed in 15 elderly patients showed a rapid rate of absorption and higher plasma levels than those observed in younger patients with hypertension (mean age 54 years)."( Nicardipine in elderly patients with hypertension: a review of experience in France.
Bouchacourt, P; Forette, F; Henry, JF; Hervy, MP; McClaran, J, 1989
)
1.72
" We conclude that until bioavailability studies are performed these three antibiotics should not be coadministered with nicardipine HCl."( The compatibility of nicardipine hydrochloride injection with various ICU medications during simulated Y-site injection.
Alicea, M; Colucci, RD; Greenstein, R; Halpern, NA, 1989
)
0.8
" 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
" Nicardipine and nitrendipine undergo extensive first-pass hepatic extraction after oral administration; oral bioavailability of bepridil is about 60%."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
2.63
" The steady-state bioavailability of nicardipine was shown to be dose-dependent and averaged 19 per cent (10 mg), 22 per cent (20 mg), 28 per cent (30 mg), and 38 per cent (40 mg)."( Single intravenous dose and steady-state oral dose pharmacokinetics of nicardipine in healthy subjects.
Freedman, D; Huang, B; Ling, TL; Massey, IJ; Mroszczak, EJ; Roe, RR; Wagner, JG; Wu, A,
)
0.64
" 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
)
0.67
" This corresponds to a bioavailability of 73%."( Intranasal delivery of nicardipine in the rat.
Bajka, E; Benjamin, E; Visor, GC, 1986
)
0.58
" 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
)
0.54
" 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
)
2.05
" 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
)
0.88
" 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
)
0.56
" These results indicate that the enhancement of the bioavailability of propranolol by coadministration of nicardipine is dependent on the delivery rate of propranolol, suggesting that the interaction is mainly due to short-term haemodynamic effects of nicardipine leading to saturation of hepatic enzymes or functional shunting."( Increase in plasma propranolol caused by nicardipine is dependent on the delivery rate of propranolol.
Dupont, AG; Massart, DL; Vercruysse, I, 1995
)
0.77
" Findings indicate that the presence of food in the gastrointestinal tract reduces the bioavailability of orally administered nicardipine."( Bioequivalence of two orally administered nicardipine products.
Buice, RG; Lane, E; Subramanian, V, 1996
)
0.76
"Serum concentration of (+)-nicardipine was approximately 2-3 times higher than that of (-)-nicardipine in 20- and 40-mg doses of conventional formulations and a non-linear increase in bioavailability with dose was demonstrated."( Pharmacokinetics of nicardipine enantiomers in healthy young volunteers.
Higuchi, S; Honda, M; Inotsume, N; Iwaoka, T; Nakano, M; Naomi, S; Okamoto, Y; Teramura, T; Tomita, K, 1997
)
0.92
" The nasal bioavailability of nicardipine from plain buffered solution was 44%, and increased steadily to 56-79% in direct proportion to the amount of PEG 400 added."( Evaluation of the effect of polyethylene glycol 400 on the nasal absorption of nicardipine and verapamil in the rat.
Lau-Cam, CA; Rahman, M, 1999
)
0.82
"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
"05) increase in the mean oral (+)- and (-)-nicardipine bioavailability (Fobs) (48."( Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site.
Higashiyama, A; Ishizaki, T; Motomura, S; Ohkubo, T; Sugawara, K; Uno, T, 2000
)
0.81
" 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 bioavailability studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady state plasma concentration of the drug with minimal fluctuations for 20 h with improved bioavailability in comparison with the immediate release capsule dosage form."( Influence of limonene on the bioavailability of nicardipine hydrochloride from membrane-moderated transdermal therapeutic systems in human volunteers.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V, 2002
)
0.8
" The drug bioavailability was considerably improved especially after the administration of the mixture of hydrophilic and hydrophobic complexes, when compared with the NC/TAbetaCD complex."( Hydrophilic and hydrophobic cyclodextrins in a new sustained release oral formulation of nicardipine: in vitro evaluation and bioavailability studies in rabbits.
Falcão, AC; Fernandes, CM; Ramos, P; Veiga, FJ, 2003
)
0.54
" The bioavailability studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations for 23 hr with improved bioavailability in comparison with the immediate-release capsule dosage form."( Formulation and in vivo evaluation of membrane-moderated transdermal therapeutic systems of nicardipine hydrochloride using carvone as a penetration enhancer.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V,
)
0.58
" In vivo studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations for 26h with improved bioavailability in comparison with the immediate release capsule dosage form."( Influence of menthol and pressure-sensitive adhesives on the in vivo performance of membrane-moderated transdermal therapeutic system of nicardipine hydrochloride in human volunteers.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V, 2003
)
0.75
"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
" The enhanced oral bioavailability of nicardipine suggests that intestinal-mediated CYP3A4 metabolism and P-gp-mediated efflux of nicardipine are inhibited by morin."( Effects of morin on the pharmacokinetics of nicardipine after oral and intravenous administration of nicardipine in rats.
Choi, JS; Piao, YJ, 2008
)
0.88
" In conclusion, pioglitazone significantly enhanced the oral bioavailability of nicardipine in rats by reducing its presystemic clearance."( Reduced prehepatic extraction of nicardipine in the presence of pioglitazone in rats.
Choi, DH; Choi, JS; Chung, JH; Han, HK; Koh, YY, 2008
)
0.85
"The present study aimed to assess the effect of resveratrol on the bioavailability of nicardipine in rats."( Effect of resveratrol on the pharmacokinetics of oral and intravenous nicardipine in rats: possible role of P-glycoprotein inhibition by resveratrol.
Choi, BC; Choi, JS; Kang, KW, 2009
)
0.81
"Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans."( An investigation into the influence of counterion on the properties of some amorphous organic salts.
Li, T; Remick, DM; Sanchez-Felix, MV; Taylor, LS; Towler, CS; Wikström, H,
)
0.13
"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
" Compared to controls (without EGCG), the AUCs of oral nicardipine and the extent of absolute oral bioavailability (F) were also greater with oral EGCG."( Effects of oral epigallocatechin gallate on the pharmacokinetics of nicardipine in rats.
Burm, JP; Choi, JS, 2009
)
0.84
"4%), and the extent of absolute oral bioavailability (F) of nicardipine was increased (by 38."( Effects of lovastatin on the pharmacokinetics of nicardipine in rats.
Choi, JS; Chung, JW; Yang, SH, 2010
)
0.86
"The oral bioavailability of some drugs is markedly lower in cynomolgus monkeys than in humans."( Species differences in intestinal metabolic activities of cytochrome P450 isoforms between cynomolgus monkeys and humans.
Komuro, S; Mizuki, Y; Nishimuta, H; Sato, K; Yabuki, M, 2011
)
0.37
" The model showed that drug bioavailability was significantly improved after oral administration of cyclodextrin complexes."( Pharmacokinetic delivery and metabolizing rate of nicardipine incorporated in hydrophilic and hydrophobic cyclodextrins using two-compartment mathematical model.
Förster, C; Shityakov, S, 2013
)
0.64
") 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
" However, the short retention time at the absorption site and slow drug transport in intranasal gel influence the drug bioavailability and outcome of ICH."( An enhanced charge-driven intranasal delivery of nicardipine attenuates brain injury after intracerebral hemorrhage.
Deng, J; Gong, Y; Guo, T; Guo, Y; Hao, S; Ji, J; Wang, B, 2019
)
0.77
"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

Dosage Studied

Nicardipine infusion was started for temporizing management of pre-eclampsia at a dosage of 3 mg/h and was subsequently titrated according to blood pressure. We carried out preliminary behavioral toxicity testing to identify a range of low, moderate, and high dosage levels. These dosage levels were to be used subsequently in formal testing.

ExcerptRelevanceReference
"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
" Tolerance of the antihypertensive effect of TC-81 in daily dosing for 2 weeks and the rebound phenomena after discontinuance of the treatment were not observed in RHD."( Antihypertensive effect of the new dihydropyridine calcium antagonist (+-)-3-(benzylmethylamino)-2,2-dimethylpropyl methyl 4-(2-fluoro-5-nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedica rbo xylate hydrochloride in dogs.
Aoki, K; Kishimoto, T; Naruchi, T; Okamiya, Y; Sunakawa, K; Takeshita, T; Tanabe, H, 1992
)
0.28
" NIC shifted the dose-response curve of ET-1 for % delta PP to the right in a parallel fashion."( Nicardipine inhibits the endothelin-1-induced constriction of systemic capacitance and resistance vessels.
Hirakawa, S; Hirose, I; Ito, H; Nagata, K; Sahashi, T; Takai, K; Wada, H, 1991
)
1.72
" In the in vitro studies, we created dose-response curves of the excised tracheal strip."( Nicardipine suppresses bronchoconstrictor actions of pharmacologic agents in guinea pigs.
Lai, YL; Zhang, HQ, 1991
)
1.72
" These increases were particularly marked during chronic dosing - AUC was increased by 163%, Cmax by 127% and apparent oral bioavailability by 90%."( Inhibitory effect of uraemia on the hepatic clearance and metabolism of nicardipine.
Ahmed, JH; Elliott, HL; Grant, AC; Murray, GR; Rodger, RS, 1991
)
0.51
" At 2 h after dosing (peak effect) both STD nicardipine (30 mg three times daily) and SR nicardipine (60 mg twice daily) for 28 days produced a highly significant reduction in sitting and standing blood pressure."( Nicardipine sustained release in hypertension.
Beard, M; Crichton, W; Dow, RJ; Jamieson, M; Jeffers, TA; MacDonald, FC; Petrie, JC; Roy-Chaudhury, P; Webster, J; Witte, K, 1991
)
1.99
" It was administered for 22 days and the average daily dosage was 187mg."( [A case presenting a severe paralytic ileus during the continuous intravenous injection of nicardipine hydrochloride].
Honmou, O; Kurokawa, Y; Ohta, K; Uede, T, 1991
)
0.5
" Endotoxin impaired responsiveness to vasopressin, phenylephrine and cirazoline, producing a shift to the right in the dose-response curves without any change in the maximum response."( Endotoxin-induced impairment of vasopressor and vasodepressor responses in the pithed rat.
Furman, BL; Guc, MO; Parratt, JR, 1990
)
0.28
"A novel calcium entry blocker, nicardipine, has been tested using a dosage of 20 mg twice a day against placebo on 30 patients suffering from migraine without aura, according to a double-blind, cross-over design; overall duration of the study was four months (two with nicardipine and two with placebo)."( Migraine treatment with nicardipine.
Leandri, M; Parodi, CI; Rigardo, S; Schizzi, R, 1990
)
0.87
" A dose-response relationship was observed, as both nicardipine dosage and plasma nicardipine concentration correlated with reduction in blood pressure."( Acute pharmacokinetic and hemodynamic effects of intravenous bolus dosing of nicardipine.
Cheung, DG; Gasster, JL; Neutel, JM; Weber, MA, 1990
)
0.76
" The usefulness of intravenous nicardipine for postoperative hypertension was demonstrated in this study by: (1) the rapid control of blood pressure, (2) its continued efficacy during maintenance, and (3) little need to adjust dosage to control blood pressure."( Nicardipine versus placebo for the treatment of postoperative hypertension.
Clark, S; Goldberg, ME; Joseph, J; Maguire, D; Moritz, H; Seltzer, JL; Turlapaty, P, 1990
)
2.01
" At a concentration of (+)-nicardipine (10(-7) M) which inhibits most of the release stimulated by 50 mM potassium, the response to 3 X 10(-5) M nicotine remains; however, the dose-response curve to nicotine is shifted slightly to the left."( Stimulus secretion coupling in cultured chromaffin cells. Dependency on external sodium and on dihydropyridine-sensitive calcium channels.
Adams, M; Boarder, MR; Marriott, D, 1987
)
0.57
" Lowering the holding potential to -80 mV shifted the dose-response curve to the right."( Blocking actions of Ca2+ antagonists on the Ca2+ channels in the smooth muscle cell membrane of rabbit small intestine.
Kitamura, K; Kuriyama, H; Terada, K, 1987
)
0.27
" Two weeks of combined treatment with nicardipine and enalapril significantly reduced the predosing blood pressure, 12 h after the last dose of nicardipine (158/96 as compared with 172/106 with placebo), and there were further significant reductions in blood pressure during the subsequent dosage interval."( An evaluation of the pharmacodynamics and pharmacokinetics of nicardipine combined with enalapril in essential hypertension.
Donnelly, R; Elliott, HL; Meredith, PA; Reid, JL, 1987
)
0.78
" 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
)
0.28
" Dosage of calcium and phosphate, Na, K, aldosterone, in blood and urine and PTH and PRA in blood had been effectuated."( [Calcium intestinal absorption in normotensive and essential hypertensive subjects before and after nicardipine].
Carre, A; Debrueres, S; Fouquoire, B; Petetin, N; Poncelet, P; Warembourg, A, 1989
)
0.49
" Patients responders, 8 males and 2 females, mean age 57 +/- 10 years, have been treated with oral nicardipine administered at the dosage of 40 mg td for 3 months."( [Delayed-action nicardipine in the prolonged treatment of chronic congestive heart failure in responsive subjects].
Masciocco, L; Mattioli, AV; Mattioli, G; Tondi, S, 1989
)
0.84
" The absolute decrements peaked 4 h after dosing (-18."( Antihypertensive effect of slow-release nicardipine. A placebo-controlled cross-over study.
Caiazza, A; Cardellino, G; Del Prato, C; Errico, M; Freda, M; Ghisoni, F; Innocenti, PF; Pesenti, M; Ponzanelli, F; Salvetti, A, 1989
)
0.54
" However, none of the treatments studied was ideal for clinical use in the twice daily dosage used in this study."( Comparison of the efficacy and acceptability of nicardipine and propranolol, alone and in combination, in mild to moderate hypertension.
Dow, RJ; Gough, KJ; Laing, EM; Macdonald, FC; Maclean, D; McDevitt, DG; Mitchell, ET, 1989
)
0.53
" The dose-response relations for the increase in blood pressure of rats receiving endothelin were comparable with those of rats receiving angiotensin II."( Characteristics of pressor response to endothelin in spontaneously hypertensive and Wistar-Kyoto rats.
Goto, K; Ishikawa, T; Ito, I; Kimura, S; Masaki, T; Miyauchi, T; Sugishita, Y; Tomobe, Y; Yanagisawa, M, 1989
)
0.28
" Phase I, a 2- to 4-week placebo washout to establish baseline supine diastolic blood pressure (BP), was followed by 4 weeks of open-label nicardipine dose titration (phase II) to establish optimal dosage on a 3-times-daily regimen for each patient."( Long-term systemic arterial blood pressure control with nicardipine.
Castle, CH; Wolbach, RA, 1989
)
0.73
" We have characterized, in vivo, the pharmacokinetics and dose-response interactions between nifedipine and cisplatin."( In vivo characterization of combination antitumor chemotherapy with calcium channel blockers and cis-diamminedichloroplatinum(II).
Honn, KV; Nelson, KK; Onoda, JM; Taylor, JD, 1989
)
0.28
" Home recordings confirmed the hypotensive effect and also revealed a consistent 'peak' effect between 2-4 h after dosing (mean difference 32/22) mm Hg)."( Evaluation of a long acting formulation of nicardipine in hypertension by clinic and home recorded blood pressures and Doppler aortovelography.
Jeffers, TA; Petrie, JC; Rawles, J; Webster, J; Witte, K, 1989
)
0.54
" 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
" After dosing with nicardipine, the results differed according to the exploratory technique: a slight increase of the laser Doppler signal (NS) and a decrease of the photoplethysmographic signal were recorded."( [Photoplethysmography and laser Doppler velocimetry in the study of cutaneous vasomotility at high altitudes].
Kayser, B; Keromes, A; Larmignat, P; Pecquet, C; Richalet, JP, 1988
)
0.6
" Nicardipine treatment (10 to 15 mg intraperitoneal dosage during 8 weeks), led to: an efficient but incomplete control of hypertension."( [Effects of nicardipine on left ventricular hypertrophy of the rat with renovascular arterial hypertension].
Besse, P; Bonoron-Adèle, S; Grellet, J; Stuyvers, B; Tariosse, L, 1988
)
1.56
" The forearm arterial blood flow (ABF) was measured using plethysmography before and after N infusion: 1st step was obtained after infusion of 1 mg during 5 min then 1 mg during 25 min; a second step was obtained after the infusion of the same dose during the same time; thus a cumulative dosage of 4 mg was infused over a total duration of 60 mn."( [Acute hemodynamic study of intravenous nicardipine in arterial hypertension].
Chaignon, M; Guédon, J; Maurel, C, 1987
)
0.54
" 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
)
0.76
" 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
" Since nicardipine, nitrendipine, and nifedipine are similar in efficacy and safety, the eventual availability of sustained-release dosage forms may determine how these drugs are ultimately used."( Nicardipine, nitrendipine, and bepridil: new calcium antagonists for cardiovascular disorders.
Hasegawa, GR, 1988
)
2.17
" Fifteen of 42 patients were treated with the lower dosage levels of nicardipine (0."( Combination of aminocaproic acid and nicardipine in treatment of aneurysmal subarachnoid hemorrhage.
Adams, HP; Beck, DW; Flamm, ES; Godersky, JC; Loftus, CM, 1988
)
0.78
" We carried out preliminary behavioral toxicity testing to identify a range of low, moderate, and high dosage levels of the calcium channel blocker, nicardipine; these dosage levels were to be used subsequently in formal testing."( Experimental spinal cord injury: effect of a calcium channel antagonist (nicardipine).
Black, P; Finkelstein, SD; Gillespie, JA; Markowitz, RS; McMonagle-Strucko, K, 1988
)
0.71
" 1) H2O2 dissolved in different concentrations produced arterial contractions similar to those by equimolar Oxy-Hb, showing similar dose-response curves."( [On the mechanism underlying spasmogenic actions of oxy-hemoglobin on the cerebral artery, analyzed from the inhibitory effects of nicardipine, procaine and indomethacin].
Doi, M, 1988
)
0.48
" In rats treated with the ganglionic blocking agent, pentolinium, nicardipine produced parallel shifts to the right in the dose-response curves for phenylephrine but had no effect on maximal responses to phenylephrine."( Greater vasodepressor sensitivity to nicardipine in spontaneously hypertensive rats (SHR) compared to normotensive rats.
Armstrong, JM; Atkinson, J; Boillat, N; de Rivaz, JC; Fluckiger, JP; Fouda, AK; Piton, MC; Porchet, PA; Sautel, M; Sonnay, M, 1988
)
0.78
"We conducted a randomized placebo-controlled double-blind study in 40 hypertensive subjects to assess the antihypertensive effect of a new galenic form of nicardipine administered at a dosage of 50 mg twice daily for 3 weeks."( Evaluation of slow release nicardipine in essential hypertension by casual and ambulatory blood pressure measurements. Effects of acute versus chronic administration.
Bellet, M; Chatellier, G; Corvol, P; Ménard, J; Pagny, JY, 1987
)
0.77
" These data suggest that nicardipine monotherapy given in a twice-daily dosing regimen has only a limited role to play in the chronic treatment of patients with essential hypertension."( Twice-daily nicardipine in the treatment of essential hypertension.
Charlap, S; Dorsa, F; Kafka, K; Kimmel, B; Laifer, L; Lazar, E; Saltzberg, S; Singer, M; Strom, J; Weinberg, P, 1986
)
0.95
" The possibilities of LC-MS in the pharmaceutical industry for the analysis of drug substances and dosage forms, metabolism studies and the elucidation of the structures of materials of biological origin are discussed."( Experience with routine applications of liquid chromatography-mass spectrometry in the pharmaceutical industry.
Erni, F; Groeppelin, A; Linder, M; Schellenberg, KH, 1987
)
0.27
" Nicardipine in a dosage of 1 mg/kg effectively attenuated the liberation of FFAs, particularly that of arachidonic acid which is known as the precursor of prostaglandins, thromboxanes, and leukotrienes."( Ca2+ antagonist and protection of the brain against ischemia. Effects of nicardipine on free fatty acid liberation in the ischemic brain in rats.
Handa, J; Kidooka, M; Matsuda, M, 1987
)
1.41
" 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
)
0.6
"The effects of two dosage schedules of nicardipine, a calcium-entry blocker, were studied in the pregnant rabbit during induced preterm uterine contractions and compared with the effects of ritodrine hydrochloride."( Cardiovascular and tocolytic effects of nicardipine HCl in the pregnant rabbit: comparison with ritodrine HCl.
Holbrook, RH; Katz, M; Lirette, M, 1987
)
0.81
"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
)
0.81
" 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
)
0.63
" 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
)
2
" 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
)
0.51
" 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,
)
0.51
" 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
)
1.46
" 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
)
2.62
" 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
)
0.95
"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,
)
0.74
" 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
)
0.47
" 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
"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
)
0.76
"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
)
0.8
"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
)
0.51
" dosage to rats, dogs, monkeys and humans."( Comparative pharmacokinetics of nicardipine hydrochloride, a new vasodilator, in various species.
Higuchi, S; Shiobara, Y, 1980
)
0.54
" Dosing regimens and possible applications in paediatric anaesthesia are discussed."( Nicardipine: perioperative applications in children.
Deshpande, JK; Lowe, S; Tobias, JD, 1995
)
1.73
" Nicardipine was administered at a dosage of 10 micrograms/kg via bolus injection 30 min after the resuscitation."( Effect of calcium antagonist, nicardipine, on cerebral blood flow in postasphyxial newborn piglets.
Imai, T; Isobe, K; Itoh, S; Kondo, M; Kusaka, T; Onishi, S; Sugihara, S, 1995
)
1.49
" 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
" 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
)
1.46
" Drugs were administered according to a predetermined dosing schedule for a 10 to 12 h period."( A comparison of intravenous nicardipine and sodium nitroprusside in the immediate treatment of severe hypertension.
Cook, E; Fletcher, E; Grandy, S; Lee, R; Maher, KE; Neutel, JM; Ram, CV; Smith, DH; Turlepaty, P; Wallin, D, 1994
)
0.58
" In pentobarbitone-anaesthetized pigs, haemodynamic indices were measured before and after intravenous administration of NG-nitro-L-arginine methyl ester (L-NAME) in a dose-response protocol (0."( Comparison of the ability of nicardipine, theophylline and zaprinast to restore cardiovascular haemodynamics following inhibition of nitric oxide synthesis.
Adgey, AA; Allen, JD; Herity, NA; Silke, B, 1994
)
0.58
" The dose-response curves for the effects of aminophylline in the presence of Ni2+ on Td and dT/dt max during direct single-pulse stimulation were significantly shifted to the right."( Some new evidence on antifatigue action of aminophylline on the isolated hemidiaphragm of the rat.
Prostran, M; Todorović, Z; Varagić, VM, 1993
)
0.29
" Plasma levels of YM-21095 after 3 mg kg-1 intravenous dosing to dogs declined biphasically and fitted a two-compartment model."( Pharmacokinetics and cardiovascular effects of YM-21095, a novel renin inhibitor, in dogs and monkeys.
Asano, M; Inagaki, O; Shibasaki, M; Takenaka, T; Usui, T, 1994
)
0.29
"The aim of this study was to evaluate the effects of nicardipine, at the dosage of 80 mg/day in two administrations, on blood pressure, intimal-media thickness of the common carotid artery and on arterial distensibility after 6 months of therapy."( Effects of nicardipine on intimal-medial thickness and arterial distensibility in hypertensive patients. Preliminary results after 6 months.
Cicatiello, AM; Giordano, G; Guarini, P; Iovino, L; Messina, V; Tagliamonte, MR; Tedeschi, C, 1993
)
0.93
" At the dosage used in this study, nicardipine modified the systemic vascular response to oxygen but not the pulmonary vascular response."( [Acute effects of nicardipine on the vascular reactivity of oxygen in patients with respiratory insufficiency and pulmonary hypertension].
Lévy, S; Paganelli, F; Philip-Joët, F; Saadjian, A; Saadjian, M, 1993
)
0.9
" Ambulatory blood pressure monitoring demonstrated that the antihypertensive effect was maintained throughout the dosing interval."( Sustained-release nicardipine in mild-to-moderate hypertension.
Fagan, TC; Kenley, S; Reitman, MA; Tyler, ED; Weber, MA, 1993
)
0.62
" Nicardipine was given orally at a mean daily dosage of 80 mg (range 40-120), for four weeks."( [Nationwide drug surveillance project on slow-release nicardipine in the short-term therapy of light/moderate arterial hypertension].
Benvenuti, C; Guerini Rocco, C; Trezzi, P, 1995
)
1.45
" Specific advantages have been identified such as stable dose-response effect, less hypotensive and tachycardial effects during the use of iv nicardipine in treatment of hypertensive patients."( Comparison of antihypertensive effects of nicardipine with nitroglycerin for perioperative hypertension.
Chen, TL; Cheng, YJ; Lee, TS; Lin, CJ; Lin, SY; Sun, WZ, 1995
)
0.76
") are bioequivalent at the daily dosage used in the study."( Comparison between a bid and a tid regimen: improved compliance with no improved antihypertensive effect. The EOL Research Group.
Alamercery, Y; Benghozi, R; Boissel, JP; Ducruet, T; Meillard, O; Perrin-Fayolle, E; Sassano, P, 1996
)
0.29
" It is suggested that a suitable dosage of fentanyl is effective without causing serious side effects for neonate."( [Anesthesia for a patient with HELLP syndrome].
Sakio, H; Satoh, T; Takahashi, H, 1996
)
0.29
" Compliance with twice a day dosage was compared with compliance with three doses a day."( [Example of a phase IV trial involving several physicians and aiming at answering a scientific question: EOL].
Alamercery, Y; Benghozi, R; Boissel, JP; Ducruet, T; Meillard, O; Perrin-Fayolle, E; Sassano, P,
)
0.13
" 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
)
0.3
"The purpose of this study was to prepare and evaluate an enteric coated dosage form of nicardipine hydrochloride (NCH)-loaded microspheres for delivery over a 12-hr period."( Influence of swelling degree on release of nicardipine hydrochloride from acrylic microspheres prepared by solvent evaporation method.
Baykara, T; Dinç, E; Onur, F; Yüksel, N, 1998
)
0.79
" Nicardipine always succeeded in maintaining low systemic vascular resistance but its dosage varied widely between patients (0."( Haemodynamic heterogeneity and treatment with the calcium channel blocker nicardipine during phaeochromocytoma surgery.
Colson, P; Dareau, S; Mann, C; Ribstein, J; Ryckwaert, F, 1998
)
1.44
" At a dosage of NPS-ACTH higher than 10 nM, the stimulative effect of steroidogenesis was partly suppressed by nicardipine and also by AA-861, a lipoxygenase inhibitor."( Calcium ion as a second messenger for o-nitrophenylsulfenyl-adrenocorticotropin (NPS-ACTH) and ACTH in bovine adrenal steroidogenesis.
Higuchi, K; Kawato, S; Kimoto, T; Kominami, S; Ohta, Y; Yamazaki, T, 1998
)
0.51
"Both additional pharmacokinetic and pharmacodynamic studies remain mandatory to improve the dosage regimens and assess the efficacy and safety of nicardipine infusion in hypertensive neonates."( Intravenous nicardipine as a first-line antihypertensive drug in neonates.
Debuche-Benouachkou, V; Germain, JF; Gouyon, JB; Milou, C; Semama, DS, 2000
)
0.89
" However, all of the mean kinetic parameters of both the enantiomers after the intravenous dosing of racemic nicardipine did not differ between the grapefruit juice- and water-intake trial phases."( Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site.
Higashiyama, A; Ishizaki, T; Motomura, S; Ohkubo, T; Sugawara, K; Uno, T, 2000
)
0.76
" Grapefruit juice appears to affect this metabolic disposal of (-)-nicardipine to a somewhat greater extent compared with that of (+)-nicardipine, with an early postdose transient tachycardia after the oral dosing of racemic nicardipine."( Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site.
Higashiyama, A; Ishizaki, T; Motomura, S; Ohkubo, T; Sugawara, K; Uno, T, 2000
)
0.78
"A floating dosage form composed of nicardipine hydrochloride (NH) and hydroxypropylmethylcellulose acetate succinate (enteric polymer) was prepared using a twin-screw extruder."( Evaluation of a floating dosage form of nicardipine hydrochloride and hydroxypropylmethylcellulose acetate succinate prepared using a twin-screw extruder.
Fukui, H; Izumi, S; Nakamichi, K; Oka, M; Yasuura, H, 2001
)
0.86
"A new nicardipine HCl oral sustained-release dosage form was evaluated for bioequivalence in comparison with a reference product, Cardene SR."( Preliminary bioequivalence testing of two nicardipine HCl sustained-release formulations with in vitro/in vivo correlations.
Ayres, JW; Sorasuchart, W,
)
0.88
"Contractile activity was assessed by calculating the area under the curve, to obtain a dose-response curve of each drug."( In vitro study of tocolytic effect of rofecoxib, a specific cyclo-oxygenase 2 inhibitor. Comparison and combination with other tocolytic agents.
Benchaib, M; Doret, M; Gharib, C; Mellier, G; Pasquier, JC; Piacenza, JM, 2002
)
0.31
"05), suggesting a linear dose-response relationship."( Effect of diaspirin cross-linked haemoglobin (DCLHb) on mean arterial pressure during cardiopulmonary bypass in swine.
Burhop, K; Chiari, P; Ferrera, R; Hadour, G; Jegaden, O; Lehot, JJ; Montagna, P, 2002
)
0.31
" The bioavailability studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady state plasma concentration of the drug with minimal fluctuations for 20 h with improved bioavailability in comparison with the immediate release capsule dosage form."( Influence of limonene on the bioavailability of nicardipine hydrochloride from membrane-moderated transdermal therapeutic systems in human volunteers.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V, 2002
)
0.8
" The bioavailability studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations for 23 hr with improved bioavailability in comparison with the immediate-release capsule dosage form."( Formulation and in vivo evaluation of membrane-moderated transdermal therapeutic systems of nicardipine hydrochloride using carvone as a penetration enhancer.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V,
)
0.58
" In vivo studies in healthy human volunteers indicated that the TTS of nicardipine hydrochloride, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations for 26h with improved bioavailability in comparison with the immediate release capsule dosage form."( Influence of menthol and pressure-sensitive adhesives on the in vivo performance of membrane-moderated transdermal therapeutic system of nicardipine hydrochloride in human volunteers.
Bhaskar, P; Krishnaiah, YS; Satyanarayana, V, 2003
)
0.75
" However, nicardipine did not alter the R/S metoprolol ratio in plasma 3 h after dosing, the plasma concentration of S-(-)-metoprolol 3 h after dosing or the beta-adrenoceptor blockade produced by metoprolol in subjects of both phenotypes."( Influence of CYP2D6-dependent metabolism on the steady-state pharmacokinetics and pharmacodynamics of metoprolol and nicardipine, alone and in combination.
Decolin, D; Funck-Brentano, C; Jaillon, P; Laurent-Kenesi, MA; Poirier, JM, 1993
)
0.9
" 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
" Nicardipine and the enantiomers could shift the dose-response curves of NE, KCl or CaCl2 to right in a nonparallel manner and decrease the maximum effective in a concentration-depended manner, respectively."( The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery.
He, L; Wang, S; Yun, B, 2005
)
1.55
"Nicardipine infusion was started for temporizing management of pre-eclampsia at a dosage of 3 mg/h and was subsequently titrated according to blood pressure."( Intravenous use of the calcium-channel blocker nicardipine as second-line treatment in severe, early-onset pre-eclamptic patients.
Bartels, PA; Bijvank, BN; Hanff, LM; Roofthooft, DW; Steegers, EA; Visser, W; Vulto, AG, 2005
)
2.03
"7 days (range, 1-26 days) using nicardipine treatment, in a maximum dosage ranging from 3 to 9 mg/h."( Intravenous use of the calcium-channel blocker nicardipine as second-line treatment in severe, early-onset pre-eclamptic patients.
Bartels, PA; Bijvank, BN; Hanff, LM; Roofthooft, DW; Steegers, EA; Visser, W; Vulto, AG, 2005
)
0.87
" CCAs can be safely used in children with renal insufficiency or failure and as a general rule there is no need to modify drug dosage in this population."( A review of calcium channel antagonists in the treatment of pediatric hypertension.
Sahney, S, 2006
)
0.33
"The dose-response studies revealed that intracarotid administration of nicardipine, compared with verapamil, was more effective in augmenting cerebral blood flow."( Augmentation of cerebral blood flow and reversal of endothelin-1-induced vasospasm: a comparison of intracarotid nicardipine and verapamil.
Etu, JJ; Joshi, S; Lavine, SD; Meyers, PM; Wang, M, 2007
)
0.78
" Real plasma samples from hypertensive patients receiving a dosing of 5mg antagonists were examined by using the proposed method."( Determination of nicardipine and amlodipine in human plasma using on-line solid-phase extraction with a monolithic weak cation-exchange column.
Chen, Y; Qi, L; Wei, X; Yang, G, 2009
)
0.69
" propofol infusion, intracarotid infusion could reach and maintain the target anaesthetic depth with less dosage and without affecting MAP."( Efficacy of intracarotid propofol infusion and impact of cerebral blood flow alteration.
Fan, YY; Lao, N; Nie, H; Wang, BR; Xiong, LZ; Xu, LX; Zhang, H, 2009
)
0.35
" Based on these results, nicardipine dosage should be adjusted when given with supplements containing resveratrol."( Effect of resveratrol on the pharmacokinetics of oral and intravenous nicardipine in rats: possible role of P-glycoprotein inhibition by resveratrol.
Choi, BC; Choi, JS; Kang, KW, 2009
)
0.89
" Compare the side effect profile of nicardipine to labetolol for the treatment of severe hypertension in pregnancy and calculate the appropriate dosing of nicardipine for the treatment of hypertension in pregnancy."( Nicardipine for the treatment of severe hypertension in pregnancy: a review of the literature.
Duvekot, JJ; Nij Bijvank, SW, 2010
)
2.08
"Our purpose was to compare the safety and efficacy of food and drug administration (FDA) recommended dosing of IV nicardipine versus IV labetalol for the management of acute hypertension."( CLUE: a randomized comparative effectiveness trial of IV nicardipine versus labetalol use in the emergency department.
Baumann, BM; Borczuk, P; Cannon, CM; Chandra, A; Cline, DM; Diercks, D; Hiestand, B; Hsu, A; Jois-Bilowich, P; Kaminski, B; Levy, P; Nowak, RM; Peacock, WF; Schrock, JW; Varon, J, 2011
)
0.82
"This is a substudy of the multicenter safety and efficacy Evaluation of intravenous Cardene (nicardipine) and Labetalol Use in the Emergency department (CLUE) trial that randomized patients to Food and Drug Administration-recommended intravenous dosing of nicardipine or labetalol to reach a physician predefined systolic BP (SBP) and target range (TR) of ±20 mm Hg within 30 minutes."( Impact of initial blood pressure on antihypertensive response in patients with acute hypertension.
Farias, S; Gonzalez, M; Levy, PD; Peacock, WF, 2014
)
0.62
" We determined factors associated with nicardipine dosing and the association of dose with clinical outcomes in hyperacute ICH."( Intravenous nicardipine dosing for blood pressure lowering in acute intracerebral hemorrhage: the Stroke Acute Management with Urgent Risk-factor Assessment and Improvement-Intracerebral Hemorrhage study.
Arihiro, S; Furui, E; Hasegawa, Y; Kario, K; Kimura, K; Koga, M; Minematsu, K; Nagatsuka, K; Nakagawara, J; Okada, Y; Okuda, S; Sato, S; Shiokawa, Y; Takasugi, J; Takizawa, H; Tokunaga, K; Toyoda, K; Yamagami, H,
)
0.78
" Following the termination of nicardipine, all children eventually required dosage increases in their tacrolimus regimens to re-achieve target serum concentrations."( Supra-therapeutic tacrolimus concentrations associated with concomitant nicardipine in pediatric liver transplant recipients.
Carpenter, TC; Clark, N; Hurst, AL; Reiter, PD; Sundaram, SS, 2015
)
0.94
" The main outcome measures were persistent severe hypertension (DBP>100mmHg>120min) despite maximum dosage of study medication and prolongation of pregnancy."( Ketanserin versus dihydralazine for the treatment of severe hypertension in early-onset preeclampsia: a double blind randomized controlled trial.
Bijvank, SW; Duvekot, JJ; Edens, MA; Hanff, LM; Roofthooft, DW; Steegers, EA; Visser, W; Vulto, AG, 2015
)
0.42
"Adequate initial dosing of antihypertensive treatment has the potential to reduce time to blood pressure control and possibly time to alteplase therapy."( Time to Blood Pressure Control Before Thrombolytic Therapy in Patients With Acute Ischemic Stroke: Comparison of Labetalol, Nicardipine, and Hydralazine.
Cortes, J; Hall, AB; McKay, C, 2015
)
0.62
"Nicardipine is frequently used in the treatment of hypertension for patients with acute stroke; however, its dosing is complicated by a high risk of phlebitis."( Reduction of Nicardipine-Related Phlebitis in Patients with Acute Stroke by Diluting Its Concentration.
Kawada, K; Miyamoto, N; Ohta, T; Tanaka, K, 2018
)
2.29
" Administration of 4 mg of nicardipine every 12 hours was the most commonly reported dosing regimen."( Systematic Review of Intrathecal Nicardipine for the Treatment of Cerebral Vasospasm in Aneurysmal Subarachnoid Hemorrhage.
Grandhi, R; Hafeez, S, 2019
)
1.09
" We unexpectedly discover a new class of aggregating ligands that exhibit negligible interactions with proteins but act as competitive sinks for the free inhibitor, resulting in bell-shaped dose-response curves."( Mechanisms of Specific versus Nonspecific Interactions of Aggregation-Prone Inhibitors and Attenuators.
Ahmed, R; Boulton, S; Cheng, X; Melacini, G; Selvaratnam, R; Van, K, 2019
)
0.51
"The initial dosage of nicardipine was dependent upon patient systolic blood pressure (SBP)."( Efficacy of low-dose nicardipine for emergent treatment of severe postpartum hypertension in maternal intensive care units: An observational study.
Gan, S; Lan, L; Li, L; Qi, H; Qin, J; Ren, L; Yan, Y; Zhang, Y, 2020
)
1.19
"We have now performed behavioral testing in groups of 10 male Tcf4(± ) PTHS mice dosing by oral gavage at 3 mg/kg once a day for 3 weeks using standard methods to assess sociability, nesting, fear conditioning, self-grooming, open field and test of force."( Repurposing the Dihydropyridine Calcium Channel Inhibitor Nicardipine as a Na
Davidow, A; Ekins, S; Puhl, AC, 2020
)
0.8
" Initial dosing with nicardipine lowered acute diastolic BP than labetalol (least square mean difference (labetalol-nicardipine)=5."( Initial antihypertensive agent effects on acute blood pressure after intracerebral haemorrhage.
Behymer, TP; Bettin, M; Christianson, T; Coleman, ER; Divani, A; Flaherty, ML; Gilkerson, LA; James, ML; King, NKK; Krishnamoorthy, V; Langefeld, CD; McCauley, JL; Ng, Y; Qi, W; Shah, S; Testai, FD; Walsh, KB; Woo, D, 2022
)
1.04
" In all cases, the low DBP resolved after discontinuing or reducing the dosage of nicardipine."( Nicardipine for treating severe antepartum hypertension during pregnancy: Nine years of experience in more than 800 women.
Cornette, JC; Duvekot, JJ; Edens, MA; Hengst, M; Huigen, S; Nij Bijvank, SW; Winkelen, AV, 2022
)
2.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (6)

ClassDescription
dihydropyridine
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
diesterA diester is a compound containing two ester groups.
methyl esterAny carboxylic ester resulting from the formal condensation of a carboxy group with methanol.
C-nitro compoundA nitro compound having the nitro group (-NO2) attached to a carbon atom.
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[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]

Protein Targets (93)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency50.45130.004023.8416100.0000AID485290
acetylcholinesteraseHomo sapiens (human)Potency13.80290.002541.796015,848.9004AID1347398
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency28.46953.189029.884159.4836AID1224846; AID1224894
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159521; AID1159523
ATAD5 protein, partialHomo sapiens (human)Potency19.72670.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency5.01190.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency31.83260.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency1.99530.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency14.30880.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency5.54040.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency27.01620.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency29.84930.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency21.37840.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.10960.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency17.29830.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency31.67040.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency24.92330.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency22.02420.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency22.22830.375827.485161.6524AID743217; AID743220; AID743239
pregnane X nuclear receptorHomo sapiens (human)Potency4.21630.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.55960.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743079
GVesicular stomatitis virusPotency0.24550.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency2.75400.00108.379861.1304AID1645840
polyproteinZika virusPotency5.01190.00308.794948.0869AID1347053
glucocerebrosidaseHomo sapiens (human)Potency16.53110.01268.156944.6684AID2101
ParkinHomo sapiens (human)Potency16.36010.819914.830644.6684AID720572
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency25.12990.001024.504861.6448AID743212; AID743215; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency20.26460.001019.414170.9645AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency25.61820.023723.228263.5986AID743223; AID743241
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.93490.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.84930.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency33.49150.001628.015177.1139AID1224843; AID1224895
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency115.82100.01262.451825.0177AID485313
D(1A) dopamine receptorHomo sapiens (human)Potency4.45750.02245.944922.3872AID488982; AID488983
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency30.13130.134610.395030.1313AID1347049
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency84.27890.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency22.38720.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.07950.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.32890.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency29.41460.042027.378961.6448AID743210; AID743228
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.12160.00669.809418.4927AID1347050
flap endonuclease 1Homo sapiens (human)Potency4.22840.133725.412989.1251AID588795
ras-related protein Rab-9AHomo sapiens (human)Potency58.04790.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency21.59700.00378.618923.2809AID2660; AID2666; AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency25.90180.000627.21521,122.0200AID743202; AID743219
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency0.00600.425612.059128.1838AID504536
gemininHomo sapiens (human)Potency31.23840.004611.374133.4983AID624296
DNA polymerase kappa isoform 1Homo sapiens (human)Potency33.58750.031622.3146100.0000AID588579
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency5.10280.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency35.48130.125912.234435.4813AID1458
M-phase phosphoprotein 8Homo sapiens (human)Potency37.68580.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.18380.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency1.99530.891312.067628.1838AID1487
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency33.49150.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency0.24550.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.24550.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency34.14660.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency33.49150.001551.739315,848.9004AID1259244
D(1A) dopamine receptorSus scrofa (pig)Potency18.49270.00378.108123.2809AID2667
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.58931.000010.475628.1838AID1457
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.24550.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency31.10850.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency34.48640.011912.222168.7989AID588378; AID651632
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.24550.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)88.00000.20005.677410.0000AID1473741
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC50 (µMol)24.10000.02201.64228.9000AID1207668
Equilibrative nucleoside transporter 1Rattus norvegicus (Norway rat)Ki5.36005.36005.36005.3600AID34011
B2 bradykinin receptorCavia porcellus (domestic guinea pig)IC50 (µMol)20.00000.00112.58648.0000AID43124; AID43125
Bile salt export pumpHomo sapiens (human)IC50 (µMol)8.31400.11007.190310.0000AID1443980; AID1443989; AID1449628; AID1473738; AID1674183
Chymotrypsinogen ABos taurus (cattle)IC50 (µMol)175.00000.98004.05607.2000AID52776
Beta-lactamaseEscherichia coli K-12IC50 (µMol)20.00000.01502.46578.0000AID43124; AID43125; AID43431
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)8.00000.06404.012610.0000AID150754; AID681128
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)7.79270.00022.318510.0000AID150752; AID150755; AID310120; AID310122; AID364884; AID678836; AID681122; AID681126; AID681127; AID681131; AID681335; AID681579; AID681580; AID681581; AID681582
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.42000.00011.753610.0000AID54923
Quinolone resistance protein NorAStaphylococcus aureusIC50 (µMol)22.80007.00008.50009.7000AID1460599
Adenosine receptor A3Homo sapiens (human)Ki3.25000.00000.930610.0000AID34564
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)1.69000.00002.800510.0000AID1210069
Cytochrome P450 2C9 Homo sapiens (human)Ki0.28000.00031.684210.0000AID54411
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)20.00000.00031.38338.4000AID43124
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)2.50000.20004.713010.0000AID150753; AID681119
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC50 (µMol)24.10000.00132.24956.9000AID1207668
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)Ki0.00080.00080.57965.4000AID45781
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)Ki0.00080.00080.74105.4000AID45781
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki11.00000.00030.91969.0000AID33356
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki63.80000.00021.494010.0000AID33788
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)1.69000.01202.53129.4700AID1210069
Voltage-dependent L-type calcium channel subunit alpha-1SRattus norvegicus (Norway rat)Ki0.00080.00080.66735.4000AID45781
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)11.31670.00032.25459.6000AID1207667; AID1207668; AID1207669
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)10.69790.00401.966610.0000AID1873206; AID364887
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily A member 1Mus musculus (house mouse)EC50 (µMol)0.50000.40002.771410.0000AID482149
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (310)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
digestionChymotrypsinogen ABos taurus (cattle)
antibiotic catabolic processBeta-lactamaseEscherichia coli K-12
response to antibioticBeta-lactamaseEscherichia coli K-12
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
gluconeogenesisMalate dehydrogenase, cytoplasmicHomo sapiens (human)
NADH metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
NADP metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
malate metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
oxaloacetate metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
tricarboxylic acid cycleMalate dehydrogenase, cytoplasmicHomo sapiens (human)
malate-aspartate shuttleMalate dehydrogenase, cytoplasmicHomo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (133)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingChymotrypsinogen ABos taurus (cattle)
serpin family protein bindingChymotrypsinogen ABos taurus (cattle)
beta-lactamase activityBeta-lactamaseEscherichia coli K-12
hydrolase activityBeta-lactamaseEscherichia coli K-12
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
malic enzyme activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
protein bindingMalate dehydrogenase, cytoplasmicHomo sapiens (human)
L-malate dehydrogenase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
diiodophenylpyruvate reductase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
hydroxyphenylpyruvate reductase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (69)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionChymotrypsinogen ABos taurus (cattle)
serine protease inhibitor complexChymotrypsinogen ABos taurus (cattle)
outer membrane-bounded periplasmic spaceBeta-lactamaseEscherichia coli K-12
periplasmic spaceBeta-lactamaseEscherichia coli K-12
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
extracellular spaceMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytoplasmMalate dehydrogenase, cytoplasmicHomo sapiens (human)
centrosomeMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytosolMalate dehydrogenase, cytoplasmicHomo sapiens (human)
extracellular exosomeMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytosolMalate dehydrogenase, cytoplasmicHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (355)

Assay IDTitleYearJournalArticle
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID33788Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID34011Ability to displace radioligand from Na+ independent Adenosine transporter in rat1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID21849In vitro clearance in dog in 1000000 cells1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID21856In vivo clearance in human1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1409468Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1209972Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1409464Reduction in viability of human AsPC1 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID310121Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID10375Hill coefficient of the compound1986Journal 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.
AID59295Effective dose against atrioventricular conduction in dogs at which they prolong atrioventricular conduction time by 30%1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID364884Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID43250Percentage inhibition against beta-Lactamase in the absence of detergent Triton X-100 was determined at a concentration of 100 uM2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
A specific mechanism of nonspecific inhibition.
AID497655Inhibition of mouse prion protein (89-230) assessed as inhibition of amyloid polymerization at 50 uM by thioflavin T fluorescence assay relative to untreated control2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID1386563Binding affinity to recombinant P-gp cys-less mutant (unknown origin) in proteoliposomes assessed as increase in ATP hydrolysis rate after 40 mins by colorimetric assay
AID1220560Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID22993Compound was tested for the volume of distribution in dogs1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents.
AID324574Increase in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 8 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1473860Ratio of drug concentration at steady state in human at 60 to 120 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological 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.
AID181663Calcium antagonistic activity was evaluated by in vitro inhibition of [3H]nitrendipine binding on rat cerebral cortex1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID106801Inhibition of malate dehydrogenase (MDH)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID43125Inhibitory activity against Beta-lactamase from DMSO stock was determined2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
A specific mechanism of nonspecific inhibition.
AID21852In vitro clearance in rat in 1000000 cells1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID19468Partition coefficient (logP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID59297Effective dose that lowers vascular resistance by, 30% in dogs when administered intravenously1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID540231Dose normalised AUC in dog after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID239884pKa value of the compound2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID34564Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1210074Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID681335TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells2002European 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.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID537132Antileishmanial activity against promastigotes of Leishmania amazonensis WHO/BR/00/LT0016 after 18 hrs by MTT assay2010Bioorganic & 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.
AID28320Mean maximal plasma concentration2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1409465Reduction in viability of human PC3 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID348822Agonist-enhancing activity in epsilon-epitope tagged TRPV1 receptor expressed in mouse NIH3T3 cells assessed as capsaicin-induced 45Ca2+ influx by microplate liquid scintillation counter2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
AID21858In vivo clearance in rat1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID406410Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID21439Compound was tested for the plasma clearance in dogs1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID537131Antileishmanial activity against amastigotes of Leishmania chagasi MHOM/BR/1972/LD after 24 hrs by MTT assay2010Bioorganic & 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.
AID1210017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (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.
AID31706Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID324383Induction of light chain 3-GFP level in human H4 cells at 4.8 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID9879Time to peak response on lowering of vascular resistance, in dogs when administered intravenously1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID33497Inhibition of adenylyl cyclase by A3 agonist IB-MECA(10e-7M) in CHO cell membranes expressing rat Adenosine A3 receptor1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1211297Drug recovery in plasma (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID537135Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay2010Bioorganic & 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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID167265Electrophysiological effect in isolated rabbit hearts in atrio-His bundle (A-H) interval1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID237474Percentage of drug bound in bovine plasma albumin2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
AID1598718Binding affinity to Triton-X 100 assessed as change in chemical shift at 150 uM by 1H-NMR spectra analysis2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Mechanisms of Specific versus Nonspecific Interactions of Aggregation-Prone Inhibitors and Attenuators.
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1386583Binding affinity to recombinant P-gp cys-less mutant (unknown origin) in proteoliposomes assessed as increase in ATP hydrolysis rate at 10'-9 to 10'-4 M after 40 mins by colorimetric assay relative to basal control
AID54411Inhibition of human cytochrome P450 2C92004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors.
AID348824Agonist-enhancing activity at TRPV1 receptor in E15 rat primary dorsal root ganglion cells assessed as capsaicin-induced 45Ca2+ influx by microplate liquid scintillation counter2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
AID324487Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 4.8 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID57004Dose at which compound induce atrioventricular block in dogs; range is 100-30001989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID482149Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx2010Journal 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.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID537134Antileishmanial activity against promastigotes of Leishmania braziliensis MHO/BR/75/M2903 after 18 hrs by MTT assay2010Bioorganic & 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.
AID52778Fold decrease in IC50 vs chymotrypsinogen on pre-incubation2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1460602Growth inhibition of Staphylococcus aureus SA1199 up to 100 ug/ml by broth microdilution assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID324584Increase in long-lived protein degradation in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID232706Selectivity ratio of Ki for rat A3 and human A3 adenosine receptors1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID180311Inhibition of [3H]nitrendipine binding to L-type calcium channels of rat cerebral cortex1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID1873206Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells assessed as reversal of BCRP-mediated mitoxantrone resistance and measured after 90 mins by FACSflow cytometry analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID681119TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID237416Distribution coeeficient for the compound at pH7.4 (Log D7.4) 2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
AID1220556Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1460598Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux at 50 uM measured after 5 mins by fluorometric method relative to control2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID227765Dissociation constant to estimate the calcium binding to the compound at the ratio of 1:11994Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
Interaction of calcium channel antagonists with calcium: structural studies on nicardipine and its Ca2+ complex.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID33496Inhibition of adenylyl cyclase by A3 agonist IB-MECA(10e-6M) in CHO cell membranes expressing rat Adenosine A3 receptor1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID1460599Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux after 5 mins by fluorometric method2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID497649Inhibition of polyhistidine tagged yeast prion protein Sup35 expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid polymerization at 50 uM in presence of 5 mg/ml BSA by thioflavin T fluorescence assay relative to untreated control2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID36707Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1598719Binding affinity to Triton-X 100 assessed as line broadening at 150 uM by 1H-NMR spectra analysis2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Mechanisms of Specific versus Nonspecific Interactions of Aggregation-Prone Inhibitors and Attenuators.
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID43267Percentage inhibition of Beta-lactamase at KPi (Potassium Phosphate) stock concentration of 13.5 uM2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
A specific mechanism of nonspecific inhibition.
AID1443992Total Cmax in human administered as single dose2014Hepatology (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.
AID36706Alpha-1-adrenolytic activity was assessed from the ability to inhibit [3H]prazosin binding to rat cerebral cortex preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID537137Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for amastigotes of Leishmania chagasi MHOM/BR/1972/LD2010Bioorganic & 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.
AID150755Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID324539Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 4.8 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1611221Aqueous solubility of compound in phosphate buffered saline at pH 7.4 incubated for 2 hrs by turbidimetric analysis2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID150753Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID324594Increase in ratio of light chain 3 subunit 2 to light chain 3 subunit 1 in human H4 cells at 4.8 uM after 4 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1409471Cytotoxicity against human HET-1A cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID21853In vivo clearance in dog1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID324585Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID678836TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells2000Pharmaceutical research, Oct, Volume: 17, Issue:10
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.
AID1220559Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID324602Effect on mTOR phosphorylation in human H4 cells at 4.8 uM after 4 hrs2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1209974Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1211298Dissociation constant, pKa of the compound2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID681122TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1409463Reduction in viability of human Caco2 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1565030Kinetic aqueous solubility of the compound in pH 7.46 phosphate buffer at 100 uM incubated for 120 mins by LC-MS/MS analysis2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists.
AID36048Alpha-2-adrenolytic activity was assessed in vitro from the ability to inhibit norepinephrine binding to guinea pig vas deferens1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID227781Dissociation constant to estimate the calcium binding to the compound at the ratio of 2:11994Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
Interaction of calcium channel antagonists with calcium: structural studies on nicardipine and its Ca2+ complex.
AID1473859Drug concentration at steady state in human at 60 to 120 mg, po QD after 24 hrs2013Toxicological 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.
AID1409461Reduction in viability of human HET-1A cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1409473Cytotoxicity against human Caco2 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1220557Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID150752Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID165539Inhibition of contraction in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID21851In vitro clearance in human in 1000000 cells1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1210071Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID680718TP_TRANSPORTER: increase in Rhodamine 123 intracellular accumulation (R123: 150 uM, Nicardipine: 2 ug/mL) in MDR1-expressing NIH3T3 cells2000The Journal of pharmacology and experimental therapeutics, Dec, Volume: 295, Issue:3
Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation.
AID324435Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 4.8 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1460603Growth inhibition of Staphylococcus aureus SA1199B up to 100 ug/ml by broth microdilution assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1460601Growth inhibition of Staphylococcus aureus SAK2378 up to 100 ug/ml by broth microdilution assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID1409470Induction of apoptosis in human PC3 cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID310120Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1210072Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID497665Inhibition of yeast prion protein Sup35 infection of PSI yeast spheroplast cells at 100 uM2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID681131TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1207668Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID681581TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1210015Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1409472Cytotoxicity against human A549 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID537133Antileishmanial activity against promastigotes of Leishmania major MHOM/1L/80/Fredlin after 18 hrs by MTT assay2010Bioorganic & 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.
AID1220558Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID497826Inhibition of polyhistidine tagged yeast prion protein Sup35 expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid polymerization preincubation of seed fibers and compound for 5 mins at 100 uM by thioflavin T fluorescence assay relati2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID1207669Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1220555Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID112426Effect on acute thrombic death induced by collagen in mice1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID497644Inhibition of polyhistidine tagged yeast prion protein Sup35 expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid polymerization at 50 uM by thioflavin T fluorescence assay relative to untreated control2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID406411Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability at 0.125 to 12.5 uM relative to toxin-treated control2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
AID540232Dose normalised AUC in monkey after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID640615Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis2012Bioorganic & 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.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID150754Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1460608Inhibition of Staphylococcus aureus SAK2378 norA assessed as potentiation of CPX-induced antibacterial activity by measuring fold reduction in CPX MIC at 12.5 to 25 ug/ml by checkerboard assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1409475Cytotoxicity against human PC3 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID43431Compound was tested for the inhibition of beta-lactamase2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID537136Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay2010Bioorganic & 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.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID165537Inhibition of [Ca2+] uptake in rabbit aorta, K+.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
New developments in Ca2+ channel antagonists.
AID540233Dose normalised AUC in human after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID1409462Reduction in viability of human A549 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1210016Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID497825Inhibition of polyhistidine tagged yeast prion protein Sup35 expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid polymerization at 100 uM by thioflavin T fluorescence assay relative to untreated control2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID681579TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID681582TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID232704Selectivity ratio of Ki for rat A1 and A3 adenosine receptor1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID52776Compound was tested for the inhibition of Chymotrypsinogen2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID106799Fold increase in IC50 vs malate dehydrogenase (MDH) with 1 mg/ml saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID218694Fold increase in IC50 vs beta-lactamase with 10x increased enzyme2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID537138Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for trypomastigotes of Trypanosoma cruzi2010Bioorganic & 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.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID43563Fold decrease in IC50 vs beta-lactamase on pre-incubation2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1473858AUC in human at 60 to 120 mg, po QD after 24 hrs2013Toxicological 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.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID324573Increase in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID679897TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical)(Vinblastine: 0.004 uM, Nicardipine: 60 uM) in Caco-2 cells2000Pharmaceutical research, Dec, Volume: 17, Issue:12
Influence of passive permeability on apparent P-glycoprotein kinetics.
AID150756Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID159531Calcium antagonistic activity was evaluated from the inhibition of CaCl2-induced contraction of depolarized pig coronary artery1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID1220554Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1460604Synergistic antibacterial activity against Staphylococcus aureus SAK1902 in presence of CPX by checkerboard assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID537130Antileishmanial activity against promastigotes of Leishmania chagasi MHOM/BR/1972/LD after 18 hrs by MTT assay2010Bioorganic & 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.
AID681132TP_TRANSPORTER: ATP hydrolysis in MDR1-expressing Sf9 cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID9718Half-recovery time (T1/2) of the vascular resistance decrease at ED30 in anesthetized dogs1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
AID1473861Ratio of drug concentration at steady state in human at 60 to 120 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological 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.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID499784Activation of phospholipase A2/C in human OC2 cells assessed as increase in intracellular calcium level at 1 uM2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Effect of [6]-shogaol on cytosolic Ca2+ levels and proliferation in human oral cancer cells (OC2).
AID1443991Induction 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 assay2014Hepatology (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.
AID540230Dose normalised AUC in rat after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID681580TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1460609Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as potentiation of CPX-induced antibacterial activity by measuring fold reduction in CPX MIC at 6.25 to 12.5 ug/ml by checkerboard assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID33356Binding affinity against rat Adenosine A3 receptor from CHO cells1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID106803Fold decrease in IC50 vs malate dehydrogenase (MDH) on pre-incubation; no change2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1460600Growth inhibition of Staphylococcus aureus SA1902 up to 100 ug/ml by broth microdilution assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID681130TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID43124Inhibitory activity against Amp C beta-Lactamase2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
A specific mechanism of nonspecific inhibition.
AID497664Inhibition of yeast prion protein Sup35 infection of PSI yeast spheroplast cells at 200 uM2008Nature chemical biology, Mar, Volume: 4, Issue:3
Small-molecule aggregates inhibit amyloid polymerization.
AID1386581Inhibition of P-gp in human NCI/ADR-RES cells assessed as rate of calcein-AM accumulation at 1 uM by fluorescence assay
AID1261691Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.
AID364887Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID324583Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID717844Inhibition 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 control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2.
AID681128TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID218692Fold increase in IC50 vs beta-lactamaase with 0.1 mg/mL saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1209973Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID21475Compound was tested for the plasma half life in dogs1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents.
AID1409474Cytotoxicity against human AsPC1 cells after 6 hrs by fluorescence assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1598717Binding affinity to Triton-X 100 assessed as peak intensity loss at 150 uM by 1H-NMR spectra analysis2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Mechanisms of Specific versus Nonspecific Interactions of Aggregation-Prone Inhibitors and Attenuators.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID36777Alpha-2-adrenolytic activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID45781Inhibition of [3H]nitrendipine binding to L-type calcium channel from rat brain cortex homogenate1986Journal 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.
AID324572Increase in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1674184Toxicity in po dosed human assessed as maximum daily dose2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1674183Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID1460605Synergistic antibacterial activity against Staphylococcus aureus SA1199 in presence of CPX by checkerboard assay2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
AID324582Increase in long-lived protein degradation in human H4 cells after 1 hr relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID43260Percentage inhibition against beta-Lactamase in the presence of detergent 0.01% Triton X-100 was determined at a concentration of 100 uM2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
A specific mechanism of nonspecific inhibition.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1443989Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to 2014Hepatology (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.
AID1207667Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1210073Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID181662Calcium antagonistic activity determined by the inhibitory effect on high-potassium depolarization-induced contracture in isolated rat aorta.2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
Synthesis and structure--activity analysis of novel dihydropyridine derivatives to overcome multidrug resistance.
AID52773Fold increase in IC50 vs chymotrypsinogen with 0.2 mg/ml saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID681120TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID232705Selectivity ratio of Ki for rat A2A and A3 adenosine receptors1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
AID310122Inhibition of P-glycoprotein by Hoechst assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID54923Inhibition of human cytochrome P450 3A42003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1409466Induction of apoptosis in human HET-1A cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay2018Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
Pathway-Based Drug Repositioning for Cancers: Computational Prediction and Experimental Validation.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1449628Inhibition 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 method2012Drug 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.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1210070Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID416747Inhibition of Escherichia coli AmpC assessed as induction of protein unfolding measured by trypsin mediated degradation of compound-AmpC enzyme complex at 250 uM after 15 mins by gel electrophoresis2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Promiscuous aggregate-based inhibitors promote enzyme unfolding.
AID537139Cytotoxicity in BALB/c mouse erythrocytes assessed as hemolysis at 50 uM after 3 hrs2010Bioorganic & 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.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID150751Inhibition of P-glycoprotein using ATPase in MDR1 membranes2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346663Rat Kv1.4 (Voltage-gated potassium channels)2003British journal of pharmacology, Jun, Volume: 139, Issue:3
Dihydropyridine Ca2+ channel antagonists and agonists block Kv4.2, Kv4.3 and Kv1.4 K+ channels expressed in HEK293 cells.
AID1345822Human A3 receptor (Adenosine receptors)1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,473)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990648 (26.20)18.7374
1990's1014 (41.00)18.2507
2000's460 (18.60)29.6817
2010's277 (11.20)24.3611
2020's74 (2.99)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 84.35

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

MetricThis Compound (vs All)
Research Demand Index84.35 (24.57)
Research Supply Index8.04 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index154.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (84.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials444 (16.78%)5.53%
Reviews123 (4.65%)6.00%
Case Studies148 (5.59%)4.05%
Observational10 (0.38%)0.25%
Other1,921 (72.60%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (40)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase IIb: Randomised, Single-Blind, Safety, Tolerability, Efficacy and Pharmacokinetic Study of NicaPlant® in Aneurysmal Subarachnoid Haemorrhage Patients Undergoing Aneurysm Clipping [NCT04269408]Phase 241 participants (Actual)Interventional2020-04-05Completed
A Randomized Comparison of Post-procedural/Pre-hemostasis Intraarterial Nitroglycerin Versus Nicardipine to Reduce Radial Artery Occlusion After Transradial Catheterization [NCT03622060]Phase 3600 participants (Actual)Interventional2018-06-04Completed
Nanjing First Hospital, Nanjing Medical University [NCT01171911]Phase 4200 participants (Anticipated)Interventional2010-10-31Not yet recruiting
Comparison of the Effects of Nicardipine and Remifentanil on Surgical Visual Field and Hemodynamic Parameters in Tympanomastoidectomy Cases [NCT06130527]64 participants (Anticipated)Interventional2023-11-30Not yet recruiting
Usefulness of Pupillary Reflex on Remifentanil and Morphine Consumption During Laparoscopic Surgery. A Bicentric, Prospective, Randomized, Controlled Trial. [NCT02116868]100 participants (Actual)Interventional2014-03-31Completed
[NCT01175746]46 participants (Actual)Interventional2010-08-31Completed
Outcome in Patients Treated With Intraarterial Thrombectomy - optiMAL Blood Pressure Control (OPTIMAL-BP) [NCT04205305]Phase 4306 participants (Actual)Interventional2020-06-18Active, not recruiting
A Study of the Pharmacokinetic and Pharmacodynamic Responses in Healthy and Altered Human Cardiovascular Systems [NCT03098680]Phase 118 participants (Actual)Interventional2017-04-24Terminated(stopped due to Unable to recruit in time before end of PhD studentship)
The Intra-arterial Vasospasm Trial(iVAST)- A Multi-center Randomized Study [NCT01996436]Phase 4330 participants (Anticipated)Interventional2016-08-29Recruiting
The Treatment of Hypertension Associated With Severe Preeclampsia. A Randomize Controlled Trial of Urapidil Versus Nicardipine. The Uranic Trial [NCT02558023]Phase 314 participants (Actual)Interventional2015-09-30Terminated(stopped due to no candidats)
Nicardipine to Avoid Spasm in Trans Radial Percutaneous Coronary Intervention [NCT04538534]Phase 31,500 participants (Actual)Interventional2020-11-01Completed
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Does Dilution of Verapamil With Normal Saline or Blood Reduce Discomfort Felt During Intraarterial Administration? [NCT05625503]Early Phase 1100 participants (Anticipated)Interventional2022-12-13Recruiting
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404]5,000 participants (Anticipated)Observational2020-03-05Recruiting
A Safety and Efficacy Study of Blood Pressure Control in Acute Heart Failure - A Pilot Study (PRONTO) [NCT00803634]Phase 3117 participants (Actual)Interventional2008-12-31Completed
A Multi-center, Randomized and Controlled Phase IV Study on the Efficacy and Safety of Two Dose Adjustment Regimens of Nicardipine Injection for Hypertensive Emergency [NCT01872039]Phase 4163 participants (Actual)Interventional2013-03-31Completed
Antihypertensive Treatment in Acute Cerebral Hemorrhage (ATACH) [NCT00415610]Phase 160 participants (Actual)Interventional2005-07-31Completed
[NCT01041066]70 participants (Anticipated)Interventional2009-09-30Recruiting
Blood Pressure After Endovascular Stroke Therapy-II: A Randomized Trial [NCT04116112]Phase 2120 participants (Actual)Interventional2020-01-17Completed
Antihypertensive Treatment of Acute Cerebral Hemorrhage (ATACH)-II: A Phase III Randomized Multicenter Clinical Trial of Blood Pressure Reduction for Hypertension in Acute Intracerebral Hemorrhage [NCT01176565]Phase 31,000 participants (Actual)Interventional2011-05-15Terminated(stopped due to Planned interim analysis: no significant outcome differences between groups)
Effect of Nicardipine on Renal Function in Deliberate Hypotension [NCT02271191]Phase 464 participants (Actual)Interventional2012-05-31Completed
An International Randomised Controlled Trial to Establish the Effects of Low-dose rtPA and the Effects of Early Intensive Blood Pressure Lowering in Patients With Acute Ischaemic Stroke [NCT01422616]Phase 34,587 participants (Actual)Interventional2012-03-31Completed
Evaluation of Clevidipine in the Postoperative Treatment of Hypertension Assessing Safety Events (With Nicardipine as Active Comparator) (ECLIPSE-NIC) [NCT00093925]Phase 3739 participants (Actual)Interventional2004-05-31Completed
Treatment of Severe Hypertension During Pre-Eclampsia.A Preliminary Equivalence Study Between URAPIDIL and NICARDIPINE [NCT00409253]Phase 372 participants (Anticipated)Interventional2007-06-30Recruiting
A Randomized, Double-blinded, Placebo-controlled, Dose-ranging Study of Cardene® I.V. in Pediatric Subjects With Hypertension [NCT00528827]Phase 20 participants (Actual)Interventional2007-09-30Withdrawn(stopped due to Due to the sale of Cardene IV, the sponsor has stopped enrollment and withdrawn the study. No safety issues were identified.)
[NCT00490464]163 participants (Actual)Observational2004-06-30Completed
A Phase IV, Randomized Trial to Determine the Efficacy and Safety of Cardene Intravenous (I.V.) Versus Labetalol for Management of Hypertensive Emergencies in the Emergency Department Setting [NCT00765648]Phase 4226 participants (Actual)Interventional2008-10-31Completed
A Randomised Trial to Establish the Effects of Early Intensive Blood Pressure Lowering on Death and Disability in Patients With Stroke Due to Acute Intracerebral Haemorrhage [NCT00226096]404 participants (Actual)Interventional2005-11-30Completed
Nicardipine Versus Esmolol for Management of Emergence Hypertension After Craniotomy [NCT01951950]Phase 140 participants (Actual)Interventional2013-09-30Completed
[NCT01634594]Phase 466 participants (Actual)Interventional2012-06-30Completed
NICardipine Neuroprotection in AortiC Surgery (NICNACS) [NCT00508118]Phase 27 participants (Actual)Interventional2008-01-31Terminated(stopped due to 3/7 subjects experienced hypotension. Study was terminated.)
A Comparison of Dexmedetomidine, Nicardipine, and Labetalol to Induce Hypotensive Anesthesia and Their Effects on Blood Loss, Surgeon Visibility, Hemodynamic Parameters, and Operation Time During Orthognathic Surgery [NCT06093893]Phase 490 participants (Anticipated)Interventional2024-03-31Not yet recruiting
Intraventricular Nicardipine for the Treatment of Cerebral Vasospasm: Prospective Pilot Study [NCT01810302]Phase 22 participants (Actual)Interventional2013-08-31Terminated(stopped due to Unable to secure drug.)
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial [NCT04330300]Phase 42,414 participants (Anticipated)Interventional2020-04-30Suspended(stopped due to Challenges with funding and very low incidence of COVID-19 at Irish study site)
Relationship Between Perioperative Carotid Blood Flow Monitoring and Cerebral Function Protection in Cardiac Surgery [NCT05586347]64 participants (Actual)Interventional2022-04-22Completed
An Open-Label Prospective Study to Evaluate the Safety and Efficacy of Double or Triple Concentrated Intravenous Nicardipine for Treatment of Hypertension in Patients With Ischemic Stroke, Intracerebral Hemorrhage or Subarachnoid Hemorrhage [NCT00325793]Phase 450 participants Interventional2004-01-31Recruiting
Effects of Subcutaneously Infiltrated Nicardipine on the Success Rate of Radial Artety Cannulation [NCT05920538]190 participants (Anticipated)Interventional2023-03-13Enrolling by invitation
An International Randomised Controlled Trial to Establish the Effects of Early Intensive Blood Pressure Lowering in Patients With Intracerebral Haemorrhage. [NCT00716079]2,839 participants (Actual)Interventional2008-09-30Completed
Effects of Different Kinds of Antihypertensive Drugs on Dynamic Hemodynamic Changing of During Laparoscopic Gastrectomy and Laparotomy [NCT03497351]59 participants (Actual)Interventional2018-04-15Completed
Prevention of Coronary Microvascular Dysfunction Post-PCI by Intracoronary Nicardipine [NCT03184155]Early Phase 150 participants (Anticipated)Interventional2025-12-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00415610 (4) [back to overview]"Number of Participants With Neurological Deteriorations (Decrease of 2 or More Points on the GCS Score or an Increase of 4 or More Points on the NIHSS Score) During the 24 Hour Treatment,"
NCT00415610 (4) [back to overview]Total Number of Serious Adverse Events Within the Initial 72 Hours From Treatment Per Subject
NCT00415610 (4) [back to overview]Particpants Who Achieve and Maintain the Systolic Blood Pressure Goals for Each Treatment Tier.
NCT00415610 (4) [back to overview]Particpants Who Tolerate Rapid Systolic Blood Pressure Reduction and Maintain Treatment Goals
NCT00508118 (1) [back to overview]Duration From Initiation of Cardiopulmonary Bypass (CPB) to Electrocerebral Silence (ECS), Defined as no Discernable Electroencephalographic Activity at an Amplification of 2 Micro Volts (μV)/mm, Confirmed for 3 Minutes
NCT00716079 (2) [back to overview]Death at 90 Days
NCT00716079 (2) [back to overview]A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)
NCT00765648 (6) [back to overview]Percentage of Subjects Achieving a Pre-defined Target Systolic Blood Pressure (BP) Within 30 Minutes.
NCT00765648 (6) [back to overview]Emergency Department(ED)Time to Disposition Decision
NCT00765648 (6) [back to overview]Average Number of Dose Titrations Within 30 Minutes
NCT00765648 (6) [back to overview]Subjects Requiring the Use of Intravenous Rescue Medications
NCT00765648 (6) [back to overview]Transition Time to Oral Medication
NCT00765648 (6) [back to overview]Treatment Failure
NCT00803634 (11) [back to overview]Percentage to First Achieve Initial Prespecified SBP Target Range [≥20 mm Hg and ≤40 mm Hg Apart] and 15% Reduction From Baseline Within First 30 Minutes
NCT00803634 (11) [back to overview]SBP Area Under the Curve (AUC) Outside Prespecified Target Range
NCT00803634 (11) [back to overview]Time to First Achieve Initial Prespecified SBP Target Range and 15% Reduction From Baseline Within First 30 Minutes
NCT00803634 (11) [back to overview]Time to Use Other IV Antihypertensives During the Study Drug Administration
NCT00803634 (11) [back to overview]Change From Baseline in Dyspnea (Measured By VAS) at Each Time Point
NCT00803634 (11) [back to overview]Number of Patients That Require Intubation During Study Drug Administration up to 96 Hours
NCT00803634 (11) [back to overview]Percentage Falling Below Lower Limit of SBP Target Range at Any Time During Study
NCT00803634 (11) [back to overview]Percentage Falling Below Lower Limit of SBP Target Range Within First 30 Minutes
NCT00803634 (11) [back to overview]Percentage of Patients Who Received Any Alternative IV Antihypertensive Drug at Any Time During Study Drug Treatment
NCT00803634 (11) [back to overview]Percentage of Patients With at Least One Episode of SBP < 90 mm Hg During Study Drug Administration (up to 96 Hours)
NCT00803634 (11) [back to overview]Percentage Reaching Prespecified Target Range Without Falling Below Lower Limit of Target Range Within First 30 Minutes
NCT01176565 (7) [back to overview]Treatment-related Serious Adverse Event Within 72 Hours of Randomization
NCT01176565 (7) [back to overview]Death or Disability According to Modified Rankin Scale Score at 90 Days (3 Months) From Randomization
NCT01176565 (7) [back to overview]Quality of Life at 90 Days Using EuroQol (EQ) Measures: EQ-5D (EuroQol Five Dimension), Consisting of Standardized EQ-5D-3L (EuroQol Five Dimension, Three-Level) Questionnaire and EQ VAS (EuroQol Visual Analog Scale) Scores
NCT01176565 (7) [back to overview]Any Serious Adverse Event Within the 90-day Study Period
NCT01176565 (7) [back to overview]Hematoma Expansion (Number of Patients With Hematoma Expansion of 33% or Greater Between the Baseline and 24 +/- 6 Hours Head CTs, as Measured by the Central Reader for Patients With Readable Scans for Both Time Points Submitted by Data Lock.)
NCT01176565 (7) [back to overview]Hypotension Within 72 Hours
NCT01176565 (7) [back to overview]Neurological Deterioration Within 24 Hours, Defined by a Decrease of 2 or More Points on the GCS Score or an Increase of 4 or More Points on the NIHSS Score From Baseline, Not Related to Sedation or Hypnotic-agent Use and Sustained for at Least 8 Hours.
NCT01951950 (1) [back to overview]Failure of Drug to Control Systolic Blood Pressure (SBP) < 140 mmHg
NCT04116112 (5) [back to overview]Number of Participants With Neurological Worsening Associated With Antihypertensive Treatment
NCT04116112 (5) [back to overview]Number of Participants With Any Hemorrhagic Transformation
NCT04116112 (5) [back to overview]Final Infarct Volume
NCT04116112 (5) [back to overview]Utility-weighted Modified Rankin Score
NCT04116112 (5) [back to overview]Number of Participants With Symptomatic Hemorrhagic Transformation

"Number of Participants With Neurological Deteriorations (Decrease of 2 or More Points on the GCS Score or an Increase of 4 or More Points on the NIHSS Score) During the 24 Hour Treatment,"

Neurological status was monitored quantitatively and independently of other adverse events using two scales. The Glasgow Coma Scale (GCS) score measures level of consciousness in eye, motor, and verbal components. At least one point is given in each category. The scale ranges from 3 to 15, with 3 indicating deep unconsciousness and 15 indicating consciousness is not impaired. The National Institutes of Health Stroke Scale (NIHSS) quantifies neurologic deficits in 11 categories. Level of consciousness, horizontal eye movements, visual fields, facial palsy, movement in each limb, sensation, language and speech, and extinction or inattention on one side of the body are tested. Scores range from 0 to 42; 0 indicates normal function and higher scores indicate greater deficit severity. (NCT00415610)
Timeframe: within the first 72 hours of treatment initiation

Interventionparticipants (Number)
Tier 11
Tier 22
Tier 34

[back to top]

Total Number of Serious Adverse Events Within the Initial 72 Hours From Treatment Per Subject

Serious adverse events were ascertained by site investigators using FDA-defined guidelines, defined as any untoward clinical events having been fatal, life-threatening, resulting in new or prolonged hospitalization, resulting in disability or congenital anomaly, or requiring intervention to prevent permanent impairment or damage. Subjects were followed closely from randomization through 90 days. The initial 72-hour period was chosen as the most meaningful time period for which to examine SAEs likely to be related to the acute safety of the study treatment. (NCT00415610)
Timeframe: from treatment initiation through 72 hours

InterventionParticipants (Count of Participants)
Tier 10
Tier 21
Tier 33

[back to top]

Particpants Who Achieve and Maintain the Systolic Blood Pressure Goals for Each Treatment Tier.

Feasibility of treatment was assessed by whether SBP reduction and maintenance within the respective target range was achieved (treatment success) or not (treatment failure), and secondarily by whether a significant difference between treatment arms was achieved. Treatment failure was defined based on the observed hourly hourly minimum SBP remaining greater than the upper limit of the target range for 2 consecutive hours after initiation of nicardipine infusion. Spontaneous decline of SBP below the lower limit of the specific tier was not considered treatment failure as all such declines were asymptomatic.The lower number in the more intensive treatment groups reflects in part the greater challenge of rapidly lowering systolic blood pressure to a more intensive (lower) range, as a higher number of treatment failures as pre-defined by meeting the SBP range goal within 3 hours of symptom onset in this group predictably occurred. (NCT00415610)
Timeframe: Within 3 hours of symptom onset and sustained through 18-24 hours.

,,
Interventionparticipants (Number)
Meeting Criteria of initial SBP > 170 mmHgNumber treated within 3 hours of symptom onsetTreatment Failure, SBP not in range by 2 hours
Tier 11870
Tier 22050
Tier 32269

[back to top]

Particpants Who Tolerate Rapid Systolic Blood Pressure Reduction and Maintain Treatment Goals

The ability to maintain the Specified Systolic Blood Pressure Range for the 18-24 Hour Period without Neurological Deterioration or Side Effects (NCT00415610)
Timeframe: 3 months

,,
Interventionparticipants (Number)
N with SAE within 72 hoursN with neurologic deterioration within 24 hoursN with symptomatic hematoma expansionN with asymptomatic hematoma expansionN with in-hospital mortalityN with 3-month mortalityN with 1-month favorable outcome, mRS 0-2N missing for 1-month outcome assessmentN with 3-month favorable outcome, mRS 0-2N missing for 3-month outcome assessment
Tier 10106234383
Tier 21212126394
Tier 33443154272

[back to top]

Duration From Initiation of Cardiopulmonary Bypass (CPB) to Electrocerebral Silence (ECS), Defined as no Discernable Electroencephalographic Activity at an Amplification of 2 Micro Volts (μV)/mm, Confirmed for 3 Minutes

(NCT00508118)
Timeframe: Day of surgery

InterventionTime (minutes) (Median)
NICARDIPINE GROUP45

[back to top]

Death at 90 Days

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering166
Guideline-Recommended Blood-Pressure Lowering170

[back to top]

A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering719
Guideline-Recommended Blood-Pressure Lowering785

[back to top]

Percentage of Subjects Achieving a Pre-defined Target Systolic Blood Pressure (BP) Within 30 Minutes.

Percentage of subjects achieving a pre-defined target systolic blood pressure (BP) range defined as a systolic blood pressure that is within +/- 20 mmHg of the target as established by the investigator. (NCT00765648)
Timeframe: 30 minutes after initiation of therapy

Interventionpercentage of participants (Number)
Nicardipine91.7
Labetalol82.5

[back to top]

Emergency Department(ED)Time to Disposition Decision

Median number of hours from hospital admission until Emergency Department(ED)disposition (NCT00765648)
Timeframe: 6 hours

Interventionhours (Median)
Nicardipine4.6
Labetalol4.6

[back to top]

Average Number of Dose Titrations Within 30 Minutes

Calculated as the mean (± standard deviation) number of titrations over 30 minutes for each treatment group (NCT00765648)
Timeframe: 30 minutes

Interventionnumber of titrations (Mean)
Nicardipine2.2
Labetalol1.3

[back to top]

Subjects Requiring the Use of Intravenous Rescue Medications

The percent of subjects requiring the use of intravenous rescue medications (NCT00765648)
Timeframe: 6 hours

Interventionpercentage of participants (Number)
Nicardipine15.5
Labetalol22.4

[back to top]

Transition Time to Oral Medication

The median transition time (in hours) to oral medication (NCT00765648)
Timeframe: 6 hours

Interventionhours (Median)
Nicardipine4.9
Labetalol6.4

[back to top]

Treatment Failure

Treatment failure is defined as admission to the hospital or observation unit for BP management (NCT00765648)
Timeframe: 6 hours

Interventionpercentage of participants (Number)
Nicardipine43.1
Labetalol37.4

[back to top]

Percentage to First Achieve Initial Prespecified SBP Target Range [≥20 mm Hg and ≤40 mm Hg Apart] and 15% Reduction From Baseline Within First 30 Minutes

Analysis of the percentage of patients achieving both components of this composite endpoint (attainment of the initial prespecified SBP target range and a 15% reduction in SBP from baseline) was calculated within each treatment group using the number of mITT patients achieving the SBP reduction goal divided by the number of mITT patients, and multiplied by 100. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

InterventionPercentage of patients (Number)
Clevidipine70.5
Standard of Care36.6

[back to top]

SBP Area Under the Curve (AUC) Outside Prespecified Target Range

The magnitude and duration of SBP excursions was calculated as the area under the curve (AUC) for each patient, using the trapezoidal rule, related to time (in minutes) that each patient's SBP was outside the target range. AUC was determined based on data collected from the initiation of study medication through the end of monotherapy treatment up to 96 hours, normalized per hour, and expressed as mmHg × minute/hour. (NCT00803634)
Timeframe: Initiation of study drug through end of monotherapy (up to 96 hours)

Interventionmm Hg x min/h (Mean)
Clevidipine494.96
Standard of Care966.15

[back to top]

Time to First Achieve Initial Prespecified SBP Target Range and 15% Reduction From Baseline Within First 30 Minutes

Time to first achieve the initial pre-specified systolic blood pressure (SBP) target range and a 15% SBP reduction from baseline is the time in minutes between the initiation of study medication and the time the patient first achieved both components. Median time was estimated using Kaplan Meier method. 95% two-sided confidence interval of the median time is from 'Simon and Lee, 1982'. If patients did not reach both components within 30 minutes from the initial treatment with study medication, or another antihypertensive agent was administered, the patient was censored at 30 minutes or the time when another antihypertensive agent is given, whichever came first. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

InterventionMinutes (Median)
Clevidipine15.0
Standard of CareNA

[back to top]

Time to Use Other IV Antihypertensives During the Study Drug Administration

The length of time to use other IV antihypertensive agents was defined as the duration in hours from the initiation of study drug through the time when any other concomitant IV antihypertensive agent was administered, thus, representing the time period without use of any other concomitant IV antihypertensive agent. Median time to use other IV antihypertensive agents was obtained using Kaplan-Meier method. If a patient did not receive any concomitant IV antihypertensive during the 96-hour treatment period, this patient was considered censored at 96 hours. If study drug was stopped less than 96 hours and the patient has no concomitant IV antihypertensive agent, the patient was considered censored when study drug was stopped. (NCT00803634)
Timeframe: Initiation of study drug through any other concomitant IV antihypertensive agent administered, up to 96 hours

InterventionHours (Median)
ClevidipineNA
Standard of Care5.7

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Change From Baseline in Dyspnea (Measured By VAS) at Each Time Point

A validated visual analog scale (VAS) with a horizontal ruler showing increments from 0 to 100 mm with 0 = Best and 100 = Worst was used. The test was asked from the patient's perspective and had to be administered with patient sitting. Relative change in VAS from baseline is the value at each time point minus the baseline value. Relative change from baseline was summarized descriptively (with associated two-tailed 95% CIs of the mean values) at 15, 30 and 45 minutes and at 1, 2, 3 hours and 12 hours, and 1 hour post termination of study drug treatment. (NCT00803634)
Timeframe: Baseline (immediately prior to study drug administration) through 1 hour after study drug termination

,
Interventionmillimeters (mm) (Mean)
Baseline Through Initial 15 Min- CLV n=44;SOC n=38Baseline Through Initial 30 Min- CLV n=43;SOC n=39Baseline Through Initial 45 Min- CLV n=43;SOC n=39Baseline Through Initial 1 H- CLV n=41;SOC n=38Baseline Through Initial 2 H- CLV n=29;SOC n=29Baseline Through Initial 3 H- CLV n=14;SOC n=22Baseline Through Initial 12 H- CLV n=0;SOC n=7Baseline Through 1 H Post Drug- CLV n=41;SOC n=33
Clevidipine-18.6-28.8-37.1-43.6-45.2-47.9NA-50.1
Standard of Care-16.1-22.8-27.9-34.6-35.3-40.5-57.9-50.1

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Number of Patients That Require Intubation During Study Drug Administration up to 96 Hours

The number of patients requiring intubation was calculated based on the total number of mITT patients. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

InterventionPatients (Number)
Clevidipine0
Standard of Care0

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Percentage Falling Below Lower Limit of SBP Target Range at Any Time During Study

The percentage of patients in whom the SBP fell below the lower limit of the prespecified target range at any time during the entire study drug treatment period (up to 96 hours) was calculated within each treatment group using the number of mITT patients achieving the endpoint divided by the number of mITT patients and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

InterventionPercentage of patients (Number)
Clevidipine68.2
Standard of Care70.7

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Percentage Falling Below Lower Limit of SBP Target Range Within First 30 Minutes

The percentage of patients in whom the SBP fell below the lower limit of the prespecified target range at any time during the first 30 minutes was calculated within each treatment group using the number of mITT patients achieving the endpoint divided by the number of mITT patients and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

InterventionPercentage of patients (Number)
Clevidipine34.1
Standard of Care2.4

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Percentage of Patients Who Received Any Alternative IV Antihypertensive Drug at Any Time During Study Drug Treatment

The percentage of patients who received any alternative IV antihypertensive drug at any time during the study drug treatment period (up to 96 hours) was calculated using mITT patients within each treatment group. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

InterventionPercentage of patients (Number)
Clevidipine15.9
Standard of Care51.2

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Percentage of Patients With at Least One Episode of SBP < 90 mm Hg During Study Drug Administration (up to 96 Hours)

The percent of patients with at least one episode of SBP <90 mm Hg was calculated as the number of mITT patients who had at least one episode of SBP<90 mm Hg during study drug administration up to 96 hours divided by mITT patients, and multiplied by 100 for each treatment group. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

InterventionPercentage of patients (Number)
Clevidipine5.9
Standard of Care1.9

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Percentage Reaching Prespecified Target Range Without Falling Below Lower Limit of Target Range Within First 30 Minutes

The percentage of patients reaching this endpoint was calculated within each treatment group using the number of mITT patients reaching the endpoint divided by the number of mITT patients, and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

InterventionPercentage of patients (Number)
Clevidipine45.5
SOC IV Therapy51.2

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Death or Disability According to Modified Rankin Scale Score at 90 Days (3 Months) From Randomization

The primary outcome was death or disability, defined by modified Rankin scale (mRS) of 4-6 at 90 days following treatment. The modified Rankin Scale score ranges from 0, indicating no symptoms, to 6, indicating death. A score of 4 indicates moderately severe disability including the inability to walk or attend to one's own bodily needs. A score of 5 indicates severe disability; bedridden, incontinent, and requiring constant nursing care. To score a 3 or lower on the mRS, a person must at least be able to walk without the assistance of another person. We chose the mRS because of its high inter-observer reliability, superiority to other indices, and consistency with previous trials in patients with ICH. Reliability was further increased by use of a structured interview template and by requiring mRS assessors to pass a certification test. Persons conducting the 90-day mRS assessment were to be unaware of the treatment arm or clinical course of the patients they assessed. (NCT01176565)
Timeframe: 90 days (± 14 days per protocol window; up to ± 30 days data is used) from randomization

,
InterventionParticipants (Count of Participants)
Death or disability at 90 days (mRS = 4 - 6)Known death at or before 90 days
Intensive SBP Reduction Arm18633
Standard SBP Reduction Arm18134

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Quality of Life at 90 Days Using EuroQol (EQ) Measures: EQ-5D (EuroQol Five Dimension), Consisting of Standardized EQ-5D-3L (EuroQol Five Dimension, Three-Level) Questionnaire and EQ VAS (EuroQol Visual Analog Scale) Scores

Standardized scales developed by the EuroQol Research Foundation were used as a secondary outcome measure in addition to the mRS scale score. The EQ-5D is a simple, standardized non-disease-specific instrument for describing and valuating health-related quality of life. The EQ-5D-3L questionnaire consists of 5 questions in 5 different domains and allows for responses from 1 (the best outcome) to 3 (the worst outcome) in each of five categories (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression). Total scores range from 5 to 15, with lower scores indicating better quality of life and a higher score indicating a worse quality of life. A second component of EuroQol outcome measurements is a printed 20 cm visual analogue scale (EQ VAS) that appears somewhat like a thermometer, on which a score from 0 (worst imaginable health state or death) to 100 (best imaginable health state) is marked by the patient (or, when necessary, their proxy) with the scale in view. (NCT01176565)
Timeframe: 90 days (± 14 days per protocol window; up to ± 30 days data is used) from randomization

,
Interventionunits on a scale (Median)
EQ-5D utility scale questionnaireEQ VAS (visual analog scale)
Intensive SBP Reduction Arm0.762.5
Standard SBP Reduction Arm0.770

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Any Serious Adverse Event Within the 90-day Study Period

The complete count of all subjects who experienced any serious adverse events throughout their participation in the trial was included in this tabulation. Adverse events (AEs) and serious adverse events (SAEs) were assessed by the site investigators for all patients. Potential relatedness to the study treatment was a required reporting element for all adverse events but was not considered in this count. Terminology from the Medical Dictionary for Regulatory Activities (MedDRA) and severity criteria from the Common Terminology Criteria for Adverse Events (CTCAE v. 4.03) were used as a basis for reporting adverse events. Serious adverse events are defined as being fatal, life-threatening, resulting in hospitalization or prolonged hospitalization, resulting in disability or congenital anomaly, or requiring intervention to prevent permanent impairment or damage and were required to be reported promptly. An Independent Oversight Committee (IOC) reviewed and adjudicated adverse event data. (NCT01176565)
Timeframe: From randomization through the 90 day visit (90 ± 14 days per protocol window; up to ± 30 days data is used) or until known death, withdrawal, or loss to follow-up.

InterventionParticipants (Count of Participants)
Standard SBP Reduction Arm100
Intensive SBP Reduction Arm128

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Hematoma Expansion (Number of Patients With Hematoma Expansion of 33% or Greater Between the Baseline and 24 +/- 6 Hours Head CTs, as Measured by the Central Reader for Patients With Readable Scans for Both Time Points Submitted by Data Lock.)

Hematoma expansion as determined by serial CT scans: Hematoma expansion was defined as an increase in the volume of intraparenchymal hemorrhage of 33% or greater as measured by a central imaging analyst who was was unaware of the treatment assignments, clinical findings, and time points of image acquisition. The area of the hematoma was delineated by image analysis software with the use of density thresholds on each slice, followed by manual correction. To ensure accuracy and consistency of the readings, images were coded randomly and independently of subject numbers and manual correction was also done without awareness of treatment assignments, clinical findings, or time points of image acquisition. This data point is defined as being present (hematoma expansion of 33% or more was calculated between the baseline scan hematoma volume and the 24 +/- 6 hours hematoma volume measures at data analysis), meaning that hematoma expansion as defined must have occurred or it was not counted. (NCT01176565)
Timeframe: From the baseline head CT to the 24 +/- 6 hours from randomization head CT

InterventionParticipants (Count of Participants)
Standard SBP Reduction Arm104
Intensive SBP Reduction Arm85

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Hypotension Within 72 Hours

Hypotension (abnormally low blood pressure) was the most likely adverse event that could be associated with the study treatment, and is the primary basis (risk) on which neurological deterioration or other untoward effects of the study treatment could occur. It is therefore examined as a numerically-measured occurrence in addition to monitoring patients closely for neurological deterioration or other symptoms. Hypotension, when named as an adverse event, was defined as the syndrome of low blood pressure with SBP < 85 mmHg. Instances of hypotension were to be avoided through close monitoring, and administration of fluid bolus for SBP < 110 mmHg. If hypotension did occur, it was to be reversed as quickly as possible through discontinuation of intravenous nicardipine and intravenous fluid administration, which can be accomplished readily in a variety of settings where patients with intracerebral hemorrhage are routinely housed during early hospitalization. (NCT01176565)
Timeframe: From randomization through 72 hours from randomization

InterventionParticipants (Count of Participants)
Standard SBP Reduction Arm3
Intensive SBP Reduction Arm6

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Failure of Drug to Control Systolic Blood Pressure (SBP) < 140 mmHg

(NCT01951950)
Timeframe: 1 hour postoperatively

Interventionparticipants (Number)
Nicardipine1
Esmolol11

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Number of Participants With Neurological Worsening Associated With Antihypertensive Treatment

Defined as number of participants with 4 points of greater increase in NIH Stroke scale associated with reduction in SBP caused by anti-hypertensive treatment initiation or titration. (NCT04116112)
Timeframe: Treatment initiation to 24 hrs after treatment initiation

InterventionParticipants (Count of Participants)
Higher Systolic Blood Pressure (SBP) Target0
Lower SBP (<160 mmHg) Target0
Lower SBP (<140mmHg) Target0

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Number of Participants With Any Hemorrhagic Transformation

Number of participants with any new bleeding within the infarcted brain tissue on 36(+/-12) hr MRI/CT scan after treatment initiation (NCT04116112)
Timeframe: 36(+/-12) hrs after treatment initiation

InterventionParticipants (Count of Participants)
Higher Systolic Blood Pressure (SBP) Target12
Lower SBP (<160 mmHg) Target12
Lower SBP (<140mmHg) Target14

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Final Infarct Volume

Infarct volume on diffusion-weighted MRI (or CT if MRI cannot be obtained) at 36 (+/-12) hrs after treatment initiation, adjusted for the baseline CT perfusion core infract volume. (NCT04116112)
Timeframe: 36 (+/-12) hrs after treatment initiation

InterventionCubic Centimeters (Mean)
Higher Systolic Blood Pressure (SBP) Target46.4
Lower SBP (<160 mmHg) Target50.7
Lower SBP (<140mmHg) Target32.4

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Utility-weighted Modified Rankin Score

"Modified Rankin score (mRS) is a scale for measuring the degree of disability or dependence of people who have suffered a stroke. 0 - no symptoms at all; 1 - no significant disability despite symptoms; able to carry out all usual duties and activities; 2- slight disability; unable to carry out all previous activities, but able to look after own affairs without assistance; 3- moderate disability; requiring some help, but able to walk without assistance; 4 - moderately severe disability; unable to walk without assistance and unable to attend to own bodily needs without assistance; 5 - severe disability; bedridden, incontinent and requiring constant nursing care and attention; 6- dead.~Patient centered utility weights are applied to these scores as 1.0 for mRS level 0; 0.91 for mRS level 1; 0.76 for mRS level 2; 0.65 for mRS level 3; 0.33 for mRS level 4; 0 for mRS level 5; and 0 for mRS level 6. Unlike the mRS, the utility-weighted mRS runs from 0 to 1, with 0 being the worst." (NCT04116112)
Timeframe: 90 days after treatment initiation

Interventionunits on a scale (Range 0-1; 1=best) (Mean)
Higher Systolic Blood Pressure (SBP) Target0.58
Lower SBP (<160 mmHg) Target0.47
Lower SBP (<140mmHg) Target0.51

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Number of Participants With Symptomatic Hemorrhagic Transformation

Defined as number of participants with any new bleeding within the infarcted brain tissue and an NIH Stroke Scale worsening of 4 or more points associated with the bleeding within 36 (+/-12) hrs of treatment initiation (NCT04116112)
Timeframe: 36(+/-12) hrs after treatment initiation

InterventionParticipants (Count of Participants)
Higher Systolic Blood Pressure (SBP) Target2
Lower SBP (<160 mmHg) Target1
Lower SBP (<140mmHg) Target2

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