1318778-70-9Relevant academic research and scientific papers
Novel quinoxaline derivatives for in vivo imaging of β-amyloid plaques in the brain
Cui, Mengchao,Ono, Masahiro,Kimura, Hiroyuki,Liu, Boli,Saji, Hideo
, p. 4193 - 4196 (2011)
In a search for new probes to detect β-amyloid plaques in the brain of patients with Alzheimer's disease (AD), we have synthesized and evaluated a series of quinoxaline derivatives containing a '6+6-6' ring system. These quinoxaline derivatives showed excellent affinity for Aβ1-42 aggregates with Ki values ranging from 2.6 to 10.7 nM. Autoradiography with sections of brain tissue from an animal model of AD mice (APP/PS1) and AD patients revealed that [125I]5 labeled β-amyloid plaques specifically. In biodistribution experiments using normal mice, [125I]5 displayed high uptake (6.03% ID/g at 2 min) into and a moderately fast washout from the brain. Although additional refinements are needed to decrease the lipophilicity and improve the washout rate, the quinoxaline scaffold may be useful as a backbone structure to develop novel β-amyloid imaging agents.
