μ/δ阿片受体双重激动剂研究进展  

Research progress of dual μ/δ opioid receptor agonists

作　　者：李京 任凤霞 史卫国 LI Jing;REN Feng-xia;SHI Wei-guo(School of Chemical Engineering and Technology,Tianjin University,Tianjin 300350,China;State Key Laboratory of Toxicology and Medical Countermeasures,Beijing Institute of Pharmacology&Toxicology,Beijing 100850,China)

机构地区：[1]天津大学化工学院,天津300350 [2]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2021年第23期2166-2172,共7页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项资助项目(2012ZX 09301003);北京市科技计划课题(Z131100002713004)。

摘　　要：阿片类镇痛药对于中度至重度剧烈疼痛的治疗仍不可替代,但由于其产生的成瘾性等不良反应,使用受到限制,临床急需新一代高效安全的阿片类镇痛药。目前有关μ与δ阿片受体间的相互调节作用的研究被大量报道,μ/δ二聚体的存在也为受体的相互作用提供了分子基础,设计具有μ/δ双重激动效应的分子是新一代具有强镇痛作用同时减少不良反应阿片类药物的发展方向。本文按照μ/δ双重激动分子设计策略分类,综述了近年来μ/δ双重激动剂的研究进展。Opioid analgesics are still irreplaceable for the treatment of moderate to severe pain, but the usage is limited because of their dependence and other adverse reactions. There is an urgent need for a new generation of efficient and safe opioid analgesics. At present, many studies on the interaction between μ and δ opioid receptors have been reported, and the existence of μ/δ dimer also provides a molecular basis for the receptor interaction. The design of molecules with double activation effect on μ and δ types is the new development direction of opioid drugs with strong analgesic effect and little or weak adverse reactions. In this paper, the research progress of μ/δ dual agonists in recent years is reviewed according to the classification of design strategy of μ/δ dual agonist.

关 键 词：μ-δ相互调节作用 多靶点配体 μ/δ双重激动剂 高效安全镇痛药 

分 类 号：R971[医药卫生—药品]