Chemical Biology and Drug Design p. 559 - 565 (2017)
Update date:2022-08-24
Topics:
Wu, Xiaowei
You, Linyi
Zhang, Deliang
Gao, Mengna
Li, Zijing
Xu, Duo
Zhang, Pu
Huang, Lumei
Zhuang, Rongqiang
Wu, Hua
Zhang, Xianzhong
To develop a novel progesterone receptor-targeting probe for positron emission tomography imaging, an ethisterone derivative [18F]EAEF was designed and prepared in high decay-corrected radiochemical yield (30–35%) with good radiochemical purity (>98%). [18F]EAEF is a lipophilic tracer (logP?=?0.53?±?0.06) with very good stability in saline and serum. In the biodistribution study, high radioactivity accumulation of [18F]EAEF were found in uterus (5.73?±?1.83% ID/g) and ovary (4.05?±?0.73% ID/g) at 2?hr postinjection (p.i.), which have high progesterone receptor expression after treated with estradiol, while the muscle background has very low uptake (0.50?±?0.17% ID/g). For positron emission tomography imaging, [18F]EAEF showed high uptake in progesterone receptor-positive MCF-7 tumor (3.15?±?0.07% ID/g at 2?hr p.i.) with good tumor to muscle ratio (2.90), and obvious lower tumor uptakes were observed in MCF-7 with EAEF blocking (1.84?±?0.05% ID/g at 2?hr p.i.) or in progesterone receptor-negative MDA-MB-231 tumor (1.80?±?0.03% ID/g at 2?hr p.i.). Based on the good stability and specificity of [18F]EAEF, it may be a good candidate for imaging progesterone receptor and worth further investigation.
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