Abstract
The nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor is the fourth and most recently discovered member of the opioid receptor superfamily that also includes μ, δ, and κ opioid receptor subtypes (MOR, DOR, and KOR, respectively). The widespread anatomic distribution of the NOP receptor enables the modulation of several physiologic processes by its endogenous agonist, N/OFQ. Accordingly, the NOP receptor has gained a lot of attention as a potential target for the development of ligands with therapeutic use in several pathophysiological states. NOP receptor activation frequently results in effects opposing classic opioid receptor action; therefore, regulation of the NOP receptor and conditions affecting its modulatory tone are important to understand. Mounting evidence reveals a heterologous interaction of the NOP receptor with other G protein–coupled receptors, including MOR, DOR, and KOR, which may subsequently influence their function. Our focus in this review is to summarize and discuss the findings that delineate the cellular mechanisms of NOP receptor signaling and regulation and the regulation of other receptors by N/OFQ and the NOP receptor.
Footnotes
- Received December 20, 2012.
- Accepted February 8, 2013.
This work was supported by the Oklahoma Center for the Advancement of Science and Technology’s OHRS Award [Project HR08-152]; the National Institutes of Health National Institute on Drug Abuse [Grant R01-DA017380]; and the Department of the Army [DMRDP W81XWH-11-2-0077].
The information and interpretations included in this article do not necessarily reflect the position or the policy of the Government, and no official endorsement should be inferred.
↵1Current affiliation: Medtronic Neuromodulation, Minneapolis, Minnesota.
- U.S. Government work not protected by U.S. copyright.
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In this issue
Cellular Mechanisms of NOP Receptor Regulation
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- Article
- Abstract
- Introduction
- NOP Receptor Signaling
- Homologous NOP Receptor Desensitization
- Heterologous Regulation of the NOP Receptor
- Heterologous Regulation by N/OFQ
- Heterodimerization
- NOP Receptor Function, Pain, and Inflammatory Response: The Role of NOP Receptor Regulation
- Conclusion
- Authorship Contributions
- Footnotes
- Abbreviations
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