GABBR1, EnkiLife, AMRe11228

Receptor for GABA. The activity of this receptor is mediated by G-proteins that inhibit adenylyl cyclase activity, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipids hydrolysis. Plays a critical role in the fine-tuning of inhibitory synaptic transmission. 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).