Alosetron (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].

Product Specifications

CAS Number

[122852-69-1]

Product Name Alternative

GR 68755C; GR 68755 (Hydrochloride) ; GR 68755X (Hydrochloride)

UNSPSC

12352005

Hazard Statement

H301, H412

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/alosetron-hydrochloride.html

Purity

99.63

Solubility

H2O : 33.33 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H19ClN4O

Molecular Weight

330.81

Precautions

H301, H412

References & Citations

[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.