Synthesis of isomers of 18F‐labelled amino acid radiopharmaceutical: Position 2− and 3‐L‐18F-α‐methyltyrosine using a separation and purification system

Synthesis of isomers of 18F‐labelled amino acid radiopharmaceutical: Position 2− and 3‐L‐18F-α‐methyltyrosine using a separation and purification system
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使用分离纯化系统合成 18F 标记氨基酸放射性药物异构体:2− 和 3-L-18F-α-甲基酪氨酸

DOI:
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发表时间:
1997
影响因子:
1.5
通讯作者:
David J. Yang
David J. Yang
中科院分区:
医学4区
文献类型:
--
作者:
K. Tomiyoshi;K. Amed;S. Muhammad;T. Higuchi;Tomio Inoue;Keigo Endo;David J. Yang

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为了应用正电子发射断层扫描技术(PET)对放射性标记氨基酸进行肿瘤诊断,我们建立了L-18 F-α-甲基酪氨酸(L-18FAmT)的分离纯化系统。该系统可以提供辐射防护和L-18FAmT的稳定生产。合成并纯化了L-18FAmT,并对该系统的效率进行了检测。基于反应容器中捕获的放射性,L-18FAmT的放射化学产率为20.3 ± 5.1%(n = 5)。放射化学纯度大于99.4 ± 0.3%(n = 5)。检查了磷酸盐缓冲盐水和人血浆中的放射化学稳定性,通过HPLC分析观察到几乎没有分解。我们的研究结果表明,分离和纯化系统提供了简单和快速的合成L-18FAmT,大大减少了辐射暴露和L-18FAmT的一致生产。
To diagnose cancers with radiolabelled amino acid using positron emission tomography, we have constructed a separation and purification system for the production of L-18F-α-methyltyrosine (L-18FAmT). This system could provide radioprotection and consistent production of L-18FAmT. L-18FAmT was synthesized and purified and the efficiency of the system was examined. The radiochemical yield of L-18FAmT was 20.3 ± 5.1% (n = 5) based on the radioactivity trapped in the reaction vessel. The radiochemical purity was greater than 99.4 ± 0.3% (n = 5). The radiochemical stability in phosphate-buffered saline and human plasma was examined and little decomposition was observed by HPLC analysis. Our results indicate that the separation and purification system gave simple and quick synthesis of L-18FAmT with a large reduction in radiation exposure and consistent production of L-18FAmT.