EXCITATORY AMINO-ACIDS - 6-PHOSPHONOMETHYLTETRAHYDRO-4-PYRIMIDINECARBOXYLIC ACIDS AND THEIR ACYCLIC ANALOGS ARE COMPETITIVE N-METHYL-D-ASPARTIC ACID RECEPTOR ANTAGONISTS

被引：12

作者：

BIGGE, CF

WU, JP

DRUMMOND, JT

COUGHENOUR, LL

HANCHIN, CM

机构：

[1] Parke-Davis Pharmaceutical Research Division Warner-Lambert Company, Ann Arbor, MI 48105

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(01)81066-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

6-Phosphonoalkyltetrahydro-4-pyrimidinecarboxylic acids and their acyclic equivalents were determined to be competitive N-methyl-D-aspartic acid (NMDA) receptor antagonists using a [H-3]-CPP binding assay. Results suggest that internal hydrogen bonding interactions may exert either a positive or negative influence on NMDA receptor affinity depending on whether an appropriate receptor active configuration is stabilized.

引用

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页码：207 / 212

页数：6

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