ArticleACS medicinal chemistry letters2014
Synthesis of [(11)C]Bexarotene by Cu-Mediated [(11)C]Carbon Dioxide Fixation and Preliminary PET Imaging.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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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.
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Who cites it
21 citing papers in PubMed, 38 citations in OpenAlex.
- Automated production ofJournal of labelled compounds & radiopharmaceuticals · 2024Article
- Visualizing GABA transporters in vivo: an overview of reported radioligands and future directions.EJNMMI research · 2023Review
- Recent Developments in Carbon-11 Chemistry and Applications for First-In-Human PET Studies.Molecules (Basel, Switzerland) · 2023Review
- Nuclear Receptor Imaging In Vivo-Clinical and Research Advances.Journal of the Endocrine Society · 2023Review
- Teratogenicity and Fetal-Transfer Assessment of the Retinoid X Receptor Agonist Bexarotene.ACS pharmacology & translational science · 2022Article
- Copper-Mediated Late-stage Radiofluorination: Five Years of Impact on Pre-clinical and Clinical PET Imaging.Clinical and translational imaging · 2020Article
- Carbon-11 carboxylation of trialkoxysilane and trimethylsilane derivatives using [Chemical communications (Cambridge, England) · 2020Article
- Copper(I)-MediatedACS omega · 2020Article
- Chemistry for Positron Emission Tomography: Recent Advances inAngewandte Chemie (International ed. in English) · 2019Review
- Recent applications of a single quadrupole mass spectrometer inJournal of fluorine chemistry · 2018Article
- Recent progress in [Journal of labelled compounds & radiopharmaceuticals · 2018Article
- "In-loop" [Journal of labelled compounds & radiopharmaceuticals · 2018Article
- [Carboxyl-ChemMedChem · 2018Article
- [Chemical communications (Cambridge, England) · 2017Article
- New methodologies for the preparation of carbon-11 labeled radiopharmaceuticals.Clinical and translational imaging · 2017Review
- (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.Chemical Society reviews · 2016Review
- A randomized controlled study to evaluate the effect of bexarotene on amyloid-β and apolipoprotein E metabolism in healthy subjects.Alzheimer's & dementia (New York, N. Y.) · 2016Article
- Synthesis of Diverse (11)C-Labeled PET Radiotracers via Direct Incorporation of [(11)C]CO2.Bioconjugate chemistry · 2016Article
- Preclinical PET Neuroimaging of [11C]Bexarotene.Molecular imaging · 2016Article
- Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Bexarotene (Targretin) is a retinoid X receptor (RXR) agonist that has applications for treatment of T cell lymphoma and proposed mechanisms of action in Alzheimer's disease that have been the subject of recent controversy. Carbon-11 labeled bexarotene ([(11)C-carbonyl]4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]benzoic acid) was synthesized using a Cu-mediated cross-coupling reaction employing an arylboronate precursor 1 and [(11)C]carbon dioxide under atmospheric pressure in 15 ± 2% uncorrected radiochemical yield (n = 3), based on [(11)C]CO2. Judicious choice of solvents, catalysts, and additives, as well as precursor concentration and purity of [(11)C]CO2, enabled the preparation of this (11)C-labeled carboxylic acid. Formulated [(11)C]bexarotene was isolated (>37 mCi) with >99% radiochemical purity in 32 min. Preliminary positron emission tomography-magnetic resonance imaging revealed rapid brain uptake in nonhuman primate in the first 75 s following intravenous administration of the radiotracer (specific activity >0.3 Ci/μmol at time of injection), followed by slow clearance (Δ = -43%) over 60 min. Modest uptake (SUVmax = 0.8) was observed in whole brain and regions with high RXR expression.
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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.