ArticleNaunyn-Schmiedeberg's archives of pharmacology2009
Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 66 citations in OpenAlex.
- Design of New Potent, Selective, and Long-Acting NOP Receptor Agonists through Multiple Sequential d-Amino Acid Substitutions of [Arg14 Lys15]N/OFQ(1-15)-NH2.Journal of medicinal chemistry · 2026Article
- Synthesis and Pharmacological Characterization of Nociceptin/Orphanin FQ Dimeric Ligands.Journal of medicinal chemistry · 2025Article
- (L)-Monomethyl Tyrosine (Mmt): New Synthetic Strategy via Bulky 'Forced-Traceless' Regioselective Pd-Catalyzed C(spPharmaceuticals (Basel, Switzerland) · 2023Article
- Synthesis, Biological Activity and Molecular Docking of Chimeric Peptides Targeting Opioid and NOP Receptors.International journal of molecular sciences · 2022Article
- A novel bioassay to detect Nociceptin/Orphanin FQ release from single human polymorphonuclear cells.PloS one · 2022Article
- In Vitro and In Vivo Pharmaco-Toxicological Characterization of 1-Cyclohexyl-x-methoxybenzene Derivatives in Mice: Comparison with Tramadol and PCP.International journal of molecular sciences · 2021Article
- Differential In Vitro Pharmacological Profiles of Structurally Diverse Nociceptin Receptor Agonists in Activating G Protein and Beta-Arrestin Signaling at the Human Nociceptin Opioid Receptor.Molecular pharmacology · 2021Article
- Novel Mixed NOP/Opioid Receptor Peptide Agonists.Journal of medicinal chemistry · 2021Article
- Synthesis and Pharmacological Evaluation of Hybrids Targeting Opioid and Neurokinin Receptors.Molecules (Basel, Switzerland) · 2019Article
- Pharmacological profile of the neuropeptide S receptor: Dynamic mass redistribution studies.Pharmacology research & perspectives · 2018Article
- Article
- In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403.Pharmacology research & perspectives · 2017Article
- A diastereoselective synthesis of Cebranopadol, a novel analgesic showing NOP/mu mixed agonism.Scientific reports · 2017Article
- Structure- and conformation-activity studies of nociceptin/orphanin FQ receptor dimeric ligands.Scientific reports · 2017Article
- Pharmacological studies on the NOP and opioid receptor agonist PWT2-[DmtEuropean journal of pharmacology · 2017Article
- In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations.European journal of pharmacology · 2016Article
- Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist.Pharmacology research & perspectives · 2016Article
- Beta-arrestin 2 rather than G protein efficacy determines the anxiolytic-versus antidepressant-like effects of nociceptin/orphanin FQ receptor ligands.Neuropharmacology · 2016Article
- Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems.Pharmacological reviews · 2016Review
- Article
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In this study, the Galpha(qi5) protein was used to force the human nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor to signal through the Ca(2+) pathway in CHO cells. [Ca(2+)](i) levels were monitored using the fluorometer FlexStation II and the Ca(2+) dye Fluo 4 AM. Concentration response curves were generated with a panel of full and partial agonists, while NOP antagonists were assessed in inhibition-response curves. The following rank order of potency of antagonists was measured: SB - 612111 > J - 113397 = Trap - 101 > or = UFP - 101 > [Nphe1]N/OF Q(1 - 13)NH2 >> naloxone, which is superimposable to literature findings. The rank order of potency of full and partial agonists is also similar to that obtained in previous studies with the exception of a panel of ligands (UFP-112, Ro 64-6198, ZP120, UFP-113) whose potency was relatively low in the Galpha(qi5)-NOP receptor calcium assay. Interestingly, these NOP ligands are characterized by slow kinetic of interaction with the NOP receptor, as demonstrated by bioassay experiments. These results demonstrated that the FlexStation II-Galpha(qi5)-NOP receptor calcium assay represents an adequate and useful screening for NOP receptor ligands, particularly for antagonists.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.