Diazepam enhancement of low affinity GABA binding to rat brain membranes

Diazepam enhancement of low affinity GABA binding to rat brain membranes

Diazepam (3 nM–3 μM) enhanced GABA binding to well-washed synaptosomal membranes in a concentration-dependent manner. Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GA...

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Veröffentlicht in:Neuroscience letters 1982-03, Vol.29 (1), p.63-66
Hauptverfasser: Skerritt, John H., Willow, Max, Johnston, Graham A.R.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Binding Sites - drug effects
Brain - anatomy & histology
Brain - metabolism
Cell Membrane - metabolism
Diazepam - pharmacology
gamma-Aminobutyric Acid - metabolism
Kinetics
Rats
Synaptosomes - metabolism
Synaptosomes - ultrastructure
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Zusammenfassung:Diazepam (3 nM–3 μM) enhanced GABA binding to well-washed synaptosomal membranes in a concentration-dependent manner. Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GABA binding to a low affinity site. These results support electrophysiological and other biochemical observations of benzodiazepine-GABA interactions.
ISSN:0304-3940
1872-7972
DOI:10.1016/0304-3940(82)90365-2