GABA(B) receptors: from monogamy to promiscuity.
The aim of this review is firstly to describe the current understanding of the diverse physiology and pharmacology of GABA(B) receptors in vivo. We will then focus on recent advances made, since the identification of the GABA(B) receptor subunit genes, in our knowledge of the molecular nature of the receptor, and the recently discovered molecular determinants of functions such as ligand binding, trafficking and signalling. We will conclude with a summary of the GABA(B) receptor-interacting proteins that have been described thus far, and discuss how these may, at least in part, account for the paradox of varied receptor pharmacology in the potential context of a single heterodimeric GABA(B) receptor.
Calver
A R
AR
Neurology & GI CEDD, GlaxoSmithKline, New Frontiers Science Park, Harlow, UK.
Davies
C H
CH
Pangalos
M
M
D000818:Animals; D006801:Humans; D008024:Ligands; D009433:Neural Inhibition / Q000187:drug effects / Q000235:genetics; D017434:Protein Structure, Tertiary / Q000187:drug effects / Q000235:genetics; D021122:Protein Subunits / Q000187:drug effects / Q000235:genetics / Q000378:metabolism; D018080:Receptors, GABA-B / Q000172:deficiency* / Q000187:drug effects / Q000235:genetics; D013569:Synapses / Q000187:drug effects / Q000378:metabolism*; D009435:Synaptic Transmission / Q000187:drug effects / Q000235:genetics*
D008024:Ligands; D021122:Protein Subunits; D018080:Receptors, GABA-B