Abstract:
In vivo PET and SPECT imaging of β-amyloid (Aβ) plagques in the brain may lead to early detection of Alzheimer’s Disease (AD), but the Aβ-detector labeled by
99Tc
m fell behind. The purpose of this study was to develop novel
99Tc
m(CO)
3+-labeled β-amyloid-detector based on the flavones. Isostructural Re/
99Tc
m(CO)
3+-flavones were designed and synthesized, and Re(CO)
3+-flavone were studied on its binding characteristic with βamyloid plaques in vitro by fluorescence. The results showed that the binding affinity(
Kd=5.43 nmol/L) of Re(CO)
3+-flavone was higher than flavone derivatives labeled by radioiodine. The biodistrubution of normal mice showed that
99Tc
m(CO)
3+-flavone displayed moderate uptake (0.46±0.23%ID/g) at 2 min postinjection) in the brain and rapid clearance (0.13±0.04%ID/g) after 120 min injection. The above results demonstrated that
99Tc
m(CO)
3+-flavone should be desirable as a potential SPECT imaging agent for β-amyloid aggregates.