Alosetron-13C,d3 (GR 68755-13C,d3) is the 13C- and deuterium labeled Alosetron. Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron 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 attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects[1][2].
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000;59(3):511-520.
[3]. 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.