Potential innovative targets in the treatment of pain: Combined μ and NOP receptor agonists

Abstract

Opioid analgesics are potent and widely used medications employed to manage moderate-to-severe acute pain; their utility in the management of chronic inflammatory and neuropathic pain is modest and is beset with adverse effects and concerns related to abuse and addiction. The discovery of the nonclassical opioid, ie, the nociception/orphanin receptor (NOP), has sparked interest into another possible analgesic target. Preclinical studies have demonstrated pain mitigating effects associated with NOP receptor activation while simultaneously reducing conventional μ-opioid-related adverse and euphoric effects. Consequently, agents possessing dual agonism of both μ and NOP receptor activations present an innovative and promising potential target for pain management.