We report a novel series of radioiodinated aurone derivatives as probes for imaging Abeta plaques in the brains of patients with Alzheimer's disease (AD) using single photon emission computed tomography (SPECT). In binding experiments in vitro, aurone derivatives showed very good affinity for Abeta aggregates (K(i) = 1.1 to 3.4 nM). No-carrier-added radioiodinated aurones were successfully prepared through an iododestannylation reaction from the corresponding tributyltin derivatives. In biodistribution experiments using normal mice, aurone derivatives displayed high brain uptake (1.7-4.5% ID/g at 2 min) and rapid clearance from the brain (0.1-0.4% ID/g at 30 min), especially [125I]15. Furthermore, a specific plaque labeling signal was observed in in vitro autoradiography of postmortem AD brain sections using [125I]15. [125I]15 may be a useful SPECT imaging agent for detecting Abeta plaques in the brain of AD.
Although PET amyloid-β imaging agents are available, they cannot be used with SPECT scanners. Maya
et al
. report that a novel SPECT imaging agent, 123I-ABC577, has a high affinity for amyloid-β, and differentiates Alzheimer's disease patients from healthy controls, with low non-specific retention in the white matter.
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