Novel Benzofurans with 99mTc Complexes as Probes for Imaging Cerebral -Amyloid Plaques.


Two novel benzofuran derivatives coupled with 99mTc complexes were tested as probes for imaging cerebral -amyloid plaques using single photon emission tomography. Although both derivatives bound to A(1-42) aggregates, 99mTc-BAT-BF showed higher affinity than 99mTc-MAMA-BF. In sections of brain tissue from an animal model of AD, 99mTc-BAT-BF clearly labeled -amyloid plaques. In biodistribution experiments using normal mice, 99mTc-BAT-BF displayed high uptake soon after its injection and washed out from the brain rapidly, a highly desirable feature for an imaging agent. 99mTc-BAT-BF may be a potential probe for imaging -amyloid plaques in Alzheimer's brains.