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.
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.
| Original language | English |
|---|---|
| Pages (from-to) | 2108-2116 |
| Number of pages | 9 |
| Journal | European Journal of Nuclear Medicine and Molecular Imaging |
| Volume | 37 |
| Issue number | 11 |
| DOIs | |
| Publication status | Published - Nov 2010 |
Keywords
- Animals
- Boric Acids
- Cell Line
- Drug Stability
- Female
- Fluorine Radioisotopes
- Genes, Reporter
- Humans
- Male
- Mice
- Molecular Imaging
- Positron-Emission Tomography
- Rats
- Symporters
- Thyroid Diseases
- Thyroid Gland
