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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。
Pain is one of the most common clinical symptoms and sodium channels are currently recognized as molecular targets for analgesic research. Sodium channel blocker analgesics can block the sodium channel effectively, which can play a good analgesic effect. However, the existing analgesic drugs in clinic have all kinds of shortcomings and can not meet the need of treatment. Therefore, looking for a new structural type and a new mechanism of action of sodium channel blockers analgesic lead compounds for the development of a new generation of analgesic drugs is of great significance. This review summarizes the reports of small molecular sodium channel blocker-type analgesics leading compounds in recent years, discusses their chemical structure, sodium channel blockade and structure-activity relationship in detail, and reviews their existing problems and future Direction of development.