Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine
文献类型：期刊论文
| 作者 | Qin, Z; Xi, CT |
| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 2002-11-29 |
| 卷号 | 455期号:2-3页码:101-107 |
| 关键词 | acetylcholinesterase isoform huperzine A tacrine donepezil rivastigmine physostigmine Alzheimer's disease (rat) |
| ISSN号 | 0014-2999 |
| DOI | 10.1016/S0014-2999(02)02589-X |
| 文献子类 | Article |
| 英文摘要 | Five inhibitors of acetylcholinesterase, huperzine A, donepezil, tacrine, rivastigmine and physostigmine, were compared with regard to their effects on different molecular forms of acetylcholinesterase in cerebral cortex, hippocampus, and striatum from the rat brain. In general, huperzine A preferentially inhibited tetrameric acetylcholinesterase (G4 form), while tacrine and rivastigmine preferentially inhibited monomeric acetylcholinesterase (G1 form). Donepezil showed pronounced selectivity for G1 acetylcholinesterase in striatum and hippocampus, but not in cortex. Physostigmine showed no form-selectivity in any brain region. In cortex, the most potent inhibitors of G4 acetylcholinesterase were huperzine A (K-i 7 X 10(-9) M) and donepezil (K-i 4 X 10(-9) M). The potent inhibitors of cortical G1 acetylcholinesterase were donepezil (K-i 3.5 X 10(-9) M) and tacrine (K-i 2.3 X 10(-8) M). In hippocampus, huperzine A and physostigmine were the most potent inhibitors of G4 acetylcholinesterase, while donepezil and tacrine were most potent against G1 acetylcholinesterase. In striatum, huperzine A and donepezil were the most potent against G4 acetylcholinesterase, while again donepezil was the most potent against G1. Although the inhibition constants (Ki) of these acetylcholinesterase inhibitors differed significantly from region to region, the nature of the inhibition did not vary. These results suggest that the use of acetylcholinesterase inhibitors in treatment of Alzheimer's disease must consider both form-specific and region-specific characteristics of acetylcholinesterase inhibition. (C) 2002 Elsevier Science B.V All rights reserved. |
| WOS关键词 | MOLECULAR-FORMS ; ALZHEIMERS-DISEASE ; SYNAPSE LOSS ; BRAIN ; LOCALIZATION ; INHIBITION ; MEMORY ; MUSCLE |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000179477100003 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274306]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Xi, CT |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Qin, Z,Xi, CT. Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2002,455(2-3):101-107. |
| APA | Qin, Z,&Xi, CT.(2002).Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine.EUROPEAN JOURNAL OF PHARMACOLOGY,455(2-3),101-107. |
| MLA | Qin, Z,et al."Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine".EUROPEAN JOURNAL OF PHARMACOLOGY 455.2-3(2002):101-107. |
入库方式： OAI收割
来源：上海药物研究所
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