Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) 是5-HT3受体拮抗剂，可作用于肠易激综合征。
CAS：122852-43-1
分子式：C21H22N4O5
分子量：410.42
纯度：98%
存储：Store at -20°C

Background:

Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: N/ATarget: 5-HT ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron’s 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.

[1]. Bleser S.Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes.Curr Med Res Opin. 2011 Mar;27(3):503-12. [2]. Lucak SL.Optimizing outcomes with alosetron hydrochloride in severe diarrhea-predominant irritable bowel syndrome.Therap Adv Gastroenterol. 2010 May;3(3):165-72. [3]. Lewis JH.Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective.Expert Rev Gastroenterol Hepatol. 2010 Feb;4(1):13-29. [4]. Painsipp E, Shahbazian A, Holzer P.Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats.Br J Pharmacol. 2009 Nov;158(5):1210-26. [5]. Targeting the 5-HT3 receptor in the treatment of irritable bowel syndrome By Spiller, Robin C.From Current Opinion in Pharmacology (2011), 11(1), 68-74.