Kawai K, Fujibayashi Y, Saji H, Konishi J, Kubodera A, Yokoyama A
Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
Int J Rad Appl Instrum B. 1990;17(4):369-76. doi: 10.1016/0883-2897(90)90103-8.
Using 11C-labeled natural amino acids, the functional diagnosis of tissue metabolism has been actively studied. Our interest has been focused on developing a clinically available 123I-labeled artificial amino acid with a single metabolic function. For this study, [123I]3-iodo-D-tyrosine ([123I]D-MIT) was selected. In vitro and in vivo studies using 125I-labeled D-MIT indicated that it showed a high pancreatic accumulation, selective affinity for membrane active transport systems, and was stable against enzymatic deiodination. A canine scintigraphic study using 123I-labeled D-MIT and kinetic analysis showed that it behaved as an "artificial amino acid" radiopharmaceutical with selective membrane amino acid transport affinity in the pancreas.
利用碳-11标记的天然氨基酸，组织代谢的功能诊断已得到积极研究。我们的兴趣集中在开发一种具有单一代谢功能、可用于临床的碘-123标记的人工氨基酸。在本研究中，选择了[123I]3-碘-D-酪氨酸（[123I]D-MIT）。使用碘-125标记的D-MIT进行的体外和体内研究表明，它在胰腺中具有较高的积聚、对膜主动转运系统具有选择性亲和力，并且对酶促脱碘稳定。一项使用碘-123标记的D-MIT的犬闪烁扫描研究和动力学分析表明，它表现为一种在胰腺中具有选择性膜氨基酸转运亲和力的“人工氨基酸”放射性药物。
