Summary

Name GABBR1
Full Name Gamma-aminobutyric acid type B receptor subunit 1
Synonyms GABA-B receptor 1, GABA-B-R1, GABA-BR1, GABABR1, Gb1 | GPRC3A
Primary ID Q9UBS5
Links - -
Type protein
Relations 4
Function Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2 (PubMed:9872316, PubMed:9872744, PubMed:15617512, PubMed:18165688, PubMed:22660477, PubMed:24305054). Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins (PubMed:18165688). 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 (PubMed:10906333, PubMed:10773016, PubMed:10075644, PubMed:9872744, PubMed:24305054). Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis (PubMed:10075644). Calcium is required for high affinity binding to GABA (By similarity). Plays a critical role in the fine-tuning of inhibitory synaptic transmission (PubMed:9844003). 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 (PubMed:9844003, PubMed:9872316, PubMed:10075644, PubMed:9872744, PubMed:22660477). 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 (PubMed:9844003, PubMed:9872316, PubMed:24305054).

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▶Modifications Tables

Relations

Regulator Mechanism target score ℹ
+ CAMK2Adown-regulates img/direct_inhibition.png phosphorylation GABBR1 0.239
Publications: 1 Organism: Homo Sapiens
Tissue: Brain
+ KIF5Bup-regulates activity img/direct-activation.png relocalization GABBR1 0.258
Publications: 1 Organism: Mus Musculus
+ JAKMIP1up-regulates quantity img/indirect-activation.png GABBR1 0.536
Publications: 1 Organism: Chlorocebus Aethiops
+ GABBR1form complex img/form-complex.png binding GABA-B receptor 0.678
Publications: 1 Organism: Homo Sapiens