Alosetron

• CAT Number: I000889
• CAS Number: 122852-42-0
• Molecular Formula: C17H18N4O
• Molecular Weight: 294.35
• Purity: ≥95%
• Target: 5-HT3 receptor antagonist
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IUPAC Name: 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one
• InChI: InChI=1S/C17H18N4O/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)
• InChIKey: JSWZEAMFRNKZNL-UHFFFAOYSA-N
• SMILES: CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C

Alosetron (Cat.No:I000889) is a selective 5-HT3 receptor antagonist used to treat irritable bowel syndrome with diarrhea (IBS-D) in women. Alosetron slows down the movement of stools in the gut, resulting in decreased frequency and urgency of bowel movements.

Reference

1:Development of a Forced Degradation Profile of Alosetron by Single Mode Reversed-Phase HPLC, LC-MS, and its Validation. Karthik Y, Babu B, Meyyanathan SN.Sci Pharm. 2014 Dec 29;83(2):311-20. doi: 10.3797/scipharm.1411-07. Print 2015 Apr-Jun. PMID: 26839817 Free PMC Article2:Rifaximin and eluxadoline – newly approved treatments for diarrhea-predominant irritable bowel syndrome: what is their role in clinical practice alongside alosetron? Cash BD, Lacy BE, Rao T, Earnest DL.Expert Opin Pharmacother. 2016;17(3):311-22. doi: 10.1517/14656566.2016.1118052. Epub 2015 Dec 8. Review. PMID: 26559529 3:Application of a UPLC-MS/MS method for the analysis of alosetron in human plasma to support a bioequivalence study in healthy males and females. Chaudhary DV, Patel DP, Shah JV, Shah PA, Sanyal M, Shrivastav PS.Biomed Chromatogr. 2015 Oct;29(10):1527-34. doi: 10.1002/bmc.3454. Epub 2015 Mar 11. PMID: 25761551 4:A 9-year evaluation of temporal trends in alosetron postmarketing safety under the risk management program. Tong K, Nicandro JP, Shringarpure R, Chuang E, Chang L.Therap Adv Gastroenterol. 2013 Sep;6(5):344-57. doi: 10.1177/1756283X13491798. PMID: 24003335 Free PMC Article5:Randomised clinical trial: alosetron improves quality of life and reduces restriction of daily activities in women with severe diarrhoea-predominant IBS. Cremonini F, Nicandro JP, Atkinson V, Shringarpure R, Chuang E, Lembo A.Aliment Pharmacol Ther. 2012 Sep;36(5):437-48. doi: 10.1111/j.1365-2036.2012.05208.x. Epub 2012 Jul 10. PMID: 22779693 Free PMC Article6:Irritable bowel syndrome and ischemic colitis: evidence supporting the increased use of alosetron. Lucak S.Therap Adv Gastroenterol. 2012 Jul;5(4):215-8. doi: 10.1177/1756283X12450934. No abstract available. PMID: 22778787 Free PMC Article7:Evaluation of treatment continuation with alosetron by IBS-D severity criteria. Nicandro JP, Shin P, Chuang E.Curr Med Res Opin. 2012 Mar;28(3):449-56. doi: 10.1185/03007995.2011.653435. Epub 2012 Feb 7. PMID: 22313141 8:Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes. Bleser S.Curr Med Res Opin. 2011 Mar;27(3):503-12. doi: 10.1185/03007995.2010.547933. Epub 2011 Jan 6. Review. PMID: 21208139 9:Optimizing outcomes with alosetron hydrochloride in severe diarrhea-predominant irritable bowel syndrome. Lucak SL.Therap Adv Gastroenterol. 2010 May;3(3):165-72. doi: 10.1177/1756283X10362277. PMID: 21180598 Free PMC Article10:Ischemic colitis and complications of constipation associated with the use of alosetron under a risk management plan: clinical characteristics, outcomes, and incidences. Chang L, Tong K, Ameen V.Am J Gastroenterol. 2010 Apr;105(4):866-75. doi: 10.1038/ajg.2010.25. Epub 2010 Mar 2. PMID: 20197759