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
Jinsoo HongV W Pike

Abstract

Metabotropic 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. [(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. The 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 occi...Continue Reading

References

Sep 1, 1985·Brain Research Bulletin·W A Banks, A J Kastin
Jul 23, 1999·Progress in Neurobiology·F Bordi, A Ugolini
Dec 20, 2003·Annals of the New York Academy of Sciences·P Jeffrey Conn
Nov 24, 2004·Neuropharmacology·Hilde LavreysenAnne S J Lesage
Jan 25, 2005·Nature Reviews. Drug Discovery·Chad J SwansonDarryle D Schoepp
May 11, 2007·Journal of Medicinal Chemistry·Jeffrey M SchkeryantzMichael P Johnson
May 24, 2007·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Robert B InnisRichard E Carson
Nov 26, 2008·Nuclear Medicine and Biology·Shil Patel, Raymond Gibson
Nov 29, 2008·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Amira K BrownRobert B Innis
Dec 30, 2008·Pharmacological Reviews·Francesco FerragutiFerdinando Nicoletti
Jul 21, 2009·Trends in Pharmacological Sciences·Victor W Pike
Jun 30, 2010·Current Topics in Medicinal Chemistry·Linjing MuSimon M Ametamey
Nov 25, 2011·European Journal of Nuclear Medicine and Molecular Imaging·Tomoteru YamasakiMing-Rong Zhang
Nov 9, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Paolo Zanotti-FregonaraRobert B Innis
Feb 14, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Dean F WongP David Mozley
Jun 28, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Jun ToyoharaKiichi Ishiwata
May 27, 2014·Nuclear Medicine and Biology·F GourandC Halldin
Jan 9, 2015·Journal of the American Chemical Society·Thomas L AndersenTroels Skrydstrup

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Citations

Oct 30, 2019·EJNMMI Radiopharmacy and Chemistry·Carlotta Taddei, Victor W Pike
Mar 10, 2020·Nuclear Medicine and Biology·Jonas ErikssonOleksiy Itsenko
May 28, 2021·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Manabu KubotaMakoto Higuchi

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