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Preliminary studies on the structure-activity and time-effect relations of the central stimulating effects of
Hao Zhan1, Gui-xiang Tang, Yi-mei Xin
1Institute of Aviation Medicine, Beijing.
Objective:
To observe the structure-activity and time-effect relations of the central stimulating effects of modafinil for further pharmaceutical design and development and rational use of this kind of stimulant.
Method:
Male mice served as subjects. The experiment was divided into two parts: 1) comparison between the dose (60, 120, 240 mg/kg) and temporal features of the effects of modafinil and its two derivatives on locomotor activity of mice; 2) Observation of the stimulating effects of modafinil (120 mg/kg) given during the day or night.
Result:
Modafinil could significantly increase the locomotor activity of mice in a dose-dependent way, the effect was best observed at the concentration of 120 mg/kg. The stimulating action of modafinil was increased by chlorination, but decreased by methylation. The central stimulating effect of modafinil showed no significant circadian difference.
Conclusion:
The central stimulating effect of modafinil shows dose and time-related features. The effect tends to be enhanced by Chlorination but reduced by methylation.
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