Pharmacology of Mammalian GABAB Receptors

  • Norman G. Bowery
Part of the The Receptors book series (REC)


At the time of publication of the first edition of The GABA Receptors in 1983, the concept of GABA receptor subtypes had only just emerged. Designation of the terms GABAA and GABAB to describe bicuculline-sensitive Cl-dependent and novel bicuculline-insensitive Cl-independent receptors, respectively, was introduced less than two years earlier (Hill and Bowery, 1981). There was no evidence for a physiological role for the novel GABAB site at that time and the molecular structure of fast channel-linked GABAA receptors was unknown. We now know that GABAB receptors have not only a physiological role in synaptic transmission (Dutar and Nicoll, 1988a), but may also be important in pathological conditions associated with pain and epilepsy. In addition, we now have information for the structural sequences of the GABAA receptor (see Chapter 2 of this volume), with evidence for marked heterogeneity (e.g., Olsen and Tobin, 1990). Evidence is also accruing for a potential subclassification of GABAB receptors based on pharmacological characteristics (see Section 3.4.). Thus, in little more than a decade we have gone from a single GABA receptor to a multiplicity of GABA sites, with at least two distinct classes of receptors namely GABAA and GABAB. A third class GABAC, associated with fast Cl-channels, has also been suggested (Johnston, 1995; see also Chapter 11 of this volume). This chapter summarizes the pharmacological properties of the GABAB receptor(s), making reference to its potential significance as a therapeutic target.


Spinal Cord Dorsal Horn Gaba Receptor Pertussis Toxin GABAB Receptor 
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© Springer Science+Business Media New York 1997

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  • Norman G. Bowery

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