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Titolo:
Differential sensitivity to inverse agonists of GABA(A)/benzodiazepine receptors in rats with genetic absence-epilepsy
Autore:
Vergnes, M; Boehrer, A; He, XH; Greney, H; Dontenwill, M; Cook, J; Marescaux, C;
Indirizzi:
Fac Med Strasbourg, INSERM U398, F-67085 Strasbourg, France Fac Med Strasbourg Strasbourg France F-67085 F-67085 Strasbourg, France Fac Med Strasbourg, LNPCV, F-67085 Strasbourg, France Fac Med Strasbourg Strasbourg France F-67085 F-67085 Strasbourg, France Univ Wisconsin, Dept Chem, Milwaukee, WI 53201 USA Univ Wisconsin Milwaukee WI USA 53201 Dept Chem, Milwaukee, WI 53201 USA
Titolo Testata:
EPILEPSY RESEARCH
fascicolo: 1-2, volume: 47, anno: 2001,
pagine: 43 - 53
SICI:
0920-1211(200111)47:1-2<43:DSTIAO>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
GABA(A) RECEPTOR; BENZODIAZEPINE RECEPTORS; STRASBOURG GAERS; BETA-CCM; SUBTYPES; BINDING; RO-15-4513; IMPAIRMENT; DIAZEPAM; IMIDAZOBENZODIAZEPINES;
Keywords:
absence-epilepsy; GABA(A)/benzodiazepine receptor; convulsion; binding;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
30
Recensione:
Indirizzi per estratti:
Indirizzo: Vergnes, M Fac Med Strasbourg, INSERM U398, 11 Rue Humann, F-67085 Strasbourg, France Fac Med Strasbourg 11 Rue Humann Strasbourg France F-67085 nce
Citazione:
M. Vergnes et al., "Differential sensitivity to inverse agonists of GABA(A)/benzodiazepine receptors in rats with genetic absence-epilepsy", EPILEPSY R, 47(1-2), 2001, pp. 43-53

Abstract

A strain of Wistar rats, genetic absence epilepsy rats from Strasbourg (GAERS), was selected and inbred over 40 generations for occurrence of spontaneous spike-wave discharges characteristic of absence seizures, simultaneously with a strain of non-epileptic rats (NER). GAERS demonstrate an excessive sensitivity to antagonists of the GABAA receptor. The sensitivity to convulsions induced by various inverse agonists of the GABA(A)/benzodiazepine receptor was compared in GAERS and NERs. The beta -carbolines FG 7142 and DMCM, and the imidazobenzodiazepines RO 19-4603 and the alpha 5-selective RY 024 were several times more convulsant in GAERS than in NERs. The largest differences were found with the non-selective RO 19-4603- and FG 7142. The proconvulsant imidazobenzodiazepine RO 15-4513, binding also to diazepam-insensitive receptors, had low efficacy. The high affinity binding of GABA(A)/BZD receptors with (3H) RO 15-1788 in the brain of naive rats and after administration of FG 7142 did not differ in GAERS and NERs. The data indicate that the hypersensitivity of GAERS to various inverse agonists of the GABAA/benzodiazepine receptor involves cortical GABAA receptors and is not related to differential activity of a subunit-selective receptor. (C) 2001 Elsevier Science B.V. All rights reserved.

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Documento generato il 09/04/20 alle ore 07:43:20