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Subtype-selective GABAA receptor mimetics—novel antihyperalgesic agents?

Zeilhofer, Hanns ; Witschi, Robert ; Hösl, Katharina

In: Journal of Molecular Medicine, 2009, vol. 87, no. 5, p. 465-469

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    Titre
    • Subtype-selective GABAA receptor mimetics—novel antihyperalgesic agents?
    Auteur
    • Zeilhofer, Hanns. Institute of Pharmacology and Toxicology, University of Zurich, Winterthurerstrasse 190, CH-8057, Zurich, Switzerland
    • Witschi, Robert. Institute of Pharmacology and Toxicology, University of Zurich, Winterthurerstrasse 190, CH-8057, Zurich, Switzerland
    • Hösl, Katharina. Institute for Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nürnberg, Erlangen, Germany
    Type de document
    • Postprint
    Langue
    • Anglais
    Publié dans
    • Journal of Molecular Medicine, 2009, vol. 87, no. 5, p. 465-469. Springer-Verlag
    Autre version électronique
    Identifiant OAI-PMH
    • oai:doc.rero.ch:315248
    Summary
    Agonists at the benzodiazepine-binding site of ionotropic γ-aminobutyric acid (GABAA) receptors are in clinical use as hypnotics, anxiolytics, and anticonvulsants since the early 1960. Analgesic effects of classical benzodiazepines have occasionally been reported in certain subgroups of patients suffering from chronic pain or after spinal delivery through intrathecal catheters. However, these drugs are generally not considered as analgesics but should in fact be avoided in patients with chronic pain. Recent evidence from genetically modified mice now indicates that agents targeting only a subset of benzodiazepine (GABAA) receptors should provide pronounced antihyperalgesic activity against inflammatory and neuropathic pain. Several such compounds have been developed recently, which exhibit significant antihyperalgesia in mice and rats and appear to be devoid of the typical side-effects of classical benzodiazepines