Synthesis and Evaluation of Novel Chalcone Derivatives with 99mTc/Re Complexes as Potential Probes for Detection of -Amyloid Plaques.


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.