AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain

被引：46
|
作者：
Hosohata, K
Quock, RM
Hosohata, Y
Burkey, TH
Makriyannis, A
Consroe, P
Roeske, WR
Yamamura, HI
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 PSYCHIAT, TUCSON, AZ 85724 USA
[5] UNIV ARIZONA, HLTH SCI CTR, PROGRAM NEUROSCI, TUCSON, AZ 85724 USA
[6] UNIV CONNECTICUT, SCH PHARM, STORRS, CT 06269 USA
[7] UNIV ILLINOIS, COLL MED, DEPT BIOMED SCI, ROCKFORD, IL 61107 USA
来源：
LIFE SCIENCES | 1997年 / 61卷 / 09期
关键词：
cannabinoid antagonist; S-35]GTP gamma S binding; guinea pig;
D O I：
10.1016/S0024-3205(97)00596-1
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：
AM630 has been demonstrated to be a cannabinoid receptor antagonist in the mouse brain and vas deferens. Conversely, it was recently reported that AM630 acts as a cannabinoid agonist in the guinea pig ileum. This research was designed to determine whether the difference in the action of AM630 is species specific. Studies conducted in guinea pig brain reveal that AM630 antagonizes the stimulatory effect of the cannabinoid agonist WIN 55,212-2 on [S-35]GTP gamma S binding suggesting that difference in AM630 activity in different tissues is not due to species (C) 1997 Elsevier Science Inc.
引用
收藏
页码：PL115 / PL118
页数：4
相关论文
共 50 条
  • [1] AM630, A COMPETITIVE CANNABINOID RECEPTOR ANTAGONIST
    PERTWEE, R
    GRIFFIN, G
    FERNANDO, S
    LI, XY
    HILL, A
    MAKRIYANNIS, A
    LIFE SCIENCES, 1995, 56 (23-24) : 1949 - 1955
  • [2] AM630 is an inverse agonist at the human cannabinoid CB1 receptor
    Landsman, RS
    Makriyannis, A
    Deng, HF
    Consroe, P
    Roeske, WR
    Yamamura, HI
    LIFE SCIENCES, 1998, 62 (09) : PL109 - PL113
  • [3] AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor
    Bolognini, Daniele
    Cascio, Maria Grazia
    Parolaro, Daniela
    Pertwee, Roger G.
    BRITISH JOURNAL OF PHARMACOLOGY, 2012, 165 (08) : 2561 - 2574
  • [4] THE EFFECTS OF THE CANNABINOID CB2 RECEPTOR ANTAGONIST, AM630, ON ISOLATION REARING-INDUCED BEHAVIOURAL DEFICITS IN RATS
    Khan, Asma
    Kendall, David A.
    Fone, Kevin C. F.
    SCHIZOPHRENIA RESEARCH, 2010, 117 (2-3) : 391 - 392
  • [5] Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons
    Patil, Mayur
    Patwardhan, Amol
    Salas, Margaux M.
    Hargreaves, Kenneth M.
    Akopian, Armen N.
    NEUROPHARMACOLOGY, 2011, 61 (04) : 778 - 788
  • [6] Inhibition of titanium particle-induced inflammatory osteolysis through inactivation of cannabinoid receptor 2 by AM630
    Geng, D. C.
    Xu, Y. Z.
    Yang, H. L.
    Zhu, X. S.
    Zhu, G. M.
    Wang, X. B.
    JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A, 2010, 95A (01) : 321 - 326
  • [7] AM630 antagonism of cannabinoid-stimulated [S-35]GTP gamma S binding in the mouse brain
    Hosohata, Y
    Quock, RM
    Hosohata, K
    Makriyannis, A
    Consroe, P
    Roeske, WR
    Yamamura, HI
    EUROPEAN JOURNAL OF PHARMACOLOGY, 1997, 321 (01) : R1 - R3
  • [8] Effects of the cannabinoid antagonists AM281 and AM630 on deprivation-induced intake in Lewis rats
    Werner, NA
    Koch, JE
    BRAIN RESEARCH, 2003, 967 (1-2) : 290 - 292
  • [9] Nrf2 is required for suppressing osteoclast RANKL-induced differentiation in RAW 264.7 cells via inactivating cannabinoid receptor type 2 with AM630
    Li, Wan
    Sun, Yongxin
    REGENERATIVE THERAPY, 2020, 14 : 191 - 195
  • [10] Inhibition of voltage-sensitive sodium channels by the cannabinoid 1 receptor antagonist AM 251 in mammalian brain
    Liao, CY
    Zheng, J
    David, LS
    Nicholson, RA
    BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY, 2004, 94 (02) : 73 - 78
12345