偏向性μ-阿片受体激动剂奥赛利定的临床应用进展  

Progress in the clinical application of the biasedμ-opioid agonist oliceridine

作　　者：朱昌茂 谢力 吴仔峰 王森 张琪 徐祥清[3] 杨春 ZHU Changmao;XIE Li;WU Zifeng;WANG Sen;ZHANG Qi;XU Xiangqing;YANG Chun(Department of Anesthesiology and Perioperative Medicine,the First Affiliated Hospital of Nanjing Medical University,Nanjing 210029,Jiangsu,China;Department of Anesthesiology,the Fourth Affiliated Hospital of Nanjing Medical University,Nanjing 211800,Jiangsu,China;Jiangsu Nhwa Pharmaceutical Co.,Ltd.Drug Research Institute&Jiangsu Provincial Key Laboratory of Central Nervous Drug Research,Xuzhou 221116,Jiangsu,China)

机构地区：[1]南京医科大学第一附属医院麻醉与围术期医学科,江苏南京210029 [2]南京医科大学第四附属医院麻醉科,江苏南京211800 [3]江苏恩华药业股份有限公司药物研究院&江苏省中枢神经药物研究重点实验室,江苏徐州221116

出　　处：《中国临床药理学与治疗学》2024年第9期1057-1061,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金(82301444,82271254,81974171,81703482);江苏省双创团队领军人才项目(JSSCTD202144);江苏省特聘医学专家(苏卫人[2020]64号);吴阶平医学基金会(320.6750.2024-05-51)。

摘　　要：阿片类药物受体μOR、δOR、κOR和NOPR均是G蛋白偶联受体(G protein-coupled receptors,GPCRs),主要通过G蛋白和β抑制蛋白发挥作用。新近研究发现G蛋白介导镇痛作用,而β抑制蛋白则降低镇痛效果并与阿片类药物的副作用发生有关。奥赛利定是第一个批准上市的偏向性μOR激动剂,主要通过激活G蛋白发挥镇痛作用,其起效迅速且镇痛效果确切;因对β抑制蛋白活性较低,其副反应发生率较阿片类经典药物吗啡低。奥赛利定代谢产物无活性,可安全用于肝肾功能不全患者。本文总结了奥赛利定的药理学研究与临床应用现状,以期为奥赛利定的临床实践提供参考。Opioid receptorsμOR,δOR,κOR and NOPR are all G protein-coupled receptors(GPCRs),which mainly function through G protein andβ-arrestin.Recent studies have found that G protein mediates analgesia,whileβ-arrestin reduces analgesia and is related to the side effects of opioids.Oliceridine is the first biasedμOR agonist approved for commerce.It mainly exerts analgesic effect by activating G protein.It has rapid onset of action and reliable analgesic effect.Due to its low activity onβ-arrestin,the incidence of side effects is low,comparing to the classic opioid morphine.Oliceridine can be safely used in patients with liver or kidney insufficiency and its metabolite is inactive.This article summarizes the current progress of pharmacological research and clinical application of oliceridine,aiming to provide reference for the clinical practice of oliceridine.

关 键 词：奥赛利定(TRV-130) 药理机制 临床应用 不良反应 

分 类 号：R614[医药卫生—麻醉学]