ArticleJournal of medicinal chemistry2014
Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4).
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
- Test-retest properties of [EJNMMI research · 2025Article
- Advances and Insights in Positron Emission Tomography Tracers for Metabotropic Glutamate Receptor 4 Imaging.Journal of medicinal chemistry · 2024Review
- Fully Automated Radiosynthesis of [iRadiology · 2023Article
- Detailed radiosynthesis of [Journal of labelled compounds & radiopharmaceuticals · 2023Article
- Design, Synthesis, and Characterization of Benzimidazole Derivatives as Positron Emission Tomography Imaging Ligands for Metabotropic Glutamate Receptor 2.Journal of medicinal chemistry · 2020Article
- A Review of Molecular Imaging of Glutamate Receptors.Molecules (Basel, Switzerland) · 2020Review
- Synthesis and Characterization of Fluorine-18-LabeledJournal of medicinal chemistry · 2020Article
- Improved Synthesis of the Thiophenol PrecursorTetrahedron · 2019Article
- Characterization of [Molecular imaging and biology · 2019Article
- Unprecedented selective homogeneous cobalt-catalysed reductive alkoxylation of cyclic imides under mild conditions.Chemical science · 2017Article
- Synthesis and evaluation of N-(methylthiophenyl)picolinamide derivatives as PET radioligands for metabotropic glutamate receptor subtype 4.Bioorganic & medicinal chemistry letters · 2016Article
- Co-operative binding assay for the characterization of mGlu4 allosteric modulators.Neuropharmacology · 2015Article
- Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.Bioorganic & medicinal chemistry letters · 2015Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Four 4-phthalimide derivatives of N-(3-chlorophenyl)-2-picolinamide were synthesized as potential ligands for the PET imaging of mGlu4 in the brain. Of these compounds, N-(3-chloro-4-(4-fluoro-1,3-dioxoisoindolin-2-yl)phenyl)-2-picolinamide (3, KALB001) exhibited improved binding affinity (IC50 = 5.1 nM) compared with ML128 (1) and was subsequently labeled with (18)F. When finally formulated in 0.1 M citrate buffer (pH 4) with 10% ethanol, the specific activity of [(18)F]3 at the end of synthesis (EOS) was 233.5 ± 177.8 GBq/μmol (n = 4). The radiochemical yield of [(18)F]3 was 16.4 ± 4.8% (n = 4), and the purity was over 98%. In vivo imaging studies in a monkey showed that the radiotracer quickly penetrated the brain with the highest accumulation in the brain areas known to express mGlu4. Despite some unfavorable radiotracer properties like fast washout in rodent studies, [(18)F]3 is the first (18)F-labeled mGlu4 radioligand, which can be further modified to improve pharmacokinetics and brain penetrability for future human studies.
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