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GABA-A receptor subtypes: Implications for the treatment of pain.

GABA-A receptor subtypes: Implications for the treatment of pain.
Author Information (click to view)

Fischer BD,


Fischer BD, (click to view)

Fischer BD,

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CNS & neurological disorders drug targets 2017 02 07() doi 10.2174/1871527316666170207155149
Abstract

Chronic severe pain is treated most successfully with opioid analgesics, although the clinical use of these drugs is constrained by unwanted side effects, including the potential for abuse. GABAergic neurons are located in spinal nociceptive circuits suggesting that drugs with affinity at these receptors, including benzodiazepine-like drugs, may provide an alternative to opioids for the treatment of pain. However, systemically administered conventional benzodiazepines fail to produce antihyperalgesic effects, likely due to their concurrent sedative properties. Recent evidence suggests that by targeting specific benzodiazepine-sensitive GABAA receptor subtypes, the sedative properties of benzodiazepines can be circumvented and these compounds may be useful alternatives to opioids for the treatment of chronic pain. In this commentary, we provide an overview of the GABAA receptor subtypes related to these effects, and also discuss the implications that this development may have for the abuse potential of analgesic medications.

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