Aβ斑块显像剂苯并噻唑衍生物的<sup>11</sup>C标记

Aβ斑块显像剂苯并噻唑衍生物的¹¹C标记

摘要: 为寻找合适的碳-11标记的在体A斑块显像剂，根据文献合成了苯并噻唑（BTA）的前体：（对胺基苯）苯并噻唑类（APBT），并用改良法碳-11碘代甲烷标记了APBT；柱色层法测标记率；改良法碳-11标记BTA的效率为58%。本文对碳-11标记方法和放射性标记率的方法作了改过，明显提高了标记效率，改进后的标记率测量方法简单、有效；正常小鼠的脑摄取11-BTA-1较高，2min全脑摄取为3.810.34%/ID；非特异区清除快，2min/30min摄取比达到10。11-BTA-1是一个有希望用于早老痴呆诊断的A斑块显像剂。

Abstract: The synthesis of 2-(4-aminophenyl)benzothiazole (APBT) was reported. The carbon-11 labeled APBT was performed by improved-methods with 11C-methyl iodide. The labeled yield was measured with column-methods. The results showed that the column-methods for labeled yields was simple and efficient. The improved-methods led to radiochemistry yield of 58%(n=10) when 11CCH3I react with APBT. Intravenous injection of 11C-BTA-1 in control mice resulted in high brain uptake. The brain uptake was 3.810.34%/ID at 2min. The uptake ratio of 2/30min was 10. 11C-BTA-1 was a promising -amyloid agent for Alzheimer’s disease.