Diazepam enhancement of low affinity GABA binding to rat brain membranes.
Diazepam (3 nM-3 microM) 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.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000033:anatomy & histology / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D003975:Diazepam / Q000494:pharmacology*; D007700:Kinetics; D051381:Rats; D013574:Synaptosomes / Q000378:metabolism / Q000648:ultrastructure; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D005680:gamma-Aminobutyric Acid; D003975:Diazepam