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ID: ALA1123727
Journal: J Med Chem
Title: Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Authors: Hagen TJ, Skolnick P, Cook JM.
Abstract: The synthesis of the first beta-carboline, 6-(benzylamino)-beta-carboline (1c), to be devoid of a substituent at the 3-position and that still binds to benzodiazepine receptors with potent affinity is described. Furthermore, 1c proved to be a partial inverse agonist when tested in mice. Addition of the benzylamino group at the 6-position of the beta-carboline nucleus is primarily responsible for the activity of beta-carbolines 1b and 1c. The importance of the Nb-nitrogen atom for binding affinity was also demonstrated since 3-(benzylamino)carbazole (6) exhibited little or no affinity for benzodiazepine receptors in vitro, in contrast to the activity of 1c.
CiteXplore: 3031296
DOI: 10.1021/jm00387a033