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Titolo:
Decreased GABA enhancement of benzodiazepine binding after a single dose of diazepam
Autore:
Holt, RA; Bateson, AN; Martin, IL;
Indirizzi:
Astonandiv, Dept Pharmaceut & Biol Sci, Birmingham B4 7ET, W Midlands, Engl Aston Univ Birmingham W Midlands England B4 7ET B4 7ET, W Midlands, Engl SUNY Albany, Dept Biol Sci, Albany, NY 12222 USA SUNY Albany Albany NY USA 12222 bany, Dept Biol Sci, Albany, NY 12222 USA Univ Alberta, Dept Pharmacol, Edmonton, AB, Canada Univ Alberta Edmonton AB Canada ta, Dept Pharmacol, Edmonton, AB, Canada Univ Alberta, Div Neurosci, Edmonton, AB, Canada Univ Alberta Edmonton ABCanada erta, Div Neurosci, Edmonton, AB, Canada
Titolo Testata:
JOURNAL OF NEUROCHEMISTRY
fascicolo: 5, volume: 72, anno: 1999,
pagine: 2219 - 2222
SICI:
0022-3042(199905)72:5<2219:DGEOBB>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMINOBUTYRIC ACID(A) RECEPTORS; EXPOSURE; CELLS; PHARMACOLOGY; SENSITIVITY; LORAZEPAM; TOLERANCE; AGONISTS; EFFICACY; SUBTYPES;
Keywords:
GABA shift; ligand-gated ion channel; benzodiazepine tolerance; benzodiazepine binding; nuclear run-off assay; gene regulation;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Martin, IL AstonWUniv, Dept Pharmaceut & Biol Sci, Aston Triangle, Birmingham B4 7ET, Aston Univ Aston Triangle Birmingham W Midlands England B4 7ET
Citazione:
R.A. Holt et al., "Decreased GABA enhancement of benzodiazepine binding after a single dose of diazepam", J NEUROCHEM, 72(5), 1999, pp. 2219-2222

Abstract

The GABA and benzodiazepine binding sites on GABA(A) receptors are allosterically coupled. The in vitro binding of 2 nM [H-3]flunitrazepam to cortical and cerebellar membranes prepared from drug-naive rats was potentiated similar to 1.6-fold by 100 mu M GABA. Potentiation in both regions was significantly reduced 4 or 12 but not 24 h after a single dose of 15 mg/kg diazepam. At 24 h after the last of 14 daily doses of diazepam, no differences inGABA potentiation were observed. Diazepam-induced changes in GABA(A) receptor gamma 2-subunit gene transcription and alpha 1-, beta 2-, and gamma 2-subunit steady-state mRNA levels did not appear to be temporally related to allosteric uncoupling.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/04/20 alle ore 17:58:24