Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Studies of the antagonist actions of (RS)-2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazoly]propionic acid (ATPO) on non-NMDA receptors in cultured rat neurones
Autore:
Dai, WM; Ebert, B; Madsen, U; Lambert, JDC;
Indirizzi:
Univ Aarhus, Dept Physiol, DK-8000 Aarhus C, Denmark Univ Aarhus Aarhus Denmark C us, Dept Physiol, DK-8000 Aarhus C, Denmark Royal Danish Sch Pharm, Dept Pharmacol, DK-2100 Copenhagen, Denmark Royal Danish Sch Pharm Copenhagen Denmark DK-2100 00 Copenhagen, Denmark Royal Danish Sch Pharm, Dept Med Chem, DK-2100 Copenhagen O, Denmark RoyalDanish Sch Pharm Copenhagen Denmark O K-2100 Copenhagen O, Denmark
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 7, volume: 125, anno: 1998,
pagine: 1517 - 1528
SICI:
0007-1188(199812)125:7<1517:SOTAAO>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
KAINATE RECEPTORS; HIPPOCAMPAL-NEURONS; GLUTAMATE RECEPTORS; AMPA RECEPTORS; HIGH-AFFINITY; PATCH-CLAMP; SYNAPTIC TRANSMISSION; CONCANAVALIN-A; SUBUNIT; DESENSITIZATION;
Keywords:
AMPA; kainate; (2S,4R)-4-methylglutamic acid; (RS)-2-amino-3-5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]-propionic acid (ATPO); cultured neurones; cyclothiazide; concanavalin A; GYKI 53655;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
54
Recensione:
Indirizzi per estratti:
Indirizzo: Lambert, JDC Univ Aarhus, Dept Physiol, DK-8000 Aarhus C, Denmark Univ Aarhus Aarhus Denmark C iol, DK-8000 Aarhus C, Denmark
Citazione:
W.M. Dai et al., "Studies of the antagonist actions of (RS)-2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazoly]propionic acid (ATPO) on non-NMDA receptors in cultured rat neurones", BR J PHARM, 125(7), 1998, pp. 1517-1528

Abstract

1 Whole-cell patch-clamp recordings from single cultured cortical neuroneshave been used to study the action of (RS)-2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid (ATPO), which has previously beenproposed to be a potent selective antagonist of 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptors.2 ATPO competitively reduced peak responses evoked by semi-rapid applications of AMPA (K-i=16 mu M) but had variable effects on plateau responses, which were on average unchanged. Following blockade of AMPA receptor desensitization by cyclothiazide (CTZ, 100 mu M), the plateau responses were reduced by ATPO to a similar extent as the peak responses, indicating that ATPO reduces desensitization of AMPA receptors.3 Semi-rapid application of kainic acid (KA) and the KA receptor-selectiveagonist, (2S,4R)-4-methylglutamic acid (MeGlu) evoked non-desensitizing responses which were competitively antagonized by ATPO (Ki values: 27 and 23 mu M, respectively).4 Responses to MeGlu were unaffected by CTZ (100 mu M), but potentiated 3 fold following blockade of KA receptor desensitization by concanavalin A (Con A, 300 mu g ml(-1)). Responses of spinal cord neurones to MeGlu were blocked by ATPO to a similar extent before and after blockade of KA receptor desensitization by Con A.5 Although selectively potentiated by Con A, plateau responses to MeGlu were reduced by 69.6% by the AMPA selective antagonist, GYKI 53655 (10 mu M). The remaining component was further reduced by ATPO with a K-i of 36 mu M,which was not significantly different from that in the absence of GYKI 53655, but was greater than that on responses to AMPA.6 It is concluded that ATPO is a moderate-potency competitive inhibitor ofnaturally expressed non-NMDA receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/07/20 alle ore 15:08:30