99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques
99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques
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DOI：
10.1016/j.bmcl.2010.08.004
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发表时间：
2010-10-01
影响因子：
2.7
通讯作者：
Nakayama, Morio
中科院分区：
文献类型：
--
作者：
Ono, Masahiro;Ikeoka, Ryoichi;Nakayama, Morio
基于黄酮和橙酮的两个Tc-99 m/Re配合物被测试为使用单光子发射计算机断层扫描成像β-淀粉样蛋白斑块的潜在探针。两种Tc-99 m-BAT标记衍生物对A β（1-42）聚集体的亲和力均高于Tc-99 m-BAT。在来自AD动物模型的脑组织切片中，Re-黄酮衍生物9和Re-橙酮衍生物19强烈染色β-淀粉样蛋白斑块。在使用正常小鼠的生物分布实验中，Tc-99 m标记的黄酮和橙酮显示出相似的放射性药代动力学。通过额外的修饰以改善其脑摄取，基于黄酮或橙酮支架的Tc-99 m复合物可用作脑β-淀粉样蛋白斑块成像的探针。(C)2010爱思唯尔有限公司保留所有权利。
Two Tc-99m/Re complexes based on flavone and aurone were tested as potential probes for imaging beta-amyloid plaques using single photon emission computed tomography. Both Tc-99m-labeled derivatives showed higher affinity for A beta(1-42) aggregates than did Tc-99m-BAT. In sections of brain tissue from an animal model of AD, the Re-flavone derivative 9 and Re-aurone derivative 19 intensely stained beta-amyloid plaques. In biodistribution experiments using normal mice, Tc-99m-labeled flavone and aurone displayed similar radioactivity pharmacokinetics. With additional modifications to improve their brain uptake, Tc-99m complexes based on the flavone or aurone scaffold may serve as probes for imaging cerebral beta-amyloid plaques. (C) 2010 Elsevier Ltd. All rights reserved.