Rhodanine and thiohydantoin derivatives for detecting tau pathology in Alzheimer's brains.
Rhodanine and thiohydantoin derivatives for detecting tau pathology in Alzheimer's brains.
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DOI：
10.1021/cn200002t
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发表时间：
2011-05
影响因子：
5
通讯作者：
M. Ono;S. Hayashi;K. Matsumura;H. Kimura;Y. Okamoto;M. Ihara;R. Takahashi;H. Mori;H. Saji
中科院分区：
文献类型：
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作者：
M. Ono;S. Hayashi;K. Matsumura;H. Kimura;Y. Okamoto;M. Ihara;R. Takahashi;H. Mori;H. Saji
设计并合成了一系列新的罗丹宁（RH）和硫代乙内酰脲（TH）衍生物，用于检测阿尔茨海默病（AD）患者脑中的tau病理。在使用tau和β-淀粉样蛋白（Aβ）聚集体的体外实验中，TH衍生物TH 2显示出与tau聚集体的高度特异性结合。在从AD患者获得的海马切片中，TH 2强烈染色的神经元缠结。在使用正常小鼠的实验中，[（125）I] TH 2显示出良好的脑摄取（1.54%ID/g，注射后2分钟）和快速的脑洗脱（0.25%ID/g，注射后60分钟）。[（123）I] TH 2应进一步研究作为检测tau病理学的潜在成像剂。
A novel series of rhodanin (RH) and thiohydantoin (TH) derivatives were designed and synthesized for detecting tau pathology in the brains of patients with Alzheimer's disease (AD). In experiments in vitro using tau and β-amyloid (Aβ) aggregates, the TH derivative, TH2, showed high specific binding to tau aggregates. In hippocampal sections obtained from AD patients, TH2 intensely stained neurofibrillary tangles. In experiments using normal mice, [(125)I]TH2 showed good uptake (1.54%ID/g, 2 min postinjection) into and a rapid washout (0.25%ID/g, 60 min postinjection) from the brain. [(123)I]TH2 should be further investigated as a potential imaging agent for detecting tau pathology.