论文部分内容阅读
目的：比较石杉碱甲、Ｅ２０２０和他克林对大鼠胆碱酯酶的抑制作用．方法：比色法测定大鼠各脑区的ＡＣｈＥ及血清中ＢｕＣｈＥ活力．结果：三药灌胃后对大鼠脑中ＡＣｈＥ均产生剂量依赖性抑制．以石杉碱甲作用最强．他克林对ＢｕＣｈＥ的抑制显著强于Ｅ２０２０和石杉碱甲，其副反应最为明显．单次经口给药后，石杉碱甲对脑内ＡＣｈＥ的抑制作用长于Ｅ２０２０和他克林．多次给药后，对胆碱酯酶的抑制作用三药均未有耐受性产生．结论：石杉碱甲是一种高选择性ＡＣｈＥ抑制剂，具有口服活性高，作用时程长，副反应小的优点，适于临床应用．
Objective: To compare the inhibitory effects of huperzine A, E2020 and tacrine on the cholinesterase in rats. Methods: The colorimetric method was used to determine the AChE and BuChE activity in various brain regions of rats. Results: The three drugs can inhibit the AChE in rat brain in a dose-dependent manner. Huperzine A strongest role. The inhibitory effect of tacrine on BuChE was significantly stronger than that of E2020 and huperzine A. The side effects were the most obvious. After a single oral administration, Huperzine A had a greater inhibitory effect on AChE in the brain than E2020 and tacrine. Repeated administration, the inhibition of cholinesterase three drugs were not tolerated. Conclusion: Huperzine A is a highly selective AChE inhibitor with the advantages of high oral activity, long duration of action and little side reaction, which is suitable for clinical application.