GABA-induced uncoupling of GABA/benzodiazepine site interactions is mediated by increased GABAA receptor internalization and associated with a change in subunit composition

Highlights • A single brief GABA exposure induces uncoupling between GABA and benzodiazepine sites. • Uncoupling is accompanied by a decrease in the proportion of α3-containing receptors. • Uncoupling mechanism is initiated by an increased GABAA receptor internalization.

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Bibliographic Details
Published in:Neuroscience 2014-01, Vol.257, p.119-129
Main Authors: Gutiérrez, M.L, Ferreri, M.C, Gravielle, M.C
Format: Article
Language:English
Subjects:
Animals
Benzodiazepines - metabolism
Benzodiazepines - pharmacology
Binding Sites - drug effects
Biological and medical sciences
Cells, Cultured
Cerebral Cortex - cytology
Embryo, Mammalian
Flunitrazepam - pharmacokinetics
Fundamental and applied biological sciences. Psychology
GABA Antagonists - pharmacology
GABA Modulators - pharmacokinetics
gamma-Aminobutyric Acid - pharmacology
Gene Expression Regulation - drug effects
Neurology
Neurons - drug effects
Picrotoxin - pharmacology
Protein Binding - drug effects
Protein Transport - drug effects
Rats
Rats, Sprague-Dawley
Receptors, GABA-A - chemistry
Receptors, GABA-A - genetics
Receptors, GABA-A - metabolism
Time Factors
Tritium - pharmacokinetics
Vertebrates: nervous system and sense organs
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Description
Summary:Highlights • A single brief GABA exposure induces uncoupling between GABA and benzodiazepine sites. • Uncoupling is accompanied by a decrease in the proportion of α3-containing receptors. • Uncoupling mechanism is initiated by an increased GABAA receptor internalization.
ISSN:0306-4522
1873-7544
DOI:10.1016/j.neuroscience.2013.10.077