PMID: 28530834DOI: 10.1021/acs.jmedchem.7b00432May 23, 2017Paper
A Facile Radiolabeling of [18 F]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation
Journal of Medicinal Chemistry
Lu WangSteven H Liang
Abstract
A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a 18F-ligand, [18F]2 ([18F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [18F]2 demonstrated saturable specific binding to TSPO, substantially elevated brain uptake, and slow washout of bound PET signal in the preclinical models of brain neuroinflammation (cerebral ischemia and Alzheimer's disease).
References
Oct 16, 2002·Glia·Richard B Banati
Jul 23, 2003·Current Medicinal Chemistry·Sylvaine GalieguePierre Casellas
Jan 4, 2005·NeuroImage·Alexander GerhardRichard B Banati
Jul 11, 2006·Trends in Pharmacological Sciences·Vassilios PapadopoulosMoshe Gavish
Apr 17, 2008·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Michelle L JamesMichael Kassiou
Oct 2, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Fabien ChauveauBertrand Tavitian
Nov 26, 2008·Nuclear Medicine and Biology·Shil Patel, Raymond Gibson
Feb 19, 2009·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Fabien ChauveauBertrand Tavitian
Feb 23, 2010·Synapse·Joji YuiMing-Rong Zhang
Molecular imaging of inflammation/infection: nuclear medicine and optical imaging agents and methods
Apr 27, 2010·Chemical Reviews·A SignoreR A Dierckx
Aug 14, 2010·NeuroImage·Joji YuiMing-Rong Zhang
Dec 2, 2010·Nature Reviews. Drug Discovery·Rainer RupprechtMichael Schumacher
Dec 18, 2010·Stroke; a Journal of Cerebral Circulation·Alexander Thiel, Wolf-Dieter Heiss
Feb 25, 2011·Current Alzheimer Research·M T Ferretti, A C Cuello
Dec 17, 2011·Nuclear Medicine and Biology·Nicolas ArlicotDenis Guilloteau
Jan 17, 2012·Bioorganic & Medicinal Chemistry Letters·Harry WadsworthWilliam Trigg
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand
Oct 16, 2012·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Marie-Anne PeyronneauHéric Valette
Jan 10, 2013·PloS One·Philippe CorciaMaria-Joao Ribeiro
Mar 26, 2013·Journal of Medicinal Chemistry·Dewei TangH Charles Manning
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Annelaure DamontFrédéric Dollé
Feb 4, 2014·Journal of Neurochemistry·Anjani K TiwariMing-Rong Zhang
Jun 19, 2014·Current Pharmaceutical Design·Dieter OryGuy Bormans
Jul 10, 2014·EJNMMI Research·Maria-Joao RibeiroDenis Guilloteau
Jul 10, 2014·Nature Communications·Benjamin H RotsteinSteven H Liang
Jan 24, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Annelaure DamontFrédéric Dollé
Feb 5, 2015·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Sandeep S V GollaJuha O Rinne
Feb 7, 2015·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Nickeisha A StephensonNeil Vasdev
Mar 21, 2015·Lancet Neurology·Michael T HenekaMarkus P Kummer
Aug 27, 2015·Angewandte Chemie·Lu WangSteven H Liang
Nov 10, 2015·Biochemical Society Transactions·Federico E TurkheimerMattia Veronese
Nov 27, 2015·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Bin LiuCynthia A Lemere
Mar 18, 2016·ACS Chemical Neuroscience·Daniel Strakis AlbrechtMarco L Loggia
Aug 6, 2016·Angewandte Chemie·Hang ShiTobias Ritter
Aug 20, 2016·Chemical Science·Benjamin H RotsteinSteven H Liang
Jan 14, 2017·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Thomas KellerOlof Solin
❮ Previous
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Citations
Oct 7, 2017·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Chongzhao RanAnna Moore
Jun 4, 2018·Human Molecular Genetics·Danielle A SimmonsFrank M Longo
Mar 16, 2019·Nuclear Medicine Communications·He ZhangDengfeng Cheng
Jan 12, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Tamara BerdyyevaAnna Katrin Szardenings
Apr 14, 2019·Nature Protocols·Steven H LiangNeil Vasdev
May 31, 2019·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Thomas KellerOlof Solin
Sep 13, 2018·Organic & Biomolecular Chemistry·Masayuki FujinagaMing-Rong Zhang
Sep 10, 2020·Adipocyte·Na NiuLi Huo
Oct 6, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Victor W Pike
Jul 29, 2018·Angewandte Chemie·Xiaoyun DengSteven H Liang
Jan 3, 2020·Journal of Labelled Compounds & Radiopharmaceuticals·Lu WangSteven H Liang
Aug 16, 2017·Scientific Reports·Jing YangChongzhao Ran
Oct 31, 2020·Scientific Reports·Tiantian MouXiang Li
Sep 1, 2018·Bioorganic & Medicinal Chemistry·Katsushi KumataMing-Rong Zhang
Mar 2, 2021·Acta Pharmaceutica Sinica. B·Lingling ZhangSteven H Liang
Mar 6, 2018·European Journal of Medicinal Chemistry·Dewei TangMing-Rong Zhang
Dec 30, 2017·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Vadim Bernard-GauthierRalf Schirrmacher
Preclinical and clinical study on [18F]DRKXH1: a novel β-amyloid PET tracer for Alzheimer's disease.
Jul 23, 2021·European Journal of Nuclear Medicine and Molecular Imaging·MiaoMiao XuHui Wang
Jul 11, 2021·European Journal of Nuclear Medicine and Molecular Imaging·Nadja Van CampHervé Boutin
Feb 27, 2018·Journal of Medicinal Chemistry·Ran ChengSteven H Liang
Sep 21, 2021·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Francisco R López-PicónOlof Solin
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