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
相关论文
共 50 条
[31]   Novel selective cannabinoid CB1 receptor antagonist MJ08 with potent in vivo bioactivity and inverse agonistic effects [J].
Wei Chen ;
Cheng Xu ;
Hong-ying Liu ;
Long Long ;
Wei Zhang ;
Zhi-bing Zheng ;
Yun-de Xie ;
Li-li Wang ;
Song Li .
Acta Pharmacologica Sinica, 2011, 32 :1148-1158
[32]   Central and peripheral consequences of the chronic blockade of CB1 cannabinoid receptor with rimonabant or taranabant [J].
Martin-Garcia, Elena ;
Burokas, Aurelijus ;
Martin, Miquel ;
Berrendero, Fernando ;
Rubi, Blanca ;
Kiesselbach, Christoph ;
Heyne, Andrea ;
Domingo Gispert, Juan ;
Millan, Olga ;
Maldonado, Rafael .
JOURNAL OF NEUROCHEMISTRY, 2010, 112 (05) :1338-1351
[33]   Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists [J].
Zhu, Bin ;
Matthews, Jay M. ;
Xia, Mingde ;
Black, Shawn ;
Chen, Cailin ;
Hou, Cuifen ;
Liang, Yin ;
Tang, Yuting ;
Macielag, Mark J. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (22) :5597-5601
[34]   Rimonabant Redux and Strategies to Improve the Future Outlook of CB1 Receptor Neutral-Antagonist/Inverse-Agonist Therapies [J].
Ward, Sara Jane ;
Raffa, Robert B. .
OBESITY, 2011, 19 (07) :1325-1334
[35]   Involvement of cannabinoid CB2 receptor-mediated response and efficacy of cannabinoid CB2 receptor inverse agonist, JTE-907, in cutaneous inflammation in mice [J].
Ueda, Y ;
Miyagawa, N ;
Matsui, T ;
Kaya, T ;
Wamura, H ;
Iwamura, H .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2005, 520 (1-3) :164-171
[36]   Allosterism and cannabinoid CB1 receptors:: the shape of things to come [J].
Ross, Ruth A. .
TRENDS IN PHARMACOLOGICAL SCIENCES, 2007, 28 (11) :567-572
[37]   Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists [J].
Madsen-Duggan, Christina B. ;
Debenham, John S. ;
Walsh, Thomas F. ;
Toupence, Richard B. ;
Huang, Song X. ;
Wang, Junying ;
Tong, Xinchun ;
Lao, Julie ;
Fong, Tung M. ;
Schaeffer, Marie-Therese ;
Xiao, Jing Chen ;
Huang, Cathy R-R. C. ;
Shen, Chun-Pyn ;
Stribling, D. Sloan ;
Shearman, Lauren P. ;
Strack, Alison M. ;
MacIntyre, D. Euan ;
Van der Ploeg, Lex H. T. ;
Goulet, Mark T. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (07) :2031-2035
[38]   Characterization of the pharmacology of imidazolidinedione derivatives at cannabinoid CB1 and CB2 receptors [J].
Govaerts, SJ ;
Muccioli, GG ;
Hermans, E ;
Lambert, DM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2004, 495 (01) :43-53
[39]   A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay [J].
Borrega-Roman, Leire ;
Hoare, Bradley L. ;
Kosar, Miroslav ;
Sarott, Roman C. ;
Patej, Kacper J. ;
Bouma, Jara ;
Scott-Dennis, Morgan ;
Koers, Eline J. ;
Gazzi, Thais ;
Mach, Leonard ;
Barrondo, Sergio ;
Salles, Joan ;
Guba, Wolfgang ;
Kusznir, Eric ;
Nazare, Marc ;
Rufer, Arne C. ;
Grether, Uwe ;
Heitman, Laura H. ;
Carreira, Erick M. ;
Sykes, David A. ;
Veprintsev, Dmitry B. .
FRONTIERS IN PHARMACOLOGY, 2025, 16
[40]   Cannabinoid CB1 receptor neutral antagonist AM4113 inhibits heroin self-administration without depressive side effects in rats [J].
Xiang-hu He ;
Chloe J. Jordan ;
Kiran Vemuri ;
Guo-hua Bi ;
Jia Zhan ;
Eliot L. Gardner ;
Alexandros Makriyannis ;
Yan-lin Wang ;
Zheng-xiong Xi .
Acta Pharmacologica Sinica, 2019, 40 :365-373
12345