Synthesis and Evaluation of Novel Chalcone Derivatives with 99mTc/Re Complexes as Potential Probes for Detection of -Amyloid Plaques.
ABSTRACT
Four 99mTc-labeled chalcone derivatives and their corresponding rhenium analogues
were tested as potential probes for imaging -amyloid plaques. The chalcones
showed higher affinity for A(1-42) aggregates than did 99m Tc complexes. In sections of brain tissue from an animal model of AD,
the four Re chalcones intensely stained -amyloidplaques. Inbiodistributionexperiments
using normal mice, 99mTc-BAT-chalcone ([99mTc]17) displayed high uptake in the brain (1.48% ID/g) at 2 min postinjection.
The radioactivity washed out from the brain rapidly (0.17% ID/g at 60 min),
a highly desirable feature for an imaging agent. [99mTc]17 may be a potential probe for imaging -amyloid plaques in Alzheimerfs
brains.