STRING | IntAct | MINT

Open Targets | OMIM

Catalytic Site Atlas

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Cell membrane,Cell junction,Synapse,Postsynaptic cell membrane,Cell projection,Dendrite;

Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2 (PubMed:10773016, PubMed:10075644). Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins (By similarity). 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:10773016, PubMed:10075644). 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 (By similarity). 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:10075644). Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (By similarity).

GO:0030673; GO:0030054; GO:0005737; GO:0043198; GO:0043197; GO:0005789; GO:0005615; GO:0038037; GO:0038039; GO:1902710; GO:0098982; GO:0098978; GO:0005887; GO:0099055; GO:0099056; GO:0043231; GO:0016020; GO:0045121; GO:0031966; GO:0043005; GO:0043025; GO:0045211; GO:0098793; GO:0042734; GO:0098685; GO:0097060; GO:0008021; GO:1990430; GO:0004965; GO:0099579; GO:0046982; GO:0008134; GO:0007193; GO:0007214; GO:0007194; GO:0008285; GO:0033602; GO:0032811; GO:0014053; GO:0050805; GO:0001649; GO:0014049; GO:0060124; GO:0014048