1383563-17-4Relevant academic research and scientific papers
Novel 18F-labeled benzoxazole derivatives as potential positron emission tomography probes for imaging of cerebral β-amyloid plaques in alzheimers disease
Cui, Mengchao,Ono, Masahiro,Kimura, Hiroyuki,Ueda, Masashi,Nakamoto, Yuji,Togashi, Kaori,Okamoto, Yoko,Ihara, Masafumi,Takahashi, Ryosuke,Liu, Boli,Saji, Hideo
, p. 9136 - 9145 (2012)
Two radiofluoro-pegylated phenylbenzoxazole derivatives, 4-(5-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)benzo[d]oxazol-2-yl)-N- methylaniline ([18F]24) and 4-(5-(2-(2-(2-[18F] fluoroethoxy)ethoxy)ethoxy)benzo[d]oxazol-2-yl)
Synthesis and biological evaluation of novel technetium-99m labeled phenylbenzoxazole derivatives as potential imaging probes for β-amyloid plaques in brain
Wang, Xuedan,Cui, Mengchao,Yu, Pingrong,Li, Zijing,Yang, Yanping,Jia, Hongmei,Liu, Boli
supporting information; experimental part, p. 4327 - 4331 (2012/09/22)
Two uncharged 99mTc-labeled phenylbenzoxazole derivatives were biologically evaluated as potential imaging probes for β-amyloid plaques. The 99mTc and corresponding rhenium complexes were synthesized by coupling monoamine-monoamide dithiol (MAMA) and bis(aminoethanethiol) (BAT) chelating ligand via a pentyloxy spacer to phenylbenzoxazole. The fluorescent rhenium complexes 6 and 9 selectively stainined the β-amyloid plaques on the sections of transgenic mouse, and showed high affinity for Aβ(1-42) aggregates (Ki = 11.1 nM and 14.3 nM, respectively). Autoradiography in vitro indicated that [99mTc]6 clearly labeled β-amyloid plaques on the sections of transgenic mouse. Biodistribution experiments in normal mice revealed that [99mTc]6 displayed moderate initial brain uptake (0.81% ID/g at 2 min), and quickly washed out from the brain (0.25% ID/g at 60 min). The preliminary results indicate that the properties of [99mTc]6 are promising, although additional refinements are needed to improve the ability to cross the blood-brain barrier.
