作者:Wenchao Qu、Mei-Ping Kung、Catherine Hou、Tyler E. Benedum、Hank F. Kung
DOI:10.1021/jm070025+
日期:2007.5.1
We report a series of radioiodinated styrylpyridines as single photon emission computed tomography probes for imaging Abeta plaques in the brain of patients with Alzheimer's disease (AD). In vitro binding showed that all of the styrylpyridines displayed very good binding affinities in postmortem AD brain homogenates (Ki = 3.6 to 15.5 nM). No-carrier-added samples of 13a, 13b, 16a, 16b, and 16e (radioiodinated
我们报告了一系列的放射性碘化苯乙烯基吡啶作为单光子发射计算机断层摄影探头,用于成像阿尔茨海默氏病(AD)患者大脑中的Abeta斑块。体外结合表明,所有苯乙烯基吡啶在死后AD脑匀浆中均具有非常好的结合亲和力(Ki = 3.6至15.5 nM)。成功制备了未添加载体的样品13a,13b,16a,16b和16e(用125 I放射性碘标记)。正常小鼠在注射后2分钟的体内生物分布显示出极好的初始脑部穿透力([125I] 13a,13b,16a和16b分别为4.03、6.22、5.43和8.04%剂量/ g)。此外,AD脑切片的体外放射自显影显示高结合信号是由于Abeta斑块的存在所致。在一起