Page last updated: 2024-12-06

indoramin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Indoramin is an α-adrenergic receptor antagonist that was initially developed as an antihypertensive agent. It is known to bind selectively to α1-adrenergic receptors, leading to vasodilation and a decrease in blood pressure. However, its use in hypertension has been limited due to potential side effects. Recent research has focused on exploring its other pharmacological properties, including its potential as an anti-inflammatory agent. Indoramin has been shown to inhibit the production of inflammatory cytokines and reduce inflammation in animal models. The mechanism underlying its anti-inflammatory effects is thought to involve its interaction with α1-adrenergic receptors on immune cells. Furthermore, studies have suggested that indoramin may have neuroprotective properties and could be beneficial in conditions like Parkinson's disease. The interest in indoramin has been reignited by its potential therapeutic applications beyond its initial use as an antihypertensive. Ongoing research aims to elucidate its complete pharmacological profile and explore its therapeutic potential in various disease settings.'

Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID33625
CHEMBL ID279516
CHEBI ID135470
SCHEMBL ID49518
SCHEMBL ID49517
MeSH IDM0011253

Synonyms (70)

Synonym
PDSP2_001083
bdbm50033113
n-{1-[2-(1h-indol-3-yl)-ethyl]-piperidin-4-yl}-benzamide(indoramin)
n-{1-[2-(1h-indol-3-yl)-ethyl]-piperidin-4-yl}-benzamide (indoramin)
indoraminn-{1-[2-(1h-indol-3-yl)-ethyl]-piperidin-4-yl}-benzamide
n-{1-[2-(1h-indol-3-yl)-ethyl]-piperidin-4-yl}-benzamide
gtpl501
baratol
wy-21901
doralese
indoramine [inn-french]
benzamide, n-(1-(2-(1h-indol-3-yl)ethyl)-4-piperidinyl)-
3-(2-(4-benzamidopiperid-1-yl)ethyl)indole
benzamide, n-(1-(2-indol-3-ylethyl)-4-piperidyl)-
n-(1-(2-(1h-indol-3-yl)ethyl)-4-piperidinyl)benzamide
indoraminum [inn-latin]
indoramine
wy 21901
einecs 248-041-5
n-(1-(2-indol-3-ylethyl)-4-piperidyl)benzamide
indoramina [inn-spanish]
brn 0494035
indoramin (usan/inn)
PDSP1_001423
26844-12-2
D04531
PDSP2_001407
PDSP1_001099
IDI1_016359
OPREA1_130443
indoramin
SR-01000631243-1
NCGC00165810-01
MAYBRIDGE3_004972
smr000567879
MLS001182179
CHEBI:135470
HMS1445B22
CHEMBL279516 ,
n-[1-[2-(1h-indol-3-yl)ethyl]piperidin-4-yl]benzamide
L001292
AKOS015994528
CCG-41146
indoraminum
indoramina
unii-0z802hmy7h
0z802hmy7h ,
indoramin [usan:inn:ban]
HMS2851P23
SCHEMBL49518
SCHEMBL49517
AF-0013
indoramin [inn]
indoramin [who-dd]
indoramin [mi]
indoramin [usan]
n-[1-(2-indol-3-ylethyl)-4-piperidyl]benzamide
DTXSID7048370
3-[2-(4-benzamido-1-piperidyl)ethyl]indole
benzamide, n-[1-[2-(1h-indol-3-yl)ethyl]-4-piperidinyl]-
benzamide, n-[1-(2-indol-3-ylethyl)-4-piperidyl]-
3-[2-(4-benzamidopiperidino)ethyl]indole
n-(1-[2-(1h-indol-3-yl)ethyl]-4-piperidinyl)benzamide #
DB08950
Q408963
indoramine;wy 21901
nsc-771684
nsc771684
HY-12760
CS-0012358

Research Excerpts

Overview

Indoramin is a competitive postsynaptic alpha-adrenoceptor antagonist with a myocardial membrane-stabilizing component of action. It reduces blood pressure without reflex tachycardia and can cause a bradycardia.

ExcerptReferenceRelevance
"Indoramin is a competitive postsynaptic alpha-adrenoceptor antagonist with a myocardial membrane-stabilizing component of action."( Indoramin in the treatment of hypertension. A mini-review and update.
Archibald, JL; Turner, P, 1983
)
2.43
"Indoramin hydrochloride is a new alpha 1-adrenoceptor antagonist. "( Effects of indoramin therapy on BP, renal function, and body fluid composition.
Bauer, JH; Gaddy, P; Jones, LB, 1984
)
2.1
"Indoramin is a selective postsynaptic alpha-adrenoceptor antagonist used for the treatment of hypertension. "( Clinical cardiac electrophysiological assessment of indoramin.
Butrous, GS; Camm, AJ, 1986
)
1.96
"Indoramin is a postsynaptic selective alpha 1-adrenoceptor antagonist used in the treatment of hypertension. "( Indoramin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and related vascular, cardiovascular and airway diseases.
Holmes, B; Sorkin, EM, 1986
)
3.16
"Indoramin is a selective post-synaptic alpha blocker. "( Clinical cardiac electrophysiology of indoramin, a post-synaptic alpha blocker.
Butrous, GS; Camm, AJ, 1986
)
1.98
"Indoramin is an alpha 1-adrenergic antagonist vasodilator of potential value in heart failure. "( Indoramin in heart failure: possible adverse effects on hemodynamics and exercise capacity.
Casebolt, P; Franciosa, JA; Galiè, N; Gimenez, H; Malloy, M; Seth, L, 1986
)
3.16
"Indoramin is a selective alpha 1-antagonist which reduces blood pressure without reflex tachycardia and can cause a bradycardia. "( Investigations into the bradycardic action of indoramin.
Harron, DW; Kobinger, W; Lillie, C, 1985
)
1.97

Effects

Indoramin was administered orally for 10 days to 21 patients with urinary retention or residual urine caused by neurogenic vesicourethral dysfunction. Indoramin has been reported to reduce blood pressure in experimental animals and humans.

ExcerptReferenceRelevance
"Indoramin has a definite inhibitory effect on the medullary vasomotor loci which contributes to the hypotension produced by this drug."( On the mechanisms of hypotensive action of indoramin.
Dhawan, BN; Gulati, K; Srimal, RC,
)
1.12
"Indoramin, which has great selectivity for alpha-1-receptors, was administered orally for 10 days to 21 patients with urinary retention or residual urine caused by neurogenic vesicourethral dysfunction. "( Possible use of indoramin in patients with chronic neurogenic bladder dysfunction.
Chary, KS; Rao, MS; Sharma, PL; Swamy, RP; Vaidyanathan, S, 1983
)
2.05
"Indoramin has been reported to reduce blood pressure in experimental animals and humans. "( Central and peripheral contribution to the antihypertensive action of indoramin.
Baum, T; Shropshire, AT, 1975
)
1.93
"Indoramin has a definite inhibitory effect on the medullary vasomotor loci which contributes to the hypotension produced by this drug."( On the mechanisms of hypotensive action of indoramin.
Dhawan, BN; Gulati, K; Srimal, RC,
)
1.12
"Indoramin has been reported to decrease baroreceptor sensitivity, whereas prazosin has been reported to increase it."( Comparison of the renal effects of indoramin and prazosin.
Strandhoy, JW, 1986
)
1.27
"Indoramin has centrally mediated hypotensive effects in anesthetized animals. "( The cardiovascular effects of centrally and peripherally administered indoramin in conscious rats.
Bonham, AC; Brody, MJ; Mangiapane, ML; Porter, JP; Webb, RL, 1985
)
1.95

Treatment

Indoramin treatment significantly protected guinea-pigs in both types of experiment. Pretreatment with indoramin did not attenuate the inhibitory effect of clonidine on stimulation-evoked 3H-overflow seen with bretylium.

ExcerptReferenceRelevance
"Indoramin treatment significantly protected guinea-pigs in both types of experiment from the effects of each challenging agent."( The effects of indoramin on histamine and antigen-induced changes in respiration in guinea-pigs.
Hamer, C; Temple, DM, 1980
)
1.34
"Pretreatment with indoramin did not attenuate the inhibitory effect of clonidine on the stimulation-evoked 3H-overflow seen with bretylium."( Pre- and postsynaptic effects of indoramin on sympathetic neuroeffector transmission in rabbit aorta and pulmonary artery.
Nedergaard, OA,
)
0.74

Toxicity

ExcerptReferenceRelevance
"An open study was undertaken to investigate the efficacy and adverse effects of indoramin in 33 patients with essential hypertension whose blood pressure was uncontrolled (diastolic blood pressure 96 to 115 mm Hg) despite previous treatment with one or two antihypertensive drugs."( [Open study on the effect and side effects of indoramin, used at the 2d and 3d therapeutic step in essential hypertension].
Hitzenberger, G; Korn, A, 1985
)
0.75

Pharmacokinetics

Indoramin was absorbed with moderate rapidity, with a median tmax of 1. In PM subjects, mean values of Cmax (158 ng/ml) and AUC(0-24) were substantially elevated. Inter-subject variation represented the main source of variability in plasma concentrations.

ExcerptReferenceRelevance
" After oral indoramin Cmax and AUC are both raised (58% and 25%, respectively, for a 50 mg dose) by co-ingested ethanol (0."( A review of the clinical pharmacokinetics and metabolism of the alpha 1-adrenoceptor antagonist indoramin.
Pierce, DM, 1990
)
0.88
" No significant differences were observed between values determined under pregnant and post-partum conditions, for any pharmacokinetic parameter."( The pharmacokinetics of oral indoramin during pregnancy.
Odendaal, HJ; Pierce, DM; Schabort, I, 1990
)
0.57
" Terminal disposition half-life is prolonged after intravenous as well as acute and chronic oral dosing (9."( Pharmacokinetics of indoramin and its metabolite 6-hydroxyindoramin after single and multiple doses to cirrhotic liver patients.
Giesing, M; Neumann, G; Pierce, DM; Reimold, WV; Wilke, G, 1986
)
0.59
" Inter-subject variation represented the main source of variability in indoramin plasma concentrations with, for example, the between-subjects sum of squares (a measure of the contribution to the total variability) representing around 97% of the total sum of squares for Cmax and AUC (0-24)."( Intra- and inter-subject variation in the pharmacokinetics of indoramin and its 6-hydroxylated metabolite.
Abrams, SM; Franklin, RA; Pierce, DM, 1988
)
0.75
" In PM subjects, mean values of Cmax (158 ng/ml) and AUC(0-24) (2556 ng X h X m-1) for indoramin were substantially elevated and t 1/2 beta (18."( The pharmacokinetics of indoramin and 6-hydroxyindoramin in poor and extensive hydroxylators of debrisoquine.
Franklin, RA; Pierce, DM; Smith, SE, 1987
)
0.8
" The results indicated that peak plasma concentrations occurred in 1 to 4 hours after treatment with a single dose of 2 tablets, with an overall elimination half-life of 5 hours."( Pharmacokinetics of oral indoramin.
Frost, T; Jeffereys, D; Latham, AN; Volans, GN, 1982
)
0.57
" 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

Bioavailability

The alpha 1-adrenoceptor antagonist indoramin is rapidly and extensively absorbed after oral administration, but with only low to moderate bioavailability (8-24% median) from the tablet (Baratol)

ExcerptReferenceRelevance
" 2 Following singleoral dosing the drug is well absorbed and extensively metabolised."( Pharmacokinetics of indoramin in man.
Dollery, CT; Draffan, GH; Firmin, JL; Jordan, TW; Lewis, PJ, 1976
)
0.58
" The alpha 1-adrenoceptor antagonist indoramin is rapidly and extensively absorbed after oral administration, but with only low to moderate bioavailability (8-24% median) from the tablet (Baratol)."( A review of the clinical pharmacokinetics and metabolism of the alpha 1-adrenoceptor antagonist indoramin.
Pierce, DM, 1990
)
0.77
" Bioavailability is increased with a wide range of distribution from 12."( Pharmacokinetics of indoramin and its metabolite 6-hydroxyindoramin after single and multiple doses to cirrhotic liver patients.
Giesing, M; Neumann, G; Pierce, DM; Reimold, WV; Wilke, G, 1986
)
0.59
" The increased bioavailability of oral indoramin in the presence of ethanol may reflect some enhanced absorption, but it is also consistent with inhibition of first-pass metabolism of a flow-limited drug."( Pharmacokinetic interaction between indoramin and ethanol.
Abrams, SM; Franklin, RA; Hedges, A; Johnston, A; Pierce, DM; Turner, P, 1989
)
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

Dosage Studied

Chronic dosing with indoramin in hypercholesterolemic monkeys significantly raises high-density lipoprotein cholesterol levels. Indoramin dosage was subsequently adjusted in 25 mg steps (to maximum 150 mg da)

ExcerptRelevanceReference
" Dosage of indoramin was individually adjusted and ranged from 125 mg to 200 mg daily."( Indoramin in the treatment of hypertension: a placebo controlled trial.
Ramirez, J, 1976
)
2.09
" 2 Following singleoral dosing the drug is well absorbed and extensively metabolised."( Pharmacokinetics of indoramin in man.
Dollery, CT; Draffan, GH; Firmin, JL; Jordan, TW; Lewis, PJ, 1976
)
0.58
" the same order of magnitude as intra-subject variation seen in volunteers dosed repeatedly with indoramin."( The pharmacokinetics of oral indoramin during pregnancy.
Odendaal, HJ; Pierce, DM; Schabort, I, 1990
)
0.79
"The haemodynamic dose-response effects of intravenous indoramin were evaluated in 12 patients with acute heart failure (pulmonary artery occluded pressure of greater than 20 mm Hg) complicating a recent myocardial infarction."( Haemodynamic dose-response effects of intravenous indoramin in acute heart failure complicating myocardial infarction.
Frais, MA; Jackson, N; Nelson, GI; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
0.77
" Chronic dosing with indoramin in hypercholesterolemic monkeys significantly raises high-density lipoprotein cholesterol levels."( Recent developments in the pharmacology and pharmacokinetics of indoramin.
Archibald, JL, 1986
)
0.83
"Pharmacokinetic data obtained after intravenous and single and repeat chronic oral dosing of indoramin in nine patients with liver cirrhosis are described."( Pharmacokinetics of indoramin and its metabolite 6-hydroxyindoramin after single and multiple doses to cirrhotic liver patients.
Giesing, M; Neumann, G; Pierce, DM; Reimold, WV; Wilke, G, 1986
)
0.81
" After at least 6 months of treatment, the mean daily dosage of indoramin was higher among patients who received indoramin alone (122 mg/day) than among those who received indoramin plus a diuretic (92 mg/day)."( Antihypertensive therapy with indoramin in the elderly.
Allen, IE; Deitch, MW; Pascucci, VL, 1986
)
0.8
"05) the phenylephrine dose-response curve to the right on days 1 and 8 compared with placebo."( Effect of acute and chronic indoramin administration on baroreflex function and tremor in humans.
Deering, AH; Harron, DW; Riddell, JG; Shanks, RG, 1988
)
0.57
"In patas monkeys fed a high cholesterol diet, chronic dosing with the antihypertensive agent indoramin increases the cholesterol ratio by raising the plasma HDL-C concentration."( The effect of indoramin on plasma lipids in hypercholesterolemic patas monkeys.
Pierce, V; Shepperson, NB; West-Watson, A, 1985
)
0.85
"The pharmacokinetics of indoramin and its active 6-hydroxylated metabolite have been studied in healthy male volunteers after repeated oral dosing with 37."( Pharmacokinetics of indoramin and its 6-hydroxylated metabolite after repeated oral dosing.
Franklin, RA; Pierce, DM; Warrington, SJ,
)
0.76
" The results imply that the kinetic behaviour of indoramin within an individual will prove relatively consistent, despite widespread inter-subject variation, once an appropriate dosage regime has been established."( Intra- and inter-subject variation in the pharmacokinetics of indoramin and its 6-hydroxylated metabolite.
Abrams, SM; Franklin, RA; Pierce, DM, 1988
)
0.77
" Plasma concentrations of an active metabolite, 6-hydroxyindoramin, after single oral doses in either dosage form, were of a similar order to those of unchanged drug and fell with similar rapidity."( Pharmacokinetics and systemic availability of the antihypertensive agent indoramin and its metabolite 6-hydroxyindoramin in healthy subjects.
Abrams, SM; Franklin, RA; Pierce, DM, 1987
)
0.75
" This limited observation suggests that indoramin is a predominant venodilator acutely in patients with heart failure but that despite this effect it may worsen functional capacity and hemodynamics during continuous dosing in these patients."( Indoramin in heart failure: possible adverse effects on hemodynamics and exercise capacity.
Casebolt, P; Franciosa, JA; Galiè, N; Gimenez, H; Malloy, M; Seth, L, 1986
)
1.98
" Cumulative dose-response curves with epinephrine and norepinephrine showed graded contraction."( Adrenergic receptors and sympathetic agents in isolated human pulmonary arteries.
Boe, J; Simonsson, BG, 1980
)
0.26
") evoked dose-dependent shifts to the right of the dose-response curves to B-HT 933 whilst having minimal effects on the methoxamine dose-response curve."( An investigation into the selectivity of a novel series of benzoquinolizines for alpha 2-adrenoceptors in vivo.
Paciorek, PM; Pierce, V; Shepperson, NB; Waterfall, JF, 1984
)
0.27
" The dosage of indoramin was increased at 2-weekly intervals until control was obtained or until a maximum daily dosage of 150 mg was reached."( Indoramin as an antihypertensive agent in the treatment of essential hypertension. A multicentre trial.
Bednarek, MR; Schoeman, HS, 1983
)
2.06
" Clinical evaluation of a new agent such as indoramin in the management of hypertension is discussed in terms of efficacy, dosage regimen, tolerance, adverse effects, interactions, withdrawal syndrome, and long-term influence on the complications of high blood pressure."( Indoramin in the treatment of hypertension. A mini-review and update.
Archibald, JL; Turner, P, 1983
)
1.97
" Indoramin dosage was subsequently adjusted in 25 mg steps (to maximum 150 mg daily), if necessary, at follow-up control visits every 14 days."( Indoramin as second step therapy in the management of benign essential hypertension.
Gherardi, S; Manzoli, U; Mazzari, M; Montenero, AS; Schiavoni, G, 1983
)
2.62
" In many elderly patients, therefore, a reduction in dosage may be required due to the apparent reduction in clearance of indoramin."( Pharmacokinetics of oral indoramin in elderly and middle-aged female volunteers.
Franklin, RA; Marrott, PK; Norbury, HM; Warrington, SJ, 1984
)
0.78
" However, involuntary urine leakage associated with a change of posture occurred in 2 patients but subsided after the dosage of indoramin was decreased."( Possible use of indoramin in patients with chronic neurogenic bladder dysfunction.
Chary, KS; Rao, MS; Sharma, PL; Swamy, RP; Vaidyanathan, S, 1983
)
0.82
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
tryptaminesTryptamine and its substitution 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 (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency11.22020.01846.806014.1254AID624417
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.11870.707936.904389.1251AID504333
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.11873.548119.542744.6684AID743266
importin subunit beta-1 isoform 1Homo sapiens (human)Potency50.11875.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency50.11875.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency50.11875.804816.996225.9290AID540253
DNA polymerase kappa isoform 1Homo sapiens (human)Potency37.68580.031622.3146100.0000AID588579
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency25.09990.005612.367736.1254AID624044
[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)
Alpha-1A adrenergic receptorOryctolagus cuniculus (rabbit)Ki0.00400.00000.02040.2512AID36753
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)125.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
Alpha-2A adrenergic receptorHomo sapiens (human)Ki2.24000.00010.807410.0000AID35951
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.52800.00020.725710.0000AID36231
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.01200.00000.50723.7020AID36461
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.47600.00030.483410.0000AID36408
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.11000.00000.929610.0000AID35328
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.11000.00000.970810.0000AID35328
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.11000.00000.937510.0000AID35328
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.61100.00000.575110.0000AID35603
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.13420.00000.360910.0000AID35328; AID35468
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00380.00000.272610.0000AID36617; AID36753
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.03130.00000.471310.0000AID37184; AID37336; AID37478
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 (121)

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)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo 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 (38)

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)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo 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 (32)

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)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (134)

Assay IDTitleYearJournalArticle
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Apr-16, Volume: 370, Issue:3
Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)1997British journal of pharmacology, Jul, Volume: 121, Issue:6
Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1997British journal of pharmacology, Jul, Volume: 121, Issue:6
Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)1997British journal of pharmacology, Jul, Volume: 121, Issue:6
Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
AID181139Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 4 hr after 12.5 mg/kg po administration;NS means nonsignificant difference between treated and control group1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID23960logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID26246Distribution coefficient between 1-Octanol and phosphate buffer at pH7.41981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID226777Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and heart rate response was reported to reduce by 10-25% after 4 hr at a peroral dose of 5 mg/kg1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID193601Percentage fall in systolic blood pressure after 4 hr at 12.5 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID226764Vasopressor responses to epinephrine as a measure of the alpha-1-adrenoceptor blocking activity at 5 mg/kg administered orally was reported to be antagonized1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
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.
AID660336Half life in human liver microsomes assessed as CYP2C19-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID26396Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID23976logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID23972logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID181297The percent fall in systolic blood pressure at 1.5 / 4 h after peroral administration of 50 mg/kg in DOCA/saline hypertensive rats at 2 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID193420Percentage fall in systolic blood pressure after 1 hr at 25 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
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.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID171603The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 40 mg/kg in conscious renal hypertensive rats (RHR).1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID59020Change in mean arterial pressure in anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID190267Starting systolic blood pressure at dose of 25 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
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.
AID226975Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and maximum decrease of mean arterial blood pressure (MABP) at 5 mg/kg oral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID35468Binding affinity was tested on human Alpha-1D adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
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.
AID540237Phospholipidosis-positive literature compound observed in rat
AID36562Affinity for alpha-1 adrenoceptor of rat cerebral cortex was determined by ligand binding using [3H]prazosin.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID181133Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 3h after 25 mg/kg po administration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID26310Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID181126Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 2 hr after 25 mg/kg po administration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID193442Percentage fall in systolic blood pressure after 2 hr at 12.5 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID226759Vasopressor responses to epinephrine as a measure of the alpha-1-adrenoceptor blocking activity at 25 mg/kg administered orally was reported to be antagonized1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID23966logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID36461The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID181119Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 1 hr after 25 mg/kg po administration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID23962logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
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.
AID193570Percentage fall in systolic blood pressure after 2 hr at 25 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID36124pA2 for Alpha-1 adrenergic receptor from human prostate.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID226972Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and maximum decrease of mean arterial blood pressure (MABP) at 2.5 mg/kg oral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID62086Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID181469Percentage fall in systolic blood pressure in spontaneously hypertensive rats after 2 hr following 50 mg/kg p.o.1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID181294The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 25 mg/kg in DOCA/saline hypertensive rats at 6 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID23973Partition coefficient (logD, measured by HPLC, log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
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.
AID23964logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID181295The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 50 mg/kg in DOCA/saline hypertensive rats at 24 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID36408Binding affinity against Alpha-2C adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID181145The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 10 mg/kg in DOCA/saline hypertensive rats at 24 hr; Non significant1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
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.
AID181293The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 25 mg/kg in DOCA/saline hypertensive rats at 2 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID26311logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID35603Binding affinity against Alpha-1D adrenergic receptor, from rat clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID181292The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 25 mg/kg in DOCA/saline hypertensive rats at 24 hr; Non significant, p>0.051980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID181125Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 2 hr after 12.5 mg/kg po administration;NS means nonsignificant difference between treated and control group1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID59018Change in mean arterial pressure in anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID193602Percentage fall in systolic blood pressure after 4 hr at 25 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID189474Apparent partition coefficient was measured as histamine releasing activity in rat mast cells.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID36645Affinity for alpha-2 adrenergic receptor of rat cerebral cortex was determined by ligand binding using [3H]yohimbine.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
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.
AID190268Starting systolic blood pressure at dose of 50 mg/kg in rat1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID23975logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID181299The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 50 mg/kg in DOCA/saline hypertensive rats at 6 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID181118Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 1 hr after 12.5 mg/kg po administration;NS means nonsignificant difference between treated and control group1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID660335Half life in human liver microsomes assessed as CYP2C9-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID62091Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID181474Percentage fall in systolic blood pressure in spontaneously hypertensive rats after 3 h following 50 mg/kg p.o.1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID37336The compound was tested for binding affinity against Alpha-1B adrenergic receptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID36231Binding affinity against Alpha-2B adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID37184The compound was tested for binding affinity against Alpha-1B adrenergic receptor, from hamster clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID193419Percentage fall in systolic blood pressure after 1 hr at 12.5 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID660333Half life in human liver microsomes assessed as CYP2B6-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID35328Binding affinity against Alpha-1D adrenergic receptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID181140Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 4 hr after 25 mg/kg po administration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID226757Vasopressor responses to epinephrine as a measure of the alpha-1-adrenoceptor blocking activity at 2.5 mg/kg administered orally was reported to be antagonized1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID37478Binding affinity was tested on human Alpha-1B adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID62090Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID190266Starting systolic blood pressure at dose of 10 mg/kg1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID181148The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 10 mg/kg in DOCA/saline hypertensive rats at 6 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID226963Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and activity rating was given with respect to MABP values at 25 mg/kg oral dose;lowering MABP by 20-30% at 5 mg/kg and by 10-20% at 1-2.5 mg/kg1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID660331Half life in human liver microsomes assessed as CYP3A4-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID59021Change in mean arterial pressure in anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID62084Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID181147The percent fall in systolic blood pressure at 1.5 / 4 hr after peroral administration of 10 mg/kg in DOCA/saline hypertensive rats at 2 hr1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antihypertensive ureidopiperidines.
AID36617The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID226973Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and maximum decrease of mean arterial blood pressure (MABP) at 25 mg/kg oral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
AID62087Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID660338Clearance in human liver microsomes at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID226780Antihypertensive activity was determined in cannulated spontaneously hypertensive rats(SHR) and marked bradycardia was reported at a dose of 25 mg/kg1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
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.
AID36753Binding affinity was tested on human Alpha-1A adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID35951The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
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.
AID193585Percentage fall in systolic blood pressure after 3 hr at 25 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID181132Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats 3h after 12.5 mg/kg po administration;NS means nonsignificant difference between treated and control group1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s.
AID193584Percentage fall in systolic blood pressure after 3 hr at 12.5 mg/kg given perorally1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID660334Half life in human liver microsomes assessed as CYP2C8-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID62088Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID181464Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats after a period of 1 hr for a dose of 50 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID62089Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID660332Half life in human liver microsomes assessed as CYP2D6-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID660337Half life in human liver microsomes assessed as CYP1A2-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID62085Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (221)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990165 (74.66)18.7374
1990's27 (12.22)18.2507
2000's16 (7.24)29.6817
2010's11 (4.98)24.3611
2020's2 (0.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.36

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index41.36 (24.57)
Research Supply Index5.71 (2.92)
Research Growth Index4.03 (4.65)
Search Engine Demand Index63.74 (26.88)
Search Engine Supply Index1.98 (0.95)

This Compound (41.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials65 (27.43%)5.53%
Reviews24 (10.13%)6.00%
Case Studies7 (2.95%)4.05%
Observational0 (0.00%)0.25%
Other141 (59.49%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]