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Target intelligence / Profile preview
γ-Hydroxybutyrate Receptor (GHBR)
- Target
- GHBR
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The γ-hydroxybutyrate receptor (GHBR) is an excitatory G protein-coupled receptor that binds the neurotransmitter γ-hydroxybutyric acid (GHB). It plays a role in neuronal energy homeostasis and sleep–wake regulation, and its activation modulates glutamate, dopamine, and serotonin systems. At low concentrations of GHB, it acts as an agonist, stimulating dopamine release. At higher concentrations, it also acts as a weak agonist at inhibitory metabotropic GABA_B receptors. This dual action explains both sedative and stimulatory properties observed with different doses of exogenous or pharmacological administration of GHB. The GHBR is densely expressed throughout various regions of the brain including the hippocampus, frontal cortex, and cerebellum.
- Other names
- GPR172ASLC52A2BVVLS2D15Ertd747eGPCR41PAR1RFT3RFVT2hRFT3Solute carrier family 52 member 2
02
Mechanism of action
Agonist or antagonist at GHB receptors, influencing downstream dopamine, glutamate and serotonin release.
03
Biological functions
NeurotransmissionSignal transductionNeuronal energy homeostasisSleep-wake regulationGlutamatergic signaling modulationDopamine release modulationSerotonin turnover modulation
04
Disease associations
Sleep disordersNeurological disordersNeurodegenerative disease
05
Safety considerations
SedationRespiratory depressionAbuse potential
06
Interacting drugs
γ-hydroxybutyric acid (GHB)
2 more in the full profile.
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