【作者】 张锦明； 郭喆； 田嘉禾； 王武尚； 刘伯里；

【Author】 Zhang Jinming Guo Zhi’Tian Jiahe, Wang Wushang, Liu Baoli DeptNucl Med, The PLA General Hospital, 100853,Beijing Dept Chemistry, The Normal University, 100875,Beijing Northwest Institute of Nuclear Technology, 710024,Xian

【机构】 解放军总医院核医学科； 北京师范大学化学系；

【摘要】 合成了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;研究了[11]-BTA-1在正常鼠体内的分布。结果显示:柱色层法测标记率简单、有效:碘代甲烷改良法碳-11标记BTA的效率为58%。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Aβ斑块显像剂。更多还原

【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). 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 β-amyloid agent for Alzheimer’s disease.更多还原