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Titolo:
EFFECTS OF A CENTRALLY ACTIVE BENZOYLPYRROLIDINE DRUG ON AMPA RECEPTOR KINETICS
Autore:
ARAI A; KESSLER M; AMBROSINGERSON J; QUAN A; YIGITER E; ROGERS G; LYNCH G;
Indirizzi:
UNIV CALIF IRVINE,CTR NEUROBIOL LEARNING & MEMORY IRVINE CA 92697 CORTEX PHARMACEUT IRVINE CA 92718
Titolo Testata:
Neuroscience
fascicolo: 2, volume: 75, anno: 1996,
pagine: 573 - 585
SICI:
0306-4522(1996)75:2<573:EOACAB>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
LONG-TERM POTENTIATION; HIPPOCAMPAL-NEURONS; GLUTAMATE RECEPTORS; QUISQUALATE RECEPTORS; SYNAPTIC TRANSMISSION; KAINATE RECEPTORS; RAT HIPPOCAMPUS; DESENSITIZATION; CYCLOTHIAZIDE; CURRENTS;
Keywords:
HIPPOCAMPUS; AMPA RECEPTOR; EXCISED PATCH; DESENSITIZATION; BINDING AFFINITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
A. Arai et al., "EFFECTS OF A CENTRALLY ACTIVE BENZOYLPYRROLIDINE DRUG ON AMPA RECEPTOR KINETICS", Neuroscience, 75(2), 1996, pp. 573-585

Abstract

A newly developed benzoylpyrrolidine drug (BDP-20) that increases thesize of fast, excitatory synaptic responses was examined for its effects on the kinetic properties of alpha-amino-3-hydroxy-5-methyl-4-isoxalepropionic acid (AMPA)-type glutamate receptors. When long pulses ofglutamate were applied to excised hippocampal patches of the rat, thecompound BDP-20 caused an approximately 15-fold reduction in the rateat which responses desensitized and a similar size increase in steady-state currents. In experiments using 1-ms glutamate pulses, BDP-20 prolonged response deactivation by a factor of about four and greatly reduced the depression in the second response when two consecutive glutamate pulses were given. Two types of equilibrium binding assays indicated that BDP-20 causes a measurable increase in the affinity of AMPA receptors; the EC(50) values for this effect were similar to those obtained in excised patch studies. The actions of BDP-20 on physiology andligand binding could be adequately reproduced in a receptor model by slowing the rate of desensitization and increasing the affinity of thesensitized states. The biochemical and physiological effects of this benzoylpyrrolidine compound were qualitatively different from those obtained with cyclothiazide, although both types of drug increased AMPA receptor-mediated synaptic responses. Moreover, interactions between the drugs were at most only partially competitive; AMPA receptors may thus have multiple modulatory sites with distinct drug preferences and different effects on receptor kinetics. Copyright (C) 1996 IBRO.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/08/20 alle ore 08:29:11