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Comparison of the synthesis and biological properties of no-carrier-added and carrier-added 4-borono-2-[ 18 F]fluorophenylalanine ([ 18 F]FBPA).
- Source :
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Nuclear medicine and biology [Nucl Med Biol] 2023 Jan-Feb; Vol. 116-117, pp. 108313. Date of Electronic Publication: 2022 Dec 30. - Publication Year :
- 2023
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Abstract
- Purpose: Boron neutron capture therapy (BNCT), an attractive strategy for cancer treatment, can kill tumor cells and avoid injury to surrounding healthy cells. 4-Borono-2-[ <superscript>18</superscript> F]fluorophenylalanine ([ <superscript>18</superscript> F]FBPA) positron emission tomography (PET) is a reliable tool for patient screening. Due to the relatively low radiochemical yield when employing the electrophilic route, this study was able to develop a new method to produce no-carrier-added (NCA) [ <superscript>18</superscript> F]FBPA and compare the biological characteristics with carrier-added (CA) characteristics.<br />Procedures: By starting from 4-bromo-2-nitrobenzaldehyde, NCA [ <superscript>18</superscript> F]FBPA was prepared using radiofluorination, alkylation, borylation, and hydrolysis. Cellular uptake analyses, microPET imaging, and biodistribution analyses were conducted to characterize the biological properties of NCA and CA [ <superscript>18</superscript> F]FBPA.<br />Results: The radiochemical yield of NCA [ <superscript>18</superscript> F]FBPA was 20 % ± 6 % (decay corrected) with a radiochemical purity of >98 % and molar activity of 56 ± 15 GBq/μmol in a 100-min synthesis. The in vitro accumulation was significantly higher for NCA [ <superscript>18</superscript> F]FBPA than for CA [ <superscript>18</superscript> F]FBPA in both SAS and CT-26 cells. However, no apparent differences in tumor uptake were observed between NCA and CA [ <superscript>18</superscript> F]FBPA-injected tumor-bearing mice.<br />Conclusions: We successfully prepared NCA [ <superscript>18</superscript> F]FBPA through nucleophilic substitution and achieved improved radiochemical yield and purity. We also demonstrated the effects of the amount of nonradioactive FBPA on in vitro cellular uptake and in vivo imaging studies.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2022 Elsevier Inc. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1872-9614
- Volume :
- 116-117
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 36621257
- Full Text :
- https://doi.org/10.1016/j.nucmedbio.2022.108313