Motilin receptor antagonist,selective
CAS：153966-48-4
分子式：C86H125N19O21
分子量：1761.05
纯度：98%
存储：Store at -20°C

Background:

ANQ 11125 is a selective antagonist of motilin receptor with pKd of 8.24 [1].

Motilin receptor is a G protein-coupled receptor for motilin and stimulates contraction of gut smooth muscle.

ANQ 11125 is a selective motilin receptor antagonist. The affinity of ANQ 11125 for motilin receptor is about 10 times less than motilin [1]. In rabbit antral smooth muscle tissue, ANQ-11125 bound to motilin receptor with pKd value of 8.16. While, ANQ-11125 didn’t induce contractions of rabbit duodenum. ANQ-11125 (10-5 M) induced contractile response by 29% compared to ACh [2].

参考文献:
[1].  Depoortere I, Macielag MJ, Galdes A, et al. Antagonistic properties of [Phe3,Leu13]porcine motilin. Eur J Pharmacol, 1995, 286(3): 241-247.
[2].  Peeters TL, Depoortere I, Macielag MJ, et al. The motilin antagonist ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit. Biochem Biophys Res Commun, 1994, 198(2): 411-416.