68Ga-Bivalent Polypegylated Styrylpyridine Conjugates for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy

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• 作者：Zhihao Zha ; Jin Song ; Seok Rye Choi ; Zehui Wu ; Karl Ploessl ; Megan Smith ; Hank Kung
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：May 18, 2016
• 年：2016
• 卷：27
• 期：5
• 页码：1314-1323
• 全文大小：454K
• 年卷期：0
• ISSN：1520-4812

文摘

Aβ plaques deposited on blood vessels are associated with cerebral amyloid angiopathy (CAA). In an effort to selectively map these Aβ plaques, we are reporting a new series of <sup>68sup>Ga labeled styrylpyridine derivatives with high molecular weights. In vitro binding to Aβ plaques in post-mortem Alzheimer’s disease (AD) brain tissue showed that these <sup>68sup>Ga labeled bivalent styrylpyridines displayed good affinities and specificity (K<sub>isub> < 30 nM). In vitro autoradiography using post-mortem AD brain sections showed specific binding of these <sup>68sup>Ga complexes to Aβ plaques. Biodistribution studies in normal mice showed very low initial brain uptakes (<0.3% dose/g) indicating a low blood-brain barrier (BBB) penetration. The preliminary results suggest that <sup>68sup>Ga labeled bivalent styrylpyridines may be promising candidates as PET imaging radiotracers for detecting CAA.