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首页> 美国卫生研究院文献>Marine Drugs >Tetrodotoxin a Candidate Drug for Nav1.1-Induced Mechanical Pain?
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Tetrodotoxin a Candidate Drug for Nav1.1-Induced Mechanical Pain?

机译：河豚毒素Nav1.1引起的机械性疼痛的候选药物？

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摘要

Tetrodotoxin (TTX), the mode of action of which has been known since the 1960s, is widely used in pharmacology as a specific inhibitor of voltage-gated sodium channels (Nav channels). This toxin has contributed to the characterization of the allosteric model of the Nav channel, and to discriminating TTX-sensitive and TTX-resistant subtypes. In addition to its role as a pharmacological tool, TTX is now considered a therapeutic molecule, and its development should lead to its use in certain pathologies involving Nav channels, particularly in the field of pain. Specifically, the blockade of Nav channels expressed in nociceptive fibres is one strategy for alleviating pain and its deleterious consequences on health. Recent work has identified, in addition to the Nav1.7, 1.8 and 1.9 channels, the Nav1.1 subtype on dorsal root ganglion (DRG) neurons as a crucial player in mechanical and non-thermal pain. The sensitivity of Nav1.1 to TTX could be exploited at the therapeutic level, especially in chronic pain conditions.
机译：河豚毒素（TTX）的作用方式自1960年代就已为人所知，在药理学中已广泛用作电压门控钠通道（Nav通道）的特异性抑制剂。该毒素有助于Nav通道的变构模型的表征，并有助于区分TTX敏感和TTX耐药亚型。除了其作为药理学工具的作用外，TTX现在还被认为是一种治疗性分子，其发展应导致其在涉及Nav通道的某些病理中使用，尤其是在疼痛领域。具体而言，以伤害感受纤维表达的Nav通道的阻滞是减轻疼痛及其对健康的有害影响的一种策略。除了Nav1.7、1.8和1.9通道外，最近的工作还确定了背根神经节（DRG）神经元上的Nav1.1亚型是机械性和非热性疼痛的关键因素。可以在治疗水平上利用Nav1.1对TTX的敏感性，特别是在慢性疼痛情况下。

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