Pharmacodynamic study of FS-0311: A novel highly potent, selective acetylcholinesterase inhibitor
文献类型：期刊论文
| 作者 | Wang, Zhi Fei; Yan, Jin; Fu, Yan; Tang, Xi Can; Feng, Song; He, Xu Chang; Bai, Dong Lu |
| 刊名 | CELLULAR AND MOLECULAR NEUROBIOLOGY
 |
| 出版日期 | 2008-02 |
| 卷号 | 28期号:2页码:245-261 |
| 关键词 | huperzine B derivative cholinesterase inhibitor Alzheimer's disease scopolamine transient brain ischemia and reperfusion water maze beta-amyloid antioxidant enzymes oxygen-glucose deprivation staurosporine |
| ISSN号 | 0272-4340 |
| DOI | 10.1007/s10571-007-9199-0 |
| 文献子类 | Article |
| 英文摘要 | (1) This study was to evaluate the anti-cholinesterase (ChE), cognition enhancing and neuroprotective effects of FS-0311, a bis-huperzine B derivative. (2) ChE activity was evaluated using a spectrophotometric method. Cognitive deficits in mice were induced by scopolamine or transient brain ischemia and reperfusion. Water maze was used to detect the cognitive performance. PC12 cell injury was induced by beta-amyloid 25-35 (A beta(25-35)), oxygen-glucose deprivation (OGD), or staurosporine treatment. (3) FS-0311 was a potent, highly specific inhibitor of acetylcholinesterase (AChE). FS-0311 bound to AChE in a reversible manner, causing linear mixed-type inhibition. FS-0311 had a high oral bioavailability and a long duration of AChE inhibitory action in vivo. FS-0311 was found to antagonize cognitive deficits induced by scopolamine or transient brain ischemia and reperfusion in a water maze task. FS-0311 possessed the ability to protect PC12 cells against A beta(25-35) peptide toxicity, OGD insult and staurosporine-induced apoptosis. The neuroprotective effects of FS-0311 appeared to reflect an attenuation of oxidative stress. (4) With the profile of anti-ChE and neuroprotective activities, FS-0311 might be a promising candidate in neurodegenerative diseases, such as Alzheimer's disease and Vascular dementia. |
| WOS关键词 | RADIAL MAZE PERFORMANCE ; ALZHEIMERS-DISEASE ; HUPERZINE-B ; OXIDATIVE STRESS ; CHOLINESTERASE-INHIBITORS ; IN-VIVO ; SCOPOLAMINE ; DEMENTIA ; DEFICITS ; MICE |
| WOS研究方向 | Cell Biology ; Neurosciences & Neurology |
| 语种 | 英语 |
| WOS记录号 | WOS:000253191900007 |
| 出版者 | SPRINGER/PLENUM PUBLISHERS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272989]  |
| 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 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Zhi Fei,Yan, Jin,Fu, Yan,et al. Pharmacodynamic study of FS-0311: A novel highly potent, selective acetylcholinesterase inhibitor[J]. CELLULAR AND MOLECULAR NEUROBIOLOGY,2008,28(2):245-261. |
| APA | Wang, Zhi Fei.,Yan, Jin.,Fu, Yan.,Tang, Xi Can.,Feng, Song.,...&Bai, Dong Lu.(2008).Pharmacodynamic study of FS-0311: A novel highly potent, selective acetylcholinesterase inhibitor.CELLULAR AND MOLECULAR NEUROBIOLOGY,28(2),245-261. |
| MLA | Wang, Zhi Fei,et al."Pharmacodynamic study of FS-0311: A novel highly potent, selective acetylcholinesterase inhibitor".CELLULAR AND MOLECULAR NEUROBIOLOGY 28.2(2008):245-261. |
入库方式： OAI收割
来源：上海药物研究所
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