用[¹⁸F]ML-10二乙酯通过PET/CT检测细胞凋亡以及用丹磺酰类似物进行荧光成像。
Detection of apoptosis by PET/CT with the diethyl ester of [¹⁸F]ML-10 and fluorescence imaging with a dansyl analogue.
作者信息
Kadirvel Manikandan, Fairclough Michael, Cawthorne Christopher, Rowling Emily J, Babur Muhammad, McMahon Adam, Birkket Paul, Smigova Alison, Freeman Sally, Williams Kaye J, Brown Gavin
机构信息
Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK; Manchester Pharmacy School, University of Manchester, M13 9PT, UK.
Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
出版信息
Bioorg Med Chem. 2014 Jan 1;22(1):341-9. doi: 10.1016/j.bmc.2013.11.019. Epub 2013 Nov 20.
The diethyl ester of [(18)F]ML-10 is a small molecule apoptotic PET probe for cancer studies. Here we report a novel multi-step synthesis of the diethyl ester of ML-10 in excellent yields via fluorination using Xtal-Fluor-E. In addition, a one-pot radiosynthesis of the diethyl ester of [(18)F]ML-10 from nucleophilic [(18)F]fluoride was completed in 23% radiochemical yield (decay corrected). The radiochemical purity of the product was ≥99%. The diethyl ester of [(18)F]ML-10 was used in vivo to detect apoptosis in the testes of mice. In parallel studies, the dansyl-ML-10 diethyl ester was prepared and used to detect apoptotic cells in an in vitro cell based assay.
[(18)F]ML-10的二乙酯是一种用于癌症研究的小分子凋亡正电子发射断层显像（PET）探针。在此，我们报告了一种通过使用Xtal-Fluor-E进行氟化反应，以优异产率合成ML-10二乙酯的新型多步合成方法。此外，由亲核性[(18)F]氟化物一锅法放射性合成[(18)F]ML-10的二乙酯，放射化学产率为23%（衰变校正）。产物的放射化学纯度≥99%。[(18)F]ML-10的二乙酯用于体内检测小鼠睾丸中的细胞凋亡。在平行研究中，制备了丹磺酰-ML-10二乙酯，并用于基于体外细胞的分析中检测凋亡细胞。
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