Recombinant Human Gamma-aminobutyric acid type B receptor subunit 1 (GABBR1), Truncated

Uniprot Id

Q9UBS5

Target Species

Human

Target Name

GABBR1

Target Full Name

Gamma-aminobutyric acid type B receptor subunit 1

Target Function

Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis. Calcium is required for high affinity binding to GABA. Plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable). Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.; Isoform 1E may regulate the formation of functional GABBR1/GABBR2 heterodimers by competing for GABBR2 binding. This could explain the observation that certain small molecule ligands exhibit differential affinity for central versus peripheral sites.

Target Subcellular Location

Cell membrane; Multi-pass membrane protein. Cell junction, synapse, postsynaptic cell membrane; Multi-pass membrane protein. Cell projection, dendrite.; [Isoform 1E]: Secreted.

Target Protein Families

G-protein coupled receptor 3 family, GABA-B receptor subfamily

Target Tissue Specificity

Highly expressed in brain. Weakly expressed in heart, small intestine and uterus. Isoform 1A: Mainly expressed in granular cell and molecular layer. Isoform 1B: Mainly expressed in Purkinje cells. Isoform 1E: Predominantly expressed in peripheral tissues

Target Synonyms

dJ271M21.1.1; dJ271M21.1.2; FLJ92613; GABA-B receptor 1; GABA-B-R1; GABA-BR1; GABAB R1; GABAB subunit 1c; GABABR1; GABBR1 3; GABBR1; GABR1_HUMAN; Gamma aminobutyric acid (GABA) B receptor 1; Gamma-aminobutyric acid type B receptor subunit 1; Gb1; GPRC3A; Seven transmembrane helix receptor

Target Background

This gene encodes a receptor for gamma-aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in the mammalian central nervous system. This receptor functions as a heterodimer with GABA(B) receptor 2. Defects in this gene may underlie brain disorders such as schizophrenia and epilepsy. Alternative splicing generates multiple transcript variants, but the full-length nature of some of these variants has not been determined.