title: GABAB receptors.
abstract: GABAB receptors are a distinct subclass of receptors for the major inhibitory transmitter 4-aminobutanoic acid (GABA) that mediate depression of synaptic transmission and contribute to the inhibition controlling neuronal excitability. The development of specific agonists and antagonists for these receptors has led to a better understanding of their physiology and pharmacology, highlighting their diverse coupling to different intracellular effectors through Gi/G(o) proteins. This review emphasises our current knowledge of the neurophysiology and neurochemistry of GABAB receptors, including their heterogeneity, as well as the therapeutic potential of drugs acting at these sites.
mesh_terms: D001418:Baclofen / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive; D002413:Cations, Divalent / Q000494:pharmacology; D002490:Central Nervous System / Q000187:drug effects / Q000378:metabolism*; D002493:Central Nervous System Diseases / Q000188:drug therapy; D018755:GABA Agonists / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D018756:GABA Antagonists / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D009482:Neurophysiology; D011869:Radioligand Assay; D018080:Receptors, GABA-B / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D002413:Cations, Divalent; D018755:GABA Agonists; D018756:GABA Antagonists; D018080:Receptors, GABA-B; D019204:GTP-Binding Proteins; D001418:Baclofen