Function
GABBR2 is a component of a heterodimeric G-protein coupled receptor for GABA, formed in conjunction with GABBR1. Within this receptor complex, GABBR1 appears to be responsible for agonist binding, while GABBR2 mediates coupling to G proteins. Upon ligand binding, a conformational change triggers signaling through guanine nucleotide-binding proteins (G proteins), ultimately modulating the activity of downstream effectors such as adenylate cyclase. The signaling process inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels, and modulates inositol phospholipid hydrolysis. GABBR2 plays a crucial role in fine-tuning inhibitory synaptic transmission. Presynaptic GABA receptors inhibit neurotransmitter release by downregulating high-voltage activated calcium channels, while postsynaptic GABA receptors decrease neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance, leading to late inhibitory postsynaptic potentials. Beyond synaptic inhibition, GABBR2 is also implicated in hippocampal long-term potentiation, slow wave sleep, muscle relaxation, and antinociception (probable).