ArticleBioorganic & medicinal chemistry2014
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 26 citations in OpenAlex.
- Structural factors for receptor binding and activation of the Nociceptin opioid receptor by full and partial agonists.Biochemical pharmacology · 2026Article
- Development of a genetically encoded sensor for probing endogenous nociceptin opioid peptide release.Nature communications · 2024Article
- Development of a genetically encoded sensor for probing endogenous nociceptin opioid peptide release.bioRxiv : the preprint server for biology · 2024Article
- Discovery and structure-activity relationships (SAR) of a novel class of 2-substituted N-piperidinyl indole-based nociceptin opioid receptor ligands.Bioorganic & medicinal chemistry · 2023Article
- Attenuated G protein signaling and minimal receptor phosphorylation as a biochemical signature of low side-effect opioid analgesics.Scientific reports · 2022Article
- Cardiovascular and renal effects of novel nonpeptide nociceptin opioid peptide receptor agonists.British journal of pharmacology · 2022Article
- Structure-Based SAR in the Design of Selective or Bifunctional Nociceptin (NOP) Receptor Agonists.The AAPS journal · 2021Article
- NOP-Related Mechanisms in Substance Use Disorders.Handbook of experimental pharmacology · 2019Article
- A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates.Science translational medicine · 2018Article
- Usefulness of knockout mice to clarify the role of the opioid system in chronic pain.British journal of pharmacology · 2018Review
- Buprenorphine requires concomitant activation of NOP and MOP receptors to reduce cocaine consumption.Addiction biology · 2018Article
- In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403.Pharmacology research & perspectives · 2017Article
- Article
- Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.Journal of medicinal chemistry · 2016Article
- Central N/OFQ-NOP Receptor System in Pain Modulation.Advances in pharmacology (San Diego, Calif.) · 2016Review
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
The nociceptin opioid receptor (NOP) and its endogenous peptide ligand nociceptin/orphanin FQ have been shown to modulate the pharmacological effects of the classical opioid receptor system. Suppression of opioid-induced reward associated with mu-opioid receptor (MOP)-mediated analgesia, without decreasing anti-nociceptive efficacy, can potentially be achieved with NOP agonists having bifunctional agonist activity at MOP, to afford 'non-addicting' analgesics. In Part II of this series, we describe a continuing structure-activity relationship (SAR) study of the NOP-selective piperidin-4-yl-1,3-dihydroindol-2-one scaffold, to obtain bifunctional activity at MOP, and a suitable ratio of NOP/MOP agonist activity that produces a non-addicting analgesic profile. The SAR reported here is focused on the influence of various piperidine nitrogen aromatic substituents on the ratio of binding affinity and intrinsic activity at both the NOP and MOP receptors.
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