THE PARTIAL OPIOID AGONIST, BUPRENORPHINE, PROTECTS AGAINST LETHAL EFFECTS OF COCAINE

被引：32

作者：

WITKIN, JM ^{[1
]}

JOHNSON, RE ^{[1
]}

JAFFE, JH ^{[1
]}

GOLDBERG, SR ^{[1
]}

GRAYSON, NA ^{[1
]}

RICE, KC ^{[1
]}

KATZ, JL ^{[1
]}

机构：

[1] NIDDKD, MED CHEM LAB, BETHESDA, MD 20892 USA

来源：

DRUG AND ALCOHOL DEPENDENCE | 1991年 / 27卷 / 02期

基金：

美国国家卫生研究院;

关键词：

COCAINE; BUPRENORPHINE; MORPHINE; METHADONE; CONVULSIONS; LETHALITY; CXBK MICE;

D O I：

10.1016/0376-8716(91)90037-Y

中图分类号：

R194 [卫生标准、卫生检查、医药管理];

学科分类号：

摘要：

Buprenorphine (0.3-3.0 mg/kg) produced dose-dependent protection against the lethal effects of cocaine in mice. The (+)-enantiomer of buprenorphine did not protect up to doses over 100 times greater than the lowest effective dose of its (-)-enantiomer. The protective effects were also produced by the opioid agonists morphine and methadone, but not by the opioid antagonist, naltrexone. Low doses of naltrexone (0.3-1.0 mg/kg) blocked the protective effects of buprenorphine. Protection conferred by buprenorphine was not observed in CXBK mice, a recombinant inbred strain relatively devoid of mu-opioid receptors. Thus, buprenorphine appears to protect against the lethal effects of cocaine by a process mediated by mu-opioid receptors. The present results should provide some additional safety assurance in future clinical trials with buprenorphine, especially in outpatient trials where cocaine abuse may continue along with treatment.

引用

页码：177 / 184

页数：8

共 33 条

[1] OPIATE RECEPTORS IN MICE - GENETIC DIFFERENCES [J].