Page last updated: 2024-11-04

alosetron

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Description

alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2099
CHEMBL ID1110
CHEBI ID253342
SCHEMBL ID631
MeSH IDM0240025

Synonyms (57)

Synonym
CHEMBL1110
a03ae01
unii-13z9hth115
13z9hth115 ,
HY-70050A
gtpl2296
lotronex
D07129
122852-42-0
alosetron (inn)
smr000469211
MLS001401464 ,
alosetron
DB00969
2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one
gr68755
1h-pyrido(4,3-b)indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-
alosetron [inn:ban]
NCGC00167528-01
5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one
5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indol-1-one
chebi:253342 ,
bdbm50014558
A804977
FT-0631108
bdbm93624
5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-3,4-dihydropyrid[4,3-b]indol-1-one;hydrochloride
cid_60758
CS-0640
alosetron [mi]
alosetron [who-dd]
alosetron [inn]
alosetron [vandf]
AB00698548-07
SCHEMBL631
DTXSID6044278 ,
5-methyl-2-(5-methyl-1h-imidazol-4-ylmethyl)-2,3,4,5-tetrahydro-pyrido[4,3-b]indol-1-one
2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-1h-pyrido[4,3-b]indol-1-one
2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-1h-pyrido[4,3-b]indol-1one
5-methyl-2-[(4-methyl-1h-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indol-1-one
Q-200612
5-methyl-2-(5-methyl-3h-imidazol-4-ylmethyl)-2,3,4,5-tetrahydro-pyrido[4,3-b]indol-1-one hydrochloride
5-methyl-2-[(5-methyl-1h-imidazol-4-yl)methyl]-1h,2h,3h,4h,5h-pyrido[4,3-b]indol-1-one
AKOS027427023
5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indol-1-one
Q416463
BCP14060
HMS3745K07
'5-methyl-2-[(4-methyl-1~{h}-imidazol-5-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one'
5-methyl-2-((4-methyl-1h-imidazol-5-yl)methyl)-2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indol-1-one
EN300-18563823
AS-83859
gtpl12214
test_ligand_3
5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-2,3,4,5-tetrahydro-1h-pyrido(4,3-b)indol-1-one
alosetronum
dtxcid4024278

Research Excerpts

Overview

Alosetron is a potent, selective 5-HT(3) receptor antagonist prescribed for women with severe diarrhea-predominant irritable bowel syndrome (IBS-D) under a risk management plan (RMP) It is well absorbed with a long pharmacodynamic half-life.

ExcerptReferenceRelevance
"Alosetron is a potent, selective 5-HT(3) receptor antagonist prescribed for women with severe diarrhea-predominant irritable bowel syndrome (IBS-D) under a risk management plan (RMP). "( Ischemic colitis and complications of constipation associated with the use of alosetron under a risk management plan: clinical characteristics, outcomes, and incidences.
Ameen, V; Chang, L; Tong, K, 2010
)
2.03
"Alosetron is a potent and highly selective serotonin 5-HT(3 )receptor antagonist that in large randomised controlled clinical trials has been shown to be clinically efficient in female patients with diarrhoea-predominant IBS."( Reassessing the benefits and risks of alosetron: what is its place in the treatment of irritable bowel syndrome?
Andresen, V; Hollerbach, S, 2004
)
1.32
"Alosetron is a highly selective 5-HT3 antagonist which normalizes perturbed small intestinal propulsion."( The pharmacological properties of the novel selective 5-HT3 receptor antagonist, alosetron, and its effects on normal and perturbed small intestinal transit in the fasted rat.
Barrett, VJ; Bountra, C; Butler, A; Cambridge, D; Clayton, NM; Gale, J; Humphrey, PP; Hunt, AA; Maxwell, MP; Sargent, R, 1999
)
1.25
"Alosetron is a highly selective, potent 5-HT3 receptor antagonist which is well absorbed with a long pharmacodynamic half-life."( Review article: the therapeutic potential of 5-HT3 receptor antagonists in the treatment of irritable bowel syndrome.
Bountra, C; Clayton, N; Humphrey, PP; Kozlowski, K, 1999
)
1.02
"Alosetron is a potent and highly selective serotonin 5-HT3 receptor antagonist which has been evaluated for the management of irritable bowel syndrome (IBS). "( Alosetron.
Balfour, JA; Goa, KL; Perry, CM, 2000
)
3.19
"Alosetron is a potent and selective 5-HT3 receptor antagonist, which has been shown to be beneficial in the treatment of female patients with non-constipated irritable bowel syndrome."( Alosetron, a 5-HT3 receptor antagonist, delays colonic transit in patients with irritable bowel syndrome and healthy volunteers.
Foster, JM; Houghton, LA; Whorwell, PJ, 2000
)
3.19
"Alosetron (Lotronex) is a potent, highly selective 5-HT(3) antagonist. "( Pharmacology and clinical experience with alosetron.
Camilleri, M, 2000
)
2.01
"Alosetron is a potent and selective serotonin antagonist that recently became the first Food and Drug Administration-approved agent for diarrhea-predominant IBS."( Ischemic colitis during treatment with alosetron.
Fisher, RS; Friedel, D; Thomas, R, 2001
)
1.3
"Alosetron (Lotronex) is a new therapeutic agent for irritable bowel syndrome (IBS) in women with diarrhea-predominant IBS. "( Tolerability and safety of alosetron during long-term administration in female and male irritable bowel syndrome patients.
Chey, WY; Dukes, GE; Harding, J; Heath, AT; Hunt, CM; McSorley, DJ; Washington, MK; Wolfe, SG, 2001
)
2.05
"Alosetron (Lotronex) is a serotonin subtype 3 (5-HT3) receptor antagonist that alleviates symptoms of irritable bowel syndrome (IBS) in female patients. "( Effects of alosetron on spontaneous migrating motor complexes in murine small and large bowel in vitro.
Bush, TG; Sanders, KM; Smith, TK; Spencer, NJ; Watters, N, 2001
)
2.14
"Alosetron is a 5-hydroxytryptamine-3 receptor antagonist reducing symptoms in female patients with diarrhoea-predominant irritable bowel syndrome, and is known to increase the colonic transit time."( Effect of alosetron on left colonic motility in non-constipated patients with irritable bowel syndrome and healthy volunteers.
Clemens, CH; Fabri, M; Samsom, M; Smout, AJ; Van Berge Henegouwen, GP, 2002
)
2.16

Effects

Alosetron has been shown to produce statistically significant improvements in abdominal pain, stool consistency and urgency in female IBS patients. At high repeated dosing, clinical signs were transient and repeated administration produced no significant adverse effects on fertility.

ExcerptReferenceRelevance
"Alosetron has been shown to produce statistically significant improvements in abdominal pain, stool consistency, stool frequency and urgency in female IBS patients."( Review article: the safety and efficacy of alosetron, a 5-HT3 receptor antagonist, in female irritable bowel syndrome patients.
Mangel, AW; Northcutt, AR, 1999
)
1.29
"Alosetron has proved safe in a range of toxicity studies; at high repeated dosing, clinical signs were transient and repeated administration produced no significant adverse effects on fertility, reproductive performance or fetal development."( Pharmacology and clinical experience with alosetron.
Camilleri, M, 2000
)
1.29

Actions

Alosetron does not cause adverse pharmacodynamic effects. It is absorbed rapidly after oral administration and is widely distributed throughout tissues after oral or iv.

ExcerptReferenceRelevance
"Alosetron does not cause adverse pharmacodynamic effects, is absorbed rapidly after oral administration and is widely distributed throughout tissues after oral or iv."( Pharmacology and clinical experience with alosetron.
Camilleri, M, 2000
)
1.29
"Alosetron appeared to increase the overall periprandial frequency in the sigmoid colon (P=0.043) and the mean amplitude of colonic contractions in the descending colon (P=0.007). "( Effect of alosetron on left colonic motility in non-constipated patients with irritable bowel syndrome and healthy volunteers.
Clemens, CH; Fabri, M; Samsom, M; Smout, AJ; Van Berge Henegouwen, GP, 2002
)
2.16

Treatment

Alosetron treatment increased basal jejunal fluid absorption (median 5.1 mL/cm/h [interquartile range 4.2 to 7.1] compared with placebo (3.8 [3.6 to 4.3] P = 0.028, two sided Wilcoxon matched pairs signed rank test) Alosetra-treated patients showed improvements in bowel functions compared to placebo- treated patients. Pretreatment with alosetro (100 microg/kg) significantly reduced numbers of Fos-LI neurones.

ExcerptReferenceRelevance
"Alosetron treatment improved HRQOL scores for all domains (p < .0001)."( Alosetron versus traditional pharmacotherapy in clinical practice: effects on resource use, health-related quality of life, safety and symptom improvement in women with severe diarrhea-predominant irritable bowel syndrome.
Chey, WD; Chuang, E; Earnest, DL; Olden, KW; Paul Nicandro, J; Shringarpure, R, 2019
)
2.68
"Alosetron-treated patients had significantly greater 48-wk average adequate relief (p= 0.01) and urgency control (p < 0.001) rates, regardless of rescue medication use, compared with placebo. "( Long-term safety and efficacy of alosetron in women with severe diarrhea-predominant irritable bowel syndrome.
Ameen, VZ; Carter, EG; Chey, WD; Chey, WY; Dukes, GE; Heath, AT; Northcutt, A, 2004
)
2.05
"Alosetron vs placebo treatments, in a randomized, double-blinded, crossover manner, were studied."( The effects of the 5-HT3 antagonist, alosetron, on brain serotonin synthesis in patients with irritable bowel syndrome.
D'Souza, D; Diksic, M; Kersey, K; Kumakura, Y; Nakai, A, 2005
)
1.32
"alosetron treated rats failed to demonstrate any alteration in the VMR."( Effects of the 5-HT3 receptor antagonist, alosetron, in a rat model of somatic and visceral hyperalgesia.
McLean, PG; Miranda, A; Peles, S; Sengupta, JN, 2006
)
1.32
"Alosetron treatment increased basal jejunal fluid absorption (median 5.1 mL/cm/h [interquartile range 4.2 to 7.1] compared with placebo (3.8 [3.6 to 4.3] P = 0.028, two sided Wilcoxon matched pairs signed rank test)). "( In vivo effects of the 5-HT3 antagonist alosetron on basal and cholera toxin-induced secretion in the human jejunum: a segmental perfusion study.
André, EA; Bearcroft, CP; Farthing, MJ, 1997
)
2.01
"Alosetron-treated patients showed improvements in bowel functions compared to placebo-treated patients."( Alosetron controls bowel urgency and provides global symptom improvement in women with diarrhea-predominant irritable bowel syndrome.
Bagby, B; Carter, E; Decker, C; Gordon, S; Jhingran, P; Lembo, T; Wright, RA, 2001
)
2.47
"Pretreatment with alosetron (100 microg/kg) significantly reduced numbers of Fos-LI neurones to 479.8."( The 5-HT(3) receptor antagonist alosetron inhibits the colorectal distention induced depressor response and spinal c-fos expression in the anaesthetised rat.
Boissonade, FM; Bountra, C; Green, A; Grundy, D; Kozlowski, CM, 2000
)
0.91

Toxicity

Constipation is the most common adverse event with alosetron treatment. Adverse events were reported by 83% (530/640) and 76% (159/210) of subjects in the alosETron and placebo groups.

ExcerptReferenceRelevance
" The only adverse event of note with alosetron was constipation, and this represents a class effect of 5-HT3 receptor antagonists."( Review article: the safety and efficacy of alosetron, a 5-HT3 receptor antagonist, in female irritable bowel syndrome patients.
Mangel, AW; Northcutt, AR, 1999
)
0.84
" Constipation is the most frequent adverse event, with a higher incidence of transient constipation in alosetron-treated patients, typically occurring in the first month of treatment."( Tolerability and safety of alosetron during long-term administration in female and male irritable bowel syndrome patients.
Chey, WY; Dukes, GE; Harding, J; Heath, AT; Hunt, CM; McSorley, DJ; Washington, MK; Wolfe, SG, 2001
)
0.82
" Adverse events and serious adverse events were similar between treatment groups, except for constipation."( Long-term safety and efficacy of alosetron in women with severe diarrhea-predominant irritable bowel syndrome.
Ameen, VZ; Carter, EG; Chey, WD; Chey, WY; Dukes, GE; Heath, AT; Northcutt, A, 2004
)
0.6
" Constipation was the most common adverse event and occurred in a dose-related manner among subjects receiving alosetron, 9% (0."( A dose-ranging, phase II study of the efficacy and safety of alosetron in men with diarrhea-predominant IBS.
Ameen, VZ; Carter, EG; Chang, L; Dukes, GE; Mayer, EA; McSorley, DJ, 2005
)
0.78
" Constipation is the most common adverse event with alosetron treatment."( A randomized, double-blind, placebo-controlled study to assess efficacy and safety of 0.5 mg and 1 mg alosetron in women with severe diarrhea-predominant IBS.
Ameen, V; Carter, EG; Gordon, SH; Heath, AT; Krause, R; Perschy, T; West, M, 2007
)
0.81
" Initial use was widespread, but infrequent serious adverse events of ischemic colitis and severe constipation-related complications prompted alosetron's voluntary withdrawal from the US market in November 2000."( Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective.
Lewis, JH, 2010
)
2
"The Federal Adverse Event Reporting System was queried for the time between January 2004 and September 2015."( Ischemic Colitis as a Complication of Medication Use: An Analysis of the Federal Adverse Event Reporting System.
Bielefeldt, K, 2016
)
0.43
" In 8 %, the adverse event contributed to the patient's death with male sex and older age predicting fatal outcomes."( Ischemic Colitis as a Complication of Medication Use: An Analysis of the Federal Adverse Event Reporting System.
Bielefeldt, K, 2016
)
0.43
" This information may not only explain the development of this serious adverse event, but could also guide treatment decisions, cautioning healthcare providers when considering these agents in persons with known risk factors or other drugs that may increase their risk of IC."( Ischemic Colitis as a Complication of Medication Use: An Analysis of the Federal Adverse Event Reporting System.
Bielefeldt, K, 2016
)
0.43
" Incidence of adverse events during alosetron use was not remarkable and was similar to that previously reported."( Alosetron versus traditional pharmacotherapy in clinical practice: effects on resource use, health-related quality of life, safety and symptom improvement in women with severe diarrhea-predominant irritable bowel syndrome.
Chey, WD; Chuang, E; Earnest, DL; Olden, KW; Paul Nicandro, J; Shringarpure, R, 2019
)
2.23

Pharmacokinetics

Alosetron co-administration did not have a significant effect on the pharmacokinetics of S- and R-fluoxetine. The results showed small delays in peak concentration but no clinically significant effect.

ExcerptReferenceRelevance
" Mean pharmacokinetic parameters of haloperidol in the presence of alosetron and placebo treatments were not significantly (P > ."( Effect of alosetron (a new 5-HT3 receptor antagonist) on the pharmacokinetics of haloperidol in schizophrenic patients.
Gupta, SK; Kunka, RL; Lloyd, T; Metz, A; Perel, JM; Rudolph, G, 1995
)
0.93
" The results showed small delays in peak concentration but no clinically significant effect of alosetron on the pharmacokinetics of S- and R-fluoxetine or S- and R-norfluoxetine."( Effect of alosetron on the pharmacokinetics of fluoxetine.
D'Souza, DL; Dimmitt, DC; Koch, KM; Nezamis, J; Robbins, DK; Simms, L, 2001
)
0.93
" This study assessed the effect of alosetron co-administration on pharmacodynamic markers of contraceptive efficacy, on the pharmacokinetics of estrogen and progesterone OC components, and on the activity of biochemical markers for the risk of thrombosis."( Pharmacodynamics and pharmacokinetics of oral contraceptives co-administered with alosetron (Lotronex).
Ameen, VZ; Baidoo, CA; Campanella, C; Kersey, KE; Koch, K; Manzo, JA, 2004
)
0.83
" 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

Alosetron is a highly selective, potent 5-HT3 receptor antagonist. It has approximately 60% bioavailability and a half-life of 1. In pharmacokinetic studies, bioavailability in healthy volunteers is approximately 60%.

ExcerptReferenceRelevance
" Alosetron is a highly selective, potent 5-HT3 receptor antagonist which is well absorbed with a long pharmacodynamic half-life."( Review article: the therapeutic potential of 5-HT3 receptor antagonists in the treatment of irritable bowel syndrome.
Bountra, C; Clayton, N; Humphrey, PP; Kozlowski, K, 1999
)
1.21
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34

Dosage Studied

High adherence to recommended dosing at baseline and follow-up suggests that the risk management programme is encouraging safe use of alosetron. Therefore, alprazolam may be safely coadministered with alsetron without the need for dosage adjustment.

ExcerptRelevanceReference
" This study evaluated the effect of oral alosetron dosing on the pharmacokinetics of haloperidol, the latter being administered daily to 13 schizophrenic patients for 56 days."( Effect of alosetron (a new 5-HT3 receptor antagonist) on the pharmacokinetics of haloperidol in schizophrenic patients.
Gupta, SK; Kunka, RL; Lloyd, T; Metz, A; Perel, JM; Rudolph, G, 1995
)
0.96
" At the end of each dosing period, both isobarometric and isovolumetric gastric distensions were performed using an electronic barostat."( Alosetron does not affect the visceral perception of gastric distension in healthy subjects.
Bruley des Varannes, S; Galmiche, JP; Isal, JP; McDonald, J; Oriola, RC; Zerbib, F, 1994
)
1.73
" dosing in animals."( Pharmacology and clinical experience with alosetron.
Camilleri, M, 2000
)
0.57
" Therefore, alprazolam may be safely coadministered with alosetron without the need for dosage adjustment."( Effect of alosetron on the pharmacokinetics of alprazolam.
D'Souza, DL; Koch, KM; Levasseur, LM; Nezamis, J; Robbins, DK; Simms, L, 2001
)
0.96
" Recommended starting dosage was 1 mg/day for 4 weeks."( The relationship between dosing of alosetron and discontinuation patterns reported by patients participating in a follow-up programme.
Andrews, E; Cook, S; Hickman, P; Hollis, K; Miller, D; Tennis, P, 2007
)
0.62
" Adherence to recommended starting dosage did not vary by status at end of follow-up, previous alosetron experience or age."( The relationship between dosing of alosetron and discontinuation patterns reported by patients participating in a follow-up programme.
Andrews, E; Cook, S; Hickman, P; Hollis, K; Miller, D; Tennis, P, 2007
)
0.84
"High adherence to recommended dosing at baseline and follow-up suggests that the risk management programme is encouraging safe use of alosetron, including adherence to dosing recommendations."( The relationship between dosing of alosetron and discontinuation patterns reported by patients participating in a follow-up programme.
Andrews, E; Cook, S; Hickman, P; Hollis, K; Miller, D; Tennis, P, 2007
)
0.82
" Multiple dosing regimens were assessed in a randomized, double-blind, placebo-controlled study (S3B30040) to determine efficacy, tolerability, and evaluate constipation rate."( A randomized, double-blind, placebo-controlled study to assess efficacy and safety of 0.5 mg and 1 mg alosetron in women with severe diarrhea-predominant IBS.
Ameen, V; Carter, EG; Gordon, SH; Heath, AT; Krause, R; Perschy, T; West, M, 2007
)
0.55
" Lower dosing regimens resulted in a decreased constipation rate."( A randomized, double-blind, placebo-controlled study to assess efficacy and safety of 0.5 mg and 1 mg alosetron in women with severe diarrhea-predominant IBS.
Ameen, V; Carter, EG; Gordon, SH; Heath, AT; Krause, R; Perschy, T; West, M, 2007
)
0.55
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
antiemeticA drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral receptors.
gastrointestinal drugA drug used for its effects on the gastrointestinal system, e.g. controlling gastric acidity, regulating gastrointestinal motility and water flow, and improving digestion.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
pyridoindole
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
[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 (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)5.30240.00011.774010.0000AID552300; AID625245
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.60000.00011.753610.0000AID1141234; AID526453; AID552299
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)10.00000.00002.015110.0000AID552304
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)10.00000.00002.800510.0000AID552302
Cytochrome P450 2B6Homo sapiens (human)IC50 (µMol)10.00000.00113.418610.0000AID552301
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)10.00000.00002.398310.0000AID552303
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.10000.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.06400.00030.769310.0000AID625217
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00050.00000.74119.9000AID1141224; AID526452; AID552106
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)3.06800.00091.901410.0000AID161281; AID243151; AID397743; AID408340; AID526455
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (106)

Processvia Protein(s)Taxonomy
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (57)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID1141237Inhibition of 5-HT induced-bradycardia in ICR mouse von Bezold-Jarisch reflex model at 1 mg/kg, po after 60 mins relative to control2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
The discovery of diazepinone-based 5-HT3 receptor partial agonists.
AID526453Inhibition of human CYP3A42010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
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.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID526462Cardioprotective effect in po dosed mouse assessed as inhibition of 5-HT-induced bradycardia administered 1 hr prior to 5-HT challenge2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
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.
AID552303Inhibition of human CYP2C192011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552301Inhibition of human CYP2B62011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID526452Binding affinity to human HT3A receptor2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
AID1141224Displacement of [9-methyl-3H]BRL-43694 from human 5-HT3A receptor after overnight incubation by scintillation proximity assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
The discovery of diazepinone-based 5-HT3 receptor partial agonists.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID552110Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells at 3 uM relative to 5HT2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552106Binding affinity to human 5HT3A receptor2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552300Inhibition of human CYP1A22011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID552302Inhibition of human CYP2C92011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1141234Inhibition of CYP3A4 (unknown origin)2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
The discovery of diazepinone-based 5-HT3 receptor partial agonists.
AID397743Inhibition of human ERG channel2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID537019Reduction in wrap restraint stress-induced defecation in rat diarrhea-predominant irritable bowel syndrome model at 1 to 10 mg/kg, po administered 1 hr prior to induction of stress2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
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.
AID552299Inhibition of human CYP3A42011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1141235Intrinsic clearance in human liver microsomes2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
The discovery of diazepinone-based 5-HT3 receptor partial agonists.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID552297Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 100 uM 5-chloroindole-induced increase in intracellular calcium release at 3 uM relative to 5-HT2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID552304Inhibition of human CYP2D62011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID526455Inhibition of human ERG expressed in HEK cells by patch clamp technique2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID526456Bioavailability in rat at 10 mg/kg, po or 1 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
AID552309Partial agonist activity at 5HT3 receptor in po dosed mouse assessed inhibition of serotonin-induced bradycardia administered 1 hr before serotonin challenge by von Bezold-Jarisch reflex test2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID552305Intrinsic clearance in human liver microsomes assessed per mg of protein2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID526454Intrinsic clearance in human liver microsomes2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
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.
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.
AID493017Wombat Data for BeliefDocking2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (217)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's21 (9.68)18.2507
2000's157 (72.35)29.6817
2010's36 (16.59)24.3611
2020's3 (1.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 71.05

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 Index71.05 (24.57)
Research Supply Index5.58 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index124.73 (26.88)
Search Engine Supply Index2.03 (0.95)

This Compound (71.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials37 (16.37%)5.53%
Reviews59 (26.11%)6.00%
Case Studies3 (1.33%)4.05%
Observational0 (0.00%)0.25%
Other127 (56.19%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A 12-Week, Randomized, Double-Blind, Placebo- Controlled Study of PRN BID and Fixed Dosing Regimens of Alosetron in Female Subjects With Severe Diarrhea-Predominant Irritable Bowel Syndrome Who Have Failed Conventional Therapy [NCT00067457]Phase 3700 participants (Actual)Interventional2003-06-30Completed
A Four-week, Open, Multicenter Study to Assess the Safety and Efficacy of 1 mg Once Daily (QD) of GR68755 in Female Subjects With Severe Diarrhea-predominant Irritable Bowel Syndrome (IBS) Who Have Frequent Bowel Urgency [NCT01855711]Phase 232 participants (Actual)Interventional2003-09-18Completed
A Randomize, Placebo-controlled, Crossover Study to Measure the Effect of Alosetron on Mucosal Blood Flow in Female Healthy Volunteers and Diarrhea-predominant IBS Subjects [NCT00370032]Phase 449 participants (Actual)Interventional2006-12-31Completed
A Twelve-Week, Randomized, Double Blind, Placebo-Controlled, Parallel-Group Study to Assess the Safety and Efficacy of 0.5 mg QD, 1 mg QD and 1 mg BID of Alosetron in Female Subjects With Severe Diarrhea-predominant IBS Who Have Failed Conventional Therap [NCT00067561]Phase 3702 participants (Actual)Interventional2003-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00370032 (3) [back to overview]Left Colon and Rectal Mucosal Blood Flow Cohort Comparisons
NCT00370032 (3) [back to overview]Left Colon Mucosal Blood Flow (MBF)
NCT00370032 (3) [back to overview]Rectal Mucosal Blood Flow (MBF)

Left Colon and Rectal Mucosal Blood Flow Cohort Comparisons

On Day 6 of each treatment period approximately 1 hour after dosing, subjects underwent a flexible sigmoidoscopy with Laser Doppler Flowmetry (LDF) to measure Mucosal Blood Flow (MBF). There was no pre-treatment LDF procedure, MBF was compared between the Healthy and d-IBS cohorts using the flow rates from the placebo treatment period. (NCT00370032)
Timeframe: Day 6 after each treatment period

Interventionml per minute per 100 grams of tissue (Mean)
d-IBS Placebo - Left Colon135.1
d-IBS Placebo - Rectal178.9
Healthy Volunteers Placebo - Left Colon149.9
Healthy Volunteers Placebo - Rectal166.6

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Left Colon Mucosal Blood Flow (MBF)

On Day 6 of each treatment period; 1 hour after dosing, subjects underwent a flexible sigmoidoscopy with Laser Doppler Flowmetry (LDF) to measure Mucosal Blood Flow (MBF). There were no pre-treatment LDF procedure, MBF was compared between the Healthy volunteers and D-irritable bowel syndrome (IBS) cohorts using the flow rates from the placebo treatment period. (NCT00370032)
Timeframe: Day 6 after each treatment period

Interventionml per minute per 100 grams of tissue (Mean)
d-IBS Placebo125.6
d-IBS Alosetron117.5
Healthy Volunteers Placebo130.7
Healthy Volunteers Alosetron121.6

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Rectal Mucosal Blood Flow (MBF)

On Day 6 of each treatment period approximately 1 hour after dosing, subjects underwent a flexible sigmoidoscopy with Laser Doppler Flowmetry (LDF) to measure Mucosal Blood Flow (MBF). There was no pre-treatment LDF procedure, MBF was compared between the Healthy and d-IBS cohorts using the flow rates from the placebo treatment period. (NCT00370032)
Timeframe: Day 6 after each treatment period

Interventionml per minute per 100 grams of tissue (Mean)
d-IBS Placebo173
d-IBS Alosetron159.1
Healthy Volunteers Placebo149.1
Healthy Volunteers Alosetron140.3

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