ArticleJournal of labelled compounds & radiopharmaceuticals2015
Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression.
Article in Journal of labelled compounds & radiopharmaceuticals, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 26 citations in OpenAlex.
- Neuroimaging of indoleamine 2,3-dioxygenase 1 (Ido1) in Alzheimer's disease: Development of a novelMaterials today. Bio · 2026Article
- The Role of Small Molecules Containing Fluorine Atoms in Medicine and Imaging Applications.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Trialkylammonium salt degradation: implications for methylation and cross-coupling.Chemical science · 2021Article
- Immune Modulation Therapy and Imaging: Workshop Report.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Article
- Evaluation of Microglial Activation in Multiple Sclerosis Patients Using Positron Emission Tomography.Frontiers in neurology · 2018Review
- Evaluation of radiofluorinated carboximidamides as potential IDO-targeted PET tracers for cancer imaging.Oncotarget · 2017Article
- Molecular Targets for PET Imaging of Activated Microglia: The Current Situation and Future Expectations.International journal of molecular sciences · 2017Review
- Imaging cerebral tryptophan metabolism in brain tumor-associated depression.EJNMMI research · 2015Article
- Molecular imaging correlates of tryptophan metabolism via the kynurenine pathway in human meningiomas.Neuro-oncology · 2015Article
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Authors and funding
3 authors at 1 institution in 1 country.
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Abstract
To synthesize (18) F-labeled positron emission tomography (PET) ligands, reliable labeling techniques inserting (18) F into a target molecule are necessary. The (18) F-fluorobenzene moiety has been widely utilized in the synthesis of (18) F-labeled compounds. The present study utilized [(18) F]-labeled aniline as intermediate in [(18) F]-radiolabeling chemistry for the facile radiosynthesis of 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide ([(18) F]IDO5L) as indoleamine 2,3-dioxygenase 1 (IDO1) targeted tracer. IDO5L is a highly potent inhibitor of IDO1 with low nanomolar IC50 . [(18) F]IDO5L was synthesized via coupling [(18) F]3-chloro-4-fluoroaniline with carboximidamidoyl chloride as a potential PET probe for imaging IDO1 expression. Under the optimized labeling conditions, chemically and radiochemically pure (>98%) [(18) F]IDO5L was obtained with specific radioactivity ranging from 11 to 15 GBq/µmol at the end of synthesis within ~90 min, and the decay-corrected radiochemical yield was 18.2 ± 2.1% (n = 4).
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