ArticleBritish journal of pharmacology2014
In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives.
Article in British journal of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 33 citations in OpenAlex.
- 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
- Review
- A Novel Multi-Target Mu/Delta Opioid Receptor Agonist, HAGD, Produced Potent Peripheral Antinociception with Limited Side Effects in Mice and Minimal Impact on Human Sperm Motility In Vitro.Molecules (Basel, Switzerland) · 2023Article
- Formulation of Solid Lipid Nanoparticles Loaded with Nociceptin/Orphanin FQ (N/OFQ) and Characterization in a Murine Model of Airway Hyperresponsiveness.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Spotlight on Nociceptin/Orphanin FQ Receptor in the Treatment of Pain.Molecules (Basel, Switzerland) · 2022Review
- Nociceptin/Orphanin FQ Peptide Receptor-Related Ligands as Novel Analgesics.Current topics in medicinal chemistry · 2020Review
- Pharmacological profile of the neuropeptide S receptor: Dynamic mass redistribution studies.Pharmacology research & perspectives · 2018Article
- Article
- Pharmacological studies on the NOP and opioid receptor agonist PWT2-[DmtEuropean journal of pharmacology · 2017Article
- Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist.Pharmacology research & perspectives · 2016Article
- Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems.Pharmacological reviews · 2016Review
- Article
- Central N/OFQ-NOP Receptor System in Pain Modulation.Advances in pharmacology (San Diego, Calif.) · 2016Review
- Spinal antinociceptive effects of the novel NOP receptor agonist PWT2-nociceptin/orphanin FQ in mice and monkeys.British journal of pharmacology · 2015Article
- In vitro and in vivo pharmacological characterization of a neuropeptide S tetrabranched derivative.Pharmacology research & perspectives · 2015Article
- Pharmacological Profile of Nociceptin/Orphanin FQ Receptors Interacting with G-Proteins and β-Arrestins 2.PloS one · 2015Article
- Pharmacological characterization of tachykinin tetrabranched derivatives.British journal of pharmacology · 2014Article
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Authors and funding
11 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeAn innovative chemical approach, named peptide welding technology (PWT), allows the synthesis of multibranched peptides with extraordinary high yield, purity and reproducibility. With this approach, three different tetrabranched derivatives of nociceptin/orphanin FQ (N/OFQ) have been synthesized and named PWT1-N/OFQ, PWT2-N/OFQ and PWT3-N/OFQ. In the present study we investigated the in vitro and in vivo pharmacological profile of PWT N/OFQ derivatives and compared their actions with those of the naturally occurring peptide. EXPERIMENTAL APPROACH: The following in vitro assays were used: receptor and [(35)S]-GTPγS binding, calcium mobilization in cells expressing the human N/OFQ peptide (NOP) receptor, or classical opioid receptors and chimeric G proteins, electrically stimulated mouse vas deferens bioassay. In vivo experiments were performed; locomotor activity was measured in normal mice and in animals with the NOP receptor gene knocked out [NOP(-/-)]. KEY
resultsIn vitro PWT derivatives of N/OFQ behaved as high affinity potent and rather selective full agonists at human recombinant and animal native NOP receptors. In vivo PWT derivatives mimicked the inhibitory effects exerted by the natural peptide on locomotor activity showing 40-fold higher potency and extremely longer lasting action. The effects of PWT2-N/OFQ were no longer evident in NOP(-/-) mice. CONCLUSIONS AND IMPLICATIONS: The results showed that the PWT can be successfully applied to the peptide sequence of N/OFQ to generate tetrabranched derivatives characterized by a pharmacological profile similar to the native peptide and associated with a higher potency and marked prolongation of action in vivo.
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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.