COMPARISON OF NALOXONAZINE AND BETA-FUNALTREXAMINE ANTAGONISM OF MU-1 AND BETA-2 OPIOID ACTIONS

被引:64
作者
PICK, CG
PAUL, D
PASTERNAK, GW
机构
[1] CORNELL UNIV,MED CTR,COLL MED,DEPT NEUROL,NEW YORK,NY 10021
[2] CORNELL UNIV,MED CTR,COLL MED,DEPT NEUROSCI,NEW YORK,NY 10021
[3] CORNELL UNIV,MED CTR,COLL MED,DEPT PHARMACOL,NEW YORK,NY 10021
关键词
D O I
10.1016/0024-3205(91)90155-5
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
beta-Funaltrexamine (beta-FNA) irreversibly blocks morphine analgesia, lethality and its inhibition of gastrointestinal transit, confirming that these actions involve mu receptors. In dose-response studies, beta-FNA antagonized all the actions with similar potencies (ID50 values of 12.1, 11.3 and 12.3 mg/kg, respectively). beta-FNA also reduced intra-cerebroventricular and intrathecal DAMGO analgesia equally well (ID50 values of 6.09 and 7.7 mg/kg, respectively). Naloxonazine blocked systemic morphine analgesia (ID50 value 9.5 mg/kg) and supraspinal DAMGO analgesia (ID50 value 6.1 mg/kg) as potently as beta-FNA. However, against spinal DAMGO analgesia, morphine's inhibition of gastro-intestinal transit or lethality, naloxonazine (ID50 values 38.8, 40.7 and 40.9 mg/kg, respectively) was significantly less active than beta-FNA (p < 0.05). beta-FNA remains a valuable tool in the classification of mu opioid actions. Within the mu category, actions can be defined as either mu-1 (naloxonazine-sensitive) or mu-2 (naloxonazine-insensitive).
引用
收藏
页码:2005 / 2011
页数:7
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