THE RAT SSTR2 SOMATOSTATIN RECEPTOR SUBTYPE IS COUPLED TO INHIBITION OF CYCLIC-AMP ACCUMULATION

被引：47

作者：

STRNAD, J ^{[1
]}

EPPLER, CM ^{[1
]}

CORBETT, M ^{[1
]}

HADCOCK, JR ^{[1
]}

机构：

[1] AMER CYANAMID CO,DIV AGR RES,BIOCHEM GRP,PRINCETON,NJ 08543

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1993年 / 191卷 / 03期

关键词：

D O I：

10.1006/bbrc.1993.1312

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：

The rat somatostatin receptor SSTR2 subtype has been cloned and expressed in Chinese Hamster Ovary (CHO) cells. Four different radioligands were used to determine the pharmacological properties of this somatostatin receptor subtype. [125ITyr11]S-14, [125ITyr25]S-28, and cyclo (D-Trp-Lys- Abu-Phe-MeAla-[125ITyr]) displayed comparable affinities for the SSTR2 subtype (˜100 pM). The affinity of a fourth radioligand, D-βNal-cyclo (Cys- [125ITyr]-DTrp-Lys-Val-Cys)-Thr-H2N, was approximately 10-fold lower (˜1000 pM) than the three other radioligands. Competition of [125I]S-14 with either S-14 or S-28 also revealed comparable IC50 values (250 pM). In CHO cells transfected with the SSTR2 cDNA, S-14 inhibited forskolin- stimulated cAMP accumulation by 75% in a dose-dependent fashion (EC50 = 350 pM). © 1993 Academic Press, Inc.

引用

页码：968 / 976

页数：9

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