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

作　　者：陆春雄[1] 吴春英[1] 蒋泉福[1] 

机构地区：[1]江苏省原子医学研究所,江苏无锡214063

出　　处：《核化学与放射化学》2005年第4期232-235,共4页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(30470496);江苏省'135'医学重点人才基金资助项目(RC2002068);江苏省'六大人才高峰'基金资助项目(2003-07);江苏省自然科学基金资助项目(BK2004423)

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。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.

关 键 词：β-淀粉样蛋白斑块 ^131Ⅰ-IMPY 合成 

分 类 号：R817[医药卫生—影像医学与核医学]