Abstract
A macromolecular moiety having high binding affinity for benzodiazepines was solubilized from a rat brain synaptosomal fraction by extraction with a combination of sodium deoxycholate and potassium chloride. This solubilized fraction exhibits pharmacological specificity for benzodiazepines. Specific 3H-flunitrazepam binding to the solubilized fraction was saturable with the apparent dissociation constant Kd = 1.8 ± 0.3 nM. The binding is sensitive to proteolytic enzymes. The binding is increased by α-aminobutyric acid and decreased by inosine and hypoxanthine. These results are similar to those obtained with intact membranes, suggesting that this moiety may be the benzodiazepine receptor. The molecular weight was estimated to be approximately 200, 000 by sucrose density gradient centrifugation.
Published Version
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