| CAS NO: | 153966-48-4 |
| 包装: | 1mg |
| 规格: | 98% |
| 市场价: | 3164元 |
| 分子量: | 1761.05 |
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.
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