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河豚毒素(TTX)是一种海洋生物毒素。TTX首次在河豚中提取得到,而后在多个海洋动植物和陆地部分动物中发现。TTX是一种电压门控钠通道(VGSCs)的阻滞剂,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。TTX具有镇痛、戒毒、抗心律失常等作用,此外,还有降低心血管药物不良反应的作用。目前已经有许多TTX在研制剂,研究者也正在针对TTX的剂型进行研究。本文就TTX的来源、结构性质、作用机制、药理活性、在研剂型进行综述,旨在为下一步TTX的药用开发提供参考。
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