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Nav1.8抑制剂在疼痛治疗中的研究进展

Research Progress on Nav1.8 Inhibitors in Pain Therapeutics

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【作者】 徐金波汤依群

【Author】 XU Jinbo;TANG Yiqun;China Pharmaceutical University;

【通讯作者】 汤依群;

【机构】 中国药科大学

【摘要】 电压门控钠通道Nav1.8特异性表达于外周伤害感受神经元,介导了动作电位上升阶段的主要内向电流,在痛觉信号的产生和传导中发挥重要作用。针对传统阿片类镇痛药物存在的成瘾性和呼吸抑制等严重不良反应,开发新型非阿片类高效镇痛药物已成为临床上疼痛管理的迫切需求。基于Nav1.8亚型外周选择性表达的特点,Nav1.8抑制剂能够有效避免传统钠通道阻滞剂的中枢神经系统和心血管不良反应,具有独特的治疗优势。本文从Nav1.8的结构和功能出发,总结了近几年来有关Nav1.8抑制剂的研究进展,为疼痛的临床治疗和药物开发提供参考。

【Abstract】 The voltage-gated sodium channel Nav1.8 is specifically expressed in peripheral nociceptive neurons and mediates the predominant inward currents during the rising phase of action potentials, playing a key role in the generation and propagation of nociceptive signaling. Given the severe adverse effects of traditional opioid analgesics,such as addictive potential and respiratory depression, the development of novel non-opioid analgesics with high efficacy has become an urgent clinical need for pain management. Based on the characteristics of peripheral selective expression of Nav1.8, inhibitors targeting this subtype demonstrate unique therapeutic advantages by effectively circumventing central nervous system and cardiovascular adverse effects associated with traditional sodium channel blockers. This review focuses on the structure and function of Nav1.8 and summarizes recent advances in the development of Nav1.8inhibitors, aiming to provide valuable insights for clinical pain management and future drug discovery.

【基金】 “重大新药创制”科技重大专项(2017ZX09301066)
  • 【文献出处】 生物化工 ,Biological Chemical Engineering , 编辑部邮箱 ,2025年03期
  • 【分类号】R965;R402
  • 【下载频次】19
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