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Comparative In vivo and In vitro Selectivity of Zolpidem for ω (Benzodiazepine) Modulatory Site Subtypes

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PET for Drug Development and Evaluation

Part of the book series: Developments in Nuclear Medicine ((DNUM,volume 26))

Abstract

Drugs acting upon the benzodiazepine binding sites of the GABAA receptor complex constitute one of the most widely used class of psychotropic agents. These drugs increase the sensitivity of the GABAA receptor to its natural agonist, γ-aminobutyric acid (GABA). This allosteric facilitation of GABAergic neurotransmission has found clinical application in the treatment of a large number of disorders [1–3]. These applications are based on the sedative, anxiolytic, anticonvulsant and myorelaxant activities of benzodiazepine receptor agonists. Moreover, these drugs also display untoward effects such as memory disruption, and after chronic treatment, induction of tolerance and dependence. These pleitropic actions constitute one of the most important drawback of benzodiazepines. For this reason, much research has tried to dissociate the effects responsible for the therapeutic activity from those considered as secondary. For example, to dissociate anxiolytic from sedative effects, or hypnotic effects from memory impairment or myorelaxant activities, and also to avoid the induction of tolerance or dependence.

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Authors and Affiliations

  1. Synthélabo Recherche, BP 110, 92290, Bagneux, France

    Jesús Benavides & Bernard Scatton

  2. Centre Cyceron, BP 5229, 14704, Caen, France

    Pascale Abadie & Jean Claude Baron

Authors
  1. Jesús Benavides
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  2. Pascale Abadie
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  3. Jean Claude Baron
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  4. Bernard Scatton
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Editors and Affiliations

  1. Hôpital Neuro-cardiologique, Lyon, France

    D. Comar

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Benavides, J., Abadie, P., Baron, J.C., Scatton, B. (1995). Comparative In vivo and In vitro Selectivity of Zolpidem for ω (Benzodiazepine) Modulatory Site Subtypes. In: Comar, D. (eds) PET for Drug Development and Evaluation. Developments in Nuclear Medicine, vol 26. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-0429-6_10

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  • DOI: https://doi.org/10.1007/978-94-011-0429-6_10

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-4191-1

  • Online ISBN: 978-94-011-0429-6

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