[C]MPC-6827 的放射性合成及体内评价，首个穿透血脑屏障的微管 PET 配体。
Radiosynthesis and in Vivo Evaluation of [C]MPC-6827, the First Brain Penetrant Microtubule PET Ligand.
机构信息
Molecular Imaging and Neuropathology Division , New York State Psychiatric Institute , 1051 Riverside Drive , New York , New York 10032 , United States.
Department of Radiology , Wake Forest Medical Center , Winston Salem , North Carolina 27157 , United States.
出版信息
J Med Chem. 2018 Mar 8;61(5):2118-2123. doi: 10.1021/acs.jmedchem.8b00028. Epub 2018 Feb 23.
Abstract
Abnormalities of microtubules (MTs) are implicated in the pathogenesis of many CNS diseases. Despite the potential of an MT imaging agents, no PET ligand is currently available for in vivo imaging of MTs in the brain. We radiolabeled [C]MPC-6827, a high affinity MTA, and demonstrated its specific binding in rat and mice brain using PET imaging. Our experiments show that [C]MPC-6827 has specific binding to MT in brain, and it is the first MT-binding PET ligand.
摘要
微管（MTs）的异常与许多中枢神经系统疾病的发病机制有关。尽管 MT 成像剂具有潜在的应用前景，但目前尚无用于脑内 MT 体内成像的 PET 配体。我们对高亲和力 MTA [C]MPC-6827 进行了放射性标记，并通过 PET 成像证明了其在大鼠和小鼠脑内的特异性结合。我们的实验表明，[C]MPC-6827 与脑内 MT 具有特异性结合，这是第一个 MT 结合 PET 配体。
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