【摘 要】
：
目的 手性药物M-2是一种新型神经兴奋剂,作用于中枢神经系统下丘脑部位,具有明显的提神、增强记忆力和缩短反应时间的作用,现已成功用于治疗发作性睡眠症及自发性睡眠过度.本研究的目的是建立液质联用法(HPLC/MS/MS)测定人肝微粒体中R/S-M2的药物浓度,旨在研究手性药物其左旋体和右旋体在体外代谢的差异.方法 于人肝微粒体孵育液中分别加入R/S-M2,用HPLC/MS/MS测定孵育液中不同时间点
【机 构】
：
军事医学科学院野战输血研究所药物代谢重点实验室,北京 100850
【出 处】
：
第十届全国药物和化学异物代谢学术会议暨第三届国际ISSX/CSSX联合学术会议
论文部分内容阅读
目的 手性药物M-2是一种新型神经兴奋剂,作用于中枢神经系统下丘脑部位,具有明显的提神、增强记忆力和缩短反应时间的作用,现已成功用于治疗发作性睡眠症及自发性睡眠过度.本研究的目的是建立液质联用法(HPLC/MS/MS)测定人肝微粒体中R/S-M2的药物浓度,旨在研究手性药物其左旋体和右旋体在体外代谢的差异.方法 于人肝微粒体孵育液中分别加入R/S-M2,用HPLC/MS/MS测定孵育液中不同时间点的M-2对映体浓度,以西达本胺为内标,采用Phenomex C18色谱柱(2.0 mm×50.0 mm,5μm),流动相以含0.1％甲酸的水溶液和含0.1％甲酸的乙腈溶液梯度洗脱,流速为0.3mL·min-1,柱温：室温.结果 R/S-M2在0.25～10000 ng·mL-1范围内对于CYP3A4、CYP2C9、CYP2D6及CYP2C19亚型均无抑制作用.S-M2在人肝微粒体中代谢比R-M2.结论 R-M2内半数消除期要长,在机体内发挥药效的时间也更持久.
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