Acta Pharmaceutica Sinica 2009;44(2):101-108

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

Wen LI 1 ; You ZHOU ; Hong-Min LIU ; Qi-Dong YOU

Affiliations

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Country

China

Language

Chinese

Abstract

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.