摘要:
Classical Tc-99m(CO)(3)(+) and novel Tc-99m(CO)(2)(NO)(2+) cores complexed with flavonol derivatives were prepared. Autoradiography of postmortem AD transgenic mice (Tg C57, APP, PS1 12-month-old) brain section confirmed the binding property of [Tc-99m(CO)(3)(+)-3-OH-flavone](0) to A beta((1-40)) aggregates, while the novel Tc-99m(CO)(2)(NO)(2+) labeled compounds showed no binding sites in AD transgenic mice sections. Intravenous administration of [ 99mTc(CO)(3)(+)-3-OH-flavone](0) resulted in moderate brain uptake (0.48 +/- 0.05% ID/g) at 5 min post-injection and slow clearance from the brain issues in 2 h post-injection (120 min: 0.39 +/- 0.08% ID/g). Then an A beta((1-40))-receptor-targeted Re(CO)(3)(+)-3-OH-flavone, was prepared to identify the structure of the technetium complex. UV-vis absorption and fluorescence emission properties have been studied at room temperature in order to determine the natures of the lowest electronically excited states of Re(CO)(3)(+)-3-OH-flavone and the ligand. The fluorescent rhenium complex Re(CO)(3)(+)-3-OH-flavone showed high affinity for A beta((1-40)) aggregates in vitro by fluorescence spectra (dissociation constant (K-d) = 11.16 nM). In conclusion, the results suggested that Tc-99m(CO)(3)(+)-3-OH-flavone should be a suitable candidate as A beta plaque SPECT imaging agent for AD. Crown Copyright (C) 2010 Published by Elsevier Ltd. All rights reserved.