Novel Benzofurans with (99m)Tc Complexes as Probes for Imaging Cerebral β-Amyloid Plaques.

Abstract

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

• Authors: Masahiro Ono, Yasufumi Fuchi, Takeshi Fuchigami, Nobuya Kobashi, Hiroyuki Kimura, Mamoru Haratake, Hideo Saji, Morio Nakayama
• Journal: ACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 1 Issue 8 Pg. 443-7 (Nov 11 2010) ISSN: 1948-5875 [Print] United States
• PMID: 24900230 (Publication Type: Journal Article)