Novel Benzofurans with Tc-99m Complexes as Probes for Imaging Cerebral beta-Amyloid Plaques

作者：Ono Masahiro^*; Fuchi Yasufumi; Fuchigami Takeshi; Kobashi Nobuya; Kimura Hiroyuki; Haratake Mamoru; Saji Hideo; Nakayama Morio

来源：ACS Medicinal Chemistry Letters, 2010, 1(8): 443-447.

DOI：10.1021/ml100140d

• Alzheimer's disease
• beta-amyloid plaque
• Tc-99m
• single photon emission computed tomography (SPECT) imaging

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

• 出版日期2010-11