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Review
. 2022 Jan 18;27(3):595.
doi: 10.3390/molecules27030595.

Spotlight on Nociceptin/Orphanin FQ Receptor in the Treatment of Pain

Amal El Daibani  1 , Tao Che  1   2
Affiliations
Review

Spotlight on Nociceptin/Orphanin FQ Receptor in the Treatment of Pain

Amal El Daibani et al. Molecules. .

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.

Keywords: N/OFQ; NOP receptor; analgesia; ligands; nociceptin; nociceptin/orphanin FQ receptor; opioid receptor.

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Conflict of interest statement

The authors have no conflict of interests to declare.

Figures

Figure 1
Figure 1
N/OFQ effect in rodent and non-human primates on pain response. (A) Supraspinal administration of N/OFQ produces hyperalgesia and blocks morphine-induced analgesia in rodent, whereas the opposite effect of analgesia and the promotion of an antinociceptive effect are produced in non-human primates. (B) Spinal administration of N/OFQ produces dose-dependent analgesia in both rodent (nanomoles and higher doses) and non-human primates (nanomoles and ultra-low doses) as well as promotes an antinociceptive effect of morphine, while ultra-low doses of N/OFQ induce hyperalgesia in rodent.
Figure 2
Figure 2
Rational design of new safer analgesics. (A) Beneficiary and side effects produced by MOP receptor activation. (B) Beneficiary (synergizing analgesic effect) and protective (ameliorating typical-opioid side effect profile) effects produced by developing a new compound with simultaneous agonistic activity at NOP receptor and MOP receptor.
Figure 3
Figure 3
Chemical structures and in vitro pharmacological profiles of bifunctional and mixed NOP receptor ligands that target pain [99,110,111,112,113,114,115,116,117,118,119].
See this image and copyright information in PMC

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