转运蛋白
放射合成
配体(生物化学)
化学
正电子发射断层摄影术
Pet成像
放射性配体
显像剂
体内
分子成像
体内分布
临床前影像学
作者
Dario Fiorenza,Emanuele Nicolai,Carlo Cavaliere,Ferdinando Fiorino,Giovanna Esposito,Marco Salvatore
出处
期刊:Molecules
[MDPI AG]
日期:2021-04-19
卷期号:26 (8): 2372-
标识
DOI:10.3390/molecules26082372
摘要
Introduction: Benzodiazepines, including temazepam are described as TSPO antagonists. In fact, TSPO was initially described as a peripheral benzodiazepine receptor (PBR) with a secondary binding site for diazepam. TSPO is a potential imaging target of neuroinflammation because there is an amplification of the expression of this receptor. Objectives: Herein, we developed a novel fluorinated benzodiazepine ligand, [18F]Fluoroethyltemazepam ([18F]F-FETEM), for positron emission tomography (PET) imaging of translocator protein (18 kDa). Methods: [18F]F-FETEM was radiolabelled with an automated synthesizer via a one-pot procedure. We conducted a [18F]F-aliphatic nucleophilic substitution of a tosylated precursor followed by purification on C18 and Alumina N SPE cartridges. Quality control tests was also carried out. Results: We obtained 2.0–3.0% decay-uncorrected radiochemical activity yield (3.7% decay-corrected) within the whole synthesis time about 33 min. The radiochemical purity of [18F]F-FETEM was over 90% by TLC analysis. Conclusions: This automated procedure may be used as basis for future production of [18F]F-FETEM for preclinical PET imaging studies.
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