期刊
MOLECULAR IMAGING AND BIOLOGY
卷 15, 期 1, 页码 12-18出版社
SPRINGER
DOI: 10.1007/s11307-012-0574-y
关键词
Fluorine-18; Radiosynthesis; Radiopharmaceuticals; Apoptosis; ML-10; Positron emission tomography; PET
资金
- Region de Basse-Normandie
- Commissariat a l'energie atomique et aux energies alternatives (CEA)
[F-18]ML-10 is the most advanced radiopharmaceutical for the clinical imaging of the apoptosis phenomenon by PET. The preparation of this radiopharmaceutical on a commercial radiosynthesis module and the requested quality controls for its release are presented herein. ML-10 as reference and its mesyloxy derivative as precursor for labelling with fluorine-18 were prepared. [F-18]ML-10 was synthesized via a [F-18]fluorine-de-mesyloxy aliphatic nucleophilic substitution via a GE TRACERLabA (R) FX-FN module. Quality controls were performed. The labelling precursor was obtained in a four step synthesis in 28 % overall yield affording ML-10 in two steps (88 % yield). Pure [F-18]ML-10 was obtained with a decay corrected yield of 39.8 % +/- 8.4 % (n = 7) in 70 min and a specific activity of 235 +/- 85 GBq/mu mol at the end of synthesis. [F-18]ML-10 was prepared on a widely available automated module and passed the quality control. A LC/MS method was developed to measure specific radioactivity.
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