Nueroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6125, USA.
Curr Top Med Chem. 2011;11(17):2210-5. doi: 10.2174/156802611796904889.
The vanilloid subfamily of transient receptor potential (TRPV) ion channels serves critical functions in sensory signaling in specialized cells and intact organisms ranging from yeast to primates. As thermosensors, chemosensors, and/or mechanosensors, these channels monitor the local environment and integrate and respond to multiple stimuli distinctively. More than a decade of research on the founding member of the subclass, TRPV1, has led to advancement of multiple antagonists into the clinic for the treatment of chronic pain. In recent years the comprehensive knowledge accessed through these studies has been applied to enhance understanding of other TRPV isoforms and, in particular, to determine whether they, too, represent promising targets for drug discovery. This review focuses on emerging data that define a role for TRPV3 in transducing signals in pain pathways and identify antagonists that demonstrate efficacy in relevant preclinical behavioral models.
辣椒素亚家族的瞬时受体电位 (TRPV) 离子通道在从酵母到灵长类动物等专门细胞和完整生物体的感觉信号转导中发挥着关键作用。作为热传感器、化学传感器和/或机械传感器，这些通道监测局部环境，并对多种独特的刺激进行整合和响应。对该亚类的创始成员 TRPV1 的十多年研究，已经有多种拮抗剂进入临床用于治疗慢性疼痛。近年来，通过这些研究获得的全面知识已被应用于增强对其他 TRPV 同工型的理解，特别是确定它们是否也代表有前途的药物发现靶点。这篇综述重点介绍了 TRPV3 在痛觉通路中传递信号的作用的新数据，并确定了在相关临床前行为模型中显示出疗效的拮抗剂。
