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GABAA -Benzodiazepine Receptors: Demonstration of Pharmacological Subtypes in the Brain

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Neuroreceptor Mechanisms in Brain

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 287))

Abstract

The GABAA receptor is a ligand-gated chloride ion channel that mediates the majority of rapid-acting inhibitory synapses in the central nervous system (Olsen and Venter, 1986). The GABAA receptors are also the target of numerous clinically important depressant and excitatory drugs (Olsen, 1981; Tallman and Gallager, 1985; Biggio and Costa, 1988). The convulsant drug bicuculline acts as a competitive antagonist at the GABA recognition site, beta-carbolines block GABA function as ’ inverse agonists’ at the benzodiazepine recognition site, and picrotoxin and cage convulsants inhibit the chloride channel function at a site on the receptor complex distinct from the GABA and benzodiazepine receptor sites. Clinically important depressant benzodiazepines enhance GABA-mediated inhibition via their own binding sites on the receptor complex. Still additional sites on the receptor-ion channel complex mediate the action of barbiturates, steroid anesthetics, and possibly ethanol to enhance GABAA receptor function at the membrane level (Olsen and Venter, 1986; Biggio and Costa, 1988).

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Author information

Authors and Affiliations

  1. Department of Pharmacology, University of California, Los Angeles, California, 90024, USA

    Richard W. Olsen, Michel Bureau, Shuichi Endo, Geoffrey Smith, Lynn Deng & Douglas Sapp

  2. Department of Biology, University of California, Los Angeles, California, 90024, USA

    Allan J. Tobin

Authors
  1. Richard W. Olsen
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  2. Michel Bureau
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  3. Shuichi Endo
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  4. Geoffrey Smith
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  5. Lynn Deng
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  6. Douglas Sapp
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  7. Allan J. Tobin
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Editor information

Editors and Affiliations

  1. Division of Health Sciences, University of the Air, 2-11 Wakaba, Chiba 260, Japan

    Shozo Kito

  2. Department of Pharmacology Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, 1-2-3 Kasumi, Minami-ku Hiroshima 734, Japan

    Tomio Segawa

  3. Department of Pharmacology Center for Health Sciences, University of California-Los Angeles School of Medicine, Los Angeles, California, 90024, USA

    Richard W. Olsen

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© 1991 Plenum Press, New York

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Olsen, R.W. et al. (1991). GABAA -Benzodiazepine Receptors: Demonstration of Pharmacological Subtypes in the Brain. In: Kito, S., Segawa, T., Olsen, R.W. (eds) Neuroreceptor Mechanisms in Brain. Advances in Experimental Medicine and Biology, vol 287. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-5907-4_30

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  • DOI: https://doi.org/10.1007/978-1-4684-5907-4_30

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4684-5909-8

  • Online ISBN: 978-1-4684-5907-4

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