Target intelligence / Profile preview

Gamma-hydroxybutyric acid receptor (None)

Target
None
Molecular classification
G protein-coupled receptor (GPCR), Receptor, Riboflavin transporter
01

Overview

The gamma-hydroxybutyric acid receptor (GHBR) is an excitatory G protein-coupled receptor that binds the endogenous neurotransmitter gamma-hydroxybutyric acid (GHB). It is distinct from the GABA_B receptor and mediates stimulant effects through increased Na+/K+ currents and neurotransmitter release. The receptor has approximately 11 transmembrane helices and is expressed in various brain regions, including the dentate gyrus, thalamus, and cerebellum. It plays a role in regulating neurotransmitter systems, sleep, mood, and anxiety.

Other names
GHB receptorGHBRGPR172ASLC52A2
02

Mechanism of action

Activation leads to increased Na+/K+ current and enhanced release of dopamine and glutamate, resulting in stimulant effects. May also enhance tryptophan transport and modulate oxytocinergic neuron activity.

03

Biological functions

NeurotransmissionSignal transductionTryptophan transportRegulation of sleepRegulation of moodRegulation of anxietyOxytocin neuron activationDopamine releaseGlutamate release
04

Disease associations

Anxiety disordersSleep disordersMood disordersEpilepsy (convulsions at high doses)
05

Safety considerations

High doses can cause convulsionsPotential for abuse due to psychoactive effects
06

Interacting drugs

Gamma-hydroxybutyric acid (GHB)

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