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2min和60min,小鼠脑摄取率分别为(7.374±4.797)%/g和(0.967士0.409)%/g。说明^131Ⅰ-IMPY在小鼠脑中初始摄取很高,清除很快。^131Ⅰ-IMPY可能是一个很有发展潜力的Aβ斑块SPECT显像剂。
The synthesis and biodistribution of β-amyloid plaques imaging agent [^131 Ⅰ]-2-(4'-dimethylaminophenyl)-6-iodoimidazo[-1, 2-α] pyridine (^131Ⅰ-IMPY) is reported. The chemical structure of the precursor compound 2-(4'-dimethylaminophenyl)-6-(tributylstanny) imidazo [1, 2-α] 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 [^131Ⅰ] 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.