μ/δ阿片受体相互调节作用及药物发现与设计策略  

Modulated interaction of μ/δ opioid receptors and the drug discovery and design strategy

作　　者：沈庆[1] 刘慧芳[1] 李炜[1] 李颖[2] 程家高[3] 刘景根[4] 付伟[1] 

机构地区：[1]复旦大学药学院药化教研室,上海201203 [2]内蒙古机电职业技术学院冶金与材料教研室,内蒙古呼和浩特010051 [3]华东理工大学药学院,上海市化学生物学(芳香杂环)重点实验室,上海200237 [4]中国科学院上海药物研究所新药研究国家重点实验室,上海201203

出　　处：《中国药理学通报》2010年第1期4-8,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助课题(No20702009);博士点新教师基金资助课题(No20070246092);上海市卫生局资助项目(No2007089)

摘　　要：阿片类镇痛药镇痛活性好,广泛用于临床。阿片受体主要分为3种亚型,即μ、δ、κ阿片受体。目前临床上使用的阿片类镇痛药大多为μ受体激动剂,但易引起成瘾性、呼吸抑制等副作用。δ受体激动剂镇痛活性较弱,但δ受体激动剂和拮抗剂均能调节μ受体激动剂的镇痛作用,同时参与成瘾性等副作用形成。因此,设计具有μ/δ双重功效的药物是新一代低毒副作用镇痛药的发展方向。该文综述了具有μ/δ双重功效药物的研究现状,为设计低毒副作用镇痛药物提供新思路。Opioid analgesics are potent pain-killer and are widely used in clinical practice. Opioid receptors are classified into μ, δ,κ subtypes. Most of the currently available opioid analgesics are μ opioid receptor agonists,but they cause undesired side effects such as physical dependence,respiratory depression and constipation and so on. The antalgic activity of δ receptor agonist is weaker than that of μ agonist,but it can modulate the activity of μ receptor and prevent its addiction. Therefore,discoveringand designing compounds with μ/δ dual action is a new way for finding analgesics with low toxicity and less side effects. This review summarizes the development of compound with dual μ/δ activities and provides a new strategy for designing analgesics with low toxicity and less side effects.

关 键 词：μ激动剂/δ拮抗剂 μ/δ双重激动剂 阿片类镇痛药 药物设计 低成瘾性 双重作用 

分 类 号：R-05[医药卫生] R392.11