Comparative effects of huperzine A, donepezil and rivastigmine on cortical acetylcholine level and acetylcholinesterase activity in rats

被引：77

作者：

Liang, YQ ^{[1
]}

Tang, XC ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China

来源：

NEUROSCIENCE LETTERS | 2004年 / 361卷 / 1-3期

基金：

中国国家自然科学基金;

关键词：

huperzine A; donepezil; rivastigmine; acetylcholine; acetylcholinesterase; Alzheimer's disease; rat;

D O I：

10.1016/j.neulet.2003.12.071

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

The cholinesterase inhibitors huperzine A, donepezil and rivastigmine were compared for their effects on extracellular acetylcholine concentration and acetylcholinesterase activity in the rat cortex. After i.p. injection, huperzine A (0.25-0.75 mumol/kg), donepezil (2-6 mumol/kg) and rivastigmine (0.75-1.5 mumol/kg) dose-dependently elevated the concentration of acetylcholine. The duration of huperzine A was longest. The time courses of cortical acetylcholinesterase inhibition with middle doses of these agents mirrored the increases of acetylcholine at the same doses. However, acetylcholinesterase inhibition was disproportionately greater after middle dose of rivastigmine than doses of huperzine A and donepezil that increased acetylcholine to a similar extent. Muscle fasciculation appeared only after donepezil with a dose-dependent incidence and intensity. In molar terms, huperzine A was 8- and 2-fold more potent than donepezil and rivastigmine, respectively, in increasing cortical acetylcholine levels, with a longer-lasting effect. (C) 2003 Elsevier Ireland Ltd. All rights reserved.

引用

页码：56 / 59

页数：4

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