5-HT_(2A)R异源二聚体功能研究进展  

Research progress of 5-HT_(2A)R heterodimers function

作　　者：高欢 谭博 杜广营[1] 苏瑞斌 GAO Huan;TAN Bo;DU Guang-ying;SU Rui-bin(School of Pharmacy,Yantai University,Yantai Shandong 264005,China;State Key Laboratory of Toxicology and Medical Countermeasures,Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850,China)

机构地区：[1]烟台大学药学院,山东烟台264005 [2]军事科学院军事医学研究院毒物药物研究所,抗毒药物与毒理学国家重点实验室,北京100850

出　　处：《中国药理学通报》2023年第7期1201-1205,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金面上项目(No.81773709)。

摘　　要：血清素2A受体(5-HT_(2A)R)作为致幻剂、抗抑郁药、抗焦虑药和非典型抗精神病药物等许多精神活性药物的作用靶点,受到人们的广泛关注。5-HT_(2A)R属于G蛋白偶联受体(GPCRs),与mGluR2、D_(2)R和CB_(1)R等多种GPCRs形成异源二聚体。二聚体中的mGluR2、D_(2)R与CB_(1)R影响5-HT_(2A)R偶联的信号通路和诱导的动物行为,并且3种受体分别被敲除后,致幻性5-HT_(2A)R激动剂诱导产生的甩头反应次数明显降低。基于5-HT_(2A)R/mGluR2、5-HT_(2A)R/D_(2)R和5-HT_(2A)R/CB_(1)R异源二聚体的重要性,该文将3种受体与5-HT_(2A)R形成异源二聚体的发现与功能进行详细综述,为探寻以5-HT_(2A)R为靶点的精神活性药物作用机制提供参考。The serotonin_(2A) receptor(5-HT_(2A) R)is the target of many psychoactive drugs such as hallucinogens,antidepressants,anxiolytics and atypical antipsychotics,and its research has attracted widespread attention.5-HT_(2A) R belongs to G protein-coupled receptors(GPCRs)and forms heterodimers with various GPCRs such as mGluR2,D_(2)R and CB_(1)R.The heterodimers of mGluR2,D_(2)R,and CB_(1)R affect 5-HT_(2A) R-coupled signaling pathways and Induced animal behavior,and after the three receptors are knocked out respectively,the number of head-twitch response induced by hallucinogenic 5-HT_(2A) R agonists is significantly reduced.Based on the importance of 5-HT_(2A) R/mGluR2,5-HT_(2A) R/D_(2)R and 5-HT_(2A) R/CB_(1)R heterodimers,this paper reviews the discovery and function of three receptors and 5-HT_(2A) R to form heterodimers in detail,so as to provide reference for exploring the mechanism of psychoactive drugs and developing new drugs.

关 键 词：5-HT_(2A)R mGluR2 D_(2)R CB_(1)R 异源二聚体 甩头反应 

分 类 号：R-05[医药卫生] R392.11R749