Abstract |
The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]- tyrosine ((99m)Tc-N4-Tyrosine), a novel amino acid-based radiotracer, and evaluate its potential in breast cancer gamma imaging. Precursor N4-Tyrosine was synthesized using a 5-step procedure, and its total synthesis yield was 38%. It was successfully labeled with (99m)Tc with high radiochemical purity (>95%). Cellular uptake of (99m)Tc-N4-Tyrosine was much higher than that of (99m)Tc-N4 and the clinical gold standard (18)F-2-deoxy-2-fluoro-glucose ((18)F-FDG) in rat breast tumor cells in vitro. Tissue uptake and dosimetry estimation in normal rats revealed that (99m)Tc-N4-Tyrosine could be safely administered to humans. Evaluation in breast tumor-bearing rats showed that although (99m)Tc-N4-Tyrosine appeared to be inferior to (18)F-FDG in distinguishing breast tumor tissue from chemical-induced inflammatory tissue, it had high tumor-to-muscle uptake ratios and could detect breast tumors clearly by planar scintigraphic imaging. (99m)Tc-N4-Tyrosine could thus be a useful radiotracer for use in breast tumor diagnostic imaging.
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Authors | Fan-Lin Kong, Mohammad S Ali, Alex Rollo, Daniel L Smith, Yinhan Zhang, Dong-Fang Yu, David J Yang |
Journal | Journal of biomedicine & biotechnology
(J Biomed Biotechnol)
Vol. 2012
Pg. 671708
( 2012)
ISSN: 1110-7251 [Electronic] United States |
PMID | 22496612
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
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Chemical References |
- Heterocyclic Compounds, 1-Ring
- Organotechnetium Compounds
- Radioactive Tracers
- Radiopharmaceuticals
- technetium Tc 99m cyclam
- Fluorodeoxyglucose F18
- Tyrosine
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Topics |
- Animals
- Cell Line, Tumor
- Female
- Fluorodeoxyglucose F18
(pharmacokinetics)
- Heterocyclic Compounds, 1-Ring
(chemical synthesis, pharmacokinetics)
- Inflammation
(diagnostic imaging, metabolism)
- Mammary Neoplasms, Experimental
(diagnostic imaging, metabolism)
- Organotechnetium Compounds
(chemical synthesis, pharmacokinetics)
- Radiation Dosage
- Radioactive Tracers
- Radionuclide Imaging
- Radiopharmaceuticals
(chemical synthesis, pharmacokinetics)
- Rats
- Rats, Inbred F344
- Tissue Distribution
- Tyrosine
(analogs & derivatives, pharmacokinetics)
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