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Titolo:
[H-3] ANIRACETAM BINDS TO SPECIFIC RECOGNITION SITES IN BRAIN MEMBRANES
Autore:
FALLARINO F; GENAZZANI AA; SILLA S; LEPISCOPO MR; CAMICI O; CORAZZI L; NICOLETTI F; FIORETTI MC;
Indirizzi:
UNIV CATANIA,INST PHARMACOL,VIALE A DORIA I-95125 CATANIA ITALY UNIV CATANIA,INST PHARMACOL I-95125 CATANIA ITALY UNIV PERUGIA,DEPT EXPTL MED & BIOCHEM SCI,PHARMACOL SECT I-06100 PERUGIA ITALY UNIV PERUGIA,INST BIOL CHEM I-06100 PERUGIA ITALY
Titolo Testata:
Journal of neurochemistry
fascicolo: 2, volume: 65, anno: 1995,
pagine: 912 - 918
SICI:
0022-3042(1995)65:2<912:[ABTSR>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
GLUTAMATE-RECEPTOR DESENSITIZATION; NOOTROPIC DRUG ANIRACETAM; SYNAPTIC CURRENTS; PRIMARY CULTURES; NEURONS; POTENTIATION; RESPONSES; REVERSES; KAINATE; NMDA;
Keywords:
[H-3] ANIRACETAM BINDING; GLUTAMATE; GYKI 52466; CYCLOTHIAZIDE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
26
Recensione:
Indirizzi per estratti:
Citazione:
F. Fallarino et al., "[H-3] ANIRACETAM BINDS TO SPECIFIC RECOGNITION SITES IN BRAIN MEMBRANES", Journal of neurochemistry, 65(2), 1995, pp. 912-918

Abstract

[H-3]Aniracetam bound to specific and saturable recognition sites in membranes prepared from discrete regions of rat brain. In crude membrane preparation from rat cerebral cortex, specific binding was Na+ independent, was still largely detectable at low temperature (4 degrees C), and underwent rapid dissociation. Scatchard analysis of [H-3]aniracetam binding revealed a single population of sites with an apparent K-Dvalue of similar to 70 nM and a maximal density of 3.5 pmol/mg of protein. Specifically bound [H-3]aniracetam was not displaced by various metabolites of aniracetam, nor by other pyrrolidinone-containing nootropic drugs such as piracetam or oxiracetam. Subcellular distribution studies showed that a high percentage of specific [H-3]aniracetam binding was present in purified synaptosomes or mitochondria, whereas specific binding was low in the myelin fraction. The possibility that at [east some [H-3]aniracetam binding sites are associated with glutamate receptors is supported by the evidence that specific binding was abolished when membranes were preincubated at 37 degrees C under fast shaking (a procedure that substantially reduced the amount of glutamate trapped in the membranes) and could be restored after addition of either glutamate or pha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) but not kainate. The action of AMPA was antagonized by DNQX, which also reduced specific [H-3]aniracetam binding in unwashed membranes. Highlevels of [H-3]aniracetam binding were detected in hippocampal, cortical, or cerebellar membranes, which contain a high density of excitatory amino acid receptors. Although synaptosomal aniracetam binding sites may well be associated with AMPA-sensitive glutamate receptors, specifically bound [H-3]- aniracetam could not be displaced by cyclothiazide or GYKI 52466, which act as a positive and negative modulator of AMPA receptors, respectively.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 12:30:18