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Titolo:
INTERACTIONS OF THE DYE EVANS-BLUE AND GYKI-52466, A 2,3-BENZODIAZEPINE, WITH LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID RECEPTORS IN CULTURED RAT CORTICAL-NEURONS - ELECTROPHYSIOLOGICAL EVIDENCE FOR AT LEAST 2 DIFFERENT BINDING-SITES FOR NONCOMPETITIVE ANTAGONISTS
Autore:
WEISER T; HERRMANN A; WIENRICH M;
Indirizzi:
BOEHRINGER INGELHEIM KG,DEPT BIOL RES,CNS PHARMACOL D-55218 INGELHEIMGERMANY UNIV GIESSEN,INST BOT 1 D-35390 GIESSEN GERMANY
Titolo Testata:
Neuroscience letters
fascicolo: 1, volume: 216, anno: 1996,
pagine: 29 - 32
SICI:
0304-3940(1996)216:1<29:IOTDEA>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
CYCLOTHIAZIDE; GYKI-52466;
Keywords:
LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID (AMPA); KAINATE; GLUTAMATE RECEPTOR; GYKI 52466; EVANS BLUE; NONCOMPETITIVE ANTAGONISM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
12
Recensione:
Indirizzi per estratti:
Citazione:
T. Weiser et al., "INTERACTIONS OF THE DYE EVANS-BLUE AND GYKI-52466, A 2,3-BENZODIAZEPINE, WITH LPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID RECEPTORS IN CULTURED RAT CORTICAL-NEURONS - ELECTROPHYSIOLOGICAL EVIDENCE FOR AT LEAST 2 DIFFERENT BINDING-SITES FOR NONCOMPETITIVE ANTAGONISTS", Neuroscience letters, 216(1), 1996, pp. 29-32

Abstract

The effects of the dye Evans Blue and GYKI 52466, a 2,3-benzodiazepine, on lpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptors in primary cultured rat cortical neurons were investigated using the patch-clamp technique. Evans Blue and GYKI 52466 reduced the currents induced by the application of 100 mu M kainate with IC50 values of 10.6 +/- 1.4 mu M and 12.1 +/- 0.4 mu M, respectively. Incontrast to the similar potencies of the two compounds, their kinetics of block were quite different with those of Evans Blue being more complex. The on-, as well as the off-reaction of the block by GYKI 52466could be described by single exponential functions, whereas two different time-constants for binding and one time-constant for the unbinding of Evans Blue were found. The block of AMPA receptors by Evans Blue was not completely reversible under the experimental conditions applied in this study. GYKI 52466 was not able to augment the recovery afterinhibiting AMPA receptors with Evans Blue. Moreover, preapplication of a high concentration of GYKI 52466 did not prevent the inhibition ofAMPA receptors by Evans Blue. We therefore conclude that GYKI 52466 and Evans Blue bind to two different sites at AMPA receptors in primarycultured cortical neurons.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/04/20 alle ore 04:19:42