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    Aβ斑块显像剂3’-131I-PIB的合成与生物分布

    Synthesis and Radioiodinelabeling of β-Amyloid Plaques Imaging Agent 3’-131I-PIB

      摘要
    • 摘要: 为了找到适合单光子计算机发射断层（SPECT）的脑内β淀粉样蛋白（Aβ）斑块的显像剂，合成了2-（3’-三正丁基锡-4’-甲氨基苯基）-6-羟基苯并噻唑,并采用双氧水标记法进行了131I标记，得到了2-（3’-碘-4’-甲氨基苯基）-6-羟基苯并噻唑（3’-131I-PIB），放化纯大于95%。对文献中原料与条件作了相应的改进，提高了合成的回收率。正常小鼠体内分布实验表明，3’-131I-PIB在2 min和60 min时，小鼠脑摄取分别为（2.45±0.43）%ID/g和（0.19±0.02）%ID/g。说明3’-131I-PIB在小鼠脑中初摄取高，清除很快。如果改用合适的核素标记，3’-I-PIB将是一个有研究前景的Aβ斑块显像剂。

       

      Abstract: The synthesis and biodistribution of β-amyloid plaques imaging agent 2-(3’-iodo-4’-methylaminophenyl)-6-hydroxy-benzothialzole（3’-131I-PIB）were reported. The chemical structure of the labeling precursor 2-(3’-tributylstannyl-4’-methylaminophenyl)-6-hydroxybenzothialzole and all its intermediates were verified by 1H NMR and MS. The radioiodinated compound was prepared using iododestannylation reaction by hydrogen peroxide. Final radiochemical purity is above 95% determined by TLC. The in vivo biodistribution of 3’-131I-PIB in normal mice shows excellent brain uptake and washout, indicating this benzothiazole (BTA) derivative has potential for in vivo imaging amyloid deposits. 

       

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