大鼠垂体前叶中血管活性肠肽鸟嘌呤核苷酸敏感受体的直接证明。

Direct demonstration of guanine nucleotide sensitive receptors for vasoactive intestinal peptide in the anterior lobe of the rat pituitary gland.

作者信息

Agui T, Matsumoto K

机构信息

Institute for Animal Experimentation, University of Tokushima School of Medicine, Japan.

出版信息

Peptides. 1990 May-Jun;11(3):609-11. doi: 10.1016/0196-9781(90)90065-d.

DOI:10.1016/0196-9781(90)90065-d

PMID:2166281

Abstract

The vasoactive intestinal peptide (VIP) receptors were identified on the membranes from the rat anterior pituitary gland with [125I]VIP. The dissociation constant (Kd) and the maximal binding capacity (Bmax) values were estimated from the competitive inhibition data. The Kd and Bmax values were 1.05 +/- 0.75 nM and 103 +/- 11 fmol/mg protein, respectively. The order of molar potency of related peptides to inhibit [125I]VIP binding was VIP greater than peptide histidine isoleucine (PHI) greater than secretin greater than glucagon. Glucagon was not effective to inhibit the binding. [125I]VIP binding was effectively inhibited by the addition of guanine nucleotides. The order of molar potency to inhibit the binding was Gpp(NH)p greater than GTP greater than GDP greater than GMP greater than ATP. These results directly suggest the coupling of VIP receptors with guanine nucleotide binding proteins in the anterior pituitary gland.

摘要

用[125I]血管活性肠肽（VIP）在大鼠垂体前叶细胞膜上鉴定出VIP受体。根据竞争抑制数据估算解离常数（Kd）和最大结合容量（Bmax）值。Kd和Bmax值分别为1.05±0.75 nM和103±11 fmol/mg蛋白质。相关肽抑制[125I]VIP结合的摩尔效力顺序为：VIP＞组异肽（PHI）＞促胰液素＞胰高血糖素。胰高血糖素对抑制结合无效。加入鸟嘌呤核苷酸可有效抑制[125I]VIP结合。抑制结合的摩尔效力顺序为：鸟苷-5'-三磷酸（Gpp(NH)p）＞三磷酸鸟苷（GTP）＞二磷酸鸟苷（GDP）＞一磷酸鸟苷（GMP）＞三磷酸腺苷（ATP）。这些结果直接表明垂体前叶中VIP受体与鸟嘌呤核苷酸结合蛋白偶联。