Subtype-selective GABAA receptor mimetics—novel antihyperalgesic agents?

Agonists at the benzodiazepine-binding site of ionotropic γ-aminobutyric acid (GABA A ) 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 s...

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Bibliographic Details
Published in:Journal of molecular medicine (Berlin, Germany) Germany), 2009-05, Vol.87 (5), p.465-469
Main Authors: Zeilhofer, Hanns Ulrich, Witschi, Robert, Hösl, Katharina
Format: Article
Language:English
Subjects:
Analgesics - pharmacology
Analgesics - therapeutic use
Animals
Benzodiazepines - pharmacology
Benzodiazepines - therapeutic use
Biological and medical sciences
Biomedical and Life Sciences
Biomedicine
Brain - drug effects
Brain - metabolism
Brain - physiopathology
GABA Agonists - pharmacology
GABA Agonists - therapeutic use
GABA-A Receptor Agonists
General aspects
Human Genetics
Humans
Internal Medicine
Lorazepam
Medical sciences
Molecular Medicine
Neuralgia - physiopathology
Neuralgia - prevention & control
Pain - physiopathology
Pain - prevention & control
Protein Subunits - agonists
Protein Subunits - metabolism
Protein Subunits - physiology
Receptors, GABA-A - metabolism
Receptors, GABA-A - physiology
Review
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Summary:Agonists at the benzodiazepine-binding site of ionotropic γ-aminobutyric acid (GABA A ) 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 (GABA A ) 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.
ISSN:0946-2716
1432-1440
DOI:10.1007/s00109-009-0454-3