Similar potency of the enantiomers of huperzine A in inhibition of [3H]dizocilpine (MK-801) binding in rat cerebral cortex

被引：15

作者：

Zhang, YH ^{[1
]}

Chen, XQ ^{[1
]}

Yang, HH ^{[1
]}

Jin, GY ^{[1
]}

Bai, DL ^{[1
]}

Hu, GY ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China

来源：

NEUROSCIENCE LETTERS | 2000年 / 295卷 / 03期

关键词：

huperzine A; cholinesterase inhibitor; Alzheimer's disease; enantiomers; H-3]dizocilpine (MK-801) binding; N-methyl-D-aspartate receptor;

D O I：

10.1016/S0304-3940(00)01615-3

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

The inhibition of huperzine A, a potential therapeutic agent to treat Alzheimer's disease, on rat cortical acetylcholinesterase was found to be highly stereospecific. In the present study the effect of the enantiomers of huperzine A on [H-3]dizocilpine (MK-801) binding to synaptic membrane of rat cerebral cortex was compared. The natural (-)-huperzine A and the synthetic (+)-huperzine A inhibited the specific binding of [H-3]MK-801 with a similar potency. The IC50 values were:65 +/- 7 and 82 +/- 12 muM (n = 5 for each enantiomer, P = 0.248), respectively. The result indicates that huperzine A inhibits N-methyl-D-aspartate (NM DA) receptor in rat cerebral cortex without stereoselectivity. (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：116 / 118

页数：3

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