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.

Original languageEnglish
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume67
Issue number2
Pages (from-to)59-66
ISSN0362-4803
DOIs
Publication statusPublished - 2024

Bibliographical note

Publisher Copyright:
© 2024 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.

    Research areas

  • chloride leaving group, fluorine-18, FTC-146, non-activated, PET, precursor, radiopharmaceutical, radiosynthesis, [F]FTC-146, σ-1 receptor

ID: 380203441