Evidence map›Paper›PMID 26320813›Full record

ArticleNuclear medicine and biology2015

[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.

Jinsoo Hong, Shuiyu Lu, Rong Xu, Jeih-San Liow, Alicia E Woock, Kimberly J Jenko, Robert L Gladding, Sami S Zoghbi, Robert B Innis, Victor W Pike

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Nuclear medicine and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 40% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 14 citations in OpenAlex.

  1. Dynamic alterations in the central glutamatergic status following food and glucose intake:Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021
    Trial
  2. PET ligands [Science translational medicine · 2020
    Article
  3. [EJNMMI radiopharmacy and chemistry · 2019
    Review
  4. Article
  5. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 2 institutions in 1 country.

Jinsoo HongMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Shuiyu LuMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Rong XuMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Jeih-San LiowMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Alicia E WoockMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Kimberly J JenkoMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Robert L GladdingMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Sami S ZoghbiMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Robert B InnisMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States.
Victor W PikeMolecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, MD, 20892-1003, United States. Electronic address: pikev@mail.nih.gov.
National Institute of Mental Health · USNational Institutes of Health · US

Funding

PET Radiopharmaceutical SciencesZIAMH002793 · NIMH · NATIONAL INSTITUTE OF MENTAL HEALTH · PI PIKE, VICTOR W · 2009 to 2025
$69.8M
Translational Evaluation Of PET RadiotracersZIAMH002795 · NIMH · NATIONAL INSTITUTE OF MENTAL HEALTH · PI INNIS, ROBERT · 2009 to 2025
$32.0M
Intramural NIH HHS ZIA MH002793
6 · The paper itself

Abstract

introductionMetabotropic glutamate subtype receptor 1 (mGluR1) is implicated in several neuropsychiatric disorders and is a target for drug development. [(18)F]FIMX ([(18)F]4-fluoro--N-methyl-N--(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide) is an effective radioligand for imaging brain mGluR1 with PET. A similarly effective radioligand with a shorter half-life would usefully allow PET studies of mGluR1 at baseline and after pharmacological or other challenge on the same day. Here we describe the preparation of [(11)C]FIMX for evaluation in monkey with PET.

methods[(11)C]FIMX was prepared via Pd-promoted carbonylation of 1-fluoro-4-iodobenzene with [(11)C]carbon monoxide, aminolysis of the [(11)C]acyl-palladium complex with the requisite Boc-protected amine, and deprotection with HCl in THF. PET scans of [(11)C]FIMX injected into a monkey were performed at baseline and after preblock of mGluR1 with measurement of the arterial input function.

resultsThe radiosynthesis required 42 min and gave [(11)C]FIMX in about 5% overall decay-corrected radiochemical yield and with a specific activity of about 100 GBq/μmol. PET in rhesus monkey at baseline showed that radioactivity peaked high in receptor-rich cerebellum and much lower in receptor-poor occipital cortex. Radioactivity in cerebellum declined to 32% of peak at 85 min. VT at baseline appeared stable in all brain regions after 60 min. Under mGluR1 pre-blocked condition, radioactivity uptake in all regions declined more rapidly to a low level. Receptor pre-block reduced VT from 13.0 to 1.5 in cerebellum and from 2.9 to 1.4 in occipital cortex.

conclusion[(11)C]FIMX is an effective radioligand for imaging mGluR1 in monkey with PET.

Indexed as

AnimalsBenzamidesBrainCarbon RadioisotopesDrug Evaluation, PreclinicalImage Processing, Computer-AssistedMacaca mulattaPositron-Emission TomographyRadiochemistryRadiopharmaceuticalsReceptors, Metabotropic GlutamateThiazoles4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamideBenzamidesCarbon Radioisotopesmetabotropic glutamate receptor type 1RadiopharmaceuticalsReceptors, Metabotropic GlutamateThiazolesBrainCarbon-11mGluR1MonkeyPETRadioligand

Identifiers

PMID26320813
PMCPMC4658304
OpenAlexW939892842

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.