Alosetron Hydrochloride  (Synonyms: GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride)

Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC₅₀ at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects^[1][2].

Dexamethasone and Alosetron-treated (1 mg/kg; ip; daily for 6 days) rats exhibits a significant decrease in the diarrhea index, in comparison with TNBS-control group, especially after the initial 2 days of treatment following the induction of colitis^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

330.81

Solid

C₁₇H₁₉ClN₄O

122852-69-1

O=C(C(C1=C2C=CC=C1)=C(N2C)CC3)N3CC4=C(NC=N4)C.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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.  [Content Brief]

  [4]. Turgeon DK, Tayeh N, Fontana RJ. Acute hepatitis associated with alosetron (Lotronex). J Clin Gastroenterol. 2005 Aug;39(7):641-2.  [Content Brief]

  [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.  [Content Brief]

  [6]. Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000;59(3):511-520.  [Content Brief]

  [7]. Motavallian A, et al. Anti-inflammatory effects of alosetron mediated through 5-HT3 receptors on experimental colitis. Res Pharm Sci. 2019;14(3):228-236.  [Content Brief]