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Titolo:
PATCH-CLAMP STUDIES ON THE KINETICS AND SELECTIVITY OF N-METHYL-D-ASPARTATE RECEPTOR ANTAGONISM BY MEMANTINE (1-AMINO-3,5-DIMETHYLADAMANTAN)
Autore:
PARSONS CG; GRUNER R; ROZENTAL J; MILLAR J; LODGE D;
Indirizzi:
MERZ & CO GMBH&CO,DEPT PHARMACOL,ECKENHEIMER LANDSTR 100-104 D-60318 FRANKFURT 1 GERMANY ROYAL VET COLL,DEPT PRECLIN VET SCI LONDON NW1 0TU ENGLAND
Titolo Testata:
Neuropharmacology
fascicolo: 12, volume: 32, anno: 1993,
pagine: 1337 - 1350
SICI:
0028-3908(1993)32:12<1337:PSOTKA>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
LONG-TERM POTENTIATION; AMINO-ACID RECEPTORS; NMDA ANTAGONIST; ANTICONVULSANT MK-801; ALZHEIMERS-DISEASE; CULTURED NEURONS; DEPENDENT BLOCK; GANGLION-CELLS; INVITRO; PHENCYCLIDINE;
Keywords:
N-METHYL-D-ASPARTATE(NMDA); LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID (AMPA); DIZOCILPINE (MK-801); GAMMA-AMINO BUTYRIC ACID (GABA); MEMANTINE (1-AMINO-3,5-DIMETHYLADAMANTAN),; KETAMINE; PHENCYCLIDINE (PCP); DEXTRORPHAN; DEXTROMETHORPHAN; MG2+; PATCH CLAMP; CULTURE; SUPERIOR COLLICULUS; HIPPOCAMPUS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
63
Recensione:
Indirizzi per estratti:
Citazione:
C.G. Parsons et al., "PATCH-CLAMP STUDIES ON THE KINETICS AND SELECTIVITY OF N-METHYL-D-ASPARTATE RECEPTOR ANTAGONISM BY MEMANTINE (1-AMINO-3,5-DIMETHYLADAMANTAN)", Neuropharmacology, 32(12), 1993, pp. 1337-1350

Abstract

Memantine (1-amino-3,5-dimethyladamantan) was tested as an antagonistof N-methyl-D-aspartate (NMDA) receptors on cultured superior collicular and hippocampal neurones using the patch clamp technique and its actions were compared to those of Mg2+ ions, ketamine, dextrorphan, dextromethorphan, phencyclidine and dizocilpine (MK-801). Memantine (2-33mu M) concentration-dependently antagonized responses to NMDA 100 mu M with an IC50 of 2.92+/-0.05 mu M. In contrast, current responses to lpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (L-AMPA 50-100mu M) and gamma-amino butyric acid (GABA 10 mu M) were unaffected by Memantine 8 mu M. Memantine 8 mu M caused a non-parallel shift of the NMDA concentration-response curve to the right in a manner indicative of uncompetitive open channel block. The effects of memantine were similar to ketamine in that both antagonists were weakly use- and strongly voltage-dependent. In contrast, MK-801, phencyclidine and dextrorphan showed much slower kinetics that was reflected in their marked use- and weaker voltage-dependency. The antagonistic effects of memantine were not reversed by increasing concentrations of glycine (0.1-100 mu M) ruling out the possibility of an interaction of memantine with the strychnine-insensitive glycine modulatory site associated with the NMDAreceptor-channel complex. Memantine (1-100 mu M) also selectively antagonized responses to NMDA (40 mu M) in the cortical wedge preparationwith IC50 of 12.9+/-1.5 mu M.

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Documento generato il 10/07/20 alle ore 17:20:27