Synthesis and Evaluation of Novel Chalcone Derivatives with 99mTc/Re Complexes as Potential Probes for Detection of β-Amyloid Plaques
Synthesis and Evaluation of Novel Chalcone Derivatives with 99mTc/Re Complexes as Potential Probes for Detection of β-Amyloid Plaques
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DOI：
10.1021/cn100042d
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发表时间：
2010-09-01
影响因子：
5
通讯作者：
Nakayama, Mono
中科院分区：
文献类型：
--
作者：
Ono, Masahiro;Ikeoka, Ryoichi;Nakayama, Mono
四种 Tc-99m 标记的查耳酮衍生物及其相应的铼类似物被测试作为 β-淀粉样斑块成像的潜在探针。与 Tc-99m 复合物相比，查耳酮对 A beta(1-42) 聚集体表现出更高的亲和力。在 AD 动物模型的脑组织切片中，四种 Re 查尔酮对 β-淀粉样蛋白斑块进行了强烈染色。在使用正常小鼠的生物分布实验中，Tc-99m-BAT-查尔酮 ([Tc-99m]17) 在注射后 2 分钟在大脑中表现出高摄取量 (1.48% ID/g)。放射性迅速从大脑中消失（60 分钟时为 0.17% ID/g），这是显像剂非常理想的特征。 [Tc-99m]17 可能是阿尔茨海默病大脑中 β-淀粉样斑块成像的潜在探针。
Four Tc-99m-labeled chalcone derivatives and their corresponding rhenium analogues were tested as potential probes for imaging beta-amyloid plaques. The chalcones showed higher affinity for A beta(1-42) aggregates than did Tc-99m complexes. In sections of brain tissue from an animal model of AD, the four Re chalcones intensely stained beta-amyloid plaques. In biodistribution experiments using normal mice, Tc-99m-BAT-chalcone ([Tc-99m]17) displayed high uptake in the brain (1.48% ID/g) at 2 min postinjection. The radioactivity washed out from the brain rapidly (0.17% ID/g at 60 min), a highly desirable feature for an imaging agent. [Tc-99m]17 may be a potential probe for imaging beta-amyloid plaques in Alzheimer's brains.