机构：[a]Department of Neurobiology, Xuanwu Hospital of Capital Medical University, Beijing 100053, China首都医科大学宣武医院[b]Beijing Institute for Brain Disorders, Capital Medical University, Beijing, 100069, China[c]Key Laboratory of Radiopharmaceuticals, Beijing Normal University, Ministry of Education, Beijing, 100875, China[d]Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
Serotonin transporters (SERT) in the brain play an important role in normal brain function. Selective serotonin reuptake inhibitors such as fluoxetine, sertraline, paroxetine, escitalopram, etc., specifically target SERT binding in the brain. Development of SERT imaging agents may be useful for studying the function of SERT by in vivo imaging. A one-step preparation of [F-18]FPBM, 2-(2'-(dimethylamino)methyl)-4'-(3-([F-18]fluoroproPoxy) phenylthio)benzenamine, for positron emission tomography (PET) imaging of SERT binding in the brain was achieved. An active OTs intermediate, 9, was reacted with [F-18]F-/K-222 to produce [F-18]FPBM in one step and in high radiochemical yield. This labeling reaction was evaluated and optimized under different temperatures, bases, solvents, and varying amounts of precursor 9. The radiolabeling reaction led to the desired [F-18]FPBM in one step and the crude product was purified by HPLC purification to give no-carrier-added [F-18]FPBM (radio-chemical yield, 24-33%, decay corrected; radiochemical purity >99%). PET imaging studies in normal monkeys (n = 4) showed fast, pronounced uptakes in the midbrain and thalamus, regions known to be rich in SERT binding sites. A displacement experiment with escitalopram (5 mg/kg iv injection at 30 min after [F-18]FPBM injection) showed a rapid and complete reversal of SERT binding, suggesting that binding by [F-18]FPBM was highly specific and reversible. A one-step radiolabeling method coupled with HPLC purification for preparation of [F-18]FPBM was developed. Imaging studies suggest that it is feasible to use this method to prepare [F-18]FPBM for in vivo PET imaging of SERT binding in the brain. (C) 2016 Elsevier Inc. All rights reserved.
基金：
the National Institutes of Health (ROI-MH068782,)
Ministry of Science and Technology, China 973 (2011 CB504105)
863 (SS2012AA020831) Programs
第一作者机构：[a]Department of Neurobiology, Xuanwu Hospital of Capital Medical University, Beijing 100053, China[b]Beijing Institute for Brain Disorders, Capital Medical University, Beijing, 100069, China[d]Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
通讯作者：
通讯机构：[*1]Key Laboratory of Radiopharmaceuticals, Beijing Normal University, Ministry of Education, No. 19, XinJieKouWai Street, HaiDian District, Beijing, 100875, P. R. China.[*2]Department of Radiology, University of Pennsylvania, 3700 Market Street, Room 305, Philadelphia, PA, 19104, USA
推荐引用方式(GB/T 7714)：
Hongwen Qiao,Yan Zhang,ZehuiWu,et al.One-step preparation of [F-18]FPBM for PET imaging of serotonin transporter (SERT) in the brain[J].NUCLEAR MEDICINE AND BIOLOGY.2016,43(8):470-477.doi:10.1016/j.nucmedbio.2016.04.003.
APA：
Hongwen Qiao,Yan Zhang,ZehuiWu,Lin Zhu,Seok Rye Choi...&Hank F. Kung.(2016).One-step preparation of [F-18]FPBM for PET imaging of serotonin transporter (SERT) in the brain.NUCLEAR MEDICINE AND BIOLOGY,43,(8)
MLA：
Hongwen Qiao,et al."One-step preparation of [F-18]FPBM for PET imaging of serotonin transporter (SERT) in the brain".NUCLEAR MEDICINE AND BIOLOGY 43..8(2016):470-477
