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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  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2010年1-8;  页码  443-447  
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[摘要]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.

 
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