Jia Yanlin, McLeod Robbie L, Hey John A
Pulmonary and Peripheral Neurobiology, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA. yanlin.jia@spcorp. com
Drug News Perspect. 2005 Apr;18(3):165-71. doi: 10.1358/dnp.2005.18.3.892761.
The TRPV1 channel is mainly expressed in sensory nerves. Activation of the channel induces neuropeptide release from central and peripheral sensory nerve terminals, resulting in the sensation of pain, neurogenic inflammation, smooth muscle contraction and cough. The TRPV1 channel can be activated by vanilloids such as capsaicin, as well as endogenous stimulators including H(+), heat, lipoxygenase products and anandamide. TRPV1 channel function is upregulated by several endogenous mediators present in inflammatory conditions, which decreases the threshold for activation of the channel. Under these conditions, TRPV1 can be activated by physiological body temperature, slight acidification or lower concentration of TRPV1 agonists. There is evidence that TRPV1 plays a role in the development of pathophysiological changes and symptoms in several diseases. In this review, we discuss TRPV1 channel activation and regulation in normal and diseased conditions, the role of TRPV1 in pain, cough, asthma and urinary incontinence, and the potential use of TRPV1 antagonists as a novel therapy for these diseases.
瞬时受体电位香草酸亚型1（TRPV1）通道主要表达于感觉神经。该通道的激活可诱导神经肽从中枢和外周感觉神经末梢释放，从而导致疼痛、神经源性炎症、平滑肌收缩和咳嗽等感觉。TRPV1通道可被辣椒素等香草酸类物质激活，也可被包括氢离子、热、脂氧合酶产物和花生四烯酸乙醇胺在内的内源性刺激物激活。在炎症状态下，几种内源性介质可上调TRPV1通道功能，降低通道激活阈值。在这些情况下，TRPV1可被生理体温、轻微酸化或较低浓度的TRPV1激动剂激活。有证据表明，TRPV1在多种疾病的病理生理变化和症状发展中起作用。在本综述中，我们讨论了正常和疾病状态下TRPV1通道的激活和调节、TRPV1在疼痛、咳嗽、哮喘和尿失禁中的作用，以及TRPV1拮抗剂作为这些疾病新疗法的潜在用途。
