title: Fully automatic synthesis of [¹⁸F]FES for reporter gene hERL expression imaging.
abstract: We have developed a fully automatic method for the synthesis of 16α-[¹⁸F]fluoroestradiol ([F]FES) using a TRACERlab FXFN module. Following [¹⁸F]fluorination, the intermediate was hydrolyzed with a mixture of 2 N HCl in acetonitrile (CH3CN) and then neutralized with sodium bicarbonate (NaHCO3). After HPLC purification, the decay-corrected radiochemical yield of [¹⁸F]FES was 50 ± 2.35% (n=4), which was stable up to 96.1 ± 0.3% (n=4) at 8 h. This new fully automated synthesis method provided high and reproducible yields and the produced [F]FES could be used to monitor in-vivo human estrogen receptor α ligand binding domain gene expression using PET images.
authors: Department of Nuclear Medicine, Ruijin Hospital, School of Medicine, Institute of Med-X, Shanghai Jiaotong University, Shanghai, China.
authors: Sheng
authors: S
authors: Liang
authors: Xiaoli
authors: X
authors: Lan
authors: Yongxue
authors: Y
authors: Zhang
authors: Xuemin
authors: X
authors: Xu
authors: Biao
authors: B
authors: Li
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D015870:Gene Expression; D017930:Genes, Reporter; D006801:Humans; D008024:Ligands; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D051381:Rats
chemical_list: D047628:Estrogen Receptor alpha; D005462:Fluorine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D004958:Estradiol; C043436:16-fluoroestradiol