TY - JOUR T1 - Styrylbenzoxazole Derivatives for <em>In Vivo</em> Imaging of Amyloid Plaques in the Brain JF - The Journal of Neuroscience JO - J. Neurosci. SP - 2535 LP - 2541 DO - 10.1523/JNEUROSCI.4456-03.2004 VL - 24 IS - 10 AU - Nobuyuki Okamura AU - Takahiro Suemoto AU - Hiroshi Shimadzu AU - Masako Suzuki AU - Tsuyoshi Shiomitsu AU - Hiroyasu Akatsu AU - Takayuki Yamamoto AU - Matthias Staufenbiel AU - Kazuhiko Yanai AU - Hiroyuki Arai AU - Hidetada Sasaki AU - Yukitsuka Kudo AU - Tohru Sawada Y1 - 2004/03/10 UR - http://www.jneurosci.org/content/24/10/2535.abstract N2 - Progressive deposition of senile plaques (SPs) is one of the major neuropathological features of Alzheimer's disease (AD) that precedes cognitive decline. Noninvasive detection of SPs could, therefore, be a potential diagnostic test for early detection of AD patients. For imaging SPs in the living brain, we have developed a series of styrylbenzoxazole derivatives that achieve high binding affinity for amyloid-β (Aβ) fibrils. One of these compounds, 6-(2-Fluoroethoxy)-2-[2-(4-methylaminophenil) ethenyl]benzoxazole (BF-168), selectively binds SPs in AD brain sections and recognizes Aβ1-42-positive diffuse plaques as well as neuritic plaques in AD brain sections. Intravenous injection of BF-168 in PS1/APP and APP23 transgenic mice resulted in specific in vivo labeling to both compact and diffuse amyloid deposits in the brain. In addition, 18F-radiolabeled BF-168 demonstrated abundant initial brain uptake (3.9% injected dose/gm at 2 min after injection) and fast clearance (t1/2 = 24.7 min) after intravenous administration in normal mice. Furthermore, autoradiograms of brain sections from APP23 transgenic mice at 180 min after intravenous injection of [18F]BF-168 showed selective labeling of brain amyloid deposits with little nonspecific binding. These findings strongly suggest that styrylbenzoxazole derivatives are promising candidate probes for positron emission tomography and single-photon emission computed tomography imaging for early detection of amyloid plaque formation. ER -