Antagonism of benzodiazepine receptors by beta carbolines
| Autor: | R.A. O'Brien, E.P. Bonetti, Nena Spirt, W. Schlosser, S. Franco, P. Polc, W.D. Horst |
|---|---|
| Rok vydání: | 1981 |
| Předmět: |
Male
Indoles medicine.drug_class Receptors Drug Endogeny Pharmacology Binding Competitive General Biochemistry Genetics and Molecular Biology medicine Animals General Pharmacology Toxicology and Pharmaceutics Evoked Potentials Benzodiazepine Diazepam Behavior Animal GABAA receptor Chemistry General Medicine Receptors GABA-A Affinities In vitro Rats Kinetics Beta Carbolines Antagonism Carbolines |
| Zdroj: | Life Sciences. 29:75-82 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(81)90117-x |
| Popis: | A number of beta carbolines were found to interact at brain benzodiazepine sites in vitro . 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. |
| Databáze: | OpenAIRE |
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