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 pain-related 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.