ArticlePloS one2017
Radiochemistry on electrodes: Synthesis of an 18F-labelled and in vivo stable COX-2 inhibitor.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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.
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.
Who cites it
16 citing papers in PubMed.
- C-H Labeling with [ACS central science · 2024Review
- Radiotracers for Imaging of Inflammatory Biomarkers TSPO and COX-2 in the Brain and in the Periphery.International journal of molecular sciences · 2023Review
- Concussion: Beyond the Cascade.Cells · 2023Review
- Para-Fluorination of Anilides Using Electrochemically Generated Hypervalent Iodoarenes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Fluorine-18 Labelled Radioligands for PET Imaging of Cyclooxygenase-2.Molecules (Basel, Switzerland) · 2022Review
- Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Review
- Photons or Electrons? A Critical Comparison of Electrochemistry and Photoredox Catalysis for Organic Synthesis.Chemical reviews · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Towards PET imaging of the dynamic phenotypes of microglia.Clinical and experimental immunology · 2021Review
- Closing the gap betweenEJNMMI radiopharmacy and chemistry · 2021Review
- Progress in PET Imaging of Neuroinflammation Targeting COX-2 Enzyme.Molecules (Basel, Switzerland) · 2021Review
- DeuterationRSC advances · 2020Article
- Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET).Molecules (Basel, Switzerland) · 2020Review
- Direct arene C-H fluorination withScience (New York, N.Y.) · 2019Article
- Electrochemical Flash Fluorination and Radiofluorination.ChemElectroChem · 2018Article
- PET Imaging of Microglial Activation-Beyond Targeting TSPO.Molecules (Basel, Switzerland) · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors.
Funding
Abstract
New radiochemistry techniques can yield novel PET tracers for COX-2 and address the shortcomings in in vivo stability and specificity, which have held back clinical translation of tracers to image COX-2 expression. Current techniques limit radiosynthesis to analogs of the COX-2 inhibitors with fluorine-18 added via a carbon chain, or on an aromatic position which renders the radiolabeled analog less specific towards COX-2, resulting in tracers with low in vivo stability or specificity. To solve this problem, we have developed a new high affinity, 18F-labelled COX-2 inhibitor that is radiolabeled directly on a heteroaromatic ring. This molecule exhibits favorable biodistribution and increased metabolic stability. Synthesis of this molecule cannot be achieved by traditional means; consequently, we have developed an automated electrochemical radiosynthesis platform to synthesize up to 5 mCi of radiochemically pure 18F-COX-2ib in 4 hours (2% decay-corrected radiochemical yield). In vitro studies demonstrated clear correlation between COX-2 expression and uptake of the tracer. PET imaging of healthy animals confirmed that the molecule is excreted from blood within an hour, mainly through the hepatobiliary excretion pathway. In vivo metabolism data demonstrated that > 95% of the injected radioactivity remains in the form of the parent molecule 1 hour after injection.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.