| Analgesics

Adrenaline Receptors

Addressing a Need

The journal of Science reports findings from researchers accessing chemotypes from a virtual library of over 300 million molecules. The authors of the study “computationally docked each virtual molecule into the highly similar α2BAR binding site, prioritizing those that physically fit and that were chemically unrelated to the known drugs.” The aim was to find a chemical compound to activate the CNS receptor but promote sedation. The researchers synthesized “agonists that produced high concentrations in the brain and reduced the sensation of pain effectively in investigations with animal models.”

The study concluded, “In animal behavioral assays, six of these previously uncharacterized agonists relieved pain behaviors in neuropathic, inflammatory, and acute thermal nociception assays. Gene mutation and reversal of receptor binding with an α2AR antagonist confirmed that analgesia occurred primarily through α2AAR. Crucially, when compared with dexmedetomidine, none of the new compounds caused sedation, even at substantially higher doses than required for pain relief.”


Access the journal article.

Holly Caster