A 5-HT3 receptor antagonist (Kis = 0.3 and 0.4 nM at rat cortical and human recombinant receptors

Alosetron (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
122852-69-1
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Alosetron is a potent and selective antagonist of the serotonin (5-HT) receptor subtype 5-HT3 with Ki values of 0.3 and 0.4 nM at the rat cortical and human recombinant receptors, respectively.{39117} It has no activity at α1-, β1-, and β2- adrenergic, M1, M2, and M3 muscarinic, GABAA, D2 dopamine, or nicotinic receptors at concentrations up to 10 μM.{39120} In vitro, alosetron blocks activation of 5-HT3 receptors, which prevents depolarization of the isolated rat vagus nerve (Ki = 0.2 nM). Alosetron (0.1 mg/kg) reduces wrap restraint stress-induced defecation and the number of abdominal muscle contractions in a rat model of irritable bowel syndrome with diarrhea (IBS-D).{39118} Formulations containing alosetron are in clinical trials for treatment of severe IBS-D in women.{39119}  

 

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Description

A 5-HT3 receptor antagonist (Kis = 0.3 and 0.4 nM at rat cortical and human recombinant receptors, respectively); no activity at α1-, β1-, and β2- adrenergic, M1, M2, and M3 muscarinic, GABAA, D2, or nicotinic receptors up to 10 μM; blocks activation of 5-HT3 receptors (Ki = 0.2 nM); reduces wrap restraint stress-induced defecation and the number of abdominal muscle contractions in a rat model of IBS-D,

Formal name: 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride

Synonyms:  GR 68755

Molecular weight: 330.8

CAS: 122852-69-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation|Gastric Disease|IBS||Research Area|Neuroscience

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