High-affinity binding site for ??-hydroxybutyrate in rat brain
摘要:
The existence of a specific synthesizing enzyme for γ-hydroxybutyric acid in rat brain has recently been reported. Here, for the first time, we demonstrate the presence of a high affinity, apparently specific binding site for this compound in the same tissue. This binding does not require Na + and takes place optimally at pH 5.5. The bound γ-hydroxybutyric acid is not displacable by GABA or baclofen. We report here on some structurally related compounds of GHB with a similar or better binding capacity than GHB itself. The number of binding sites increases with age up to adulthood and differs depending on the brain region. In primary tissue cultures of pure chicken neurones and glia, γ-hydroxybutyric acid binding occurs exclusively-- in the neuronal preparations.
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关键词:
Animals Rats Brain Hydroxybutyrates Sodium Oxybate Binding Sites Hydrogen-Ion Concentration Structure-Activity Relationship
DOI:
10.1016/0024-3205(82)90624-5
被引量:
年份:
1982
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