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The purpose of this study was to investigate the in vivo antidopaminergic activities of polygalasaponins which are included in the roots of Polygalae tenuifolia, one of the natural plants used to treat psychotic disorders in traditional medicine. Chemical separations were performed using chromatography with various columns and the chemical structures were identified using spectroscopy, NMR and other techniques. The apomorphine-induced stereotyped behaviors and climbing behavior of mice were used as animal models of psychotic disorders in order to explore the antidopaminergic activity. The active compounds with antidopaminergic effects in the roots of Polygalae tenuifolia were identified as polygalasaponin A-D. These polygalasaponins were shown to suppress the apomorphine-induced stereotyped behaviors and climbing behavior in a dose-related fashion. This study suggests that polygalasaponins might have antipsychotic activities. These natural products need to be explored extensively as a source of new medication in the psychiatric field. Further explorations of the chemical and pharmacological properties of these polygalasaponins are required.

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