Synthesis and biological evaluation of 99mTc, Re-monoamine-monoamide conjugated to 2-(4-aminophenyl) benzothiazole as potential probes for β-amyloid plaques in the brain

The benzothiazole aniline (BTA) conjugated with monoamine-monoamide ( MAMA) was synthesized and then labeled with Tc-99m. Its corresponding rhenium analogue was synthesized, and the fluorescent staining was performed in brain sections of both Tg mouse and Alzheimer's disease ( AD) patient. The. uorescent rhenium complex Re-MAMA-BTA selectively bound to the amyloid aggregates in the brain sections of both APP Tg mouse and AD patient. The analogous Tc-99m-MAMA-BTA complex could enter the normal mouse brain with high initial uptake. These results are encouraging for further exploration of their derivatives as imaging agents for Ab plaques in the brain. (c) 2007 Elsevier Ltd. All rights reserved.