Title:GABA<sub>A</sub> Receptors as Targets for the Management of Pain-related Disorders: Historical Perspective and Update
VOLUME: 16 ISSUE: 6
Author(s):Bradford D. Fischer*
Affiliation:Cooper Medical School of Rowan University, Camden, NJ
Keywords:Antihyperalgesic, benzodiazepine, drug development, disorders, GABAA, pain.
Abstract:Background: Chronic pain is treated most commonly with opioid analgesics, anti-inflammatory
steroids and nonsteroidal anti-inflammatory drugs.
Method: However, these compounds are not uniformly effective and their clinical use is constrained by
unwanted side effects. 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.
Results: Recent evidence suggests that by targeting specific benzodiazepine-sensitive GABA
A 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.
Conclusion: The present review provides an overview of the GABA
A receptor subtypes involved in
pain transmission as well as implications for the development of analgesic medications.
