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Titolo:
AMPA receptor antagonists, GYKI 52466 and NBQX, do not block the inductionof long-term potentiation at therapeutically relevant concentrations
Autore:
Kapus, G; Szekely, JI; Durand, J; Ruiz, A; Tarnawa, I;
Indirizzi:
EGIS Pharmaceut Ltd, CNS Pharmacol, H-1475 Budapest, Hungary EGIS Pharmaceut Ltd Budapest Hungary H-1475 ol, H-1475 Budapest, Hungary Inst Drug Res Ltd, Budapest, Hungary Inst Drug Res Ltd Budapest HungaryInst Drug Res Ltd, Budapest, Hungary Unite Neurocybernet Cellulaire, Marseille, France Unite Neurocybernet Cellulaire Marseille France aire, Marseille, France Gedeon Richter Chem Works Ltd, Budapest, Hungary Gedeon Richter Chem WorksLtd Budapest Hungary s Ltd, Budapest, Hungary
Titolo Testata:
BRAIN RESEARCH BULLETIN
fascicolo: 6, volume: 52, anno: 2000,
pagine: 511 - 517
SICI:
0361-9230(200008)52:6<511:ARAG5A>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
GLUTAMATE-RECEPTOR; RAT HIPPOCAMPUS; NMDA RECEPTORS; SYNAPTIC TRANSMISSION; KAINATE RECEPTORS; FIELD POTENTIALS; GYKI-52466; LTP; EXPRESSION; ACTIVATION;
Keywords:
long-term potentiation; hippocampus; AMPA receptors; GYKI 52466; NBQX;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
41
Recensione:
Indirizzi per estratti:
Indirizzo: Kapus, G EGIS Pharmaceut Ltd, CNS Pharmacol, POB 100, H-1475 Budapest, Hungary EGIS Pharmaceut Ltd POB 100 Budapest Hungary H-1475 est, Hungary
Citazione:
G. Kapus et al., "AMPA receptor antagonists, GYKI 52466 and NBQX, do not block the inductionof long-term potentiation at therapeutically relevant concentrations", BRAIN RES B, 52(6), 2000, pp. 511-517

Abstract

The involvement of alpha-amino-3-hydroxy-5-methylizoxazole-4-propionic acid (AMPA) receptors in induction of long-term potentiation (LTP) was examined in rat hippocampal slice preparation. Using conventional extracellular recording, excitatory postsynaptic potentials (EPSPs) and population action potentials (PSs), evoked by low-frequency stimulation of the Schaffer collateral-commissural fibres, were recorded in the CA1 region. The effects of a competitive AMPA receptor antagonist, 6-nitro-7-sulfamoylbenzo(f)quinoxaline-2,3-dione (NBQX), and that of a non-competitive blocker, 1-(4-aminophenyl)-4-methyl-7,8-methylendioxy-5H-2,3-benzodiazepine (GYKI 52466) have been examined. 0.25-0.5 mu M of NBOX and 20-40 mu M of GYKI 52466 did not suppress the induction of LTP. LTP was attenuated only at the highest concentrations tested (1 mu M NBQX or 80 mu M GYKI 52466), These in vitro concentrations, however, exceed the brain levels needed for in vivo anticonvulsant action. Furthermore, even at the highest concentrations both compounds suppressed only the expression but not the induction of LTP, Namely after their washout LTP reappeared. Thus, at pharmacologically relevant concentrations these AMPA receptor antagonists apparently do not suppress LTP, a cellular mechanism underlying memory formation. These experiments suggest that in clinical practice AMPA receptor blockade may have some advantage over N-methyl-D-aspartate receptor antagonism, which is accompanied by severe memory impairment. (C) 2000 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 23:50:50