Spermidine antagonizes the inhibitory effect of huperzine A on [H-3]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex
文献类型:期刊论文
作者 | Zhang, YH; Zhao, XY; Chen, XQ; Wang, Y; Yang, HH; Hu, GY |
刊名 | NEUROSCIENCE LETTERS
![]() |
出版日期 | 2002-02-15 |
卷号 | 319期号:2页码:107-110 |
关键词 | huperzine A cholinesterase inhibitor Alzheimer's disease [H-3]dizocilpine (MK-801) binding N-methyl-D-aspartate receptors polyamine |
ISSN号 | 0304-3940 |
DOI | 10.1016/S0304-3940(01)02565-4 |
文献子类 | Article |
英文摘要 | Huperzine A, a novel cholinesterase inhibitor, was found to inhibit the N-methyl-D-aspartate (NMDA) receptors in the brain. In this study, the mechanisms of the NMDA receptor inhibition were investigated using [3 H]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex. Changing the concentrations of L-glutamate and L-glycine did not alter the potency of huperzine A. Spermidine caused rightward shift of the concentration-response curve of huperzine A, and considerably increased its IC50 value. Huperzine A did not affect the potency of unlabeled (+)-MK-801 in [H-3]MK-801 binding. Saturation binding studies reveal that huperzine A exerts a negative allosteric modulation on the MK-801 binding site within the NMDA receptor-channel. The results suggest that huperzine A is a non-competitive antagonist of the NMDA receptors, acting at one of the polyamine binding sites. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved. |
WOS关键词 | NMDA RECEPTOR ; SITE |
WOS研究方向 | Neurosciences & Neurology |
语种 | 英语 |
WOS记录号 | WOS:000173916600013 |
出版者 | ELSEVIER SCI IRELAND LTD |
源URL | [http://119.78.100.183/handle/2S10ELR8/274387] ![]() |
专题 | 药理学第一研究室 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 | Hu, GY |
作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Materia Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
推荐引用方式 GB/T 7714 | Zhang, YH,Zhao, XY,Chen, XQ,et al. Spermidine antagonizes the inhibitory effect of huperzine A on [H-3]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex[J]. NEUROSCIENCE LETTERS,2002,319(2):107-110. |
APA | Zhang, YH,Zhao, XY,Chen, XQ,Wang, Y,Yang, HH,&Hu, GY.(2002).Spermidine antagonizes the inhibitory effect of huperzine A on [H-3]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex.NEUROSCIENCE LETTERS,319(2),107-110. |
MLA | Zhang, YH,et al."Spermidine antagonizes the inhibitory effect of huperzine A on [H-3]dizocilpine (MK-801) binding in synaptic membrane of rat cerebral cortex".NEUROSCIENCE LETTERS 319.2(2002):107-110. |
入库方式: OAI收割
来源:上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。