gamma-Hydroxybutyrate receptor binding in rat brain is inhibited by guanyl nucleotides and pertussis toxin.

gamma-Hydroxybutyrate is an endogenous substance of mammalian brain which is primarily derived from GABA. This compound exhibits neuromodulatory influences on dopamine and serotonin synthesis and release in rat brain. These effects are mediated by specific brain receptors which are mainly distributed in the hippocampus, cortex and striatum. In order to characterize this type of receptor, we have studied the possibility that guanosine triphosphate (GTP) and/or pertussis toxin mediated modification of the affinity for gamma-hydroxybutyrate binding to the receptor. Results presented in this paper favor the presence of guanine nucleotide binding proteins (G0 or Gi family), which are coupled to the gamma-hydroxybutyrate receptor, modifying the high-affinity gamma-hydroxybutyrate binding. We conclude that the gamma-hydroxybutyrate receptor in brain belongs to the G-protein family of receptors.