莫达芬尼对小鼠中枢兴奋作用的构效和时效关系的初步研究(英文)  

Preliminary Studies on the Structure-activity and Time-effect Relations of the Central Stimulating Effects of Modafinil in Mice

作　　者：詹皓[1] 唐桂香[1] 辛益妹[1] 李砚锋[1] 李彤[1] 韦四煌[1] 穆报春[1] 雷光清[1] 

机构地区：[1]空军航空医学研究所,北京,100036

出　　处：《航天医学与医学工程》2004年第1期12-15,共4页Space Medicine & Medical Engineering

基　　金：supportedbyPLAMedicalResearchFoundation(KH0 10 80 11)

摘　　要：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。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.

关 键 词：中枢兴奋药 莫达芬尼 构效关系 量效关系 时效关系 自主活动 

分 类 号：R859[医药卫生—航空、航天与航海医学]