Antagonism of benzodiazepine receptors by beta carbolines |
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Authors: | RA OBrien W Schlosser NM Spirt S Franco WD Horst P Polc EP Bonetti |
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Institution: | 1. Hoffmann-La Roche Inc. Nutley, New Jersey, U.S.A.;2. F. Hoffmann-La Roche & Co., Ltd. Basle, Switzerland |
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Abstract: | A number of beta carbolines were found to interact at brain benzodiazepine sites . The compounds we evaluated had affinities in the low nanomolar range and had Hill slopes less than unity. In addition to being potential antagonists at benzodiazepine receptors, they may specifically label the BZ1 site. After intravenous administration, these compounds antagonized benzodiazepine actions in the cat spinal cord and in a mouse free behavioral model. Aspects of this antagonism and their proposed role as endogenous benzodiazepine ligands in brain are discussed. |
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