Effect of Monofluorosulphonate, Difluorophosphate and Fluoroborate Ions on the Iodine Uptake of the Thyroid Gland

Anbar, M.; Guttmann, S.; Lewitus, Z

doi:10.1038/1831517a0

Cited by 41 publications

(15 citation statements)

References 8 publications

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“…5). Over the entire pH range studied (3)(4)(5)(6)(7)(8)(9)(10)(11), the Zeta potential of GR was negative and was lower than Thus, the incorporation of QA functional groups into GR increased the surface potential of reed. These findings are in agreement with published data [23,25,32,37].…”

Section: Isotherm Studiesmentioning

confidence: 94%

Perchlorate removal by quaternary amine modified reed

Baidas

Gao

Meng

2011

Journal of Hazardous Materials

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Section: Isotherm Studiesmentioning

confidence: 94%

Perchlorate removal by quaternary amine modified reed

Baidas

Gao

Meng

2011

Journal of Hazardous Materials

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“…Plot of ionic volume against inhibitory potency (logIC 50 based on ability to block anion uptake in NIS-expressing cells) for univalent anions examined in this work and other published works (5)(6)(7)9,17). Differing methods, cell lines, probes, and counter-ions were used in each study; further details are given in Supplemental (59 6 10 %ID/g), and salivary glands (18 6 4 %ID/g); uptake in these organs was reduced to 4.3 6 4.6, 3.0 6 1.7, and 2.6 6 1.7 % ID/g, respectively, in mice administered NaClO 4 (Fig.…”

Section: Ex Vivo Biodistribution In Micementioning

confidence: 99%

“…Both SO 3 F 2 and PO 2 F 2 2 are known to inhibit radioiodide uptake in mouse thyroid (9), yet in quantitative terms their effectiveness as substrates or inhibitors of hNIS is unknown. PF 6 2 is a highly potent inhibitor of rat NIS (IC 50 , 15 nM (10)).…”

mentioning

confidence: 99%

¹⁸F-Fluorosulfate for PET Imaging of the Sodium–Iodide Symporter: Synthesis and Biologic Evaluation In Vitro and In Vivo

et al. 2016

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Anion transport by the human sodium-iodide symporter (hNIS) is an established target for molecular imaging and radionuclide therapy. Current radiotracers for PET of hNIS expression are limited to 124 I 2 and 18 F-BF 4 2 . We sought new 18 F-labeled hNIS substrates offering higher specific activity, higher affinity, and simpler radiochemical synthesis than 18 F-BF 4 2 . Methods: The ability of a range of anions, some containing fluorine, to block 99m TcO 4 2 uptake in hNIS-expressing cells was measured. SO 3 F 2 emerged as a promising candidate. 18 F-SO 3 F 2 was synthesized by reaction of 18 F 2 with SO 3 -pyridine complex in MeCN and purified using alumina and quaternary methyl ammonium solid-phase extraction cartridges. Chemical and radiochemical purity and serum stability were determined by radiochromatography. Radiotracer uptake and efflux in hNIS-transduced HCT116-C19 cells and the hNIS-negative parent cell line were evaluated in vitro in the presence and absence of a known competitive inhibitor (NaClO 4 ). PET/CT imaging and ex vivo biodistribution measurement were conducted on BALB/c mice, with and without NaClO 4 inhibition. Results: Fluorosulfate was identified as a potent inhibitor of 99m TcO 4 2 uptake via hNIS in vitro (half-maximal inhibitory concentration, 0.55-0.56 mM (in comparison with 0.29-4.5 mM for BF 4 2 , 0.07 mM for TcO 4 2 , and 2.7-4.7 mM for I 2 ). Radiolabeling to produce 18 F-SO 3 F 2 was simple and afforded high radiochemical purity suitable for biologic evaluation (radiochemical purity . 95%, decay-corrected radiochemical yield 5 31.6%, specific activity $ 48.5 GBq/mmol). Specific, blockable hNIS-mediated uptake in HCT116-C19 cells was observed in vitro, and PET/CT imaging of normal mice showed uptake in thyroid, salivary glands (percentage injected dose/g at 30 min, 563 6 140 and 32 6 9, respectively), and stomach (percentage injected dose/g at 90 min, 68 6 21). Conclusion: Fluorosulfate is a high-affinity hNIS substrate. 18 F-SO 3 F 2 is easily synthesized in high yield and very high specific activity and is a promising candidate for preclinical and clinical PET imaging of hNIS expression and thyroid-related disease; it is the first example of in vivo PET imaging with a tracer containing an S-18 F bond.

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“…Because various anions (e.g., I 2 , SeCN 2 , SCN 2 , ReO 4 2 , TcO 4 2 , NO 3 2 ) are transported by NIS (6), the critical physicochemical feature of these well-transported substrates is anionic monovalency with size and space-filling properties similar to the iodide ion. Before the advent of clinical PET, in the1950s and early 1960s, Anbar et al (11,12) reported that the tetrafluoroborate (TFB, BF 4 2 ) anion was effective to inhibit thyroid uptake of iodide ion. These researchers also showed that 18 F-labeled TFB, synthesized from reactor-produced 18 F-fluoride, specifically accumulated in rat thyroid.…”

mentioning

confidence: 99%

Synthesis of ¹⁸F-Tetrafluoroborate via Radiofluorination of Boron Trifluoride and Evaluation in a Murine C6-Glioma Tumor Model

et al. 2016

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Effect of Monofluorosulphonate, Difluorophosphate and Fluoroborate Ions on the Iodine Uptake of the Thyroid Gland

Cited by 41 publications

References 8 publications

Perchlorate removal by quaternary amine modified reed

Perchlorate removal by quaternary amine modified reed

¹⁸F-Fluorosulfate for PET Imaging of the Sodium–Iodide Symporter: Synthesis and Biologic Evaluation In Vitro and In Vivo

Synthesis of ¹⁸F-Tetrafluoroborate via Radiofluorination of Boron Trifluoride and Evaluation in a Murine C6-Glioma Tumor Model

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Effect of Monofluorosulphonate, Difluorophosphate and Fluoroborate Ions on the Iodine Uptake of the Thyroid Gland

Cited by 41 publications

References 8 publications

Perchlorate removal by quaternary amine modified reed

Perchlorate removal by quaternary amine modified reed

18F-Fluorosulfate for PET Imaging of the Sodium–Iodide Symporter: Synthesis and Biologic Evaluation In Vitro and In Vivo

Synthesis of 18F-Tetrafluoroborate via Radiofluorination of Boron Trifluoride and Evaluation in a Murine C6-Glioma Tumor Model

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Product

Resources

About

¹⁸F-Fluorosulfate for PET Imaging of the Sodium–Iodide Symporter: Synthesis and Biologic Evaluation In Vitro and In Vivo

Synthesis of ¹⁸F-Tetrafluoroborate via Radiofluorination of Boron Trifluoride and Evaluation in a Murine C6-Glioma Tumor Model