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.