GABAA Receptors

Autoradiographic Localization of Different Ligand Sites and Identification of Subtypes of the Benzodiazepine Binding Site
  • Cyrille Sur
  • John Atack
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


GABA is generally accepted as the major inhibitory neurotransmitter within the vertebrate brain. Pharmacologically, the responses to GABA were initially characterized in terms of their sensitivity to a variety of agonists and antagonists. Thus, fast, ion channel-mediated effects that can be blocked by bicuculline, SR 95531 (both of which act at the GABA binding site), and picrotoxin and stimulated by GABA, muscimol, and isoguvacine, are mediated by GABAA receptors. On the other hand, bicuculline-insensitive effects which are stimulated by GABA and baclofen and inhibited by phaclofen, are mediated by G-protein linked, metabotropic GABAB receptors. In addition, a third type of GABA receptor, the so-called GABAC receptor, has been identified on the basis of its bicuculline and baclofen insensitivity (1). In the present chapter, we will concentrate on the autoradiographic identification of bicuculline-sensitive GABAA receptors.


GABAA Receptor Globus Pallidus Granule Cell Layer Pregnenolone Sulfate GABAA Receptor Subtype 
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Copyright information

© Humana Press Inc., Totowa, NJ 2001

Authors and Affiliations

  • Cyrille Sur
    • 1
  • John Atack
    • 1
  1. 1.Department of Biochemistry, Neuroscience Research CentreMerck Sharp and Dohme Research LaboratoriesEssexUK

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