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Since chemical structures of ginsenoside as active ingredient of Panaxdences have shown that ginsenoside is one of bio-active ligands through the diverse physiological and pharmacologicalevaluations. Chemical structure of ginsenoside could be divided into three parts depending on diol or triol ginsenoside:Steroid- or cholesterol-like backbone structure, carbohydrate portions, which are attached at the carbon-3, -6 or -20, andaliphatic side chain coupled to the backbone structure at the carbon-20. Ginsenosides also exist as stereoisomer at the car-about the relationship of chemical structure and biological activity. Recent reports have shown that ginsenoside Rg3, oneof active ginsenosides, exhibits differential physiological or pharmacological actions depending on its chemical struc-ture. This review will show how ginsenoside Rg3, as a model compound, is functionally coupled to voltage-gated ionchannel or ligand-gated ion channel regulations in related with its chemical structure.