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Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents
Joint Authors
Shih, I-Hong
Duan, Xu-Dong
Yu, Dong-Fang
Kong, Fan-Lin
Yang, David J.
Zhang, Yin-Han
Ali, Mohammad S.
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-9, 9 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-07-09
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Abstract EN
Radiolabeled tyrosine analogs enter cancer cells via upregulated amino acid transporter system and have been shown to be superior to 18F-fluoro-2-deoxy-D-glucose (18F-FDG) in differential diagnosis in cancers.
In this study, we synthesized O-[3-19F-fluoropropyl]-α-methyl tyrosine (19F-FPAMT) and used manual and automated methods to synthesize O-[3-18F-fluoropropyl]-α-methyl tyrosine (18F-FPAMT) in three steps: nucleophilic substitution, deprotection of butoxycarbonyl, and deesterification.
Manual and automated synthesis methods produced 18F-FPAMT with a radiochemical purity >96%.
The decay-corrected yield of 18F-FPAMT by manual synthesis was 34% at end-of-synthesis (88 min).
The decay-corrected yield of 18F-FPAMT by automated synthesis was 15% at end-of-synthesis (110 min).
18F-FDG and 18F-FPAMT were used for in vitro and in vivo studies to evaluate the feasibility of 18F-FPAMT for imaging rat mesothelioma (IL-45).
In vitro studies comparing 18F-FPAMT with 18F-FDG revealed that 18F-FDG had higher uptake than that of 18F-FPAMT, and the uptake ratio of 18F-FPAMT reached the plateau after being incubated for 60 min.
Biodistribution studies revealed that the accumulation of 18F-FPAMT in the heart, lungs, thyroid, spleen, and brain was significantly lower than that of 18F-FDG.
There was poor bone uptake in 18F-FPAMT for up to 3 hrs suggesting its in vivo stability.
The imaging studies showed good visualization of tumors with 18F-FPAMT.
Together, these results suggest that 18F-FPAMT can be successfully synthesized and has great potential in mesothelioma imaging.
American Psychological Association (APA)
Shih, I-Hong& Kong, Fan-Lin& Ali, Mohammad S.& Zhang, Yin-Han& Yu, Dong-Fang& Duan, Xu-Dong…[et al.]. 2013. Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents. BioMed Research International،Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-1030562
Modern Language Association (MLA)
Shih, I-Hong…[et al.]. Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents. BioMed Research International No. 2013 (2013), pp.1-9.
https://search.emarefa.net/detail/BIM-1030562
American Medical Association (AMA)
Shih, I-Hong& Kong, Fan-Lin& Ali, Mohammad S.& Zhang, Yin-Han& Yu, Dong-Fang& Duan, Xu-Dong…[et al.]. Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents. BioMed Research International. 2013. Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-1030562
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1030562