Tominaga Makoto
Section of Cell Signaling, Okazaki Institute for Integrative Bioscience (National Institute for Physiological Sciences), National Institutes of Natural Sciences, Higashiyama 5-1, Myodaiji, Okazaki, Aichi 444-8787, Japan.
Brain Nerve. 2008 May;60(5):493-501.
Transient receptor potential vanilloid 1 (TRPV1) is a receptor for capsaicin, which is a main ingredient in hot chili peppers, and belongs to the TRP ion channel superfamily. Researchers have confirmed that TRPV1 is activated by multiple nociceptive stimuli including protons, noxious heat and some lipids both in the heterologous expression system using the cloned channels and native sensory neurons. In addition, studies using mice lacking TRPV1 revealed its importance at the behavioral level. Since 1997, when TRPV1 was first cloned, a considerable amount of information has accumulated regarding its agonists, the mechanisms involved in its activation and regulation, and the structural bases of these mechanisms. Furthermore, several clinical trials involving the use of TRPV1 antagonists as analgesic agents are currently underway. With success, some of these agents may enter the market in the near future.
瞬时受体电位香草酸亚型1（TRPV1）是辣椒素的受体，辣椒素是辣椒中的主要成分，属于瞬时受体电位（TRP）离子通道超家族。研究人员已经证实，在使用克隆通道的异源表达系统和天然感觉神经元中，TRPV1可被多种伤害性刺激激活，包括质子、有害热和一些脂质。此外，对缺乏TRPV1的小鼠的研究揭示了其在行为水平上的重要性。自1997年TRPV1首次被克隆以来，已经积累了大量关于其激动剂、激活和调节机制以及这些机制的结构基础的信息。此外，目前正在进行几项使用TRPV1拮抗剂作为镇痛药的临床试验。如果成功，其中一些药物可能在不久的将来进入市场。
