GABA-B-R1 is a receptor for GABA. The activity of GABA-B-R1 is mediated by G-proteins that inhibit adenylyl cyclase activity, stimulate phospholipase A2, activate potassium channels, inactivate voltage-dependent calcium-channels and modulates inositol phospholipids hydrolysis. GABA-B-R1 plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA-B-R inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA-B-R decreases neuronal e, Xenopus/Amphibian,citability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. GABA-B-R1 is not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep,Mouse,uscle rela, Xenopus/Amphibian,ation and antinociception.