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

ABSTRACT

Two novel benzofuran derivatives coupled with 99mTc complexes were tested as probes for imaging cerebral ƒÀ-amyloid plaques using single photon emission tomography. Although both derivatives bound to AƒÀ(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 ƒÀ-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 ƒÀ-amyloid plaques in Alzheimer's brains.