ArticleJournal of medicinal chemistry2013
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 33 citations in OpenAlex.
- The PET Radioligand 18F-FIMX Images and Quantifies Metabotropic Glutamate Receptor 1 in Proportion to the Regional Density of Its Gene Transcript in Human Brain.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2016Trial
- Genetically modified non-human primate models for research on neurodegenerative diseases.Zoological research · 2024Review
- Novel PET Biomarkers to Disentangle Molecular Pathways across Age-Related Neurodegenerative Diseases.Cells · 2020Review
- Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development.European journal of nuclear medicine and molecular imaging · 2020Review
- [EJNMMI radiopharmacy and chemistry · 2019Review
- Hypervalent aryliodine compounds as precursors for radiofluorination.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Crystal Structures of Diaryliodonium Fluorides and Their Implications for Fluorination Mechanisms.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Measuring specific receptor binding of a PET radioligand in human brain without pharmacological blockade: The genomic plot.NeuroImage · 2016Article
- Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.Current medicinal chemistry · 2016Review
- Synthesis and evaluation of N-(methylthiophenyl)picolinamide derivatives as PET radioligands for metabotropic glutamate receptor subtype 4.Bioorganic & medicinal chemistry letters · 2016Article
- [carbonyl-11C]4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([11C]FIMX) is an effective radioligand for PET imaging of metabotropic glutamate receptor 1 (mGluR1) in monkey brain.Nuclear medicine and biology · 2015Article
- Development of PET and SPECT probes for glutamate receptors.TheScientificWorldJournal · 2015Review
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
We sought to develop a PET radioligand that would be useful for imaging human brain metabotropic subtype 1 receptors (mGluR1) in neuropsychiatric disorders and in drug development. 4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide (FIMX, 11) was identified as having favorable properties for development as a PET radioligand. We developed a method for preparing [(18)F]11 in useful radiochemical yield and in high specific activity from [(18)F]fluoride ion and an N-Boc-protected (phenyl)aryliodonium salt precursor (15). In baseline experiments in rhesus monkey, [(18)F]11 gave high brain radioactivity uptake, reflecting the expected distribution of mGluR1 with notably high uptake in cerebellum, which became 47% lower by 120 min after radioligand injection. Pharmacological challenges demonstrated that a very high proportion of the radioactivity in monkey brain was bound specifically and reversibly to mGluR1. [(18)F]11 is concluded to be an effective PET radioligand for imaging mGluR1 in monkey brain and therefore merits further evaluation in human subjects.
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