DECS, Cell, Protein, and Structure Sciences, AstraZeneca R&D, Mölndal SE-43183, Sweden.
Adv Exp Med Biol. 2011;704:637-65. doi: 10.1007/978-94-007-0265-3_34.
TRPV1 is a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons, and act as an important signal integrator in sensory nociceptors. Because of its integrative signaling properties in response to inflammatory stimuli, TRPV1 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 chapter, we firstly summarize the physiological and pathological roles of TRPV1 and then describe the pharmacology of TRPV1 agonists and antagonists. Finally, we give an update and the status on TRPV1 therapies that have progressed into clinical trials.
TRPV1 是一种非选择性阳离子通道，由有害热、香草素和细胞外质子门控，作为感觉伤害感受器中重要的信号整合器。由于其对炎症刺激的整合信号特性，TRPV1 拮抗剂预计可抑制慢性疼痛患者报告的持续性或灼痛感觉，因此在选择性抑制起始部位的疼痛信号方面具有前所未有的优势。在本章中，我们首先总结 TRPV1 的生理和病理作用，然后描述 TRPV1 激动剂和拮抗剂的药理学。最后，我们介绍 TRPV1 治疗方法的最新进展和临床试验状况。
