Synthesis of Oxorhenium(V) and Oxotechnetium(V) Complexes That Bind to Amyloid-β Plaques
作者:David J. Hayne、Jonathan M. White、Catriona A. McLean、Victor L. Villemagne、Kevin J. Barnham、Paul S. Donnelly
DOI:10.1021/acs.inorgchem.6b00972
日期:2016.8.15
ligands were prepared that form charge-neutral complexes with oxorhenium(v) as well as a ligand featuring a styrylpyridyl functional group designed to bind to Aβ plaques. All three ligands formed complexes with oxorhenium(V), and each complex was characterized by NMR spectroscopy, mass spectrometry, and X-ray crystallography. The oxorhenium(V) complex with a styrylpyridyl functional group binds to
阿尔茨海默氏病的特征是大脑中存在淀粉样蛋白斑块。斑块的主要成分是淀粉样β(Aβ)肽的聚集形式。与制备锝-99的目标米复合物,其结合至Aβ斑块潜力成为阿尔茨海默病的诊断成像剂,新的四齿配体能够与oxotechentium(V)和oxorhenium(V)形成中性和亲脂性复合体来制备的。not的非放射性同位素不可用,因此rh被用作探索化学的替代物。两个平面四齿N 3制备了与氧杂鎓(v)形成电荷中性复合物的O配体,该配体具有设计成与Aβ斑块结合的具有苯乙烯基吡啶基官能团的配体。所有三个配体都与氧ium(V)形成了配合物,并通过NMR光谱,质谱和X射线晶体学对每种配合物进行了表征。具有苯乙烯基吡啶基官能团的oxorhenium(V)络合物与验尸后人脑组织中存在的Aβ斑块结合。化学推算到tech 99 m在两个配体的示踪剂水平上。生成的氧络合物具有足够的亲脂性和电荷中性,表明它们具有穿越血脑屏障的潜