PHOSPHONOETHYLPHENYLALANINE DERIVATIVES AS NOVEL ANTAGONISTS OF NON-NMDA IONOTROPIC GLUTAMATE RECEPTORS

被引:4
|
作者
HAMILTON, GS
HUANG, Z
PATCH, RJ
GUZEWSKA, ME
ELLIOTT, RL
BOROSKY, SA
BEDNAR, DL
FERKANY, JW
KARBON, EW
机构
[1] Nova Pharmaceutical Corp. 6200 Freeport Centre Baltimore
关键词
D O I
10.1016/S0960-894X(00)80228-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Substituted phosphonoethylphenylalanines were evaluated for their ability to antagonize kainic acid (KA)- and AMPA-induced currents in Xenopus oocytes. Compounds which were substituted in the 5-position of the aromatic ring were found to selectively antagonize these currents. In addition, selected members of the series of compounds were demonstrated to possess anticonvulsant activity and to protect against KA-induced striatal toxicity in vivo. The effects of altering the position and identity of the aryl substituents were explored.
引用
收藏
页码:1269 / 1274
页数:6
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