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目的初步探讨莫达芬尼 (Mod)中枢兴奋作用的构效和时效关系特征以利于此类药物的设计开发和合理使用。方法以小鼠为实验对象 ,比较Mod及两种衍生物中枢兴奋作用的量效 ( 60、1 2 0、2 4 0mg/kg)和时效特征 ;观察Mod ( 1 2 0mg/kg)昼夜给药兴奋作用的差异。结果Mod可剂量相关地提高小鼠自主活动 ,以 1 2 0mg/kg效果最佳 ;氯化有增强其作用的趋势、而甲基化使作用降低。昼夜给予Mod的兴奋作用无明显差别。结论Mod中枢兴奋作用具有明显的量效时效特征 ,氯化有增强其作用的趋势、而甲基化使作用降低
Objective To explore the structure-activity and time-effect characteristics of modal center excitability in order to facilitate the design, development and rational use of these drugs. Methods The mice were used as experimental subjects to compare the dose-effect (60,120,440 mg / kg) and time-lapse characteristics of mod and the excitatory effects of the two derivatives. Mod (120 mg / kg) Differences in excitement. Results Mod can increase the autonomic activity of mice in a dose-dependent manner, with the best effect being at 120 mg / kg. Chloride has a tendency of increasing its effect, and the effect of methylation decreases. Day and night to give Mod the excitement no significant difference. Conclusion The excitatory effect of Mod central has obvious dose-effect and time-dependent characteristics. Chlorination has a tendency of increasing its effect, while the methylation reduces the effect