2016
DOI: 10.1371/journal.pone.0156897
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Characterisation of the Novel Mixed Mu-NOP Peptide Ligand Dermorphin-N/OFQ (DeNo)

Abstract: IntroductionOpioid receptors are currently classified as Mu (μ), Delta (δ), Kappa (κ) plus the opioid related nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP). Despite compelling evidence for interactions and benefits of targeting more than one receptor type in producing analgesia, clinical ligands are Mu agonists. In this study we have designed a Mu-NOP agonist named DeNo. The Mu agonist component is provided by dermorphin, a peptide isolated from the skin of Phyllomedusa frogs and the NOP component by t… Show more

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Cited by 29 publications
(49 citation statements)
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“…A more conventional strategy is to use radiolabelled probes. For NOP, this includes [ 3 H]‐N/OFQ (McDonald et al ., ), [ 3 H]‐N/OFQ(1–13)‐NH 2 (Hashiba et al ., ), [ 125 I]‐N/OFQ (Singh et al ., ) and [ 3 H]‐UFP‐101 [(Bird et al ., ); their use is best employed where there is favourable access to tissue or where radioligand specific activity is high (e.g. with 125 I).…”
Section: Discussionmentioning
confidence: 99%
“…A more conventional strategy is to use radiolabelled probes. For NOP, this includes [ 3 H]‐N/OFQ (McDonald et al ., ), [ 3 H]‐N/OFQ(1–13)‐NH 2 (Hashiba et al ., ), [ 125 I]‐N/OFQ (Singh et al ., ) and [ 3 H]‐UFP‐101 [(Bird et al ., ); their use is best employed where there is favourable access to tissue or where radioligand specific activity is high (e.g. with 125 I).…”
Section: Discussionmentioning
confidence: 99%
“…To investigate functional selectivity of ligands that bind to the NOP receptor, we recently developed a BRET-based assay that measures NOP interaction with G protein and b-arrestin 2. This assay was first validated with a large series of standard NOP ligands and used for characterizing the functional selectivity of novel NOP compounds Bird et al 2016;Rizzi et al 2016). We used the BRETbased assay to characterize the functional selectivity of the nonpeptide NOP full agonists for the G-protein or arrestin pathway.…”
Section: Discussionmentioning
confidence: 99%
“…Radioactivity was determined following an 8 h extraction of filters in ScintiSafe Gel using liquid scintillation spectroscopy (Bird et al. ).…”
Section: Methodsmentioning
confidence: 99%
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“…The BRET assay used to investigate the ability of [Dmt 1 ]N/OFQ(1-13)-NH 2 and PWT2-[Dmt 1 ] to promote receptor interaction with G protein and β-arrestin 2 has been previously validated for classical opioid (Molinari et al, 2010) as well as NOP receptors (Malfacini et al, 2015) and then used for characterizing novel ligands (Asth et al, 2016; Bird et al, 2016; Rizzi et al, 2016) or for selecting the best compounds for inducing receptor stability and crystallogenesis (Miller et al, 2015). In line with previous findings (Malfacini et al, 2015; Rizzi et al, 2016), the standard peptides N/OFQ and dermorphin behaved as potent and selective agonists in promoting receptor interaction both with G protein and β-arrestin 2.…”
Section: Discussionmentioning
confidence: 99%