GABA(B) receptors are a distinct subclass of receptors for the major i
nhibitory transmitter 4-aminobutanoic acid (GABA) that mediate depress
ion of synaptic transmission and contribute to the inhibition controll
ing neuronal excitability. The development of specific agonists and an
tagonists for these receptors has led to a better understanding of the
ir physiology and pharmacology, highlighting their diverse coupling to
different intracellular effecters through G(i)/G(o) proteins. This re
view emphasises our current knowledge of the neurophysiology and neuro
chemistry of GABA(B) receptors, including their heterogeneity, as well
as the therapeutic potential of drugs acting at these sites.