Development of molecular probe for SPECT imaging of amyloid in the brain

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We have reported that^<125> I,^<11> C and^<18> F labeled flavonoid derivatives showed excellent characteristics such as high affinity forβ-amyloid(Aβ) aggregates and good uptake into and rapid clearance from the brain. In this study, we have synthesized and evaluated that novel flavonoid derivatives labeled with^<99> mTc that has become the most commonly used radionuclide in diagnostic nuclear medicine. The monoamine-monoamide dithiol(MAMA) and bis-amino-bis-thiol(BAT) were introduced to flavonoid derivatives as chelating site for the formation of stable and lipophilic^<99m> Tc complexes. Some^<99m> Tc-flavonoid derivatives showed high binding affinity for Aβ(1-42) aggregates. In biodistribution experiments using normal mice,^<99m> Tc-BAT-chalcone displayed high uptake in the brain and the radioactivity washed out from the brain rapidly, which is highly desirable for Aβimaging agents