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Chinese Academy of Sciences Institutional Repositories Grid
Comparative studies of huperzine A, donepezil, and rivastigmine on brain acetylcholine, dopamine, norepinephrine, and 5-hydroxytryptamine levels in freely-moving rats

文献类型:期刊论文

作者Liang, Yan-qi; Tang, Xi-can
刊名ACTA PHARMACOLOGICA SINICA
出版日期2006-09
卷号27期号:9页码:1127-1136
关键词huperzine A donepezil rivastigmine acetylcholine dopamine norepinephrine 5-hydroxy tryptamine Alzheimer's disease rats
ISSN号1671-4083
DOI10.1111/j.1745-7254.2006.00411.x
文献子类Article
英文摘要Aim: To assess the effects of cholinesterase inhibitors huperzine A, donepezil and rivastigmine on cerebral neurotransmitters in the cortex and hippocampus in freely-moving rats. Methods: Double-probe cerebral microdialysis and HPLC with electrochemical detection were used to detect neurotransmitters. Results: Our results showed that huperzine A (0.25, 0.5, and 0.75 mu mol/kg, po) dose-dependently elevated extracellular acetylcholine (ACh) levels in the medial prefrontal cortex (mPFC) and hippocampus. Oral administration of donepezil (5.4 mu mol/kg) or rivastigmine (1 mu mol/kg) also elicited significant increases in ACh in the MPFC and hippocampus. The time course of cortical acetylcholinesterase (AChE) inhibition with the 3 inhibitors mirrored the increases of ACh at the same dose. The marked elevation of ACh after oral administration of huperzine A (0.5 mu mol/kg) and donepezil (5.4 mu mol/kg) was associated with a significantly increased release of dopamine (DA) in the mPFC or hippocampus. None of the 3 inhibitors affected norepinephrine (NE) and 5-hydroxytryptamine (5-HT) levels in the mPFC and hippocampus. The effects of huperzine A and rivastigmine did not depend on the route of administration, but donepezil was less efficacious by the oral route than by ip injection. The ability of huperzine A to increase ACh levels was unchanged when tests were performed after multiple oral administration of the drug at 0.5 pmol/kg, once per day for 30 d. Conclusion: The present findings showed that, in molar terms, huperzine A had similar potency on increasing mPFC ACh and DA levels as compared to the 11- and 2-fold dosages of donepezil and rivastigmine, respectively, and had longer lasting effects after oral dosing.
WOS关键词SPATIAL WORKING-MEMORY ; CHOLINESTERASE INHIBITOR ; ALZHEIMERS-DISEASE ; EXTRACELLULAR ACETYLCHOLINE ; HIPPOCAMPAL ACETYLCHOLINE ; CHOLINERGIC SYSTEM ; PREFRONTAL CORTEX ; AGED RATS ; IN-VIVO ; 2ND-GENERATION
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
CSCD记录号CSCD:2462109
WOS记录号WOS:000240554800004
出版者ACTA PHARMACOLOGICA SINICA
源URL[http://119.78.100.183/handle/2S10ELR8/273498]  
专题院士及顾问专家
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Tang, Xi-can
作者单位Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai Inst Biol Sci,Grad Sch, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714
Liang, Yan-qi,Tang, Xi-can. Comparative studies of huperzine A, donepezil, and rivastigmine on brain acetylcholine, dopamine, norepinephrine, and 5-hydroxytryptamine levels in freely-moving rats[J]. ACTA PHARMACOLOGICA SINICA,2006,27(9):1127-1136.
APA Liang, Yan-qi,&Tang, Xi-can.(2006).Comparative studies of huperzine A, donepezil, and rivastigmine on brain acetylcholine, dopamine, norepinephrine, and 5-hydroxytryptamine levels in freely-moving rats.ACTA PHARMACOLOGICA SINICA,27(9),1127-1136.
MLA Liang, Yan-qi,et al."Comparative studies of huperzine A, donepezil, and rivastigmine on brain acetylcholine, dopamine, norepinephrine, and 5-hydroxytryptamine levels in freely-moving rats".ACTA PHARMACOLOGICA SINICA 27.9(2006):1127-1136.

入库方式: OAI收割

来源:上海药物研究所

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