ANQ 11125 是一种有效的选择性胃动素拮抗剂，pKd 为 8.24。
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.
动态评分
0.0