Identification of Inosine and Hypoxanthine as Endogenous Ligands for the Brain Benzodiazepine-Binding Sites

Two endogenous ligands for the brain benzodiazepine-binding sites were isolated from bovine brain through gel filtration, paper electrophoresis, and paper chromatography. These ligands were identified as inosine and hypoxanthine, and both had a higher affinity for the brain benzodiazepine-binding si...

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Bibliographic Details
Published in:Proceedings of the National Academy of Sciences - PNAS 1979-02, Vol.76 (2), p.977-981
Main Authors: Asano, Tomiko, Spector, Sydney
Format: Article
Language:English
Subjects:
Animals
Antibodies
Benzodiazepines
Benzodiazepines - immunology
Benzodiazepines - metabolism
Binding Sites, Antibody
Binding, Competitive
Brain
Brain - metabolism
Brain hypoxia
Cattle
Diazepam - metabolism
Electrophoresis
Hypoxanthines - metabolism
Hypoxia
Inosine - metabolism
Ligands
Paper chromatography
Radioimmunoassay
Receptors
Receptors, Drug - metabolism
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Description
Summary:Two endogenous ligands for the brain benzodiazepine-binding sites were isolated from bovine brain through gel filtration, paper electrophoresis, and paper chromatography. These ligands were identified as inosine and hypoxanthine, and both had a higher affinity for the brain benzodiazepine-binding sites than for benzodiazepine sites in some peripheral tissues. They did not bind to any other receptors tested, such as the opiate, muscarinic cholinergic, γ -aminobutyric acid, and β -adrenergic receptors. Both inosine and hypoxanthine competitively inhibited the binding of [3H]diazepam to the brain binding site.
ISSN:0027-8424
1091-6490
DOI:10.1073/pnas.76.2.977