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Synthesis and biological evaluation of N-(2-[(18)F]Fluoropropionyl)-L-methionine for tumor imaging.
- Source :
-
Nuclear medicine and biology [Nucl Med Biol] 2013 Oct; Vol. 40 (7), pp. 926-32. Date of Electronic Publication: 2013 Jul 23. - Publication Year :
- 2013
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Abstract
- Introduction: N-position radiolabeled amino acids, such as N-(2-[(18)F]fluoropropionyl)-L-methionine ([(18)F]FPMET) as a derivative of L-methionine (MET), can potentially serve as a PET tracer for tumor imaging. In the current study, radiosynthesis and biological evaluation of [(18)F]FPMET as a new PET tumor agent are performed.<br />Methods: [(18)F]FPMET was synthesized by reacting 4-nitrophenyl 2-[(18)F]fluoropropionate ([(18)F]NFP) with MET. In vitro competitive inhibition and protein incorporation experiments were performed with Hepa1-6 hepatoma cell lines. The biodistribution of [(18)F]FPMET was determined in S180 fibrosarcoma-bearing mice. PET/CT studies of [(18)F]FPMET were conducted in S180 fibrosarcoma-bearing mice, A549 lung adenocarcinoma-bearing nude mice, and PC-3 prostate cancer-bearing nude mice.<br />Results: [(18)F]FPMET was synthesized in 72%± 4% uncorrected radiochemical yield (n=10) from [(18)F]NFP. In vitro experiments showed that [(18)F]FPMET was primarily transported through Na(+)-dependent system A, system ASC, and system B(0,+), and was not incorporated into protein. Biodistribution and PET/CT imaging studies indicated that [(18)F]FPMET could delineate S180 fibrosarcoma, A549 lung adenocarcinoma, and PC-3 prostate cancer.<br />Conclusion: An efficient synthesis of N-position [(18)F]labeled amino acids with a classic [(18)F]NFP prosthetic group is developed. The results support that [(18)F]FPMET seems to be a potential tracer for tumor imaging with PET.<br /> (© 2013.)
- Subjects :
- Animals
Cell Line
Cell Line, Tumor
Chemistry Techniques, Synthetic
Drug Stability
Methionine chemistry
Methionine pharmacokinetics
Mice
Octanols chemistry
Radiochemistry
Water chemistry
Fibrosarcoma diagnostic imaging
Methionine analogs & derivatives
Methionine chemical synthesis
Positron-Emission Tomography methods
Subjects
Details
- Language :
- English
- ISSN :
- 1872-9614
- Volume :
- 40
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 23886847
- Full Text :
- https://doi.org/10.1016/j.nucmedbio.2013.06.006