GABAB Receptors


γ‐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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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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Wojcik JW and Holopainen I (1992) Role of central GABAB receptors in physiology and pathology. Neuropsychopharmacology 6: 201–214.

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How to Cite close
Kaupmann, Klemens, Froestl, Wolfgang, and Bettler, Bernhard(Apr 2001) GABAB Receptors. In: eLS. John Wiley & Sons Ltd, Chichester. [doi: 10.1038/npg.els.0000234]