AM630 is an inverse agonist at the human cannabinoid CB1 receptor

被引：46

作者：

Landsman, RS

Makriyannis, A

Deng, HF

Consroe, P

Roeske, WR

Yamamura, HI ^{[1
]}

机构：

[1] Univ Arizona, Hlth Sci Ctr, Coll Med, Dept Pharmacol, Tucson, AZ 85724 USA

[2] Univ Arizona, Hlth Sci Ctr, Dept Pharmacol & Toxicol, Tucson, AZ 85724 USA

[3] Univ Arizona, Hlth Sci Ctr, Dept Biochem, Tucson, AZ 85724 USA

[4] Univ Arizona, Hlth Sci Ctr, Dept Med, Tucson, AZ 85724 USA

[5] Univ Arizona, Hlth Sci Ctr, Dept Psychiat, Tucson, AZ 85724 USA

[6] Univ Arizona, Hlth Sci Ctr, Program Neurosci, Tucson, AZ 85724 USA

[7] Univ Connecticut, Sch Pharm, Storrs, CT 06269 USA

来源：

LIFE SCIENCES | 1998年 / 62卷 / 09期

关键词：

human cannabinoid CB1 receptor; inverse agonism; AM630; WIN 55,212-2; GTP gamma S; CHO cells; inverse agonist; negative intrinsic activity;

D O I：

10.1016/S0024-3205(97)01187-9

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1, receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [S-35]GTP gamma S binding to cell membranes was determined. WIN 55,212-2 (100 mu M) stimulated basal [S-35]GTP gamma S binding 77.9% with an EC50 value of 0.36 mu M. Conversely, AM630 (100 mu M) inhibited basal [S-35]GTP gamma S binding by 20.9% with an EC50 value of 0.90 mu M These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system. (C) 1998 Elsevier Science Inc.

引用

页码：PL109 / PL113

页数：5

共 12 条

[1] A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor 1 - Evidence for a new model of receptor/ligand interactions [J].