小分子钠通道阻滞剂镇痛构效关系的研究进展  

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

作　　者：李雯[1] 周游[2] 刘宏民[2] 尤启冬[3] 

机构地区：[1]郑州大学化学工程学院,河南郑州450001 [2]郑州大学药学院,河南郑州450001 [3]中国药科大学药学院,江苏南京210009

出　　处：《药学学报》2009年第2期101-108,共8页Acta Pharmaceutica Sinica

摘　　要：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 common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.

关 键 词：钠通道阻滞剂 先导化合物 镇痛药物 构效关系 

分 类 号：R916.2[医药卫生—药学]