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

癌のPETイメージングのための新規チロシン誘導体、3-[$$^{76}$$Br]bromo-$$alpha$$-methyl-L-tyrosineの合成と生物学的評価

大島 康宏; 花岡 宏史*; 渡邉 茂樹; 須郷 由美; 渡辺 智; 富永 英之*; 織内 昇*; 遠藤 啓吾*; 石岡 典子

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 positron emission tomography (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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パーセンタイル:51.28

分野:Radiology, Nuclear Medicine & Medical Imaging

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