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Synthesis of para-[18F]Fluorofenbufen Octylamide for PET Imaging of Brain Tumors
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Synthesis of para-[18F]Fluorofenbufen Octylamide for PET Imaging of Brain Tumors

Ying-Cheng Huang, Shiou-Shiow Farn, Yo-Cheng Chou, Chun-Nan Yeh, Chi-Wei Chang, Yi-Hsiu Chung, Tsong-Wen Chen, Wen-Sheng HuangChung-Shan Yu
Journal of the Chinese Chemical Society
2018

摘要

Cyclooxygenase-2 Fenbufen Fluorine gas Imaging In vivo Chemistry (all)
Glioma is a brain tumor associated with a poor therapeutic outcome with an average life expectancy of 14months. Cyclooxygenase-2 (COX-2) expression is associated with the progression of the tumor and is considered a therapeutic target of chemo agents. Para-[ 18 F]Fluorofenbufen octylamide ([ 18 F]FFOA) was obtained with the radiochemical yield of 16% and specific activity of 4GBq/μmol, and the IC 50 values of COX-1 and COX-2 were 26.5 and 32.7 μM, respectively. The stability of cold FFOA in plasma was significantly improved with a half-life of 30min, and the uptake ratio of [ 18 F]FFOA in rats with brain tumor was 1.5 as determined from accumulation of 3.9% injection dose (ID/g) in the brain tumor and 2.5% ID/g in the brain. [ 18 F]FFOA with COX-2 micromolar affinity can be used to differentiate between brain tumor and normal region.

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