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␥-Hydroxybutyric acid (GHB) is a therapeutic drug, a drug of abuse, and an endogenous substance that binds to low-and high-affinity sites in the mammalian brain. I]BnOPh-GHB) binds to one site in rat brain cortical membranes with low nanomolar affinity (K d , 7 nM; B max , 61 pmol/mg protein). The binding is inhibited by GHB and selected analogs, but not by ␥-aminobutyric acid. Autoradiography using horizontal slices from rat brain demonstrates the highest density of binding in hippocampus and cortical regions and the lowest density in the cerebellum. Altogether, the findings correlate with the labeling and brain regional distribution of highaffinity GHB sites or [

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