Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [H-3]noradrenaline release from rat hippocampal and frontal cortex slices
Autore:
Lockhart, B; Iop, F; Closier, M; Lestage, P;
Indirizzi:
Inst Rech Servier, Div Cerebral Pathol, F-78290 Croissy Sur Seine, France Inst Rech Servier Croissy Sur Seine France F-78290 ssy Sur Seine, France
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2, volume: 401, anno: 2000,
pagine: 145 - 153
SICI:
0014-2999(20000804)401:2<145:((>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
NON-NMDA RECEPTORS; H-3 NOREPINEPHRINE RELEASE; GLUTAMATE RECEPTORS; ALLOSTERIC POTENTIATION; NORADRENALINE RELEASE; S,S-DIOXIDE IDRA-21; DESENSITIZATION; MEMORY; CYCLOTHIAZIDE; FACILITATION;
Keywords:
AMPA receptor; S18986-1; hippocampus; noradrenaline release; allosteric modulator;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
41
Recensione:
Indirizzi per estratti:
Indirizzo: Lockhart, B Inst Rech Servier, Div Cerebral Pathol, 125 Chemin Ronde, F-78290 Croissy Sur Seine, France Inst Rech Servier 125 Chemin Ronde Croissy Sur Seine France F-78290
Citazione:
B. Lockhart et al., "(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [H-3]noradrenaline release from rat hippocampal and frontal cortex slices", EUR J PHARM, 401(2), 2000, pp. 145-153

Abstract

The present study describes the effect of (S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide (S18986-1), a positive allosteric modulator of the alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors with cognitive-enhancing effects, on(S)-AMPA-induced [H-3]noradrenaline release in rat hippocampal and frontal cortex slices. (S)-AMPA significantly increased [H-3]noradrenaline release in rat hippocampus and frontal cortex slices, whereas S18986-1 (3-1000 mu M) alone, was inactive. However, S18986-1 between 30 and 1000 mu M potently enhanced (+200%) (S)-AMPA-mediated [H-3]noradrenaline release in both hippocampal and frontal cortex slices. The capacity of S18986-1 to potentiate [H-3]noradrenaline release was specific for AMPA receptors as S18986-1 failed to potentiate either kainate and N-methyl-D-aspartate (NMDA)-mediated release of [H-3]noradrenaline in rat hippocampal slices. Moreover, 1,2,3,4-tetrahydro-6-nitro-2,3-dioxo-benzo[f]quinoxaline-7-sulfonamide (NBQX) and 1-(4-aminophenyl)-3-methylcarbamoyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine (GYKI-53655) but not (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine ((+)-MK-801), inhibited (S)-AMPA and S18986-induced stimulationof (S)-AMPA-mediated [H-3]noradrenaline release. In addition, S18986-1-induced stimulation of (S)-AMPA-evoked [3H]noradrenaline release was markedly attenuated in the presence of tetrodotoxin (1 mu M) and in Ca2+-free buffer. S18986-1 enhanced (S)-AMPA-mediated [H-3]noradrenaline release to a greater extent than its corresponding (R)-enantiomer S19024-1 and racemic mixture S17951-1. However, positive allosteric modulators of AMPA receptors such as aniracetam failed to potentiate AMPA-mediated noradrenaline release in hippocampal slices, whereas cyclothiazide potently enhanced (S)-AMPA-mediated [H-3]noradrenaline release. These results suggest that the capacity of S18986-1 to enhance AMPA receptor-mediated release of noradrenaline in rat hippocampus and frontal cortex, could contribute to the cognition enhancing mechanisms of S18986-1. (C) 2000 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/08/20 alle ore 20:00:21