Human Gamma-aminobutyric Acid Type B Receptor Subunit 2, GABBR2 ELI

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: 10075644, PubMed: 10773016, PubMed: 24305054).

Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium Channels, inactivates voltage-dependent calcium-Channels and modulates inositol phospholipid hydrolysis (PubMed: 10075644, PubMed: 9872744, PubMed: 10906333, PubMed: 10773016).

Plays a critical role in the fine-tuning of inhibitory synaptic transmission (PubMed: 9872744, PubMed: 22660477).

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: 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).