ARTICLE | Distillery Therapeutics

Therapeutics: κ opioid receptor (KOR; OPRK1); μ opioid receptor (MOR; OPRM1)

January 15, 2015 8:00 AM UTC

In vitro and rat studies identified salvinorin A analogues that could treat addiction without sedative side effects. In cell-based assays, analogs of the natural KOR agonist salvinorin A with small substitutions in the furan ring had agonist activity comparable to the parent compound and 250-fold selectivity for KOR over MOR. In a rat model of cocaine addiction, intraperitoneal administration of the analogs decreased cocaine-seeking behavior without sedative side effects. Next steps could include additional studies to evaluate the side effects and efficacy of novel KOR agonists in vivo.

Mundipharma International Ltd., Purdue Pharma L.P. and Shionogi & Co. Ltd. market the KOR and MOR agonist Targin oxycodone/naloxone to pain. Munipharma and Purdue also market the compound to treat restless leg syndrome. ...