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Pharmacological Assays for Investigating the NOP Receptor

  • Davide Malfacini
  • Girolamo CalóEmail author
Chapter
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 254)

Abstract

The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is a G protein-coupled receptor involved in the regulation of several physiological functions and pathological conditions. Thus, researchers from academia and industry are pursuing NOP to discover and study novel pharmacological entities. In a multidisciplinary effort of pharmacologists, medicinal chemists, and molecular and structural biologists the mechanisms of NOP activation and inhibition have been, at least partially, disentangled. Here, we review the in vitro methodologies employed, which have contributed to our understanding of this target. We hope this chapter guides the reader through the mostly established assay platforms to investigate NOP pharmacology, and gives some hints taking advantage from what has already illuminated the function of other GPCRs. We analyzed the pharmacological results obtained with a large panel of NOP ligands investigated in several assays including receptor binding, stimulation of GTPγS binding, decrease of cAMP levels, calcium flux stimulation via chimeric G proteins, NOP/G protein and NOP/β-arrestin interaction, label-free assays such as dynamic mass redistribution, and bioassays such as the electrically stimulated mouse vas deferens.

Keywords

N/OFQ Pharmacological assays Recombinant and native NOP receptors Signal transduction 

Notes

Acknowledgment

We would like to thank T. Kenakin (Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina) for helpful discussion.

Details of Authors’ Contributions

DM and GC wrote the chapter and approved its final version.

Declaration of Interests

DM and GC have nothing to declare.

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© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.Molecular, Cellular and Pharmacobiology SectionInstitute for Pharmaceutical Biology, University of BonnBonnGermany
  2. 2.Section of Pharmacology, Department of Medical SciencesNational Institute of Neurosciences, University of FerraraFerraraItaly

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