[HTML][HTML] Synthesis and biological evaluation of [18F]tetrafluoroborate: a PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide …
M Jauregui-Osoro, K Sunassee, AJ Weeks… - European journal of …, 2010 - Springer
M Jauregui-Osoro, K Sunassee, AJ Weeks, DJ Berry, RL Paul, M Cleij, JP Banga…
European journal of nuclear medicine and molecular imaging, 2010•SpringerPurpose The human sodium/iodide symporter (hNIS) is a well-established target in thyroid
disease and reporter gene imaging using gamma emitters 123 I-iodide, 131 I-iodide and
99m Tc-pertechnetate. However, no PET imaging agent is routinely available. The aim of
this study was to prepare and evaluate 18 F-labelled tetrafluoroborate ([18 F] TFB) for PET
imaging of hNIS. Methods [18 F] TFB was prepared by isotopic exchange of BF 4− with [18 F]
fluoride in hot hydrochloric acid and purified using an alumina column. Its identity, purity and …
disease and reporter gene imaging using gamma emitters 123 I-iodide, 131 I-iodide and
99m Tc-pertechnetate. However, no PET imaging agent is routinely available. The aim of
this study was to prepare and evaluate 18 F-labelled tetrafluoroborate ([18 F] TFB) for PET
imaging of hNIS. Methods [18 F] TFB was prepared by isotopic exchange of BF 4− with [18 F]
fluoride in hot hydrochloric acid and purified using an alumina column. Its identity, purity and …
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.
Springer