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European Journal of Nuclear Medicine and Molecular Imaging
Published in: European Journal of Nuclear Medicine and Molecular Imaging 11/2010

Open Access 01-11-2010 | Original Article

Synthesis and biological evaluation of [18F]tetrafluoroborate: a PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide symporter

Authors: Maite Jauregui-Osoro, Kavitha Sunassee, Amanda J. Weeks, David J. Berry, Rowena L. Paul, Marcel Cleij, Jasvinder Paul Banga, Michael J. O’Doherty, Paul K. Marsden, Susan E. M. Clarke, James R. Ballinger, Istvan Szanda, Sheue-Yann Cheng, Philip J. Blower

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 11/2010

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Abstract

Purpose

The human sodium/iodide symporter (hNIS) is a well-established target in thyroid disease and reporter gene imaging using gamma emitters 123I-iodide, 131I-iodide and 99mTc-pertechnetate. However, no PET imaging agent is routinely available. The aim of this study was to prepare and evaluate 18F-labelled tetrafluoroborate ([18F]TFB) for PET imaging of hNIS.

Methods

[18F]TFB was prepared by isotopic exchange of BF 4 − with [18F]fluoride in hot hydrochloric acid and purified using an alumina column. Its identity, purity and stability in serum were determined by HPLC, thin-layer chromatography (TLC) and mass spectrometry. Its interaction with NIS was assessed in vitro using FRTL-5 rat thyroid cells, with and without stimulation by thyroid-stimulating hormone (TSH), in the presence and absence of perchlorate. Biodistribution and PET imaging studies were performed using BALB/c mice, with and without perchlorate inhibition.

Results

[18F]TFB was readily prepared with specific activity of 10 GBq/mg. It showed rapid accumulation in FRTL-5 cells that was stimulated by TSH and inhibited by perchlorate, and rapid specific accumulation in vivo in thyroid (SUV = 72 after 1 h) and stomach that was inhibited 95% by perchlorate.

Conclusion

[18F]TFB is an easily prepared PET imaging agent for rodent NIS and should be evaluated for hNIS PET imaging in humans.
Appendix
Available only for authorised users
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Metadata
Title
Synthesis and biological evaluation of [18F]tetrafluoroborate: a PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide symporter
Authors
Maite Jauregui-Osoro
Kavitha Sunassee
Amanda J. Weeks
David J. Berry
Rowena L. Paul
Marcel Cleij
Jasvinder Paul Banga
Michael J. O’Doherty
Paul K. Marsden
Susan E. M. Clarke
James R. Ballinger
Istvan Szanda
Sheue-Yann Cheng
Philip J. Blower
Publication date
01-11-2010
Publisher
Springer-Verlag
Published in
European Journal of Nuclear Medicine and Molecular Imaging / Issue 11/2010
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-010-1523-0

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