Luxen A, Guillaume M, Melega W P, Pike V W, Solin O, Wagner R
Cyclotron, Hôpital Erasme, Université Libre de Bruxelles, Belgium.
Int J Rad Appl Instrum B. 1992 Feb;19(2):149-58. doi: 10.1016/0883-2897(92)90002-g.
This report critically appraises methods for the synthesis of 6-[18F]fluoro-L-3,4-dihydroxyphenylalanine (6-FDOPA) that are based on labelling by non-regioselective electrophilic fluorination, regioselective fluorodemetalation or nucleophilic substitution. Recommendations for the standardization of labelling procedures, the optimization of radiochemical yield and the assurance of product quality and safety are given. Studies of the metabolism of 6-FDOPA in vivo are also reviewed to emphasize the importance of the biochemical component of the development of this tracer for positron emission tomography (PET).
本报告批判性地评估了基于非区域选择性亲电氟化、区域选择性氟脱金属或亲核取代进行标记的6-[¹⁸F]氟-L-3,4-二羟基苯丙氨酸(6-FDOPA)的合成方法。给出了标记程序标准化、放射化学产率优化以及产品质量和安全性保证的建议。还综述了6-FDOPA在体内的代谢研究,以强调该示踪剂用于正电子发射断层扫描(PET)开发中生化成分的重要性。