Influence of selective VIP receptor agonists in the rat gastric fundus

被引:29
|
作者
Robberecht, P
De Neef, P
Lefebvre, RA [1 ]
机构
[1] Free Univ Brussels, Sch Med, Dept Biochem & Nutr, B-1070 Brussels, Belgium
[2] State Univ Ghent, Sch Med, Heymans Inst Pharmacol, B-9000 Ghent, Belgium
关键词
stomach; smooth muscle; relaxation; VIP (vasoactive intestinal polypeptide); secretin;
D O I
10.1016/S0014-2999(98)00662-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The receptor subtypes involved in the relaxant effect of vasoactive intestinal polypeptide (VIP) in the rat gastric fundus were investigated in vitro. The selective VIP2 receptor agonist [Ac-H-1,E-8,K-12,Nle(17),A(19),D-25,L-26,K-27,K-28,G(29,30)]VIP(cyclo21-25) (RO25-1553) induced a concentration-dependent relaxation (EC50 2.8 nM), while the selective VIP1 receptor agonist derived from growth hormone-releasing factor (GRF) [K-15,R-16,L-27]VIP-(1-7)/GRF-(8-27) had no effect up to 1 mu M. [R-16] chicken secretin, a selective VIP1 receptor agonist, induced relaxation with a potency of 4.8 nM but its maximal effect was clearly lower than that of VIP, pituitary adenylate cyclase-activating peptide [PACAP-(1-27)] and RO25-1553. This effect was reproduced by porcine secretin (EC50 2.1 nM). It is concluded that the rat gastric fundus contains functional VIP2 receptors but not VIP1 receptors, and that specific secretin receptors are also present. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:77 / 80
页数:4
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