药学学报2024,Vol.59Issue(9) :2417-2428.DOI:10.16438/j.0513-4870.2024-0259

靶向Nav1.7的镇痛药物开发:临床试验进展与选择性抑制剂发现

Development of analgesic drugs targeting Nav1.7:advances in clinical trials and discovery of selective inhibitors

韩蕊 蔡怡琳 郑晓彤 林凡祺 张凡
药学学报2024,Vol.59Issue(9) :2417-2428.DOI:10.16438/j.0513-4870.2024-0259

靶向Nav1.7的镇痛药物开发:临床试验进展与选择性抑制剂发现

Development of analgesic drugs targeting Nav1.7:advances in clinical trials and discovery of selective inhibitors

韩蕊 1蔡怡琳 1郑晓彤 1林凡祺 1张凡1
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作者信息

  • 1. 中国药科大学中药学院,江苏南京 211198
  • 折叠

摘要

电压门控钠离子通道亚型Nav1.7在伤害性感觉神经元中高表达,是多种人类遗传性疼痛综合征的关键致病靶点.近年来,大量研究表明Nav1.7在炎性、神经病理性及伤害性刺激诱发的疼痛中具有重要作用.因此,靶向抑制Nav1.7是新型镇痛药研制的新策略和热点.本文介绍了Nav1.7的结构与功能、在疼痛中的调节作用,重点总结了临床试验中Nav1.7小分子抑制剂的开发进展,并对临床前Nav1.7高专一性抑制剂的开发进行了分析,以期为Nav1.7镇痛药物的开发提供参考.

Abstract

The voltage-gated sodium channel subtype Nav1.7 is highly expressed in nociceptive sensory neurons and is a key pathogenic target in several human hereditary pain syndromes.In recent years,a large number of studies have shown that Nav1.7 plays an important role in inflammatory,neuropathic,and nociceptive pain.Therefore,targeting Nav1.7 is a new strategy and hotspot for the development of novel analgesics.This review introduces the structure and function of Nav1.7,its regulatory role in pain,highlights the development progress of small-molecule Nav1.7 inhibitors in clinical trials,and analyzes the preclinical development of highly specific Nav1.7 inhibitors,with a view to providing reference for the development of Nav1.7 analgesic drugs.

关键词

Nav1.7/疼痛/镇痛药物/临床研究/选择性抑制剂

Key words

Nav1.7/pain/analgesic drug/clinical trial/selective inhibitor

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出版年

2024
药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
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