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Synthesis of para ‐[ 18 F]Fluorofenbufen Octylamide for PET Imaging of Brain Tumors
Author(s) -
Huang YingCheng,
Farn ShiouShiow,
Chou YoCheng,
Yeh ChunNan,
Chang ChiWei,
Chung YiHsiu,
Chen TsongWen,
Huang WenSheng,
Yu ChungShan
Publication year - 2018
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.201700300
Subject(s) - chemistry , brain tumor , glioma , cyclooxygenase , specific activity , nuclear medicine , cancer research , enzyme , pathology , biochemistry , medicine
Glioma is a brain tumor associated with a poor therapeutic outcome with an average life expectancy of 14 months. 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 4 GBq/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 30 min, 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.