以TRPV3为靶点开发新型镇痛药。
Targeting TRPV3 for the Development of Novel Analgesics.
作者信息
Huang Susan M, Chung Man-Kyo
机构信息
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.
Department of Neural and Pain Sciences, School of Dentistry, Program in Neuroscience, University of Maryland, 650 W. Baltimore Street, Baltimore, MD 21201, USA.
出版信息
Open Pain J. 2013;6(Spec Iss 1):119-126. doi: 10.2174/1876386301306010119.
Decades of characterization of the transient receptor potential vanilloid subtype 1 (TRPV1) has led to the realization of its central role in thermosensation and pain perception. A large number of pharmaceutical companies have had interest in developing TPRV1 antagonists for the treatment of pain. The subsequent discovery of multiple other members of this TRPV family has not gone unnoticed. TRPV3 exhibits approximately 40% homology to TRPV1, and has common as well as distinct features from TRPV1 in channel physiology, expression and function. Here we review the current understanding of TRPV3 channel biology, activation, sensitization and the consequences of TRPV3 manipulation for thermosensation and nociception, as well as additional considerations regarding the expression of TRPV3 in the skin. We weigh in on the available evidence in the context of potential development of TRPV3 modulating agents as analgesics.
数十年来对瞬时受体电位香草酸亚型1（TRPV1）的特性研究，使人们认识到它在热感觉和痛觉感知中发挥着核心作用。大量制药公司对开发TRPV1拮抗剂用于疼痛治疗产生了兴趣。随后该TRPV家族其他多个成员的发现也受到了关注。TRPV3与TRPV1具有约40%的同源性，在通道生理学、表达和功能方面与TRPV1既有共同特征，也有不同特征。在此，我们综述了目前对TRPV3通道生物学、激活、敏化以及TRPV3调控对热感觉和伤害感受影响的理解，以及关于TRPV3在皮肤中表达的其他相关考量。我们在TRPV3调节剂作为镇痛药潜在开发的背景下，对现有证据进行了权衡。
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