@ARTICLE{Nag20192270,
author={Nag, S. and Krasikova, R. and Airaksinen, A.J. and Arakawa, R. and Petukhovd, M. and Gulyas, B.},
title={Synthesis and biological evaluation of [18F]fluorovinpocetine, a potential PET radioligand for TSPO imaging},
journal={Bioorganic and Medicinal Chemistry Letters},
year={2019},
volume={29},
number={16},
pages={2270-2274},
doi={10.1016/j.bmcl.2019.06.037},
note={cited By 0},
url={https://www.scopus.com/inward/record.uri?eid=2-s2.0-85067891805&doi=10.1016%2fj.bmcl.2019.06.037&partnerID=40&md5=039425a06c8d92bde0fe18f6ade9f6de},
affiliation={Karolinska Institutet, Department of Clinical Neuroscience, Stockholm, Sweden; N.P. Bechtereva Institute of Human Brain Russian Academy of Sciences, St.-Petersburg, Russian Federation; Department of Chemistry – Radiochemistry, University of Helsinki, Finland; Petersburg Nuclear Physics Institute named after B.P. Konstantinov, NRC “Kurchatov Institute”, Gatchina, Russian Federation; Peter the Great St.-Petersburg Polytechnic University, St.-Petersburg, Russian Federation; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore},
abstract={Despite of various PET radioligands targeting the translocator protein TSPO 18-KDa are used for the investigations of neuroinflammatory conditions associated with neurological disorders, development of new TSPO radiotracers is still an active area of the researches with a major focus on the 18F-labelled radiotracers. Here, we report the radiochemical synthesis of [18F]vinpocetine, fluorinated analogue of previously reported TSPO radioligand, [11C]vinpocetine. Radiolabeling was achieved by [18F]fluoroethylation of apovincaminic acid with [18F]fluoroethyl bromide. [18F]vinpocetine was obtained in quantities >2.7 GBq in RCY of 13% (non–decay corrected), and molar activity >60 GBq/µmol within 95 min synthesis time. Preliminary PET studies in a cynomolgus monkey and metabolite studies by HPLC demonstrated similar results by [18F]vinpocetine as for [11C]vinpocetine, including high blood-brain barrier permeability, regional uptake pattern and fast washout from the NHP brain. These results demonstrate that [18F]fluorovinpocetine warrants further evaluation as an easier accessible alternative to [11C]vinpocetine. © 2019 Elsevier Ltd},
author_keywords={Fluorine-18;  Kinetics;  Monkey;  PET;  Radiometabolites;  TSPO radioligands;  Vinpocetine},
correspondence_address1={Nag, S.; Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska HospitalSweden; email: sangram.nag@ki.se},
publisher={Elsevier Ltd},
issn={0960894X},
coden={BMCLE},
pubmed_id={31257082},
language={English},
abbrev_source_title={Bioorg. Med. Chem. Lett.},
document_type={Article},
source={Scopus},
}

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Bechtereva Institute of Human Brain Russian Academy of Sciences, St.-Petersburg, Russian Federation; Department of Chemistry – Radiochemistry, University of Helsinki, Finland; Petersburg Nuclear Physics Institute named after B.P. Konstantinov, NRC “Kurchatov Institute”, Gatchina, Russian Federation; Peter the Great St.-Petersburg Polytechnic University, St.-Petersburg, Russian Federation; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore","abstract":"Despite of various PET radioligands targeting the translocator protein TSPO 18-KDa are used for the investigations of neuroinflammatory conditions associated with neurological disorders, development of new TSPO radiotracers is still an active area of the researches with a major focus on the 18F-labelled radiotracers. Here, we report the radiochemical synthesis of [18F]vinpocetine, fluorinated analogue of previously reported TSPO radioligand, [11C]vinpocetine. Radiolabeling was achieved by [18F]fluoroethylation of apovincaminic acid with [18F]fluoroethyl bromide. [18F]vinpocetine was obtained in quantities >2.7 GBq in RCY of 13% (non–decay corrected), and molar activity >60 GBq/µmol within 95 min synthesis time. Preliminary PET studies in a cynomolgus monkey and metabolite studies by HPLC demonstrated similar results by [18F]vinpocetine as for [11C]vinpocetine, including high blood-brain barrier permeability, regional uptake pattern and fast washout from the NHP brain. 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Konstantinov, NRC “Kurchatov Institute”, Gatchina, Russian Federation; Peter the Great St.-Petersburg Polytechnic University, St.-Petersburg, Russian Federation; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore},\r\nabstract={Despite of various PET radioligands targeting the translocator protein TSPO 18-KDa are used for the investigations of neuroinflammatory conditions associated with neurological disorders, development of new TSPO radiotracers is still an active area of the researches with a major focus on the 18F-labelled radiotracers. Here, we report the radiochemical synthesis of [18F]vinpocetine, fluorinated analogue of previously reported TSPO radioligand, [11C]vinpocetine. Radiolabeling was achieved by [18F]fluoroethylation of apovincaminic acid with [18F]fluoroethyl bromide. [18F]vinpocetine was obtained in quantities >2.7 GBq in RCY of 13% (non–decay corrected), and molar activity >60 GBq/µmol within 95 min synthesis time. Preliminary PET studies in a cynomolgus monkey and metabolite studies by HPLC demonstrated similar results by [18F]vinpocetine as for [11C]vinpocetine, including high blood-brain barrier permeability, regional uptake pattern and fast washout from the NHP brain. These results demonstrate that [18F]fluorovinpocetine warrants further evaluation as an easier accessible alternative to [11C]vinpocetine. © 2019 Elsevier Ltd},\r\nauthor_keywords={Fluorine-18; Kinetics; Monkey; PET; Radiometabolites; TSPO radioligands; Vinpocetine},\r\ncorrespondence_address1={Nag, S.; Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska HospitalSweden; email: sangram.nag@ki.se},\r\npublisher={Elsevier Ltd},\r\nissn={0960894X},\r\ncoden={BMCLE},\r\npubmed_id={31257082},\r\nlanguage={English},\r\nabbrev_source_title={Bioorg. Med. Chem. 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