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
  • [21] Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors
    MacLennan, SJ
    Reynen, PH
    Kwan, J
    Bonhaus, DW
    BRITISH JOURNAL OF PHARMACOLOGY, 1998, 124 (04) : 619 - 622
  • [22] Use of cannabinoid CB1 receptor antagonists for the treatment of metabolic disorders
    Scheen, Andre J.
    Paquot, Nicolas
    BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM, 2009, 23 (01) : 103 - 116
  • [23] Binding of the Hemopressin Peptide to the Cannabinoid CB1 Receptor: Structural Insights
    Scrima, Mario
    Di Marino, Sara
    Grimaldi, Manuela
    Mastrogiacomo, Antonia
    Novellino, Ettore
    Bifulco, Maurizio
    D'Ursi, Anna Maria
    BIOCHEMISTRY, 2010, 49 (49) : 10449 - 10457
  • [24] Effects of the cannabinoid CB1-receptor neutral antagonist AM4113 and antagonist/inverse agonist rimonabant on fentanyl discrimination in male rats
    AlKhelb, Dalal
    Kirunda, Andre
    Ho, Thanh C.
    Makriyannis, Alexandros
    Desai, Rajeev I.
    DRUG AND ALCOHOL DEPENDENCE, 2022, 240
  • [25] Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties
    Bergman, Jack
    Delatte, Marcus S.
    Paronis, Carol A.
    Vemuri, Kiran
    Thakur, Ganesh A.
    Makriyannis, Alex
    PHYSIOLOGY & BEHAVIOR, 2008, 93 (4-5) : 666 - 670
  • [26] Rimonabant, a potent CB1 cannabinoid receptor antagonist, is a Gαi/o protein inhibitor
    Porcu, Alessandra
    Melis, Miriam
    Turecek, Rostislav
    Ullrich, Celine
    Mocci, Ignazia
    Bettler, Bernhard
    Gessa, Gian Luigi
    Castelli, M. Paola
    NEUROPHARMACOLOGY, 2018, 133 : 107 - 120
  • [27] CB1 cannabinoid receptor agonist mouse VD-hemopressin(α) produced supraspinal analgesic activity in the preclinical models of pain
    Zheng, Ting
    Zhang, Run
    Zhang, Ting
    Zhang, Meng-Na
    Xu, Biao
    Song, Jing-jing
    Li, Ning
    Tang, Hong-Hai
    Wang, Pei
    Wang, Rui
    Fang, Quan
    BRAIN RESEARCH, 2018, 1680 : 155 - 164
  • [28] Recent Development of CB2 Selective and Peripheral CB1/CB2 Cannabinoid Receptor Ligands
    Nevalainen, Tapio
    CURRENT MEDICINAL CHEMISTRY, 2014, 21 (02) : 187 - 203
  • [29] 3-Substituted Pyrazole Analogs of the Cannabinoid Type 1 (CB1) Receptor Antagonist Rimonabant: Cannabinoid Agonist-Like Effects in Mice via Non-CB1, Non-CB2 Mechanism
    Wiley, Jenny L.
    Selley, Dana E.
    Wang, Pinglang
    Kottani, Rudresha
    Gadthula, Srinivas
    Mahadeven, Anu
    JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2012, 340 (02) : 433 - 444
  • [30] Novel selective cannabinoid CB1 receptor antagonist MJ08 with potent in vivo bioactivity and inverse agonistic effects
    Chen, Wei
    Xu, Cheng
    Liu, Hong-ying
    Long, Long
    Zhang, Wei
    Zheng, Zhi-bing
    Xie, Yun-de
    Wang, Li-li
    Li, Song
    ACTA PHARMACOLOGICA SINICA, 2011, 32 (09) : 1148 - 1158
12345