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Development of a widely usable amino acid tracer; $$^{76}$$Br-$$alpha$$-methyl-phenylalanine for tumor PET imaging

腫瘍PETイメージングにおいて幅広い応用性を備えたアミノ酸トレーサー、$$^{76}$$Br-$$alpha$$-Methyl-Phenylalanineの開発

花岡 宏史*; 大島 康宏; 鈴木 結利花*; 山口 藍子*; 渡辺 茂樹; 上原 知也*; 永森 收志*; 金井 好克*; 石岡 典子; 対馬 義人*; 遠藤 啓吾*; 荒野 泰*

Hanaoka, Hirofumi*; Ohshima, Yasuhiro; Suzuki, Yurika*; Yamaguchi, Aiko*; Watanabe, Shigeki; Uehara, Tomoya*; Nagamori, Shushi*; Kanai, Yoshikatsu*; Ishioka, Noriko; Tsushima, Yoshito*; Endo, Keigo*; Arano, Yasushi*

Radiolabeled amino acids are superior PET tracers for imaging of malignant tumors, and amino acids labeled with $$^{76}$$Br, an attractive positron emitter due to its relatively long half-life (t$$_{1/2}$$=16.2 h), could potentially be widely usable tumor imaging tracer. In this study, in consideration of stability and tumor specificity, 2-$$^{76}$$Br-bromo-$$alpha$$-methyl-L-phenylalanine (2-$$^{76}$$Br-BAMP) and 4-$$^{76}$$Br-bromo-$$alpha$$-methyl-L-phenylalanine (4-$$^{76}$$Br-BAMP) were designed and their potential as a tumor imaging agent was evaluated. No-carrier-added $$^{76}$$Br and $$^{77}$$Br, the latter of which is suitable radiobromine for basic studies due to its longer half-life (t$$_{1/2}$$ = 57.1 h), were produced. Both $$^{77}$$Br-BAMPs were stable in the plasma and in the murine body. In biodistribution studies, 2-$$^{77}$$Br-BAMP showed more rapid blood clearance and lower renal accumulation than did 4-$$^{77}$$Br-BAMP. More than 90% of injected radioactivity was excreted in the urine by 6 h post-injection of 2-$$^{77}$$Br-BAMP. High tumor accumulation of 2-$$^{77}$$Br-BAMP was observed in tumor-bearing mice and PET imaging with 2-$$^{76}$$Br-BAMP enabled clear visualization of the tumor. These findings suggest that 2-$$^{76}$$Br-BAMP would constitute a potential new PET tracer for tumor imaging and may eventually enable the wider use of amino acid tracers.

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パーセンタイル:48.99

分野:Radiology, Nuclear Medicine & Medical Imaging

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