Geppetti Pierangelo, Materazzi Serena, Nicoletti Paola
Clinical Pharmacology Unit, Department of Critical Care Medicine and Surgery, University of Florence, Italy.
Eur J Pharmacol. 2006 Mar 8;533(1-3):207-14. doi: 10.1016/j.ejphar.2005.12.063. Epub 2006 Feb 7.
The transient receptor potential vanilloid 1 (TRPV1) is an excitatory cation channel, rather selectively expressed in a subpopulation of nociceptive, primary sensory neurons that promote neurogenic inflammation via neuropeptide release. TRPV1 is activated by noxious temperature, low extracellular pH and diverse lipid derivatives, and is uniquely sensitive to vanilloid molecules, including capsaicin. TRPV1 expression and sensitivity is highly regulated by diverse G protein-coupled and tyrosine kinase receptors. Other exogenous or endogenous chemical agents, including reactive oxygen species, ethanol and hydrogen sulphide sensitize/activate TRPV1. In the airways, TRPV1 agonists cause cough, bronchoconstriction, microvascular leakage, hyperreactivity and hypersecretion. Patients with asthma and chronic obstructive pulmonary disease are more sensitive to the tussive effect of TRPV1 agonists and TRPV1 activation may contribute to respiratory symptoms caused by acidic media present in the airways during asthma exacerbation, gastroesophageal reflux induced asthma or in other conditions. TRPV1 antagonists may be useful in the treatment of these diseases.
瞬时受体电位香草酸亚型1（TRPV1）是一种兴奋性阳离子通道，在伤害性初级感觉神经元亚群中选择性表达，这些神经元通过释放神经肽促进神经源性炎症。TRPV1可被有害温度、低细胞外pH值和多种脂质衍生物激活，并且对包括辣椒素在内的香草酸类分子具有独特的敏感性。TRPV1的表达和敏感性受到多种G蛋白偶联受体和酪氨酸激酶受体的高度调节。其他外源性或内源性化学物质，包括活性氧、乙醇和硫化氢，可使TRPV1敏感/激活。在气道中，TRPV1激动剂可引起咳嗽、支气管收缩、微血管渗漏、高反应性和分泌亢进。哮喘和慢性阻塞性肺疾病患者对TRPV1激动剂的咳嗽作用更敏感，TRPV1激活可能导致哮喘加重、胃食管反流诱发哮喘或其他情况下气道中酸性介质引起的呼吸道症状。TRPV1拮抗剂可能对这些疾病的治疗有用。
