A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination
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The σ-1 receptor is a non-opioid transmembrane protein involved in various human pathologies including neurodegenerative diseases, inflammation, and cancer. The previously published ligand [18F]FTC-146 is among the most promising tools for σ-1 molecular imaging by positron emission tomography (PET), with a potential for application in clinical diagnostics and research. However, the published six- or four-step synthesis of the tosyl ester precursor for its radiosynthesis is complicated and time-consuming. Herein, we present a simple one-step precursor synthesis followed by a one-step fluorine-18 labeling procedure that streamlines the preparation of [18F]FTC-146. Instead of a tosyl-based precursor, we developed a one-step synthesis of the precursor analog AM-16 containing a chloride leaving group for the SN2 reaction with 18F-fluoride. 18F-fluorination of AM-16 led to a moderate decay-corrected radiochemical yield (RCY = 7.5%) with molar activity (Am) of 45.9 GBq/μmol. Further optimization of this procedure should enable routine radiopharmaceutical production of this promising PET tracer.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Labelled Compounds and Radiopharmaceuticals |
Vol/bind | 67 |
Udgave nummer | 2 |
Sider (fra-til) | 59-66 |
ISSN | 0362-4803 |
DOI | |
Status | Udgivet - 2024 |
Bibliografisk note
Funding Information:
This research was funded by the internal grants of the UCT Prague Nos. A2_FPBT_2022_067 and A1_FPBT_2022_007. The authors thank Martin Breza (Slovak Technical University) for a fruitful discussion. The tg‐ArcSwe tissue sections used in this study were kindly provided by Stina Syvänen and Dag Sehlin (Uppsala University).
Publisher Copyright:
© 2024 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.
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