CAJ | 학술논문

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、120、240 mg/kg)和时效特征;观察Mod (120 mg/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120 mg/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.
목적초보탐토막체분니(Mod)중추흥강작용적구효화시효관계특정이리우차류약물적설계개발화합리사용.방법이소서위실험대상,비교Mod급량충연생물중추흥강작용적량효(60、120、240 mg/kg)화시효특정;관찰Mod (120 mg/kg) 주야급약흥강작용적차이.결과 Mod가제량상관지제고소서자주활동,이120 mg/kg효과최가;록화유증강기작용적추세、이갑기화사작용강저.주야급여Mod적흥강작용무명현차별.결론 Mod중추흥강작용구유명현적량효시효특정,록화유증강기작용적추세、이갑기화사작용강저.
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.