Update 1988 pp 528-534 | Cite as

Clinical Use of Benzodiazepine Antagonists

  • P. Lheureux
  • R. Askenasi
Part of the Update in Intensive Care and Emergency Medicine book series (UICM, volume 5)


The benzodiazepins were introducted in the early sixties. Their various pharmacological properties and their high toxic/therapeutic ratio explain the wide development of their clinical use (and abuse?). Their mechanism of action on the central nervous system (CNS) was only elucidated in 1977 when high affinity binding sites, closely related to GABA-ergic synapses, were discovered in the mammalian cerebral cortex and related to the pharmacologic action of benzodiazepines [1, 2]. A specific antagonist of benzodiazepine-receptors (Ro 15-1788 — flumazenil), able to inhibit all the effects of classical benzodiazepines without inducing any own action, was discovered by Hunkeleer et al. in 1981 [3].


Hepatic Encephalopathy Inverse Agonist Central Receptor Partial Inverse Agonist Mammalian Cerebral Cortex 
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© Springer-Verlag Berlin Heidelberg 1988

Authors and Affiliations

  • P. Lheureux
  • R. Askenasi

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