Alosetron (hydrochloride)

Alosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Kis = 0.3 and 0.4 nM for the rat cortical and human recombinant receptors, respectively). It is selective for 5-HT3 over 5-HT2 and 5-HT1A receptors (Kis = 6.3 and >100 µM, respectively), as well as alpha1-, beta1-, and beta2- adrenergic, M1, M2, and M3 muscarinic, GABAA, dopamine D2, and nicotinic receptors at 10 µM. Alosetron (0.3-10 nM) inhibits 5-HT-induced depolarization of isolated rat vagus nerve. It 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) when administered at a dose of 0.1 mg/kg. Formulations containing alosetron have been used in the treatment of diarrhea-predominant irritable bowel syndrome in women.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. CAS Number: 122852-69-1. Synonyms: GR 68755. Molecular Formula: C17H18N4O . HCl. Formula Weight: 330.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/mL, DMSO: 20 mg/mL, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/mL, Ethanol: 0.5 mg/mL. lambdamax: 218, 259, 294 nm. SMILES: CN(C1=C2C=CC=C1)C3=C2C(N(CC4=C(C)NC=N4)CC3)=O.Cl. InChi Code: InChI=1S/C17H18N4O.ClH/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2,/h3-6,10H,7-9H2,1-2H3,(H,18,19),1H. InChi Key: FNYQZOVOVDSGJH-UHFFFAOYSA-N.