Trial reportJournal of nuclear medicine : official publication, Society of Nuclear Medicine2016
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.
Trial report in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed, 36 citations in OpenAlex.
- Test-retest properties of [EJNMMI research · 2025Article
- 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
- Characterization of [Molecular imaging and biology · 2019Article
- Evaluation of a PET Radioligand to ImageJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Innovative Molecular Imaging for Clinical Research, Therapeutic Stratification, and Nosography in Neuroscience.Frontiers in medicine · 2019Review
- Anti-stress neuropharmacological mechanisms and targets for addiction treatment: A translational framework.Neurobiology of stress · 2018Review
- Hypervalent aryliodine compounds as precursors for radiofluorination.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Comparison of two PET radioligands, [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- mGlu1 receptor as a drug target for treatment of substance use disorders: time to gather stones together?Psychopharmacology · 2017Review
- Positron emission tomography in amyotrophic lateral sclerosis: Towards targeting of molecular pathological hallmarks.European journal of nuclear medicine and molecular imaging · 2017Review
- Measuring specific receptor binding of a PET radioligand in human brain without pharmacological blockade: The genomic plot.NeuroImage · 2016Article
- MENGA: A New Comprehensive Tool for the Integration of Neuroimaging Data and the Allen Human Brain Transcriptome Atlas.PloS one · 2016Article
- Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.Current medicinal chemistry · 2016Review
- Spectral Analysis of Dynamic PET Studies: A Review of 20 Years of Method Developments and Applications.Computational and mathematical methods in medicine · 2016Review
- [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
- PET Imaging in Huntington's Disease.Journal of Huntington's disease · 2015Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 3 countries.
Funding
Abstract
unlabelledA recent study from our laboratory found that (18)F-FIMX is an excellent PET radioligand for quantifying metabotropic glutamate receptor 1 (mGluR1) in monkey brain. This study evaluated the ability of (18)F-FIMX to quantify mGluR1 in humans. A second goal was to use the relative density of mGluR1 gene transcripts in brain regions to estimate specific uptake and nondisplaceable uptake (VND) in each brain region.
methodsAfter injection of 189 ± 3 MBq of (18)F-FIMX, 12 healthy volunteers underwent a dynamic PET scan over 120 min. For 6 volunteers, images were acquired until 210 min. A metabolite-corrected arterial input function was measured from the radial artery. Four other subjects underwent whole-body scanning to estimate radiation exposure.
results(18)F-FIMX uptake into the human brain was high (SUV = 4-6 in the cerebellum), peaked at about 10 min, and washed out rapidly. An unconstrained 2-tissue-compartment model fitted the data well, and distribution volume (VT) (mL⋅cm(-3)) values ranged from 1.5 in the caudate to 11 in the cerebellum. A 120-min scan provided stable VT values in all regions except the cerebellum, for which an acquisition time of at least 170 min was necessary. VT values in brain regions correlated well with mGluR1 transcript density, and the correlation suggested that VND of (18)F-FIMX was quite low (0.5 mL⋅cm(-3)). This measure of VND in humans was similar to that from a receptor blocking study in monkeys, after correcting for differences in plasma protein binding. Similar to other (18)F-labeled ligands, the effective dose was about 23 μSv/MBq.
conclusion(18)F-FIMX can quantify mGluR1 in the human brain with a 120- to 170-min scan. Correlation of brain uptake with the relative density of mGluR1 transcript allows specific receptor binding of a radioligand to be quantified without injecting pharmacologic doses of a blocking agent.
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