Nonpeptidyl somatostatin agonists demonstrate that sst2 and sst5 inhibit stimulated growth hormone secretion from rat anterior pituitary cells

被引：42

作者：

Parmar, RM ^{[1
]}

Chan, WWS ^{[1
]}

Dashkevicz, M ^{[1
]}

Hayes, EC ^{[1
]}

Rohrer, SP ^{[1
]}

Smith, RG ^{[1
]}

Schaeffer, JM ^{[1
]}

Blake, AD ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1999年 / 263卷 / 02期

关键词：

somatostatin; growth hormone; secretion; receptor subtypes;

D O I：

10.1006/bbrc.1999.1376

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Somatostatin (SST) regulates growth hormone (GH) secretion from pituitary somatotrophs by interacting with members of the SST family of G-protein-coupled receptors (sst1-5). We have used potent, nonpeptidyl SST agonists with sst2 and sst5 selectivity to-determine whether these receptor subtypes are involved in regulating growth hormone releasing hormone (GHRH) stimulated secretion. GHRH stimulated GH release from pituitary cells in a dose-dependent manner, and this secretion was inhibited by Tyr(11)-SST-14, a nonselective SST analog. A sst2 selective agonist, L-779,976, potently inhibited GHRH-stimulated GH release. In addition, L-817,818, a potent sst5 receptor selective agonist, also inhibited GH secretion, but was approximately 10-fold less potent (P < 0.01, ANOVA) in inhibiting GH release than either Tyr(11)-SST-14 or L-779,976. These results show that both sst2 and sst5 receptor subtypes regulate GHRH-stimulated GH release from rat pituitary cells. (C) 1999 Academic Press.

引用

页码：276 / 280

页数：5

共 36 条

[1] Discovery of a novel non-peptide somatostatin agonist with SST4 selectivity [J].