A strategy for the study of cerebral amino acid transport using iodine-123-labeled amino acid radiopharmaceutical: 3-iodo-alpha-methyl-L-tyrosine.
A strategy for the study of cerebral amino acid transport using iodine-123-labeled amino acid radiopharmaceutical: 3-iodo-alpha-methyl-L-tyrosine.
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使用碘 123 标记的氨基酸放射性药物研究脑氨基酸转运的策略：3-碘-α-甲基-L-酪氨酸。
DOI：
10.1016/0006-2952(89)90080-4
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
A. Yokoyama
中科院分区：
文献类型：
--
作者：
K. Kawai;Y. Fujibayashi;H. Saji;Y. Yonekura;J. Konishi;A. Kubodera;A. Yokoyama
我们研究了碘-123-碘-α-甲基-L酪氨酸(123I-L-AMT)在小鼠和大鼠脑内的蓄积。I-L-AMT在小鼠和大鼠体内均有较高的脑蓄积，大鼠脑摄取指数超过14C-L-酪氨酸。脑摄取指数和脑切片研究表明，I-L-AMT对载体介导的和立体选择性的主动转运系统分别具有亲和力；这两种系统都可以跨越血脑屏障和脑细胞膜。组织匀浆分析表明，大部分累积的放射性属于完整的I-L-AMT，这表明其稳定性。因此，~(123)I-L-AMT有望成为选择性测定脑内氨基酸转运的放射性药物。
We examined the brain accumulation of iodine-123-iodo-alpha-methyl-L-tyrosine (123I-L-AMT) in mice and rats. I-L-AMT showed high brain accumulation in mice, and in rats; rat brain uptake index exceeded that of 14C-L-tyrosine. The brain uptake index and the brain slice studies indicated the affinity of I-L-AMT for carrier-mediated and stereoselective active transport systems, respectively; both operating across the blood-brain barrier and cell membranes of the brain. The tissue homogenate analysis revealed that most of the accumulated radioactivity belonged to intact I-L-AMT, an indication of its stability. Thus, 123I-L-AMT appears to be a useful radiopharmaceutical for the selective measurement of cerebral amino acid transport.