1346502-20-2Relevant academic research and scientific papers
68Ga-Bivalent Polypegylated Styrylpyridine Conjugates for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy
Zha, Zhihao,Song, Jin,Choi, Seok Rye,Wu, Zehui,Ploessl, Karl,Smith, Megan,Kung, Hank
, p. 1314 - 1323 (2016/06/09)
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 68Ga 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 68Ga labeled bivalent styrylpyridines displayed good affinities and specificity (Ki 68Ga complexes to Aβ plaques. Biodistribution studies in normal mice showed very low initial brain uptakes (68Ga labeled bivalent styrylpyridines may be promising candidates as PET imaging radiotracers for detecting CAA.
Multidentate 18F-polypegylated styrylpyridines As imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA)
Zha, Zhihao,Choi, Seok Rye,Ploessl, Karl,Lieberman, Brian P.,Qu, Wenchao,Hefti, Franz,Mintun, Mark,Skovronsky, Daniel,Kung, Hank F.
, p. 8085 - 8098 (2012/01/13)
β-Amyloid plaques (Aβ plaques) in the brain are associated with cerebral amyloid angiopathy (CAA). Imaging agents that could target the Aβ plaques in the living human brain would be potentially valuable as biomarkers in patients with CAA. A new series of 18F styrylpyridine derivatives with high molecular weights for selectively targeting Aβ plaques in the blood vessels of the brain but excluded from the brain parenchyma is reported. The styrylpyridine derivatives, 8a-c, display high binding affinities and specificity to Aβ plaques (Ki = 2.87, 3.24, and 7.71 nM, respectively). In vitro autoradiography of [18F]8a shows labeling of β-amyloid plaques associated with blood vessel walls in human brain sections of subjects with CAA and also in the tissue of AD brain sections. The results suggest that [18F]8a may be a useful PET imaging agent for selectively detecting Aβ plaques associated with cerebral vessels in the living human brain.
