Evidence map›Paper›PMID 27546294›Full record

ArticleBioorganic & medicinal chemistry letters2016

Radiosynthesis and preliminary PET evaluation of (18)F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors.

Gengyang Yuan, Graham B Jones, Neil Vasdev, Steven H Liang

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Preclinical Evaluation of [Molecular imaging and biology · 2026
    Article
  2. First-in-Human Study ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2025
    Article
  3. Article
  4. Synthesis and evaluation of 6-(Bioorganic & medicinal chemistry letters · 2020
    Article
  5. Article
  6. Chemistry for Positron Emission Tomography: Recent Advances inAngewandte Chemie (International ed. in English) · 2019
    Review
  7. Review
  8. Synthesis, pharmacology and preclinical evaluation ofEuropean journal of medicinal chemistry · 2018
    Article
  9. Hypervalent aryliodine compounds as precursors for radiofluorination.Journal of labelled compounds & radiopharmaceuticals · 2018
    Review
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

4 authors.

Gengyang YuanDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Ave., Boston, MA 02115, USA; Gordon Center for Medical Imaging & Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital and Department of Radiology, Harvard Medical School, 55 Fruit St., Boston, MA 02114, USA.
Graham B JonesDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Ave., Boston, MA 02115, USA.
Neil VasdevGordon Center for Medical Imaging & Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital and Department of Radiology, Harvard Medical School, 55 Fruit St., Boston, MA 02114, USA. Electronic address: vasdev.neil@mgh.harvard.edu.
Steven H LiangGordon Center for Medical Imaging & Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital and Department of Radiology, Harvard Medical School, 55 Fruit St., Boston, MA 02114, USA. Electronic address: liang.steven@mgh.harvard.edu.

Funding

New PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927k
NIDA NIH HHS K01 DA038000
6 · The paper itself

Abstract

To prompt the development of (18)F-labeled positron emission tomography (PET) tracers for the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, we have prepared (18)F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile ([(18)F]8). The radiosynthesis was achieved by a one-pot two-step method that utilized a spirocyclic hypervalent iodine(III) mediated radiofluorination to prepare the (18)F-labeled 1-bromo-3-fluorobenzene ([(18)F]15) intermediate with K(18)F. A subsequent copper(I) iodide mediated coupling reaction was carried out with 2-(2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile (10) to [(18)F]8 in 10±2% uncorrected radiochemical yield relative to starting (18)F-fluoride with >99% radiochemical purity and 29.6±7.4Gbq/μmol specific activity at the time of injection. PET imaging studies with the title radiotracer in normal mice demonstrated good brain uptake (peak standardized uptake value (SUV)=2.3±0.1) and warrants further in vivo validation.

Indexed as

AnimalsBlood-Brain BarrierBrainFluorine RadioisotopesMicePositron-Emission TomographyReceptors, AMPAFluorine RadioisotopesReceptors, AMPAAMPA receptorFluorine-18PerampanelPositron emission tomographyRadiotracer

Identifiers

PMID27546294
PMCPMC5018461

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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.