| 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 as kidney, lung, trachea, colon, small intestine, stomach, bone marrow, thymus and mammary gland. |
| 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. |
| Protein Name | Gamma-Aminobutyric Acid Type B Receptor Subunit 1Gaba-B Receptor 1Gaba-B-R1Gaba-Br1Gababr1Gb1 |
| Database Links | Reactome: R-HSA-1296041Reactome: R-HSA-418594Reactome: R-HSA-420499Reactome: R-HSA-977444Reactome: R-HSA-997272 |
| Cellular Localisation | Cell MembraneMulti-Pass Membrane ProteinPostsynaptic Cell MembraneCell ProjectionDendriteColocalizes With Atf4 In Hippocampal Neuron Dendritic MembranesCoexpression Of Gabbr1 And Gabbr2 Is Required For Gabbr1 Maturation And Transport To The Plasma MembraneIsoform 1e: Secreted |
| Alternative Antibody Names | Anti-Gamma-Aminobutyric Acid Type B Receptor Subunit 1 antibodyAnti-Gaba-B Receptor 1 antibodyAnti-Gaba-B-R1 antibodyAnti-Gaba-Br1 antibodyAnti-Gababr1 antibodyAnti-Gb1 antibodyAnti-GABBR1 antibodyAnti-GPRC3A antibody |
Information sourced from Uniprot.org
