Abstract
In our society today, pain has become a main source of strain on most individuals. It is crucial to develop novel treatments against pain while focusing on decreasing their adverse effects. Throughout the extent of development for new pain therapies, the nociceptin/orphanin FQ receptor (NOP receptor) has appeared to be an encouraging focal point. Concentrating on NOP receptor to treat chronic pain with limited range of unwanted effects serves as a suitable alternative to prototypical opioid morphine that could potentially lead to life-threatening effects caused by respiratory depression in overdose, as well as generate abuse and addiction. In addition to these harmful effects, the uprising opioid epidemic is responsible for becoming one of the most disastrous public health issues in the US. In this article, the contributing molecular and cellular structure in controlling the cellular trafficking of NOP receptor and studies that support the role of NOP receptor and its ligands in pain management are reviewed.
Highlights
Persistent pain affects more than 30% of North America’s population throughout their life and it attributes to substantial expense in the US with annual costs ranging between $560 and $635 billion, which is larger than the cost of the nation’s priority health conditions [1].This main socio-economic issue is expected to have a two-fold increase within the 10 years especially in the elderly, as reported by the 2010 Medical Expenditure Panel Survey (MEPS)
The current literature for NOP receptor’s crystal structure, distribution, signaling pathway, and the rational design of NOP receptor ligands with various pharmacological profiles as a promising alternative for conventional opioid analgesic is reviewed to assess its therapeutic potential as analgesics
The rational design of NOP receptor ligands with various pharmacological profiles as a promising alternative for conventional opioid analgesic is discussed
Summary
Persistent pain affects more than 30% of North America’s population throughout their life and it attributes to substantial expense in the US with annual costs ranging between $560 and $635 billion, which is larger than the cost of the nation’s priority health conditions [1]. For this reason, several research institutes have made it a priority to develop safe, effective, and non-addictive therapeutics for chronic pain management and address opioid-use disorders with innovative medications, to save lives and encourage recovery. Several research institutes have made it a priority to develop safe, effective, and non-addictive therapeutics for chronic pain management and address opioid-use disorders with innovative medications, to save lives and encourage recovery Opioids exert their effect via opioid receptors, a member of a large superfamily of seven-transmembrane-spanning (7TM) G-protein-coupled receptors (GPCRs), mu (MOP receptor), kappa (KOP receptor), delta (DOP receptor), and nociceptin (NOP receptor) [10]. The bifunctional and multifunctional NOP/opioid receptor agonists have recently displayed potent antinociceptive activity with favorable side effect profiles Among these agonists, cebranopadol represents a promising therapeutic candidate for pain, according to the results of its clinical trials. The current literature for NOP receptor’s crystal structure, distribution, signaling pathway, and the rational design of NOP receptor ligands with various pharmacological profiles as a promising alternative for conventional opioid analgesic is reviewed to assess its therapeutic potential as analgesics
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