GABAB Receptors

-Aminobutyric acid (GABA), the principal inhibitory neurotransmitter in the brain, signals through ionotropic (GABAA/C) and metabotropic (GABAB) receptor systems. GABAB receptors modulate synaptic transmission and are structurally related to the metabotropic glutamate receptors. The properties of the recently cloned GABABR1a and -b receptors are compared to brain GABAB receptors.

Keywords: baclofen; expression cloning; metabotropic; mGluR; G-protein; epilepsy

Figure 1. Structural model of GABAB receptors. The putative GABA-binding site is located in the extracellular domain. GABABR1a and -b are N-terminal splice variants derived from the same gene. The N-terminal 147 amino acids of the mature GABABR1a are replaced by 18 different residues in GABABR1b. The putative GABA-binding site located in the extracellular N-terminal domain is identical in the two splice variants.
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 References
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 Further Reading
    Bowery NG, Kerr DIB and Ong J (1997) GABAB receptors: role and therapeutic implications in CNS disorders. CNS Drugs 7: 167–175.
    Kenakin T (1997) Differences between natural and recombinant G-protein coupled receptor systems with varying receptor/G-protein stoichiometry. Trends in Pharmacological Sciences 18: 456–464.
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    Mody I, De Konninck Y, Otis S and Soltesz I (1994) Bridging the cleft at GABA synapses in the brain. Trends in Neuroscience 17: 517–525.
    Thompson SM, Capogna M and Scanziani M (1993) Presynaptic inhibition in the hippocampus. Trends in Neuroscience 16: 222–227.
    Wojcik JW and Holopainen I (1992) Role of central GABAB receptors in physiology and pathology. Neuropsychopharmacology 6: 201–214.
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Kaupmann, Klemens, Froestl, Wolfgang, and Bettler, Bernhard(Apr 2001) GABAB Receptors. In: eLS. John Wiley & Sons Ltd, Chichester. http://www.els.net [doi: 10.1038/npg.els.0000234]