TRPV1型
瞬时受体电位通道
背景(考古学)
神经科学
化学
离子通道
感觉系统
计算生物学
心理学
受体
生物化学
生物
古生物学
作者
Kun Zhu,Lin Wang,Tingting Liao,Wen Li,Jing Zhou,Yaodong You,Jianyou Shi
标识
DOI:10.1016/j.ejmech.2023.115806
摘要
Transient receptor potential vanilloid 1 (TRPV1) channels are widely distributed in sensory nerve endings, the central nervous system, and other tissues, functioning as ion channel proteins responsive to thermal pain and chemical stimuli. In recent years, the TRPV1 receptor has garnered significant interest as a potential therapeutic approach for various pain-related disorders, particularly TRPV1 antagonists. The present review offers a comprehensive, systematic exploration of both first- and second-generation TRPV1 antagonists in the context of pain management. Antagonists are categorized and explicated according to their structural characteristics. Detailed examination of binding modes, structural features, and pharmacological activities, alongside a critical appraisal of the advantages and limitations inherent to typical compounds within each structural category, are undertaken. Detailed discussions of the binding modes, structural features, pharmacological activities, advantages, and limitations of typical compounds within each structural category offer valuable insights and guidance for the future research and development of safer, more effective, and more targeted TRPV1 antagonists.
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