Target intelligence / Profile preview

Gamma Aminobutyric Acid Type B Receptor (GABAB receptor)

Target
GABAB receptor
Molecular classification
G protein-coupled receptor, GPCR, Class C GPCR, Receptor
01

Overview

The GABAB receptor is a metabotropic, G protein-coupled receptor (GPCR) for gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system. It mediates slow and prolonged inhibitory synaptic transmission and is broadly expressed throughout the nervous system. The functional GABAB receptor is an obligate heterodimer composed of two subunits: GABA B1 and GABA B2. Activation leads to neuronal inhibition.

Other names
GABABGABABR
02

Mechanism of action

Activation by GABA leads to activation of Gi/o-type proteins, resulting in the opening of inwardly rectifying potassium channels (GIRKs), inhibition of voltage-gated calcium channels, and inhibition of adenylyl cyclase activity. These actions cause hyperpolarization and reduced excitability in neurons.

03

Biological functions

Signal transductionInhibition of neurotransmitter releaseRegulation of neuronal excitabilitySynaptic transmissionNeuronal hyperpolarization
04

Disease associations

EpilepsyAlcohol use disorderAnxietySpasticityAddiction disorders
05

Interacting drugs

Baclofen

2 more in the full profile.

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