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Potentiation of GABAergic Neurotransmission by Steroids

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Neurosteroids

Part of the book series: Contemporary Endocrinology ((COE,volume 16))

Abstract

The endogenous 3α-hydroxy ring A-reduced steroids allopregnanolone and pregnanolone are among the most active ligands of gamma amino butric acid A (GABAA) receptors, with affinities equal to or greater than those of other known ligands such as barbiturates, and even benzodiazepines (1,2). It is, therefore, not surprising that numerous 3α-hydroxy steroids have anxiolytic, hypnotic, anticonvulsant, and anesthetic effects when administered to laboratory animals (2). These pharmacological actions, together with their low intrinsic toxicity and lack of hormonal activity, have led an expanding number of laboratories to investigate their physiological and pharmacological properties in both laboratory animals and humans. Efforts are also underway to develop novel synthetic anxiolytic, hypnotic, and anticonvulsant steroids as therapeutic agents. In this chapter, we discuss a few selected areas related to the pharmacology, physiology, and chemistry of GABAergic neuroactive steroids, including their potential roles in alcohol dependence and withdrawal, as well as in affective disorders.

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Authors
  1. Robert H. Purdy PhD
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  2. Steven M. Paul MD
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Editors and Affiliations

  1. Institut National de la Santé et de la Recherche Médicale, Collége de France, Le Kremlin-Bicêtre, France

    Etienne-Emile Baulieu MD, PhD , Paul Robel MD, PhD  & Michael Schumacher PhD ,  & 

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Purdy, R.H., Paul, S.M. (1999). Potentiation of GABAergic Neurotransmission by Steroids. In: Baulieu, EE., Robel, P., Schumacher, M. (eds) Neurosteroids. Contemporary Endocrinology, vol 16. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-693-5_8

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  • DOI: https://doi.org/10.1007/978-1-59259-693-5_8

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-61737-068-7

  • Online ISBN: 978-1-59259-693-5

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