[摘要]阿片类镇痛药物布托啡诺是阿片受体激动-拮抗剂,其药物的滥用引发了许多的社会问题。布托啡诺能与三个主要的阿片受体μ、δ、κ阿片受体结合,其亲和力之比是1:4:25。体内实验表明布托啡诺与κ阿片受体的结合能调控其药物耐受性和交叉耐受性,调控脑内阿片受体效应系统的代偿性改变。当前的研究热点在于明确κ阿片受体亚型的功能和长期应用布托啡诺后脑内磷酸化蛋白的表达。

    [关键词]布托啡诺; κ-阿片受体; 依赖性

    [中图分类号]R971+.1[文献标识码]A [文章编号] 1005-0515(2010)-7-010-02

    [Abstract]The opioid analgesic,butorphanol is a agonist-antagonist,opioidagent whose abuse has been the cause of many social problems. Butorphanol can bind to the three major opioid receptor μ, δ, κ with the affinity ratio 1:4:25..A body of evidence has developed butorphanol on theκ-opioid receptor mediates drug tolerance and cross -tolerance brain compensatory changes of opioid receptor. The current researchs focus on the functions of κ-opioid receptor and the expression of protein phosphorylation in brain following chronic treatment with butorphanol.

    [Keywords]butorphanol;κ-opioid receptor;dependence

    阿片类镇痛药物酒石酸布托啡诺最早出现于1973年,其最初生产的目的是作为一种麻醉药物产生的致幻副作用的拮抗剂[1] ......