ArticleMolecular pharmaceutics2014
One-pot two-step radiosynthesis of a new (18)F-labeled thiol reactive prosthetic group and its conjugate for insulinoma imaging.
Article in Molecular pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Comparison of Exendin-4 and Its Single Amino Acid Substitutions as Parent Peptides for GLP-1 Receptor Imaging Probes.Molecules (Basel, Switzerland) · 2025Article
- From molecules to medicine: thiol selective bioconjugation in synthesis of diagnostic and therapeutic radiopharmaceuticals.Theranostics · 2024Review
- Small peptide-based GLP-1R ligands: an approach to reduce the kidney uptake of radiolabeled GLP-1R-targeting agents?EJNMMI radiopharmacy and chemistry · 2021Article
- Distinctive detection of insulinoma using [Scientific reports · 2021Article
- Non-invasive Beta-cell Imaging: Visualization, Quantification, and Beyond.Frontiers in endocrinology · 2021Review
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- Rapid synthesis of maleimide functionalized fluorine-18 labeled prosthetic group using "radio-fluorination on the Sep-Pak" method.Journal of labelled compounds & radiopharmaceuticals · 2018Article
- Radiosynthesis and evaluation of anEJNMMI radiopharmacy and chemistry · 2018Article
- Quinuclidine and DABCO Enhance the Radiofluorinations of 5-Substituted 2-Halopyridines.European journal of organic chemistry · 2017Article
- Review
- Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Low kidney uptake of GLP-1R-targeting, beta cell-specific PET tracer,EJNMMI research · 2016Article
- Facile room temperature synthesis of fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester without azeotropic drying of fluorine-18.Nuclear medicine and biology · 2016Article
- Development & automation of a novel [(18)F]F prosthetic group, 2-[(18)F]-fluoro-3-pyridinecarboxaldehyde, and its application to an amino(oxy)-functionalised Aβ peptide.Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine · 2016Article
- Fluorine-18 radiochemistry, labeling strategies and synthetic routes.Bioconjugate chemistry · 2015Review
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
N-(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethyl)-6-fluoronicotinamide ([(18)F]FNEM), a novel prosthetic agent that is thiol-specific, was synthesized using a one-pot two-step strategy: (1) (18)F incorporation by a nucleophilic displacement of trimethylammonium substrate under mild conditions; (2) amidation of the resulting 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester with N-(2-aminoethyl)maleimide trifluoroacetate salt. The radiosynthesis of the maleimide tracer was completed in 75 min from [(18)F]fluoride with 26 ± 5% decay uncorrected radiochemical yield, and specific activity of 19-88 GBq/μmol (decay uncorrected). The in vitro cell uptake, in vivo biodistribution, and positron emission tomography (PET) imaging properties of its conjugation product with [Cys(40)]-exendin-4 were described. [(18)F]FNEM-Cys(40)-exendin-4 showed specific targeting of glucagon-like peptide 1 receptor (GLP-1R) positive insulinomas and comparable imaging results to our recently reported [(18)F]FPenM-Cys(40)-exendin-4.
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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.