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The GABA Receptors

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Book cover The GABA Receptors

Part of the book series: The Receptors ((REC))

Abstract

γ-Aminobutyric acid (GABA), an amino acid neurotransmitter, is widely distributed throughout the neuraxis. Two pharmacologically and molecularly distinct GABA receptors have been identified, GABAA and GABAB. GABAA receptors are pentameric ligand-gated chloride-ion channels, whereas GABAB receptors are heterodimeric G protein-coupled sites. Although GABAA receptor subtypes can display pharmacological differences, the two molecularly distinct GABAB receptors have similar substrate specificities, limiting the ability to selectively manipulate this site. Gene deletion and point mutation studies have revealed the importance of GABA receptors in neural development and function, with subtle modifications in subunit amino acid composition having profound effects on behavioral phenotype and responses to drugs. The characterization of GABAA receptors has contributed substantially to the knowledge about allosteric regulation of ligand-gated ion channels. Such information is invaluable in defining precisely the mechanisms of action of numerous drugs, such as the benzodiazepines, and toxic agents. Research on GABAB receptors has proven the existence of dimeric metabotropic receptors and has provided the chemical tools necessary for defining such systems. The characterization of the pentameric GABAA and dimeric GABAB receptors has been crucial for understanding the neurobiological basis of some nervous system disorders. Given the importance of GABA in central nervous system function, further work on its receptors is likely to yield novel therapeutics for treating a host of neurological and psychiatric conditions.

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  1. Department of Molecular and Integrative Physiology, Department of Pharmacology, Toxicology and Therapeutics, University of Kansas, Kansas City, KS

    S. J. Enna PhD

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  1. Departments of Molecular and Integrative Physiology and of Pharmcology, Toxicology and Therapeutics, University of Kansas, Kansas City, KS

    S. J. Enna

  2. Department of Chemistry and Applied Biosciecnes Swiss Federal Institute of Technology (ETH), Institute of Pharmacology University of Zurich, Zurich

    Hanns Möhler

  3. Collegium Helveticum, Zurich, Switzerland

    Hanns Möhler

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Enna, S.J. (2007). The GABA Receptors. In: Enna, S.J., Möhler, H. (eds) The GABA Receptors. The Receptors. Humana Press. https://doi.org/10.1007/978-1-59745-465-0_1

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