Design, Synthesis, and Characterization of Novel, Subtype-Selective Fluorescent Antagonists Targeting the Nociceptin/Orphanin FQ Opioid Peptide Receptor.

George J Farmer, Julie Sanchez, Annabell Millns, Tamzin Antony, Meritxell Canals, J Robert Lane, Shailesh N Mistry

Abstract read

In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0cells of the map it votes in

0citing papers in PubMed

–field-weighted citation impact

1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors.

George J FarmerDivision of Physiology, Pharmacology and Neuroscience, Medical School, School of Life Sciences, University of Nottingham, Nottingham NG7 2UH, U.K.

Julie SanchezDivision of Biomolecular Science and Medicinal Chemistry, School of Pharmacy, University of Nottingham Biodiscovery Institute, University Park, University of Nottingham, Nottingham NG7 2RD, U.K.

Annabell MillnsDivision of Physiology, Pharmacology and Neuroscience, Medical School, School of Life Sciences, University of Nottingham, Nottingham NG7 2UH, U.K.

Tamzin AntonyDivision of Biomolecular Science and Medicinal Chemistry, School of Pharmacy, University of Nottingham Biodiscovery Institute, University Park, University of Nottingham, Nottingham NG7 2RD, U.K.

Meritxell CanalsDivision of Physiology, Pharmacology and Neuroscience, Medical School, School of Life Sciences, University of Nottingham, Nottingham NG7 2UH, U.K.

J Robert LaneDivision of Physiology, Pharmacology and Neuroscience, Medical School, School of Life Sciences, University of Nottingham, Nottingham NG7 2UH, U.K.ORCID 0000-0002-7361-7875

Shailesh N MistryDivision of Biomolecular Science and Medicinal Chemistry, School of Pharmacy, University of Nottingham Biodiscovery Institute, University Park, University of Nottingham, Nottingham NG7 2RD, U.K.ORCID 0000-0002-2252-1689

Funding

Wellcome Trust

6 · The paper itself

Abstract

The nociceptin/orphanin FQ opioid peptide receptor (NOPr) is a member of the opioid receptor family under investigation for the treatment of depression, Parkinson's disease, addiction, and pain. Opioid analgesics such as morphine act through μ-opioid receptor (MOPr) activation but cause MOPr-driven side effects that include respiratory depression, tolerance, addiction, and constipation. Bivalent NOPr/MOPr agonists have been shown to confer effective analgesia with an improved side effect profile. However, the development of new NOPr-targeting drugs is challenged by a paucity of pharmacological tools to characterize NOPr-ligands and visualize receptor expression. We report the design, synthesis, and pharmacological evaluation of the first high affinity small molecule NOPr-targeting fluorescent ligands, based on the antagonist: (2

Indexed as

Drug DesignFluorescent DyesNarcotic AntagonistsReceptors, OpioidAnimalsCHO CellsCricetulusHEK293 CellsHumansLigandsNociceptin ReceptorReceptors, Opioid, muStructure-Activity RelationshipFluorescent DyesLigandsNarcotic AntagonistsNociceptin ReceptorReceptors, OpioidReceptors, Opioid, mu

Identifiers

PMID41474378

DOI10.1021/acs.jmedchem.5c02707

PMCPMC12833874

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Registered trials

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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.