CPPS, DECS, AstraZeneca R&D, Sweden.
Curr Top Med Chem. 2011;11(17):2180-91. doi: 10.2174/156802611796904843.
Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons. TRPV1 is acting as an important signal integrator in sensory nociceptors under physiological and pathological conditions including inflammation and neuropathy. Because of its integrative signaling properties in response to inflammatory stimuli, TRPV1 agonists and antagonists are predicted to inhibit the sensation of ongoing or burning pain that is reported by patients suffering from chronic pain, therefore offering an unprecedented advantage in selectively inhibiting painful signaling from where it is initiated. In this article, we firstly summarize recent advances in the understanding of the role of TRPV1 in pain signaling, including a overview of clinical pharmacological trials using TRPV1 agonists and antagonists. Finally, we also present an update on the mechanistic understanding and controlling of hyperthermia caused by TRPU1 antagonists, and provide perspective for future study.
瞬时受体电位香草酸 1 型通道（TRPV1）是一种非选择性阳离子通道，由有害热、香草酸和细胞外质子门控。TRPV1 在生理和病理条件下（包括炎症和神经病变）作为感觉伤害感受器中的重要信号整合器发挥作用。由于其对炎症刺激的整合信号特性，TRPV1 激动剂和拮抗剂预计将抑制慢性疼痛患者报告的持续性或灼痛感觉，因此在选择性抑制疼痛信号的起始部位方面具有前所未有的优势。在本文中，我们首先总结了 TRPV1 在疼痛信号转导中的作用的最新进展，包括使用 TRPV1 激动剂和拮抗剂的临床药理学试验概述。最后，我们还介绍了 TRPU1 拮抗剂引起的高热的机制理解和控制的最新进展，并为未来的研究提供了展望。
