κ阿片受体中枢副作用评价方法和发生机制研究进展  

Progress in evaluation methods and mechanisms of opioid receptor-mediated side effects

作　　者：马艳 刘景根 王瑜珺 MA Yan;LIU Jing-gen;WANG Yu-jun(School of Life Sciences, Shanghai University, Shanghai 200444, China;Key Lab of Receptor Research, Chinese Academy of Sciences Shanghai Institute of Materia Medica, Shanghai 201203, China)

机构地区：[1]上海大学生命科学学院,上海200444 [2]中国科学院上海药物研究所,受体结构与功能重点实验室,上海201203

出　　处：《中国药理学通报》2019年第11期1501-1504,共4页Chinese Pharmacological Bulletin

基　　金：中国科学院战略性先导科技专项(No XDA12040319)

摘　　要：κ阿片受体激动会产生较强的镇痛作用,但不会诱发经典阿片样副作用,同时还可以拮抗阿片类物质成瘾。但由于其中枢镇静、烦躁不安副作用的存在,目前临床以κ阿片受体为靶标的药物多为κ/μ混合激动剂,尚缺乏选择性κ受体激动剂。开发中枢副作用小的κ受体激动剂将是新型镇痛药物的重要研究方向。该文对目前临床使用的以κ阿片受体为靶标的镇痛药、κ受体中枢副作用评价方法和发生机制进行综述。κ opioid receptor agonists produce potent antinociception without morphine-like side effects. However, selective κ opioid receptor agonists exhibit severe dysphoria, limiting their clinical use. Developing new κ agonists with less CNS side effects appears to offer some advantages over μ agonist for the treatment of pain. In this review, we summarize the representative analgesics targeting κ opioid receptors in the clinic and introducethe latest progress of methodology and underlying mechanism of κ receptor-mediated dysphoria.

关 键 词：疼痛 镇痛药 阿片受体 κ受体激动剂 中枢副作用 烦躁不安 

分 类 号：R322.81[医药卫生—人体解剖和组织胚胎学] R392.11[医药卫生—基础医学]