Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities
文献类型：期刊论文
| 作者 | Cheng, DH; Tang, XC
|
| 刊名 | PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
 |
| 出版日期 | 1998-06 |
| 卷号 | 60期号:2页码:377-386 |
| 关键词 | Alzheimer's disease cholinesterase inhibitor huperzine A E2020 tacrine rat radial maze learning and memory cholinesterase |
| ISSN号 | 0091-3057 |
| DOI | 10.1016/S0091-3057(97)00601-1 |
| 文献子类 | Article |
| 英文摘要 | Comparative effects of cholinesterase inhibitors (ChEI) huperzine A with E2020 and tacrine on the radial maze performance in ethylcholine mustard aziridinium ion (AF64A)-treated rat and inhibition of cholinesterase activity were studied. The intracerebroventricular (ICV) injection of AF64A (3 nmol/side) caused significant impairment in the rat's ability to fulfill the partially baited maze paradigm. Oral huperzine A (0.5-0.8 mg/kg), E2020 (1.0-2.0 mg/kg), and tacrine (8.0 mg/kg) effectively reversed AF64A-induced working memory deficit. The doses that improved AFB4A-induced memory deficit were correlated to about 25-30% (huperzine A) and less than 10% (E2020, tacrine) inhibition of acetylcholinesterase (AChE) activity in the cortex and hippocampus. Huperzine A, E2020 and tacrine all produced dose-dependent inhibition of brain AChE following ICV and oral administration. Oral huperzine A exhibited higher efficacy on the inhibition of AChE in the cortex and hippocampus than those of E2020 and tacrine. Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BuChE) than it was brain AChE. Conversely, the BuChE activity was less affected by huperzine A and E2020. The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus. Huperzine A fits more closely with the established criteria for an ideal AChE inhibitor to be used in clinical studies. (C) 1998 Elsevier Science Inc. |
| WOS关键词 | AZIRIDINIUM ION AF64A ; CENTRAL CHOLINERGIC HYPOFUNCTION ; ALZHEIMERS-DISEASE ; SYSTEM ; MEMORY ; RATS ; ACETYLCHOLINESTERASE ; INHIBITOR ; BINDING ; RELEASE |
| WOS研究方向 | Behavioral Sciences ; Neurosciences & Neurology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000073815600010 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274832]  |
| 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, XC |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cheng, DH,Tang, XC. Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,1998,60(2):377-386. |
| APA | Cheng, DH,&Tang, XC.(1998).Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,60(2),377-386. |
| MLA | Cheng, DH,et al."Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities".PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 60.2(1998):377-386. |
入库方式： OAI收割
来源：上海药物研究所
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