Development of dual functional SPECT/fluorescent probes for imaging cerebral beta-amyloid plaques

作者：Ono, Masahiro^*; Ishikawa, Manami; Kimura, Hiroyuki; Hayashi, Shun; Matsumura, Kenji; Watanabe, Hiroyuki; Shimizu, Yoichi; Cheng, Yan; Cui, Mengchao; Kawashima, Hidekazu; Saji, Hideo

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(13): 3885-3888.

DOI：10.1016/j.bmcl.2010.05.027

• Alzheimer's disease
• beta-Amyloid plaque
• Positron emission tomography
• Single photon emission computed
• tomography
• Fluorescence
• Dual imaging

he imaging of beta-amyloid (A beta) aggregates in the brain may lead to the early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to develop dual modality SPECT and fluorescent probes based on boron dipyrromethane (BODIPY) as a core structure. We designed and synthesized an I-125-labeled derivative of BODIPY (BODIPY7). BOD-IPY7 had a K-i value of 108 nM for A beta(1-42) aggregates and exhibited peaks of absorption/emission aL 606/613 nm. It detected A beta plaques in sections of brain tissue from an animal model of AD and displayed low uptake in the brain and high uptake in the liver in normal mice. Although additional modifications of the BODIPY scaffold are necessary to improve brain uptake, these results should aid the development of dual functional SPECT/fluorescent probes for the imaging of Ab plaques in the brain.

• 出版日期2010-7-1