GABAAReceptors as Targets for the Management of Pain-related Disorders: Historical Perspective and Update.
BACKGROUND
Chronic pain is treated most commonly with opioid analgesics, anti-inflammatory steroids and nonsteroidal anti-inflammatory drugs.


METHODS
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 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.


CONCLUSIONS
The present review provides an overview of the GABAA; receptor subtypes involved in pain transmission as well as implications for the development of analgesic medications.
Cooper Medical School of Rowan University, Camden, NJ. United States.
Bradford D
BD
Fischer
D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D006801:Humans; D010146:Pain / Q000188:drug therapy*; D011963:Receptors, GABA-A / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000700:Analgesics; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid
Antihyperalgesic; GABAA; benzodiazepine; disorders; drug development; pain