Article (Scientific journals)
Enabling efficient PET imaging of Synaptic Vesicle glycoprotein 2A (SV2A) with a robust and one-step radiosynthesis of a highly potent 18F-labelled ligand ([18F]UCB-H)
Warnier, Corentin; Lemaire, Christian; Becker, Guillaume et al.
2016In Journal of Medicinal Chemistry, 59, p. 8955-8966
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Keywords :
[18F]UCB-H; fluorine-18; 18F; iodonium; SV2A; PET
Abstract :
[en] We herein describe the straightforward synthesis of a stable pyridyl(4- methoxyphenyl)iodonium salt and its [18F]radiolabelling within a one-step, fully automated and cGMP compliant radiosynthesis of [18F]UCB-H ([18F]7), a PET tracer for the imaging of Synaptic Vesicle glycoprotein 2A (SV2A). Over the course of one year, 50 automated productions provided 34±2% of injectable [18F]7 from up to 285 GBq (7.7 Ci) of [18F]fluoride in 50 minutes (uncorrected radiochemical yield. Specific Activity = 815±185 GBq/μmol). The successful implementation of our synthetic strategy within routine, high-activity and cGMP productions attests to its practicality and reliability for the production of large doses of [18F]7. In addition to enabling efficient and cost-effective clinical research on a range of neurological pathologies through the imaging of SV2A, this work further demonstrates the real value of iodonium salts for the cGMP 18F-PET tracer manufacturing industry, and their ability to fulfill practical and regulatory requirements in that field.
Research center :
Giga-CRC In vivo Imaging
Disciplines :
Life sciences: Multidisciplinary, general & others
Author, co-author :
Warnier, Corentin ;  Université de Liège > Centre de recherches du cyclotron
Lemaire, Christian ;  Université de Liège > Centre de recherches du cyclotron
Becker, Guillaume ;  Université de Liège > Centre de recherches du cyclotron
Zaragoza, Guillermo
Giacomelli, Fabrice ;  Université de Liège > Centre de recherches du cyclotron
Aerts, Joël ;  Université de Liège > Centre de recherches du cyclotron
Otabashi, Muhammad
Bahri, Mohamed Ali  ;  Université de Liège > Département de physique > Département de physique
Mercier, Joël
Plenevaux, Alain  ;  Université de Liège > Département de chimie (sciences) > Département de chimie (sciences)
Luxen, André ;  Université de Liège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse
Language :
English
Title :
Enabling efficient PET imaging of Synaptic Vesicle glycoprotein 2A (SV2A) with a robust and one-step radiosynthesis of a highly potent 18F-labelled ligand ([18F]UCB-H)
Publication date :
06 September 2016
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
eISSN :
1520-4804
Publisher :
American Chemical Society, Washington, United States - District of Columbia
Volume :
59
Pages :
8955-8966
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
since 20 September 2016

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