Evidence map›Paper›PMID 33448685›Full record

ArticleChemMedChem2020

Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline-Based κ-Opioid Receptor (KOR) Agonists Designed for PET Studies.

Giovanni Tangherlini, Frederik Börgel, Dirk Schepmann, Samuel Slocum, Tao Che, Stefan Wagner, Katrin Schwegmann, Sven Hermann, Nadine Mykicki, Karin Loser and 1 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.6field-weighted citation impact, top 38% of its field
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

4 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Review
  3. Evaluation of Specific Binding of [ACS medicinal chemistry letters · 2021
    Article
  4. Article
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

11 authors at 4 institutions in 2 countries.

Giovanni TangherliniInstitut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, 48149, Münster, Germany.
Frederik BörgelInstitut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, 48149, Münster, Germany.
Dirk SchepmannInstitut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, 48149, Münster, Germany.
Samuel SlocumDepartment of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC 27599, USA.
Tao CheDepartment of Anesthesiology, Washington University School of Medicine, 660 S. Euclid Ave., St. Louis, MO 63110, USA.
Stefan WagnerDepartment of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, 48149, Münster, Germany.
Katrin SchwegmannEuropean Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstraße 15, 48149, Münster, Germany.
Sven HermannEuropean Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstraße 15, 48149, Münster, Germany.
Nadine MykickiDepartment of Dermatology, University of Münster, von-Esmarch-Str. 58, 48149, Münster, Germany.
Karin LoserCells-in-Motion Cluster of Excellence (EXC 1003-CiM), Westfälische Wilhelms-Universität Münster, 48149, Münster, Germany.
Bernhard WünschInstitut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, 48149, Münster, Germany.ORCID 0000-0002-9030-8417
University of Münster · DEUniversity Hospital Münster · DEUniversity of North Carolina at Chapel Hill · USWashington University in St. Louis · US

Funding

Structure-Function of Opioid ReceptorsP01DA035764 · NIDA · UNIVERSITY OF SOUTHERN CALIFORNIA · PI ROTH, BRYAN L., STEVENS, RAYMOND C · 2014 to 2018
$7.1M
NIDA NIH HHS P01 DA035764
6 · The paper itself

Abstract

κ-Opioid receptors (KORs) play a predominant role in pain alleviation, itching skin diseases, depression and neurodegenerative disorders such as multiple sclerosis. Therefore, imaging of KOR by a fluorinated PET tracer was envisaged. Two strategies were followed to introduce a F atom into the very potent class of cis,trans-configured perhydroquinoxalines. Whereas the synthesis of fluoroethyltriazole 2 has already been reported, fluoropyrrolidines 14 (1-[2-(3,4-dichlorophenyl)acetyl]-8-[(R)-3-fluoropyrrolidin-1-yl]-perhydroquinoxalines) were prepared by S

Indexed as

AnimalsAnti-Inflammatory Agents, Non-SteroidalBrainCells, CulturedCytokinesFluorine RadioisotopesGuinea PigsHalogenationHumansMiceMice, Inbred C57BLPositron-Emission TomographyQuinoxalinesRadiopharmaceuticalsReceptors, Opioid, kappaAnti-Inflammatory Agents, Non-SteroidalCytokinesFluorine-18Fluorine RadioisotopesQuinoxalinesRadiopharmaceuticalsReceptors, Opioid, kappaanti-inflammatory activityeffector cellsfluorineopioid receptor agonistsperhydroquinoxalinePET tracers

Identifiers

PMID33448685
PMCPMC7589326
OpenAlexW3045584327

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.