Beta-carboline binding indicates the presence of benzodiazepine receptor subclasses in the bovine central nervous system

Receptor binding studies were performed with tritiated propyl beta-carboline-3-carboxylate ( [3H]PrCC), tritiated ethyl beta-carboline-3-carboxylate ( [3H]ECC), and tritiated flunitrazepam ( [3H]FNT) in membrane preparations from different regions of the bovine brain and retina. Specific binding in...

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Bibliographic Details
Published in:Naunyn-Schmiedeberg's archives of pharmacology 1982-05, Vol.319 (2), p.172-177
Main Authors: Fehske, K J, Zube, I, Borbe, H O, Wollert, U, Müller, W E
Format: Article
Language:English
Subjects:
Adenosine - analogs & derivatives
Adenosine - pharmacology
Animals
benzodiazepines
beta -carboline
Binding Sites
brain
Brain Chemistry
Carbolines - metabolism
Cattle
gamma-Aminobutyric Acid - pharmacology
Indoles - metabolism
Receptors, Drug - analysis
Receptors, Drug - drug effects
Receptors, GABA-A
retina
Substrate Specificity
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Summary:Receptor binding studies were performed with tritiated propyl beta-carboline-3-carboxylate ( [3H]PrCC), tritiated ethyl beta-carboline-3-carboxylate ( [3H]ECC), and tritiated flunitrazepam ( [3H]FNT) in membrane preparations from different regions of the bovine brain and retina. Specific binding in all regions investigated was associated with benzodiazepine receptor sites. However, not all benzodiazepine receptors in the regions investigated as determined by the specific binding of tritiated flunitrazepam ( [3H]FNT) are available for [3H]PrCC suggesting that specific [3H]PrCC binding labels only one subclass or subpopulation of the benzodiazepine receptor. This benzodiazepine receptor subclass is sensitive to GABAergic modulation and amounts for about 60% of the benzodiazepine receptors in bovine cortex, hippocampus, and retina but for about 80% of the benzodiazepine receptors in the bovine cerebellum. By contrast, specific [3H]ECC binding in the cerebellum and the hippocampus labeled the same number of benzodiazepine receptors as [3H]FNT, giving no evidence for a benzodiazepine receptor subclass specificity of this compound in the bovine CNS.
ISSN:0028-1298
DOI:10.1007/BF00503933