| Bioactivity | 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]. |
| In Vivo | 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]. |
| Name | Alosetron Hydrochloride |
| CAS | 122852-69-1 |
| Formula | C17H19ClN4O |
| Molar Mass | 330.81 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. [6]. Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000;59(3):511-520. [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. |
Alosetron Hydrochloride
CAS: 122852-69-1 F: C17H19ClN4O W: 330.81
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydr
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