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作为疼痛靶点的感觉神经元钠通道;从可卡因到Journavx(VX-548,舒泽曲明)。

Sensory neuron sodium channels as pain targets; from cocaine to Journavx (VX-548, suzetrigine).

作者信息

Wood John N, Yan Nieng, Huang Jian, Zhao Jing, Akopian Armen, Cox James J, Woods C Geoffrey, Nassar Mohammed A

机构信息

Molecular Nociception Group, Wolfson Institute for Biomedical Research, UCL , London, UK.

Beijing Frontier Research Center for Biological Structures, State Key Laboratory of Membrane Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Life Sciences, Tsinghua University , Beijing, China.

出版信息

J Gen Physiol. 2025 Jul 7;157(4). doi: 10.1085/jgp.202513778. Epub 2025 Apr 28.

Abstract

Voltage-gated sodium channels underpin electrical signaling in sensory neurons. Their activity is an essential element in the vast majority of pain conditions, making them significant drug targets. Sensory neuron sodium channels play roles not only in afferent signaling but also in a range of efferent regulatory mechanisms. Side effects through actions on other cell types and efferent signaling are thus important issues to address during analgesic drug development. As an example, the human genetic evidence for NaV1.7 as an ideal pain target contrasts with the side effects of NaV1.7 antagonists. In this review, we describe the history and progress toward the development of useful analgesic drugs and the renewed focus on NaV1.8 as a key target in pain treatment. NaV1.8 antagonists alone or in combination with other analgesics are likely to provide new opportunities for pain relief for the vast number of people (about 33% of the population) impacted by chronic pain, particularly present in aging populations.

摘要

电压门控钠通道是感觉神经元电信号传导的基础。它们的活性是绝大多数疼痛病症的关键要素,使其成为重要的药物靶点。感觉神经元钠通道不仅在传入信号传导中发挥作用,还参与一系列传出调节机制。因此,在镇痛药研发过程中,药物作用于其他细胞类型及传出信号传导所产生的副作用是需要重点关注的问题。例如,NaV1.7作为理想疼痛靶点的人类遗传学证据,与其拮抗剂的副作用形成了鲜明对比。在这篇综述中,我们阐述了开发有效镇痛药的历史与进展,以及将NaV1.8重新作为疼痛治疗关键靶点的研究动态。单独使用或与其他镇痛药联合使用NaV1.8拮抗剂,可能为受慢性疼痛影响的广大人群(约占总人口的33%),尤其是老年人群体,带来缓解疼痛的新机遇。

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