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Radiosynthesis and in Vivo Evaluation of [11C]MPC-6827, the First Brain Penetrant Microtubule PET Ligand
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2018-02-19 00:00:00 , DOI: 10.1021/acs.jmedchem.8b00028
J. S. Dileep Kumar 1 , Kiran Kumar Solingapuram Sai 2 , Jaya Prabhakaran 1, 3 , Hakeem R. Oufkir 2 , Gayathri Ramanathan 2 , Christopher T. Whitlow 2 , Hima Dileep 1, 3 , Akiva Mintz 2 , J. John Mann 1, 3
Affiliation  

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 [11C]MPC-6827, a high affinity MTA, and demonstrated its specific binding in rat and mice brain using PET imaging. Our experiments show that [11C]MPC-6827 has specific binding to MT in brain, and it is the first MT-binding PET ligand.

中文翻译:

[ 11 C] MPC-6827,第一个脑渗透微管PET配体的放射性合成和体内评估。

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成像剂具有潜力,但目前尚无PET配体可用于大脑中MT的体内成像。我们对[ 11 C] MPC-6827(高亲和力MTA)进行了放射性标记,并使用PET成像证明了其在大鼠和小鼠大脑中的特异性结合。我们的实验表明[ 11 C] MPC-6827与大脑中的MT具有特异性结合,并且是第一个与MT结合的PET配体。
更新日期:2018-02-19
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