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Titolo:
MODULATION OF AMPA KAINATE RECEPTORS BY ANALOGS OF DIAZOXIDE AND CYCLOTHIAZIDE IN THIN SLICES OF RAT HIPPOCAMPUS/
Autore:
BERTOLINO M; BARALDI M; PARENTI C; BRAGHIROLI D; DIBELLA M; VICINI S; COSTA E;
Indirizzi:
GEORGETOWN UNIV,MED CTR,SCH MED,FIDIA GEORGETOWN INST NEUROSCI,3900 RESERVOIR RD NW WASHINGTON DC 20007 UNIV MODENA,SCH PHARM I-41100 MODENA ITALY
Titolo Testata:
Receptors & channels
fascicolo: 4, volume: 1, anno: 1993,
pagine: 267 - 278
SICI:
1060-6823(1993)1:4<267:MOAKRB>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXCITATORY AMINO-ACIDS; AMPA-KAINATE RECEPTORS; MULTIPLE-CONDUCTANCE CHANNELS; GLUTAMATE-ACTIVATED CHANNELS; CENTRAL NERVOUS-SYSTEM; MOUSE CENTRAL NEURONS; SPINAL-CORD NEURONS; FUNCTIONAL EXPRESSION; QUISQUALATE RECEPTORS; SYNAPTIC TRANSMISSION;
Keywords:
CYCLOTHIAZIDE; DESENSITIZATION; DIAZOXIDE; NON-NMDA RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
67
Recensione:
Indirizzi per estratti:
Citazione:
M. Bertolino et al., "MODULATION OF AMPA KAINATE RECEPTORS BY ANALOGS OF DIAZOXIDE AND CYCLOTHIAZIDE IN THIN SLICES OF RAT HIPPOCAMPUS/", Receptors & channels, 1(4), 1993, pp. 267-278

Abstract

Among the non-NMDA (non-N-methyl-D-aspartic acid) glutamate receptors, the AMPA no-2,3-dihydro-5-methyl-3-oxo-4-isoxazolepropanoic acid) selective receptors are characterized by a fast occurring desensitization. We and others have searched for specific modifiers of the rapid desensitization of AMPA responses in hippocampal slices using the patch-clamp technique. Aniracetam (1-(4-methoxybenzoyl)-2-pyrrolidinone) and diazoxide (7-chloro-3-methyl-2H-1,2,4-benzo-thiadiazine 1,1-dioxide) (1 mM) increased glutamate-activated currents recorded from voltage-clamped CA1 pyramidal neurons in presence of 5 muM MK-801 (dizocilpine; ro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine) by 2-5 fold. Cyclothiazide -5-en-2-yl-6-chloro-3,4-dihydro-2H-1,2,4-benzothia diazine-7-sulfonamide 1,1-dioxide) (100 muM), a chemical congener of diazoxide, completely removed the desensitization of the AMPA response measured with fast application in excised outside-out patches. At this concentration cyclothiazide produced an 18 fold enhancement of the glutamate current. Eighteen diazoxide analogues (2H-1,2,4-benzothiadizines: IDRA 2-19) were then tested but none of them was as effective as diazoxide. Three analogues of cyclothiazide (3,4-dihydro-2H-1,2,4-benzothia-diazines: IDRA 20-22) were also tested and none of them were as potent as theparent compound, However, IDRA 21 produced a response 3 times larger than diazoxide. Moreover, while cyclothiazide and diazoxide potentiated kainate responses for all the doses that decreased AMPA receptor desensitization, IDRA 21, similarly to aniracetam, inhibited AMPA receptor desensitization preferentially. These results suggest that similarlyto NMDA receptors the structure of AMPA receptors may include a center that regulates desensitization.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/07/20 alle ore 07:54:20