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
收藏
页码：PL109 / PL113
页数：5
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