| 河豚毒素的药用研究进展 |
| 投稿时间：2022-07-30 修订日期：2022-11-18 点此下载全文 |
| 引用本文：王琦,樊莉,卢光照,张翮,操雯,鲁莹.河豚毒素的药用研究进展[J].药学实践杂志,2023,41(5):273~276,328 |
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| 基金项目:军队“双重”项目：1-16生物毒素战剂控释研究与应用 |
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| 中文摘要:河豚毒素（TTX）是在河豚鱼和其他海洋动物中发现的一种神经毒素。它是一种电压门控钠通道（VGSCs）阻滞剂，能够选择性地与VGSCs外前庭上的α-亚基结合，阻止钠离子进入通道，从而产生药理活性。作为典型的钠离子通道阻滞剂，TTX具有显著的镇痛作用。TTX能够选择性地阻断Na+通道而不影响其他离子通道，减少了常用抗心律失常药物引起不良反应的概率，降低了用药风险。此外，TTX在戒毒等方面亦有显著作用。因此，TTX具有很大的成药潜力。本文对河豚毒素的结构与性质、作用机制、药理活性和在研制剂进行综述，为其成药性评价研究和在药学领域的应用提供概要性支撑。 |
| 中文关键词:河豚毒素 神经毒素 镇痛作用 药理活性 制剂 |
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| Advances in medicinal research on tetrodotoxin |
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| Abstract:Tetrodotoxin (TTX) is a neurotoxin found in puffer fish and other marine organisms. It has been used as an inhibitor of voltage-gated sodium channels (VGSCs), which could selectively bind to the α-subunit on the outer vestibule of VGSCs, preventing sodium ions from entering the channel, resulting in pharmacological activities. As a typical sodium channel blocker, TTX shows a significant analgesic effect. TTX could selectively block Na+ channels without affecting other ion channels, therefore it could reduce the probability of adverse reactions caused by commonly used antiarrhythmic drugs. In addition, TTX has a significant role in detoxification and prevention of renal failure, so TTX has great potential as a medicine. The structure and physicochemical properties, mechanism of action, pharmacological activities and preparations of tetrodotoxin have been reviewed in this paper, so as to provide a general support for the evaluation of its druggability and application in the field of pharmacy. |
| keywords:tetrodotoxin neurotoxin analgesic effect pharmacological activity preparation |
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