|Other Names||Gamma-aminobutyric acid type B receptor subunit 1, GABA-B receptor 1, GABA-B-R1, GABA-BR1, GABABR1, Gb1, GABBR1, GPRC3A|
|Format||Synthetic peptide was lyophilized with 100% acetonitrile and is supplied as a powder. Reconstitute with 0.1 ml DI water for a final concentration of 1 mg/ml.|
|Storage||Maintain refrigerated at 2-8°C for up to 6 months. For long term storage store at -20°C.|
|Precautions||This product is for research use only. Not for use in diagnostic or therapeutic procedures.|
|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. Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.|
|Cellular Location||Cell membrane; Multi-pass membrane protein. Cell junction, synapse, postsynaptic cell membrane; Multi-pass membrane protein. Cell projection, dendrite Note=Colocalizes with ATF4 in hippocampal neuron dendritic membranes (By similarity). Coexpression of GABBR1 and GABBR2 is required for GABBR1 maturation and transport to the plasma membrane.|
|Tissue Location||Highly expressed in brain and weakly in heart, small intestine and uterus. Isoform 1A is mostly expressed in granular cell and molecular layer. Isoform 1B is mostly expressed in Purkinje cells. Isoform 1E is predominantly expressed in peripheral tissues as kidney, lung, trachea, colon, small intestine, stomach, bone marrow, thymus and mammary gland|
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Gamma-aminobutyric acid (GABA) is the main inhibitoryneurotransmitter in the mammalian central nervous system. GABAexerts its effects through ionotropic [GABA(A/C)] receptors, toproduce fast synaptic inhibition, and metabotropic [GABA(B)]receptors, to produce slow, prolonged inhibitory signals. TheGABA(B) receptor consists of a heterodimer of two related7-transmembrane receptors, GABA(B) receptor 1 and GABA(B) receptor2. The GABA(B) receptor 1 gene is mapped to chromosome 6p21.3within the HLA class I region close to the HLA-F gene.Susceptibility loci for multiple sclerosis, epilepsy, andschizophrenia have also been mapped in this region. Alternativesplicing of this gene generates multiple transcript variants.
Cramer, N.P., et al. Adv. Pharmacol. 58, 397-426 (2010) :Gonzalez-Burgos, G. Adv. Pharmacol. 58, 175-204 (2010) :Tabata, T., et al. Adv. Pharmacol. 58, 149-173 (2010) :Padgett, C.L., et al. Adv. Pharmacol. 58, 123-147 (2010) :Terunuma, M., et al. Adv. Pharmacol. 58, 113-122 (2010) :
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