~(125)I标记苯并噻唑类Aβ斑块显像剂的合成及生物分布

Synthesis and Biodistribution of ~(125)I-Labelled Benzothiazole Derivatives as β-Amyloid Imaging Agents

摘要: 为了研制123I标记的、诊断阿尔茨海默病的苯并噻唑类Aβ斑块显像剂,合成了4个125I标记的苯并噻唑类衍生物,放射化学纯度大于95%。动物体内分布实验表明,3′ 125I BTA,3′ 125I CBTA,3′ 125I BTA Ac和3′ 125I CBTA Ac在小鼠脑中有较高的初始摄取,给药后2min的脑摄取量分别为:10.28,3.62,3.33和3.71%/g;3′ 125I BTA,3′ 125I BTA Ac和3′ 125I CBTA Ac脑清除较快,2min与6min的脑摄取量之比分别为:7.3,6.2和5.7。研究结果表明,3′ 123I BTA是一个很有发展潜力的Aβ斑块SPECT显像剂。

Abstract: In order to develop ~(123)I labelled probe for SPET imaging of A β plaques in Alzheimer's (disease), Four ~(125)I labelled benzothiazole derivatives are synthesized and their radiochemical purity are more than 95%. The biodistribution results in normal mice indicate that the radiolabelled probes have higher initial brain uptake:10.28, 3.62, 3.33 and 3.71%/g at 2 min post i.v. injection for 3′-~(125)I-BTA,3′-~(125)I-CBTA,3′-~(125)I-BTA-Ac and 3′-~(125)I-CBTA-Ac, respectively. Brain uptake ratios at 2 min to 60 min of 3′-~(125)I-BTA,3′-~(125)I-BTA-Ac and 3′-~(125)I-CBTA-Ac are 7.3, 6.2 and 5.7 respectively. The results reveal that 3′-~(123)I-BTA is a very potential agent for SPECT imaging of A β plaques in Alzheimer's disease.