ANTICONVULSANT EFFECTS OF ANTAGONISTS OF THE N-METHYL-D-ASPARTATE RECEPTOR COMPLEX IN A GENETIC MODEL OF EPILEPSY - THE QUAKING MOUSE

被引：7

作者：

MITROVIC, N ^{[1
]}

BESSON, MJ ^{[1
]}

MAURIN, Y ^{[1
]}

机构：

[1] HOP LA PITIE SALPETRIERE,INSERM,U134,F-75651 PARIS 13,FRANCE

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 176卷 / 03期

关键词：

Anticonvulsant effects; NMDA receptor antagonists; Quaking mutant mice;

D O I：

10.1016/0014-2999(90)90030-A

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Tonic-clonic convulsions of mutant quaking mice were antagonized by the intracerebroventricular injection of N-methyl-D-aspartate receptor antagonists. The competitive antagonists, CPP (3-((±)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid) and CGS 19755 (cis-4-(phosphonomethyl)-2-piperidine carboxylic acid), exerted a partial anticonvulsant action, with ED50S of 0.115 and 0.076 nmol, respectively. The non-competitive antagonists, TCP (1-(1-(2-thienyl)cyclohexyl)piperidine) and MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5,10-amine), provided full protection, with ED50s of 4.49 and 2.67 nmol, respectively. The competitive antagonists elicited a marked ataxia whereas the non-competitive antagonists did not have side-effects. These results might reflect the involvement of glutamatergic neurotransmission in the convulsions of the quaking mutants. © 1990.

引用

页码：357 / 361

页数：5

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