Alosetron-13C,d3 (GR 68755-13C,d3) 是一种 13C- 和氘代标记的 Alosetron。Alosetron (GR 68755) 是一种高效、高选择性的 5-HT3 受体 (5-HT3 receptor) 拮抗剂。Alosetron 用于肠易激综合征 (IBS) 的研究。Alosetron 阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50 在 ~55 nM。Alosetron 减轻清醒或麻醉犬直肠扩张的内脏伤害性效应。具有抗炎活性。
货号:ajcx37278
CAS:N/A
分子式:C1613CH15D3N4O
分子量：298.36
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.