Alosetron Hydrochloride (GR 68755 Hydrochloride) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: Target: 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.
References:
[1]. 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.
[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]. Turgeon DK, Tayeh N, Fontana RJ.Acute hepatitis associated with alosetron (Lotronex).J Clin Gastroenterol. 2005 Aug;39(7):641-2.
[5]. Miller DP, Alfredson T, Cook SF, Sands BE, Walker AM.Incidence of colonic ischemia, hospitalized complications of constipation, and bowel surgery in relation to use of alosetron hydrochloride.Am J Gastroenterol. 2003 May;98(5):1117-22.