STRUCTURAL REQUIREMENTS FOR THE BINDING OF BENZODIAZEPINES TO THEIR PERIPHERAL-TYPE SITES

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  • 1 January 1984
    • journal article
    • research article
    • Vol. 25  (3) , 349-351
Abstract
The murine DS19 Friend erythroleukemia cells possess peripheral-type benzodiazepine recognition sites that are similar to those characterized in other tissues and cells. These sites recognize only specific and well-defined ligand structures. In order for the benzodiazepines to bind to these sites, an alkyl group of 3 carbons or less is required at position 1, together with a carbonyl group at position 2. The binding affinity is enhanced by 4''-halogen or 4''-methoxy substituents, and by 7- or 2''-halogens. The affinity is decreased by substitutions at position 3 or 4. Central-type benzodiazepine binding in brain is not affected by 1-alkyl groups and is inhibited by 4''-substitutions. Unlike the peripheral-type site, the brain receptor is stereoselective. The 2 binding sites are evidently fundamentally different in their recognition of benzodiazepine ligands.