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Titolo:
Functional modulation of gamma-aminobutyric acid(A) receptors by etifoxineand allopregnanolone in rodents
Autore:
Verleye, M; Schlichter, R; Neliat, G; Pansart, Y; Gillardin, JM;
Indirizzi:
Zac Mercieres, Lab Biocodex, Dept Pharmacol, F-60200 Compiegne, France ZacMercieres Compiegne France F-60200 rmacol, F-60200 Compiegne, France Univ Louis Pasteur Strasbourg 1, CNRS, UMR 7519, F-67084 Strasbourg, France Univ Louis Pasteur Strasbourg 1 Strasbourg France F-67084 sbourg, France CEREP, F-86600 Celle Levescault, France CEREP Celle Levescault France F-86600 , F-86600 Celle Levescault, France
Titolo Testata:
NEUROSCIENCE LETTERS
fascicolo: 3, volume: 301, anno: 2001,
pagine: 191 - 194
SICI:
0304-3940(20010406)301:3<191:FMOGAR>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
GABA-A RECEPTORS; CHLORIDE IONOPHORE; NEUROSTEROIDS; MECHANISM; LIGANDS; ANXIETY;
Keywords:
allopregnanolone; etifoxine; anxiolytic; anticonvulsant; (+)bicuculline; [S-35]t-butylbicyclophosphorothionate binding; additive effect; allosteric modulator;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
20
Recensione:
Indirizzi per estratti:
Indirizzo: Verleye, M Zac Mercieres, Lab Biocodex, Dept Pharmacol, Chemin Armancourt,F-60200 Compiegne, France Zac Mercieres Chemin Armancourt Compiegne France F-60200 rance
Citazione:
M. Verleye et al., "Functional modulation of gamma-aminobutyric acid(A) receptors by etifoxineand allopregnanolone in rodents", NEUROSCI L, 301(3), 2001, pp. 191-194

Abstract

We looked for an interaction between etifoxine and the neurosteroid allopregnanolone at central gamma-aminobutyric acid (GABA(A)) receptors. Etifoxine (2 muM) did not affect the affinity of allopregnanolone (IC50 = 108 nM) for its site in preparations of Sprague-Dawley rat cerebral cortex membranes, as determined by the inhibition of [S-35] t-butylbicyclo-phosphorothionate binding, a specific ligand of the GABA(A) receptor chloride channel site. Etifoxine and allopregnanolone were anticonvulsants, blocking the clonic convulsions induced by bicuculline tan antagonist of the GABA(A) receptor) in CD1 mice. A combination of subactive doses of the two compounds showed additive anticonvulsant effects. These results suggest that etifoxine and allopregnanolone bind to distinct putative recognition sites at or near the chloride channel site. Functionally, their binding may have an additive effect by enhancing GABA(A) inhibitory transmission. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/05/20 alle ore 15:23:16