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Recent advances in the structure-activity relationship study of small-molecule sodium channel blockers with analgesic effects

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Author:: No author available

Journal Title:: ACTA PHARMACEUTICA SINICA

Issue:: 2

DOI:: 10.3321/j.issn:0513-4870.2009.02.001

Key Word:: 钠通道阻滞剂;先导化合物;镇痛药物;构效关系

Abstract：疼痛是常见的临床症状之一,目前钠通道被公认为镇痛药物研究的分子靶位.钠通道阻滞剂型镇痛药物通过有效阻滞钠通道,能起到很好的镇痛作用,但临床上现有的镇痛药物均存在种种缺陷,难以满足治疗需要.因此,寻找全新结构类型和全新作用机制的钠通道阻滞剂型镇痛先导化合物对研发新一代镇痛药物具有重要意义.本文综述了近年来报道的小分子钠通道阻滞剂型镇痛药物先导化合物的研究,详细讨论了它们的化学结构、钠通道阻滞作用和构效关系,并评述了它们的现有问题和未来发展方向.

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