靶向TRPV1通道的镇痛剂研究进展  

Research Progress on TRPV1 Channel Targeted Analgesics

作　　者：高宇豪 于烨 GAO Yuhao;YU Ye(School of Basic Medicine and Clinical Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学基础医学与临床药学学院,江苏南京211198

出　　处：《生物化工》2024年第3期195-198,203,共5页Biological Chemical Engineering

基　　金：长沙市“揭榜挂帅”重大科技项目(KQ2301004)。

摘　　要：瞬时受体电位香草酸亚型1(Transient Receptor Potential Vanilloid 1,TRPV1)通道广泛分布于感觉神经末梢、中枢神经系统和其他组织,是响应热痛和化学刺激的离子通道蛋白。近年来,TRPV1受体作为治疗各种疼痛相关疾病的潜在方法引起了人们的广泛关注。本文探讨疼痛治疗中的TRPV1激动剂和拮抗剂,根据其结构特征进行分类和阐述,并对配体的结合模式、构效关系、优势和局限性进行讨论,为今后开发更安全有效的TRPV1镇痛剂提供参考。Transient receptor potential vanilloid 1(TRPV1)channels are widely distributed in sensory nerve endings,central nervous system,and other tissues,and are ion channel proteins in response to heat pain and chemical stimuli.In recent years,TRPV1 receptors have attracted a lot of attention as a potential treatment for various painrelated diseases.This article discusses TRPV1 agonists and antagonists in pain treatment,classifies and elaborates them according to their structural characteristics,and discusses the binding mode,structure-activity relationship,advantages and limitations of ligands,so as to provide a reference for the development of safer and more effective TRPV1 analgesics in the future.

关 键 词：瞬时受体电位香草酸亚型1(Transient Receptor Potential Vanilloid 1 TRPV1) 镇痛剂 构效关系 

分 类 号：R741[医药卫生—神经病学与精神病学]