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].
[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.
