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用于治疗神经性疼痛的电压门控性钠通道阻滞剂

Voltage-gated sodium channel blockers for the treatment of neuropathic pain.

作者信息

Cummins Theodore R, Rush Anthony M

机构信息

Assistant Professor of Pharmacology & Toxicology, Stark Neurosciences Research Institute, Indiana University, School of Medicine, 950 W Walnut St, R2-Room 468, Indianapolis, IN 46202, USA.

出版信息

Expert Rev Neurother. 2007 Nov;7(11):1597-612. doi: 10.1586/14737175.7.11.1597.

Abstract

Pain serves a crucial physiological function, warning the body of impending or actual tissue damage, preventing further damage and aiding the healing process. Neuropathic pain, resulting from nervous system injury or dysfunction, can be a serious medical problem and especially difficult to treat. Although sodium channel blockers are clinically useful for treating pain, they often provide only partial relief and adverse effects associated with nonspecific actions can limit their use. Research on the roles of sodium channels in neuronal excitability and pain shows that specific sodium channel isoforms are crucial determinants of nociception and neuropathic pain, indicating that it should be possible to develop sodium channel blockers with lower toxicity and enhanced efficacy for treating neuropathic pain.

摘要

疼痛起着至关重要的生理作用,它能警告身体即将发生或实际存在的组织损伤,防止进一步损伤并辅助愈合过程。神经性疼痛由神经系统损伤或功能障碍引起,可能是一个严重的医学问题,尤其难以治疗。尽管钠通道阻滞剂在临床上可用于治疗疼痛,但它们通常只能提供部分缓解,且与非特异性作用相关的不良反应会限制其使用。关于钠通道在神经元兴奋性和疼痛中作用的研究表明,特定的钠通道亚型是伤害感受和神经性疼痛的关键决定因素,这表明应该有可能开发出毒性更低、疗效更强的钠通道阻滞剂来治疗神经性疼痛。

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