Department of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, Brisbane, QLD, Australia.
Br J Pharmacol. 2018 Jun;175(12):2138-2157. doi: 10.1111/bph.13962. Epub 2017 Sep 2.
Voltage-gated sodium channels (Na channels) are essential for the initiation and propagation of action potentials that critically influence our ability to respond to a diverse range of stimuli. Physiological and pharmacological studies have linked abnormal function of Na channels to many human disorders, including chronic neuropathic pain. These findings, along with the description of the functional properties and expression pattern of Na channel subtypes, are helping to uncover subtype specific roles in acute and chronic pain and revealing potential opportunities to target these with selective inhibitors. High-throughput screens and automated electrophysiology platforms have identified natural toxins as a promising group of molecules for the development of target-specific analgesics. In this review, the role of toxins in defining the contribution of Na channels in acute and chronic pain states and their potential to be used as analgesic therapies are discussed.
This article is part of a themed section on Recent Advances in Targeting Ion Channels to Treat Chronic Pain. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.12/issuetoc.
电压门控钠离子通道（Na 通道）对动作电位的产生和传播至关重要，而动作电位则会极大地影响我们对各种刺激的反应能力。生理和药理学研究将 Na 通道的异常功能与许多人类疾病联系起来，包括慢性神经性疼痛。这些发现，以及 Na 通道亚型的功能特性和表达模式的描述，正在帮助揭示其在急性和慢性疼痛中的特定亚型作用，并揭示了用选择性抑制剂靶向这些作用的潜在机会。高通量筛选和自动化电生理学平台已经确定天然毒素是开发靶向特定镇痛药的有希望的分子群。在这篇综述中，讨论了毒素在确定 Na 通道在急性和慢性疼痛状态中的作用及其用作镇痛疗法的潜力。
本文是针对靶向离子通道治疗慢性疼痛的最新进展这一主题部分的一部分。要查看该部分中的其他文章，请访问 http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.12/issuetoc.
