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Aβ斑块显像剂3’-^131I-PIB的合成与生物分布 被引量:1

Synthesis and Radioiodinelabeling of β-Amyloid Plaques Imaging Agent 3'-^(131)I-PIB
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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。 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-hydroxybenzothialzole 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.
出处 《核化学与放射化学》 EI CAS CSCD 北大核心 2008年第3期162-166,共5页 Journal of Nuclear and Radiochemistry
基金 国家自然科学基金资助项目(30470496) 江苏省自然科学基金资助项目(BK2004423)
关键词 β-淀粉样蛋白斑块 3'-^131I-PIB 合成 β-amyloid plaques 3'-^131I-PIB synthesis
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参考文献7

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