Formulation: A crystalline solid
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
Purity: ≥98%
Formula Markup: C17H18N4O • HCl
Formula Weight: 330,8
Shelf life (days): 1460
CAS Number: 122852-69-1
Notes: 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).{39117} It is selective for 5-HT3 over 5-HT2 and 5-HT1A receptors (Kis = 6.3 and >100 µM, respectively), as well as α1-, β1-, and β2- adrenergic, M1, M2, and M3 muscarinic, GABAA, dopamine D2, and nicotinic receptors at 10 μM.{39120} Alosetron (0.3-10 nM) inhibits 5-HT-induced depolarization of isolated rat vagus nerve.{39117} 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.{39118} Formulations containing alosetron have been used in the treatment of diarrhea-predominant irritable bowel syndrome in women.
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