Synthesis and Evaluation of Amino Acid-Based Radiotracer 99mTc-N4-AMT for Breast Cancer Imaging. (20th March 2011)

• Record Type: Journal Article
• Authors: Kong, Fan-Lin; Ali, Mohammad S.; Zhang, Yinhan; Oh, Chang-Sok; Yu, Dong-Fang; Chanda, Mithu; Yang, David J.
• Other Names: Shen Lie-Hang Academic Editor.
• Is Part Of: Journal of biomedicine and biotechnology. Volume 2011(2011)
• Publication Date: 2011-03-20
• Subjects: Medicine -- Periodicals; Biology -- Periodicals; Biotechnology -- Periodicals; Medicine; Biology; Biotechnology; Médecine; Biologie; Biotechnologie; Biology; Biotechnology; Medicine; Biotechnology; Biomedicine; Electronic journals; Periodical; Periodicals; Electronic journals; 610
• DOI: 10.1155/2011/276907
• Languages: English
• ISSNs: 1110-7243

Abstract

Abstract : Purpose . This study was to develop an efficient synthesis of 99m Tc-O-[3-(1, 4, 8, 11-tetraazabicyclohexadecane)-propyl]-α -methyl tyrosine ( 99m Tc-N4-AMT) and evaluate its potential in cancer imaging. Methods . N4-AMT was synthesized by reacting N4-oxalate and 3-bromopropyl AMT (N-BOC, ethyl ester). In vitro cellular uptake kinetics of 99m Tc-N4-AMT was assessed in rat mammary tumor cells. Tissue distribution of the radiotracer was determined in normal rats at 0.5–4 h, while planar imaging was performed in mammary tumor-bearing rats at 30–120 min. Results . The total synthesis yield of N4-AMT was 14%. Cellular uptake of 99m Tc-N4-AMT was significantly higher than that of 99m Tc-N4. Planar imaging revealed that 99m Tc-N4-AMT rendered greater tumor/muscle ratios than 99m Tc-N4. Conclusions . N4-AMT could be synthesized with a considerably high yield. Our in vitro and in vivo data suggest that 99m Tc-N4-AMT, a novel amino acid-based radiotracer, efficiently enters breast cancer cells, effectively distinguishes mammary tumors from normal tissues, and thus holds the promise for breast cancer imaging.