石杉碱甲、E2020和他克林对大鼠的抗胆碱酯酶作用。
Anticholinesterase effects of huperzine A, E2020, and tacrine in rats.
作者信息
Wang H, Tang X C
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
出版信息
Zhongguo Yao Li Xue Bao. 1998 Jan;19(1):27-30.
AIM
To compare the anticholinesterase effects of huperzine A (Hup A), E2020, and tacrine in rats.
METHODS
Spectrophotometry was used to determine AChE activity in brain and BuChE activity in serum.
RESULTS
Following intragastric gavage, Hup A, E2020, and tacrine all produced dose-dependent inhibitions of brain AChE. Oral Hup A exhibited a higher inhibition than E2020 and tacrine. Tacrine was more effective in inhibiting serum BuChE correlated with severe peripheral adverse effects. The BuChE activity was less affected by Hup A and E2020. After a single oral dose of Hup A, a relatively steady state of AChE inhibition produced, which was longer than that after E2020 and tacrine. No change in the cholinesterase inhibition was seen for the 3 drugs following repeated i.g. medications.
CONCLUSION
Hup A i.g. exhibited a higher efficacy, a longer duration of action, and a more selective inhibition on AChE than E2020 and tacrine.
目的
比较石杉碱甲（Hup A）、E2020和他克林对大鼠的抗胆碱酯酶作用。
方法
采用分光光度法测定脑内乙酰胆碱酯酶（AChE）活性和血清中丁酰胆碱酯酶（BuChE）活性。
结果
灌胃给药后，Hup A、E2020和他克林均对脑AChE产生剂量依赖性抑制。口服Hup A的抑制作用高于E2020和他克林。他克林在抑制血清BuChE方面更有效，但伴有严重的外周不良反应。Hup A和E2020对BuChE活性的影响较小。单次口服Hup A后，AChE抑制作用产生相对稳定的状态，且持续时间长于E2020和他克林。重复灌胃给药后，3种药物的胆碱酯酶抑制作用均未见变化。
结论
灌胃给予Hup A比E2020和他克林具有更高的疗效、更长的作用持续时间以及对AChE更具选择性的抑制作用。
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