β-淀粉样蛋白斑块显像剂~(131)I-IMPY的合成与生物分布

Synthesis and Biodistribution of β Amyloid Plaques Imaging Agent ~(131)I-IMPY

摘要: 为了找到合适的123I标记的脑内β淀粉样蛋白(Aβ)斑块的显像剂,根据文献资料,合成了2-(4′-二甲基氨基苯基)-6-三正丁基锡咪唑并1,2-α吡啶(IMPY),并采用双氧水标记法进行了131I标记,得到标记物131I-IMPY,放射化学纯度大于95%。方法对合成原料和条件作了相应的改进,提高了合成的收率。正常小鼠体内分布试验表明,在注射131I-IMPY后2 min和60 min,小鼠脑摄取率分别为(7.374±4.797)%/g和(0.967±0.409)%/g。说明131I-IMPY在小鼠脑中初始摄取很高,清除很快1。31I-IMPY可能是一个很有发展潜力的Aβ斑块SPECT显像剂。

Abstract: The synthesis and biodistribution of β-amyloid plaques imaging agent _2-(4′-dimethylaminophenyl)-6-iodoimidazo\ pyridine(~(131)I-IMPY) is reported.The chemical structure of the precursor compound 2-(4′-dimethylaminophenyl)-6-(tributylstanny) imidazo\ pyridine and all other intermediates are verified by IR,~1H NMR and MS.The radioiodinated compound is prepared(using) iododestannylation reaction by hydrogen peroxide.The radiochemical purity of the final product is above 95% as determined by TLC.The in vivo biodistribution of \ IMPY in normal mice shows that excellent brain uptake and washout,indicating this thioflavin-T based small molecular probe has potential for in vivo imaging amyloid deposits.