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Preparation and biological evaluation of 3-[$$^{76}$$Br]bromo-$$alpha$$-methyl-L-tyrosine, a novel tyrosine analog for PET imaging of tumors

Ohshima, Yasuhiro; Hanaoka, Hirofumi*; Watanabe, Shigeki; Sugo, Yumi; Watanabe, Satoshi; Tominaga, Hideyuki*; Oriuchi, Noboru*; Endo, Keigo*; Ishioka, Noriko

3-[$$^{18}$$F]Fluoro-$$alpha$$-methyl-L-tyrosine ([$$^{18}$$F]FAMT) is a useful amino acid tracer for PET imaging of malignant tumors. FAMT analogs labeled with $$^{76}$$Br, a positron emitter with a long half-life (t$$_{1/2}$$=16.1 h), could be widely used as tracers for tumor imaging. In this study, 3-[$$^{76}$$Br]bromo-$$alpha$$-methyl-L-tyrosine ([$$^{76}$$Br]BAMT) was designed, and its usefulness was evaluated as a novel PET tracer for imaging malignant tumors. In this study, both [$$^{76}$$Br]BAMT and [$$^{77}$$Br]BAMT were prepared. [$$^{77}$$Br]BAMT was stable in vitro, but was catabolized after administration in mice. Cellular accumulation and retention of [$$^{77}$$Br]BAMT using LS180 colon adenocarcinoma cells were significantly higher than those of [$$^{18}$$F]FAMT. In biodistribution studies using LS180 tumor-bearing mice, the tumor accumulation of [$$^{77}$$Br]BAMT was higher than that of [$$^{18}$$F]FAMT. However, some level of debromination was seen, and this debromination caused more retention of radioactivity in the blood and organs than was seen with [$$^{18}$$F]FAMT. PET imaging with [$$^{76}$$Br]BAMT enabled clear visualization of the tumor. In conclusion, although an improvement in stability is still needed, $$^{76}$$Br-labeled FAMT analogs could potentially serve as PET tracers for the imaging of malignant tumors.



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