Modulation of NMDA receptor by huperzine A in rat cerebral cortex

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	Modulation of NMDA receptor by huperzine A in rat cerebral cortex
	Wang, XD; Zhang, JM; Yang, HH; Hu, GY
刊名	ACTA PHARMACOLOGICA SINICA
	1999-01
卷号	20 期号:1 页码:31-35
关键词	huperzine A cholinesterase inhibitors N-methyl-D-aspartate receptors sodium glutamate dizocilpine maleate hippocampus pyramidal cells cerebral cortex patch-clamp techniques radioligand assay
ISSN号	0253-9756
文献子类	Article
英文摘要	AIM: To investigate the effects of huperzine A (Hup A) on NMDA receptors in rat cerebral cortex. METHODS: 1) The effect of hup A on NMDA-induced current was studied in acutely dissociated rat hippocampal pyramidal neurons using whole-cell recording. 2) The effect of Hup A on NMDA receptor binding was assessed using [H-3] dizocilpine (Diz) binding assay in synaptic membrane preparation of rat cerebral cortex. RESULTS: I) Hup A reversibly inhibited NMDA-induced current in a concentration-dependent manner with IC50 of 45.4 mu mol.L-1. 2) Hup A inhibited the specific binding of [H-3]MK-801 to extensively washed synaptic membrane of rat cerebral cortex in a concentration-dependent manner with ICS, of 0.5 (0.1 - 1.9) mu mol.L-1(n = 4). 3) L-Glutamate 10 mu mol.L-1 markedly increased [H-3] MK-801 binding. In the presence of L-glutamate, Hup A 0.001 - 0.1 mu mol.L-1 caused a further increase of the binding, whereas Hup A 1 - 300 mu mol.L-1 inhibited the binding in concentration-dependent manner with IC50 of 12.3 (5.8 - 26.3) mu mol.L-1(n = 5). CONCLUSION: Hup A acted as an antagonist of NMDA receptor in cerebral cortex in addition to its inhibitory effect on acetylcholinesterase.
WOS关键词	H-3 MK-801 BINDING ; ALZHEIMERS-DISEASE ; GLUTAMATE ; GLYCINE ; COMPLEX
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000077978900006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274769]
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 Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China
推荐引用方式 GB/T 7714	Wang, XD,Zhang, JM,Yang, HH,et al. Modulation of NMDA receptor by huperzine A in rat cerebral cortex[J]. ACTA PHARMACOLOGICA SINICA,1999,20(1):31-35.
APA	Wang, XD,Zhang, JM,Yang, HH,&Hu, GY.(1999).Modulation of NMDA receptor by huperzine A in rat cerebral cortex.ACTA PHARMACOLOGICA SINICA,20(1),31-35.
MLA	Wang, XD,et al."Modulation of NMDA receptor by huperzine A in rat cerebral cortex".ACTA PHARMACOLOGICA SINICA 20.1(1999):31-35.