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Titolo:
EFFECT OF GLUTAMATE-RECEPTOR ANTAGONISTS ON N-METHYL-D-ASPARTATE ACIDAND LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID-INDUCED CONVULSANT EFFECTS IN MICE AND RATS
Autore:
BISAGA A; KRZASCIK P; JANKOWSKA E; PALEJKO W; KOSTOWSKI W; DANYSZ W;
Indirizzi:
UMERZ & CO,DEPT PHARMACOL D-60318 FRANKFURTT GERMANY INST PSYCHIAT & NEUROL,DEPT PHARMACOL PL-02957 WARSAW POLAND MERZ & CO,DEPT PHARMACOL D-60318 FRANKFURT GERMANY
Titolo Testata:
European journal of pharmacology
fascicolo: 3, volume: 242, anno: 1993,
pagine: 213 - 220
SICI:
0014-2999(1993)242:3<213:EOGAON>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
INSENSITIVE GLYCINE SITE; NMDA-RECEPTOR; ION CHANNEL; 1-AMINOCYCLOBUTANE-1-CARBOXYLATE ACBC; HA-966 1-HYDROXY-3-AMINOPYRROLIDONE-2; POTENT ANTAGONIST; SEIZURE MODEL; ANIMAL-MODELS; ANTICONVULSANT; BRAIN;
Keywords:
NMDA (N-METHYL-D-ASPARTATE); AMPA LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID); CONVULSIONS; (SCREENING); (NEONATAL RAT); (MOUSE); (RAT);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
54
Recensione:
Indirizzi per estratti:
Citazione:
A. Bisaga et al., "EFFECT OF GLUTAMATE-RECEPTOR ANTAGONISTS ON N-METHYL-D-ASPARTATE ACIDAND LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID-INDUCED CONVULSANT EFFECTS IN MICE AND RATS", European journal of pharmacology, 242(3), 1993, pp. 213-220

Abstract

Selected antagonists of N-methyl-D-aspartate (NMDA) and lpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, acting through different recognition sites were studied in three in vivo experimental procedures: systemic administration of NMDA or AMPA to mice and 7-day-old rats or i.c.v. injection in adult rats. Antagonists were given i.p. before the agonists. Of the substances tested hyl-10,11-dihydro-5H-dibenzocyclohepten-5,10-imine maleate ((+)-MK-801, MK-801, an uncompetitive NMDA receptor antagonist) and DL-(E)-2-amino-4-methyl-5-phosphono-3-pentanoic acid (CGP-7849, 37849, a competitive NMDA receptor antagonist) were the most potent and selective NMDA receptor antagonists, having ED50s below 1 mg/kg in all three tests. 1-Amino-3,5-dimethyladamantane (memantine, an uncompetitive NMDA receptor antagonist) was less potent and, additionally, inhibited AMPA-induced seizures in adult rats. Aminocyclopropane carboxylic acid - a partial agonist at the glycine site coupled to NMDA receptors (Gly,) - was a weakantagonist (ED50 > 150 mg/kg) in mice. Other partial Gly, receptor agonists, aminocyclobutane carboxylic acid, (+,R)-3-amino-1-hydroxy-2-pyrrolidone ((+,R)-HA-966) and d-cycloserine, and antagonists, 5,7-dinitroquinoxaline-2,3-dione (MNQX) and 5,7-dichlorokynurenic acid, were ineffective in mice after systemic administration. The last two agents however were active in adult rats when given i.c.v. Thus affinity, intrinsic activity (Gly(B) receptor partial agonists) and/or penetration into the brain (Gly(B) receptor antagonists) seem to be important factors in determining the effectiveness of these agents. None of the Gly, receptor antagonists or partial agonists was active in 7-day-old rats,indicating different properties of this modulatory site at this age. AMPA receptor antagonists dihydroxy-6-nitro-7-sulfamoyl-benzo(F)-quinoxaline (NBQX) and -4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride (GYKI-52466), inhibited AMPA-induced convulsions in both young (7 days) and adult rats. NBQX was 3-10 times more potent and more selective than GYKI-52466.

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Documento generato il 05/04/20 alle ore 00:07:24