偏向性μ-阿片受体激动剂的研究进展  

Research progress ofμ-opioid receptor biased agonists

作　　者：朱胜男 彭卫娟[1] 周英珍[1] 许向阳 ZHU Sheng-nan;PENG Wei-juan;ZHOU Ying-zhen;XU Xiang-yang(Nhwa Institute of Pharmaceutical Research,Jiangsu Nhwa Pharmaceutical Co.,Ltd.,Xuzhou 221116,China)

机构地区：[1]江苏恩华药业股份有限公司恩华药物研究院,江苏徐州221116

出　　处：《中国药物化学杂志》2022年第4期323-329,共7页Chinese Journal of Medicinal Chemistry

基　　金：江苏省中枢神经药物研究重点实验室资助项目(BM2019004)。

摘　　要：偏向性μ-阿片受体激动剂可选择性激活G蛋白通路而不激活β-抑制蛋白通路,与传统的阿片受体激动剂相比,减少了阿片样不良反应,如严重恶心、呕吐、呼吸抑制和成瘾性等。本文综述了近几年偏向性μ-阿片受体激动剂的最新研究进展,以全球首个且唯一获得FDA批准上市的偏向性μ-阿片受体激动剂TRV-130为代表,还介绍了其他处于临床或临床前研发阶段的药物,以期为镇痛药的研发及临床治疗提供新的思路。μ-Opioid receptor biased agonists can selectively activate G protein signaling with littleβ-arrestin recruitment.Therefore,compared with traditional opioid,μ-opioid receptor biased agonists have little opioid side effects,such as severe nausea,vomiting,respiratory depression and addiction etc.This paper reviews the development ofμ-opioid receptor biased agonists in recent years.Representative drug TRV-130 is emphasized,which is the firstμ-opioid receptor biased agonist approved by FDA.Otherμ-opioid receptor biased agonists in clinical or preclinical studies are also introduced,so as to provide new ideas for the development of analgesics and clinical treatment of pain.

关 键 词：偏向性 μ-阿片受体激动剂 阿片样不良反应 镇痛 

分 类 号：R914[医药卫生—药物化学]