Page last updated: 2024-12-05

urapidil

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Cross-References

ID SourceID
PubMed CID5639
CHEMBL ID279229
CHEBI ID32278
SCHEMBL ID48992
MeSH IDM0064935

Synonyms (139)

Synonym
BRD-K73196317-003-03-1
BRD-K73196317-001-02-7
DIVK1C_006779
eupressyl
b-66256
1,3-dimethyl-6-[(3-{4-[2-(methyloxy)phenyl]piperazin-1-yl}propyl)amino]pyrimidine-2,4(1h,3h)-dione
nsc-310405
2,3h)-pyrimidinedione, 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-
mls003115907 ,
6-[[3-[4-(o-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil
nsc310405
uracil,3-dimethyl-6-[3-[4-(o-methoxyphenyl)-1-piperazinyl]proppylamino]-
ebrantil
urapidil
34661-75-1
6-[3-[4-(o-methoxyphenyl)-1-piperazinyl]propylamino]-1,3-dimethyluracil
SPECTRUM_001360
lopac-u-100
NCGC00016066-01
tocris-1772
NCGC00025290-01
NCGC00016066-02
BSPBIO_003034
NCGC00178336-02
NCGC00178336-01
PRESTWICK3_000905
BSPBIO_000750
PRESTWICK2_000905
BPBIO1_000826
SPECTRUM5_001611
AB00514699
urapidil (jp17/inn)
D01333
NCGC00025290-02
NCGC00025290-05
NCGC00025290-03
brn 0725782
nsc 310405
mediatensyl
6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1h,3h)-pyrimidinedione
2,4(1h,3h)-pyrimidinedione, 6-((3-(4-(2-methoxyphenyl)-1-piperazinyl)propyl)amino)-1,3-dimethyl-
6-((3-(4-(2-methoxyphenyl)-1-piperazinyl)propyl)amino)-1,3-dimethyl-2,4(1h,3h)-pyrimidinedione
uraprene
uracil, 1,3-dimethyl-6-(3-(4-(o-methoxyphenyl)-1-piperazinyl)proppylamino)-
6-((3-(4-(o-methoxyphenyl)-1-piperazinyl)propyl)amino)-1,3-dimethyluracil
6-(3-(4-(o-methoxyphenyl)-1-piperazinyl)propylamino)-1,3-dimethyluracil
einecs 252-130-4
urapidilum [inn-latin]
KBIO2_001840
KBIO1_001723
KBIOGR_000925
KBIOSS_001840
KBIO2_004408
KBIO2_006976
KBIO3_002534
PRESTWICK1_000905
SPECPLUS_000683
PRESTWICK0_000905
SPECTRUM3_001557
SPECTRUM4_000233
SPBIO_001183
SPECTRUM2_001172
SPBIO_002949
SPECTRUM1503100
LOPAC0_001265
NCGC00025290-04
NCGC00016066-10
CHEMBL279229
smr001831470
L005359
HMS1922E11
6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethylpyrimidine-2,4-dione
NCGC00016066-07
A822334
6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethyl-pyrimidine-2,4-dione;urapidil
6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil
tox21_110298
cas-34661-75-1
dtxsid9021425 ,
dtxcid501425
CCG-40329
NCGC00016066-09
NCGC00016066-08
NCGC00016066-11
NCGC00016066-04
NCGC00016066-03
NCGC00016066-05
NCGC00016066-06
unii-a78gf17hjs
urapidilum
a78gf17hjs ,
5-25-15-00402 (beilstein handbook reference)
urapidil [inn:ban:jan]
BCPP000025
BCP0726000257
FT-0639207
AKOS015896920
urapidil [mart.]
urapidil [who-dd]
urapidil [jan]
urapidil [inn]
urapidil [mi]
S5965
SCHEMBL48992
U0085
KS-5208
W-106718
ICMGLRUYEQNHPF-UHFFFAOYSA-N
uracil, 1,3-dimethyl-6-(3-(4-(o-methoxyphenyl)-1-piperazinyl)propylamino)-
2,4(1h,3h)-pyrimidinedione, 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-
6-((3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl)amino)-1,3-dimethyl-2,4(1h,3h)-pyrimidinedione #
6-[3-[4-(2-methoxyphenyl)piperazinyl]propylamino]-1,3-dimethyluracil
AB00053328_11
AB00053328_10
bdbm50237617
6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1h,3h)-dione
STL454353
AC-8246
mfcd00133908
CHEBI:32278
SBI-0051232.P003
NCGC00016066-16
HY-B0716
CS-0009600
DB12661
Q418922
F15008
6-((3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)amino)-1,3-dimethylpyrimidine-2,4(1h,3h)-dione
urapidil,(s)
2,4(1h,3h)-dione
propylamino)-1,3-dimethylpyrimidine-
6-(3-(4-(2-methoxyphenyl)piperazin-1-yl)
BCP02494
BRD-K73196317-003-07-2
A17074
6-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propylamino)-1,3-dimethylpyrimidine-2,4(1h,3h)-dione
SDCCGSBI-0051232.P004
NCGC00016066-22
ebrantil, 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]- amino]-1,3-dimethyl-2,4(1h,3h)-pyrimidinedione

Research Excerpts

Overview

Urapidil is a potent antihypertensive drug that has been in clinical use for more than 20 years. It is an alpha 1-adrenoceptor antagonist and an agonist of 5HT1A-receptors.

ExcerptReferenceRelevance
"Urapidil is an antihypertensive agent, usually administered through intravenous bolus injection, slow-intravenous infusion, or continuous-drug infusion by perfusor. "( Physical and Chemical Stability of Urapidil in 0.9% Sodium Chloride in Elastomeric Infusion Pump.
Baietto, L; D'Avolio, A; De Nicolò, A; De Perri, G; Fulcheri, C; Leggieri, A; Rabbia, F; Tomasello, C; Veglio, F,
)
1.85
"Urapidil is a therapeutic option for the multifactor heart failure patients complicated with hypertension and DM."( A multicenter, randomized, trial comparing urapidil and nitroglycerin in multifactor heart failure in the elderly.
Chen, XM; Fu, Y; Guo, JC; Hua, Q; Qin, J; Qin, S; Yang, W; Zhou, YJ, 2015
)
1.4
"urapidil is a safe and efficient alternative during surgical management of phaeochromocytoma."( Effects of perioperative alpha1 block on haemodynamic control during laparoscopic surgery for phaeochromocytoma.
Ballanger, P; Gosse, P; Sesay, M; Tauzin-Fin, P, 2004
)
1.04
"Urapidil is a potent antihypertensive drug that has been in clinical use for more than 20 years. "( Neonatal transient respiratory depression after maternal urapidil infusion for hypertension.
Allegaert, K; Hanssens, M; Vanhaesebrouck, S, 2009
)
2.04
"Urapidil, which is an alpha 1- and alpha 2-antagonist, was infused intravenously at 2 and 5 mg/kg, and suppressed reflex tachycardia elicited by bradykinin at both dose levels."( Suppression of reflex tachycardia following alpha-adrenoceptor blockade in conscious dogs: comparison of urapidil with prazosin.
Shebuski, RJ; Zimmerman, BG,
)
1.07
"Urapidil is a vasodilator acting on peripheral vessels by alpha-1 adrenoceptor blockade, and on central nervous system by alphaadrenoceptor blockade on the tractus solitarius nuclei and stimulation of serotoninergic receptors. "( [Role of urapidil in the treatment of acute hypertension].
Bastien, O; Bonnefoy, E; Dalmas, JP; Filley, S; George, M; Lehot, JJ, 1995
)
2.15
"Urapidil is known to be an alpha 1-adrenoceptor antagonist and an agonist of 5HT1A-receptors."( Comparison of the hemodynamic effects of urapidil and flesinoxan in healthy volunteers.
Bruning, TA; Van Zwieten, PA, 1994
)
1.28
"Urapidil is an antihypertensive agent known to have central 5HT1A agonistic properties in addition to alpha-1 blocking effects. "( A comparison of the hemodynamic effects of urapidil, prazosin, and clonidine in healthy volunteers.
Compagnon, P; Fresel, J; Joannidès, R; Moore, N; Thuillez, C, 1994
)
1.99
"Urapidil is an antagonist of postsynaptic alpha 1 receptors, which leads to a diminution of the increased blood pressure by reducing the peripheral vascular resistance. "( [Anti-hypertensive therapy in pregnancy-induced hypertension with urapidil].
Bastert, G; Grischke, EM; Müller, J; Unkels, R; Wacker, J, 1994
)
1.97
"Urapidil appears to be a safe antihypertensive agent in the treatment of mild to moderate essential hypertension. "( [Antihypertensive effect of urapidil in mild to moderate arterial hypertension. Randomized, double-blind versus placebo study].
Amodeo, C; Barros, LM; Batlouni, M; Sousa, JE, 1993
)
2.02
"Urapidil is an alpha-adrenergic receptor antagonist with serotonin-1A receptor-agonist activity in the central nervous system."( Blood pressure management during aortic surgery: urapidil compared to isosorbide dinitrate.
Lacroix, H; Nevelsteen, A; Suy, R; Van Aken, H; Van Hemelrijck, J; Waets, P, 1993
)
1.26
"Urapidil is known to be an alpha 1-adrenoceptor antagonist and an agonist of central 5HT1A-receptors, and should be considered as a vasodilator."( Treatment of pulmonary hypertension in patients with chronic obstructive pulmonary disease: position of vasodilators with special focus on urapidil.
Adnot, S; Samoyeau, R; Weitzenblum, E, 1995
)
1.21
"Urapidil is an effective antihypertensive agent without deleterious effect on renal hemodynamics, lipid and glucose metabolism."( [The effect of urapidil on blood pressure, renal hemodynamics, lipid and glucose metabolism].
Fagundes, VG; Francischetti, EA; Sanjuliani, AF, 1995
)
2.09
"Urapidil is a post-synaptic alpha 1 adrenoceptor antagonist, which is widely used to control hypertensive crises unrelated to pregnancy. "( Treatment of hypertension in patients with pre-eclampsia: a prospective parallel-group study comparing dihydralazine with urapidil.
Bastert, G; Wacker, J; Walter-Sack, I; Werner, P, 1998
)
1.95
"Urapidil is a hypotensor with a wide range of indications (critical hypertension, prophylaxis for hypertensive peaks and treatment of hypertension during surgery) and few side effects."( [Urapidil in anesthesiology: pharmacology and indications].
Ledesma, M; Santiveri, X, 1998
)
1.93
"Urapidil is a peripheral postsynaptic alpha 1-adrenoceptor antagonist with central agonistic action at serotonin 5-HT1A receptors. "( Urapidil. A reappraisal of its use in the management of hypertension.
Dooley, M; Goa, KL, 1998
)
3.19
"Urapidil seems to be a good alternative to labetalol for attenuating the hypertensive response to ECT in cases where there is a contraindication to beta-antagonists."( Comparative hemodynamic effects of urapidil and labetalol after electroconvulsive therapy.
Arcega, JM; Bernardo, M; Blanch, J; Faulí, A; Gomar, C; Imaz, ML; Martínez-Pallí, G; Navinés, R; Santos, P, 2001
)
1.31
"Urapidil is a centrally and peripherally acting anti-hypertensive drug, able to decrease elevated pulmonary vascular resistance in patients with either chronic obstructive pulmonary disease or heart failure."( Urapidil reduces elevated pulmonary vascular resistance in patients before heart transplantation.
Gombotz, H; Grasser, B; Metzler, H; Rehak, P; Wasler, A; Zink, M, 2002
)
2.48
"Urapidil is a peripherally acting alpha 1-adrenoceptor antagonist, and, in this regard, is comparable with prazosin and its successor compounds (e.g."( [Pharmacologic profile of urapidil. Consequences for use as an antihypertensive drug].
van Zwieten, PA, 1992
)
1.31
"(2) Urapidil is a selective alpha 1-adrenoceptor antagonist and, as such, a peripheral vasodilator."( Pharmacological profile of antihypertensive drugs with serotonin receptor and alpha-adrenoceptor activity.
Blauw, GJ; van Brummelen, P; van Zwieten, PA, 1990
)
0.76
"Urapidil is an antihypertensive drug that has a dual mode of action: peripheral alpha-adrenoceptor antagonism and interaction with 5-HT1A receptors in the brain."( Evidence for the interaction of urapidil with 5-HT1A receptors in the brain leading to a decrease in blood pressure.
Beller, KD; Kolassa, N; Sanders, KH, 1989
)
1.28
"Urapidil is a new antihypertensive agent involving both a peripheral and a central mode of action. "( Acute responses to urapidil in hypertensive persons.
Birkenhäger, WH; de Leeuw, PW, 1989
)
2.05
"Urapidil is a postsynaptic alpha 1-adrenoceptor antagonist with a pharmacodynamic profile similar to prazosin. "( Urapidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension.
Langtry, HD; Mammen, GJ; Sorkin, EM, 1989
)
3.16
"Urapidil is an antihypertensive vasodilator agent whose pharmacological action in man has not yet been fully defined. "( The assessment of the beta-blocking activity of urapidil: a new method.
Flanagan, PH; Galbraith, H; Jackson, SH; Jamieson, MJ; Patel, SS; Shepherd, AM; Stewart, W, 1986
)
1.97
"Urapidil appears to be an effective antihypertensive drug with a wide spectrum of action and few side effects."( Do hybrid drugs offer an additional benefit over pure alpha 1-blockade for hypertensive patients?
Doyle, AE, 1988
)
1
"Urapidil is a new antihypertensive vasodilator agent whose pharmacologic action in man has not yet been fully defined. "( Alpha adrenergic blocking activity of urapidil in man.
Flanagan, PH; Galbraith, H; Jackson, SH; Jamieson, MJ; Patel, SS; Shepherd, AM, 1988
)
1.99
"Urapidil is a new antihypertensive drug which is thought to possess unique antiadrenergic properties. "( Relative presynaptic and postsynaptic effects of urapidil on adrenoceptors in the rabbit pulmonary artery.
Zelis, R, 1986
)
1.97
"Urapidil is an alpha 1-adrenoceptor antagonist which also has a central antihypertensive effect, the mechanism of which has yet to be conclusively defined. "( Urapidil in the treatment of hypertension.
Rosendorff, C, 1988
)
3.16
"Urapidil is a phenylpiperazine-substituted uracil derivative used in hypertension. "( Human pharmacology of urapidil.
Shepherd, AM, 1988
)
2.03
"Urapidil is a selective alpha 1-adrenoceptor antagonist with central antihypertensive action which is increasingly used in the treatment of hypertension. "( Clinical pharmacokinetics of urapidil.
Haerlin, R; Kirsten, R; Nelson, K; Steinijans, VW; Zech, K, 1988
)
2.01
"Urapidil is a new vasodilator that acts by postsynaptic alpha 1-blockade while inhibiting the aortic pressure baroreceptor reflex and reducing central sympathetic tone."( Hemodynamic effects of urapidil in patients with pulmonary hypertension. A comparative study with hydralazine.
Abrouk, F; Adnot, S; Brun-Buisson, C; Defouilloy, C; Lemaire, F; Piquet, J, 1987
)
1.3
"Urapidil is a novel antihypertensive agent, chemically related to uracil. "( Cardiovascular effects and interaction with adrenoceptors of urapidil.
Beckeringh, JJ; de Jonge, A; Thoolen, MJ; Timmermans, PB; van Zwieten, PA; Wilffert, B, 1985
)
1.95
"Urapidil (Ebrantil) is a new antihypertensive agent exerting central and peripheral action which is recognized for the treatment of both chronic and acute hypertension. "( [Circulatory changes with urapidil (Ebrantil) in general and regional anesthesia. Studies with normo- and hypertensive patients].
Heimig, T; Lehmann, KA, 1985
)
2.01

Effects

Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT(1A) receptors in the central nervous system. It has been approved as sustained-release capsules containing 30, 60 and 90 mg, respectively, for treatment of all grades of hypertension.

ExcerptReferenceRelevance
"Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT(1A) receptors in the central nervous system."( Urapidil, a dual-acting antihypertensive agent: Current usage considerations.
Buch, J, 2010
)
2.52
"Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT(1A) receptors in the central nervous system."( Urapidil, a dual-acting antihypertensive agent: Current usage considerations.
Buch, J, 2010
)
2.52
"Urapidil (U) has both peripheral alpha-1-adrenoreceptor blocking activity and a central antihypertensive effect at the level of the 5HT-1A serotonergic receptor, resulting in enhanced peripheral sympathetic inhibition (3,4)."( Comparison of the effects of urapidil and nitroprusside on hemodynamics and myocardial function in hypertension following cardiac surgery.
Koolen, JJ; Van der Stroom, JG; Van Wezel, HB; Van Zwieten, PA; Visser, CA, 1994
)
1.3
"Urapidil has been approved as sustained-release capsules containing 30, 60 and 90 mg, respectively, and as ampules containing 25 and 50 mg for treatment of all grades of hypertension, in several countries in Europe, South America, as well as in Japan and other Asian regions. "( Overview of clinical trials with urapidil.
Radtke, H; Schook, CE; Thieme, G; Wurst, W, 1989
)
2
"Urapidil has also been used successfully in the treatment of hypertensive emergencies, including eclampsia and pre-eclampsia, hypertensive crisis and hypertension occurring during general and cardiac surgery, rapidly lowering blood pressure without altering heart rate."( Urapidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension.
Langtry, HD; Mammen, GJ; Sorkin, EM, 1989
)
2.44
"Urapidil has been successfully administered also in patients with congestive heart failure and in hypertensive crises during or following surgical procedures; in all these conditions urapidil lowers total peripheral resistance, but blood pressure is lowered only in patients with hypertensive crises and no clinically relevant reduction in blood pressure is found in patients with congestive heart failure."( Systemic haemodynamic and humoral changes during urapidil treatment in hypertensive patients.
Leonetti, G; Terzoli, L; Zanchetti, A, 1988
)
1.25
"Urapidil has been reported to have alpha 2-agonistic actions, and therefore was compared to the prototypic alpha 2 agonists, clonidine and B-HT 920."( Prejunctional alpha 2-adrenoceptor mediated inhibitory action of clonidine and B-HT 920, but not urapidil in guinea pig ileum.
Shebuski, RJ; Zimmerman, BG, 1985
)
1.21

Actions

Urapidil is thought to lower blood pressure by both a peripheral and a central mechanism. It does not inhibit the exercise increase in heart rate.

ExcerptReferenceRelevance
"Urapidil is thought to lower blood pressure by both a peripheral and a central mechanism. "( Importance of central nervous system serotonin-1A receptors for mediating the hypotensive effect of urapidil.
Friedman, E; Gillis, RA; Hamosh, P; Kellar, KJ; Mandal, AK; Pineo, SV, 1989
)
1.94
"Urapidil does not inhibit the exercise increase in heart rate."( Urapidil, a multiple-action alpha-blocking drug.
Prichard, BN; Renondin, JC; Tomlinson, B, 1989
)
2.44
"Urapidil did not inhibit contractions induced by muscarinic agonists in both organs."( Interaction with histamine H1-receptors and bronchospasmolytic effects of urapidil.
Eltze, M; Kilian, U; Kolassa, N, 1987
)
1.23

Treatment

Urapidil treatment improves coronary flow, myocardial perfusion and left ventricular function following PCI in patients with ST-elevation ACS. Treatment with urapidil alone was effective in 80 cases.

ExcerptReferenceRelevance
"Urapidil treatment improves coronary flow, myocardial perfusion and left ventricular function following PCI in patients with ST-elevation ACS. "( Therapeutic effect of urapidil on myocardial perfusion in patients with ST-elevation acute coronary syndrome.
Jia, SQ; Li, HW; Wang, L; Wang, LX; Wang, YL; Yao, DK; Zhang, YC, 2009
)
2.11
"Urapidil treatment resulted in significantly greater reductions in the systolic and diastolic blood pressures (by 12.1% and 8.6%, respectively) (P(s)<0.001, P(d)=0.019)."( [Efficacy of sublingual nifedipine and intravenous urapidil for treatment of acute postoperative hypertension].
Lou, N; Wang, DF; Wang, Z, 2011
)
1.34
"Urapidil treatment proved to be better controllable."( Antihypertensive therapy in patients with pre-eclampsia: A prospective randomised multicentre study comparing dihydralazine with urapidil.
Bartz, C; Briese, V; Heilmann, L; Hopp, H; Schauf, B; Wacker, JR; Wagner, BK, 2006
)
1.26
"With urapidil treatment, the decrease in vascular resistance was distributed throughout all circulations, with no change in heart rate or cardiac index."( Systemic and regional hemodynamic effects of acute and prolonged treatment with urapidil or prazosin in normotensive and spontaneously hypertensive rats.
Frohlich, ED; Gallo, AJ; Kobrin, I; Natsume, T; Pegram, BL, 1984
)
0.95
"Urapidil treatment resulted to be effective in preventing hypertensive reactions following algogenic stimulation."( [Prevention of hypertensive crises in the perioperative period. Efficacy and safety of the use of urapidil].
Mastronardi, P; Mazzarella, B; Noseda, A; Santagata, T, 1996
)
1.23
"Urapidil-treated rats showed significant inhibition of neointima formation for both parameters in a dose-dependent fashion."( Alpha 1-receptor antagonists urapidil and prazosin inhibit neointima formation in rat carotid artery induced by balloon catheter injury.
Fingerle, J; Fotev, Z; Sanders, KH, 1991
)
1.29
"Treatment with urapidil alone was effective in 80 cases (80%). "( [Use of injectable urapidil in pregnancy-induced hypertension and preeclampsia].
Alassas, N; Carles, G; Dallah, F; Helou, J; Ibrahim, N; Youssef, M, 2012
)
1.06
"treatment with urapidil at a diastolic blood pressure of more than 100 mm Hg."( [Anti-hypertensive therapy in pregnancy-induced hypertension with urapidil].
Bastert, G; Grischke, EM; Müller, J; Unkels, R; Wacker, J, 1994
)
0.87

Toxicity

Intravenous administration of urapidil, compared with nitroglycerin, was associated with better control of blood pressure and preserved cardiac function. Due to a smaller number of adverse events, urapodil is a reasonable alternative to nitroprusside in the treatment of hypertensive emergencies.

ExcerptReferenceRelevance
" 24 patients discontinued the study due to adverse effects (n = 2), an inadequate effect (n = 2), or for reasons unrelated to therapy (n = 20); 58 (28."( [Long-term antihypertensive therapy with urapidil. A 3-year open, multicenter trial of tolerance, safety and effectiveness].
Harder, I; Liebau, H; Solleder, P; Wurst, W, 1990
)
0.54
" Due to a smaller number of adverse events, urapidil is a reasonable alternative to nitroprusside in the treatment of hypertensive emergencies."( Safety and efficacy of urapidil and sodium nitroprusside in the treatment of hypertensive emergencies.
Binder, M; Bur, A; Herkner, H; Hirschl, MM; Laggner, AN; Müllner, M; Woisetschläger, C, 1997
)
0.87
" All adverse effects had little relevance."( Effectiveness and safety of prehospital urapidil for hypertensive emergencies.
Alijotas-Reig, J; Angles-Coll, R; Bove-Farre, I; de Cabo-Frances, F, 2001
)
0.58
" Patients given urapidil had fewer associated adverse events, specifically headache (p=0."( Efficacy and Safety of Intravenous Urapidil for Older Hypertensive Patients with Acute Heart Failure: A Multicenter Randomized Controlled Trial.
Chen, XM; Fu, Y; Guo, JC; He, JY; Hua, Q; Li, J; Qin, J; Qin, S; Wang, Z; Yang, W; Zhan, H; Zhou, YJ, 2017
)
1.08
"Intravenous administration of urapidil, compared with nitroglycerin, was associated with better control of blood pressure and preserved cardiac function, as well as fewer adverse events, for elderly patients with hypertension and acute heart failure."( Efficacy and Safety of Intravenous Urapidil for Older Hypertensive Patients with Acute Heart Failure: A Multicenter Randomized Controlled Trial.
Chen, XM; Fu, Y; Guo, JC; He, JY; Hua, Q; Li, J; Qin, J; Qin, S; Wang, Z; Yang, W; Zhan, H; Zhou, YJ, 2017
)
1.02

Pharmacokinetics

Urapidil is a postsynaptic alpha 1-adrenoceptor antagonist with a pharmacodynamic profile similar to prazosin. The optimum use of urapidil in clinical practice depends on an understanding of the pharmacokinetic properties of the drug.

ExcerptReferenceRelevance
"Urapidil is a postsynaptic alpha 1-adrenoceptor antagonist with a pharmacodynamic profile similar to prazosin."( Urapidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension.
Langtry, HD; Mammen, GJ; Sorkin, EM, 1989
)
3.16
" Studies on the relationship between pharmacodynamics and pharmacokinetics show that the optimum use of urapidil in clinical practice depends on an understanding of the pharmacokinetic properties of the drug."( Clinical pharmacokinetics of urapidil.
Haerlin, R; Kirsten, R; Nelson, K; Steinijans, VW; Zech, K, 1988
)
0.78
" Estimated pharmacokinetic parameters included Vz (0."( Pharmacokinetics and pharmacodynamics of urapidil in severe hypertension.
Bottorff, MB; Gerlach, PA; Hoon, TJ; Ramanathan, KB; Rodman, JH, 1988
)
0.54
"The pharmacokinetic parameters, including the relative bioavailabilities of two experimental batches of a 60-mg urapidil slow release-capsule and a 30-mg urapidil drinking ampoule (Ebrantil) had to be evaluated in a randomized, three-period change-over study with 12 healthy volunteers after single dosing."( [The pharmacokinetics and bioavailability of urapidil. In vitro/in vivo correlations of different experimental formulations].
Gielsdorf, W; Haerlin, R; Jaeger, H; Molz, KH; Nieder, M; Radtke, HW, 1986
)
0.74
" These drugs must be administered parenterally and have a half-life of only a few minutes."( Clinical pharmacokinetics of vasodilators. Part II.
Heintz, B; Kirsten, D; Kirsten, R; Nelson, K, 1998
)
0.3
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The method was successfully applied to quantify urapidil concentrations in a preclinical pharmacokinetic study after a single oral administration of urapidil at 3 mg/kg to rats."( Quantification of urapidil, α-1-adrenoreceptor antagonist, in plasma by LC-MS/MS: validation and application to pharmacokinetic studies.
Aleti, R; Boggavarapu, R; Kandikere, V; Komarneni, P; Madala, P; Nirogi, R, 2011
)
0.96
" The method was successfully applied to human pharmacokinetic study of urapidil and aripiprazole in healthy human male volunteers."( Liquid chromatography-tandem mass spectrometry method for simultaneous quantification of urapidil and aripiprazole in human plasma and its application to human pharmacokinetic study.
Ambavaram, VB; Gajulapalle, M; Kalluru, GR; Nandigam, V; Vemula, M, 2013
)
0.84
" The proposed method was used for studying pharmacokinetics of urapidil hydrochloride in rat plasma and the main pharmacokinetic parameters of the peak concentration (Cmax), half life time (T1/2) and peak concentration time (Tmax) were 240."( Capillary electrophoresis with end-column electrochemiluminescence for ultrasensitive determination of urapidil hydrochloride in rat plasma and its application to pharmacokinetics study.
Deng, B; Long, C; Sun, S; Wei, Y, 2015
)
0.87

Compound-Compound Interactions

Urapidil combined with phentolamine can control hypertension during extracorporeal circulation without causing hypotension.

ExcerptReferenceRelevance
"To study the effect of urapidil combined with phentolamine in the management of hypertension during extracorporeal circulation."( [Effect of urapidil combined with phentolamine on hypertension during extracorporeal circulation].
Chen, B; Liu, Y; Tu, F; Wang, F, 2014
)
1.1
"Urapidil combined with phentolamine can control hypertension during extracorporeal circulation without causing hypotension."( [Effect of urapidil combined with phentolamine on hypertension during extracorporeal circulation].
Chen, B; Liu, Y; Tu, F; Wang, F, 2014
)
2.23

Bioavailability

Urapidil is well absorbed orally with a bioavailability of about 70% and a time to peak concentration of about 4 hours after a sustained release capsule. Food intake did not influence theBioavailability of urapidil in tablet form.

ExcerptReferenceRelevance
" Urapidil is well absorbed orally with a bioavailability of about 70% and a time to peak concentration of about 4 hours after a sustained release capsule."( Urapidil, a multiple-action alpha-blocking drug.
Prichard, BN; Renondin, JC; Tomlinson, B, 1989
)
2.63
" Food intake did not influence the bioavailability of urapidil in tablet form."( Influence of food intake on the bioavailability of urapidil in healthy volunteers.
Gielsdorf, W; Haerlin, R; Kirsten, R; Molz, KH; Nelson, K, 1989
)
0.78
" The geometric mean and nonparametric 95% confidence limits of digoxin relative bioavailability were 97% (93%-103%)."( Effect of urapidil on steady-state serum digoxin concentration in healthy subjects.
Haerlin, R; Klingmann, I; Mosberg, H; Solleder, P; Wurst, W, 1989
)
0.68
" Urapidil is well absorbed orally with a bioavailability of about 70% and a tmax at about 4 h after a sustained release capsule."( Clinical pharmacology of urapidil.
Prichard, BN; Renondin, JC; Tomlinson, B, 1988
)
1.49
" Oral bioavailability is 78% (range 72 to 84%) and distribution half-life and terminal half-life are about 35 minutes and 3 hours, respectively."( Human pharmacology of urapidil.
Shepherd, AM, 1988
)
0.59
" Both batches of the capsules showed equivalence with respect to the extent of absorption, in connection with 100% relative bioavailability on average."( [The pharmacokinetics and bioavailability of urapidil. In vitro/in vivo correlations of different experimental formulations].
Gielsdorf, W; Haerlin, R; Jaeger, H; Molz, KH; Nieder, M; Radtke, HW, 1986
)
0.53
"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
"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
"Modified-release pellets containing urapidil were developed and its in vivo bioavailability was investigated."( Preparation of pH-dependent modified-release pellets of urapidil to improve its bioavailability.
He, H; Li, H; Tang, X, 2011
)
0.89
" The bioavailability of the pellets (T(1), T(2), containing 30 mg urapidil) was determined in six healthy subjects after oral administration of a single dose, for a period of three weeks, in the form of a crossover design with a wash-out period of one week."( Preparation of pH-dependent modified-release pellets of urapidil to improve its bioavailability.
He, H; Li, H; Tang, X, 2011
)
0.85
"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

Urapidil at a dosage of 25 mg intravenously reduced WHVP from 33. Theophylline, at a 100-fold higher dosage than urapidil, protected the animals against both histamine and acetylcholine challenges.

ExcerptRelevanceReference
" (-)-Pindolol (30 and 100 nmol/kg) shifted the dose-response curves of both drugs significantly and in a similar manner to the right."( Involvement of 5-HT1A receptors in blood pressure reduction by 8-OH-DPAT and urapidil in cats.
Beller, KD; Kolassa, N; Sanders, KH, 1990
)
0.51
" If necessary, dosage adjustments were performed every 2 weeks."( Clinical aspects of antihypertensive therapy with urapidil. Comparison with hydrochlorothiazide.
Distler, A; Haerlin, R; Hilgenstock, G; Passfall, J, 1990
)
0.53
" Since this concentration corresponds to the serum concentrations generally reached in oral therapy of hypertension with urapidil, antiarrhythmic side effects should only occur under exceptional conditions like parenteral administration of high dosage or increased myocardial sensitivity."( Influence of the alpha-adrenoceptor antagonist urapidil on transmembrane action potentials of mammalian myocardium.
Gülch, RW; Mohrmann, J; Schultheiss, S, 1986
)
0.74
"1-10 micrograms/kg) given through the left vertebral artery of chloralose-anesthetized cats, lowered blood pressure by a biphasic dose-response curve."( Central 5-HT1A receptors and the mechanism of the central hypotensive effect of (+)8-OH-DPAT, DP-5-CT, R28935, and urapidil.
Boddeke, HW; Doods, HN; Hoyer, D; Kalkman, HO; Mathy, MJ; van Zwieten, PA, 1988
)
0.48
" A shift to the right in the dose-response curve to phenylephrine has been found after urapidil, whereas responses to angiotensin are not affected."( Urapidil, a multiple-action alpha-blocking drug.
Prichard, BN; Renondin, JC; Tomlinson, B, 1989
)
1.94
" A dose-response test with both drugs was performed before and after administration of spiroxatrine (3 and 10 nmol/kg); the latter was given through the vertebral artery, thus delivering the antagonist to the brain stem."( Involvement of brain 5-HT1A receptors in the hypotensive response to urapidil.
Beller, KD; Kolassa, N; Sanders, KH, 1989
)
0.51
" Cumulative dose-response (i."( Evidence that different regional sympathetic outflows vary in their sensitivity to the sympathoinhibitory actions of putative 5-HT1A and alpha 2-adrenoceptor agonists in anaesthetized cats.
Ramage, AG; Wilkinson, SJ, 1989
)
0.28
" Propranolol 5 mg iv, the positive control, significantly shifted the isoproterenol dose-response curve to the right."( The assessment of the beta-blocking activity of urapidil: a new method.
Flanagan, PH; Galbraith, H; Jackson, SH; Jamieson, MJ; Patel, SS; Shepherd, AM; Stewart, W, 1986
)
0.53
" Theophylline, at a 100-fold higher dosage than urapidil, protected the animals against both histamine and acetylcholine challenges."( Interaction with histamine H1-receptors and bronchospasmolytic effects of urapidil.
Eltze, M; Kilian, U; Kolassa, N, 1987
)
0.76
" Peripheral alpha 1-blocking activity has been demonstrated in man, and a shift to the right in the dose-response curve to phenylephrine has been found after administration of urapidil, while responses to angiotensin are not affected."( Clinical pharmacology of urapidil.
Prichard, BN; Renondin, JC; Tomlinson, B, 1988
)
0.77
") and prazosin (5 mg orally) induced significant shifts to the right in the blood pressure dose-response curve of norepinephrine."( A clinical approach for the identification of peripheral pre- and post-synaptic alpha-adrenergic receptors.
Magometschnigg, D; Schütz, W, 1986
)
0.27
" An alternative dosing regimen is suggested."( Pharmacokinetics and pharmacodynamics of urapidil in severe hypertension.
Bottorff, MB; Gerlach, PA; Hoon, TJ; Ramanathan, KB; Rodman, JH, 1988
)
0.54
" Because the study was carried out in a small number of patients who received different dosages of urapidil over a short period of time, the optimal dosage was not established."( Clinical evaluation of urapidil, a new antihypertensive drug: preliminary findings in Japan.
Fujiwara, H; Iesaka, Y; Iizumi, T; Inada, M; Ito, H; Kirigaya, H; Nakamura, S; Nitta, M; Takeuchi, J; Taniguchi, K, 1985
)
0.8
" However, basal blood pressure was significantly lowered after 4 days of treatment with urapidil at the high dosage and no further reduction was achieved on the fifth day."( Blood pressure response and renin release following 4 days of treatment with dihydralazine and urapidil in conscious dogs.
Bacher, S; Beck, A; Kraupp, O; Raberger, G; Seitelberger, R, 1984
)
0.71
" In summary, a daily dosage of 60 mg urapidil proved to be the most beneficial in the treatment of patients with BPH."( Effect on urapidil on benign prostatic hypertrophy: a multicenter, double-blind study.
Kageyama, S; Kawabe, K; Morita, T; Shimazaki, J; Tsuchida, S; Yasuda, K, 1993
)
0.96
" The postpartum dosage of dihydralazine was diminished step by step and finally discontinued."( [Anti-hypertensive therapy in pregnancy-induced hypertension with urapidil].
Bastert, G; Grischke, EM; Müller, J; Unkels, R; Wacker, J, 1994
)
0.53
" In the dosage used, urapidil seems to be unable to prevent postanesthetic shivering."( A comparison of urapidil, clonidine, meperidine and placebo in preventing postanesthetic shivering.
Boldt, J; Maleck, WH; Piper, SN; Reich, DG; Schmidt, CC; Suttner, SW, 2000
)
0.97
" In the dosage used, we were unable to show a significant benefit of urapidil."( A comparison of urapidil, clonidine, meperidine and placebo in preventing postanesthetic shivering.
Boldt, J; Maleck, WH; Piper, SN; Reich, DG; Schmidt, CC; Suttner, SW, 2000
)
0.89
" It is suggested that the cardiovascular response to tracheal intubation and incision may be effectively inhibited in combination URA with fentanyl, and the dosage of fentanyl might reduce."( [Effects of urapidil on cardiovascular response to tracheal intubation and incision during fentanyl co-induction].
Cai, HW; Yang, HB, 2000
)
0.69
"Urapidil at a dosage of 25 mg intravenously reduced WHVP from 33."( [Effects of urapidil and cimetidine on wedged hepatic venous pressure and systemic hemodynamics in cirrhotic patients with portal hypertension].
Du, R; Feng, H; Leng, X; Li, S; Zhong, C; Zhu, J, 2000
)
2.13
" This information includes detection of circulating metabolites, dosing vehicle, interfering matrix components, and potential interfering drug conjugates."( Collection of selected reaction monitoring and full scan data on a time scale suitable for target compound quantitative analysis by liquid chromatography/tandem mass spectrometry.
Fernández-Metzler, CL; Gundersdorf, R; King, RC, 2003
)
0.32
" In a group of patients receiving urapidil during monotherapy, the average dosage of the medicine required to lower arterial blood pressure amounted to 26."( [Usefulness of urapidil during intraoperative rise of arterial blood pressure in patients operated under general anesthesia].
Grabowska-Gaweł, A; Grześk, G; Porzych, K, 2005
)
0.96
" Average dosage of urapidil applied during monotherapy amounted to 26."( [Usefulness of urapidil during intraoperative rise of arterial blood pressure in patients operated under general anesthesia].
Grabowska-Gaweł, A; Grześk, G; Porzych, K, 2005
)
1.01
" We analysed the number of sessions until completion of ECT treatment (used as a surrogate parameter for outcome), psychopathology as assessed by pre- and post-ECT Mini-Mental State Examination (MMSE) and Hamilton Rating Scale for Depression (HAM-D) scores as well as ECT and seizure parameters (stimulation dose, seizure duration and concordance, urapidil dosage for post-seizure blood pressure management)."( Clinically favourable effects of ketamine as an anaesthetic for electroconvulsive therapy: a retrospective study.
Hoyer, C; Kammerer-Ciernioch, J; Kranaster, L; Sartorius, A, 2011
)
0.54
" Comparison of DR(10) values (the dose required to shift the dose-response curve 10-fold to the right) in both tissues showed that the inhibitory effect of silodosin was significantly more potent in the salivary gland than in the urethra (18-fold), but tamsulosin (2."( Effects of α1-adrenoceptor antagonists on phenylephrine-induced salivary secretion and intraurethral pressure elevation in anesthetized rats.
Hatanaka, T; Noguchi, Y; Ohtake, A; Sasamata, M; Sato, S; Suzuki, M; Ueshima, K; Yanai-Inamura, H, 2012
)
0.38
" Low dosed urapidil was used for α1A-adrenergic receptor blockade."( Underlying mechanism of subcortical brain protection during hypoxia and reoxygenation in a sheep model - Influence of α1-adrenergic signalling.
Bischoff, SJ; Huber, O; Lehmann, T; Lemke, C; Matziolis, G; Rakers, F; Rupprecht, S; Schiffner, R; Schmidt, M; Schubert, H; Schwab, M, 2018
)
0.87
" The resolution-IV of 24-1 reduced factorial design was selected to screen the possible and significant independent variables or factors in the dosage form design."(
Nandi, S; Nayak, BS; Roy, H, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[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 (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency19.09350.100020.879379.4328AID488773; AID588453
GLS proteinHomo sapiens (human)Potency12.58930.35487.935539.8107AID624170
Microtubule-associated protein tauHomo sapiens (human)Potency25.51540.180013.557439.8107AID1460; AID1468
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.58930.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency26.85451.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.94330.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.58930.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency31.62280.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency0.01580.039816.784239.8107AID995
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency25.11890.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.98710.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.50120.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency7.94330.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency10.73090.00638.235039.8107AID881; AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency25.11891.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[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)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)93.10000.11007.190310.0000AID1443980; AID1449628; AID1473738
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.21300.00010.532610.0000AID1380687
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.12790.00010.949010.0000AID1380686
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.12790.00000.575110.0000AID1380686
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.12790.00000.965010.0000AID1380686
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (77)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
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)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
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)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
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)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (69)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
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
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.
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.
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.
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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
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.
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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine 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.
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.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
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.
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.
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.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID207305Steroid 5-alpha-reductase inhibitory activity was determined using the prostate of male Dawley rats; no data1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.
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.
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.
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.
AID1380687Binding affinity to 5-HT1A receptor (unknown origin)
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.
AID1380686Displacement of [3H]prazosin from rat cerebral cortex adrenergic receptor alpha1 by liquid scintillation counting method
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.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID36278Antagonistic Alpha-1 adrenergic receptor activity against phenylephrine-induced contraction of rabbit prostate1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.
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.
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.
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.
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.
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.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
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.
AID1613973Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates assessed as residual activity at 100 uM using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening.
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.
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.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (489)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990156 (31.90)18.7374
1990's171 (34.97)18.2507
2000's79 (16.16)29.6817
2010's69 (14.11)24.3611
2020's14 (2.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 79.82

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 Index79.82 (24.57)
Research Supply Index6.50 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index142.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (79.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials142 (27.05%)5.53%
Reviews53 (10.10%)6.00%
Case Studies28 (5.33%)4.05%
Observational0 (0.00%)0.25%
Other302 (57.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (14)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
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
TCD Monitoring Technology Guides the Precise Control of Blood Pressure After EVT [NCT03529149]Phase 490 participants (Anticipated)Interventional2018-04-08Recruiting
Effect of Cafedrine/Theodrenaline and Urapidil During Carotid Endarterectomy on Cerebral Oxygenation Measured by Near Infrared Spectroscopy [NCT01311414]0 participants (Actual)InterventionalWithdrawn(stopped due to The study was suspended due to organizational problems)
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)
Comparsion of the Effect of High Versus Low Mean Arterial Pressure (MAP) Levels on Clinical Outcomes in Elderly Patients During Noncardiothoracic Surgery Under General Anesthesia [NCT02857153]322 participants (Anticipated)Interventional2016-07-31Recruiting
Intensive Ambulance-delivered Blood Pressure Reduction in Hyper-Acute Stroke Trial [NCT03790800]Phase 32,425 participants (Actual)Interventional2020-03-20Completed
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
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 Trial on Hemodynamic Optimization of Cerebral Perfusion After Endovascular Therapy in Patients With Acute Ischemic Stroke (HOPE Study) [NCT04892511]Phase 4814 participants (Anticipated)Interventional2021-06-01Recruiting
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
Clevidipine (Cleviprex®) Compared With Urapidil (Ebrantil®) for Blood Pressure Reduction in Patients With Primary Intracerebral Hemorrhage: A Randomized Controlled Trial [NCT03300479]Phase 40 participants (Actual)Interventional2017-06-15Withdrawn(stopped due to No patient enrolled. No study conduct due to lack of human resources.)
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
Intensive Blood PRessure Control in Patients With Acute Type B AortIc Dissection (RAID): Study Protocol for Randomized Controlled Trial [NCT03001739]Phase 1360 participants (Anticipated)Interventional2016-12-31Recruiting
Effects of Different Kinds of Antihypertensive Drugs on Dynamic Hemodynamic Changing of During Laparoscopic Gastrectomy and Laparotomy [NCT03497351]59 participants (Actual)Interventional2018-04-15Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
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)
NCT00716079 (2) [back to overview]Death at 90 Days

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]

Death at 90 Days

(NCT00716079)
Timeframe: 90 days

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

[back to top]