Research ArticlePain

A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates

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Science Translational Medicine  29 Aug 2018:
Vol. 10, Issue 456, eaar3483
DOI: 10.1126/scitranslmed.aar3483

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A dual-targeting painkiller

Opioids are among the most effective treatments for severe pain. Their pain-relieving effects are mediated by activation of the mu opioid peptide (MOP) receptor. Unfortunately, selective MOP agonists induce diverse side effects, including respiratory depression, tolerance, hyperalgesia, and dependence. Recently, activation of the nociceptin/orphanin FQ peptide (NOP) receptor has been reported to enhance MOP agonist–induced analgesia without producing side effects. Now, Ding et al. have developed a bifunctional MOP/NOP agonist, called AT-121, that showed potent analgesic effects in nonhuman primates without inducing hyperalgesia, respiratory depression, or dependence. The results suggest that bifunctional MOP/NOP agonists might represent a safe and effective pharmacological tool for treating severe pain.