Pretze M, Wängler C, Wängler B
Molecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.
Biomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, Germany.
Biomed Res Int. 2014;2014:674063. doi: 10.1155/2014/674063. Epub 2014 May 28.
For many years, the main application of [(18)F]F-DOPA has been the PET imaging of neuropsychiatric diseases, movement disorders, and brain malignancies. Recent findings however point to very favorable results of this tracer for the imaging of other malignant diseases such as neuroendocrine tumors, pheochromocytoma, and pancreatic adenocarcinoma expanding its application spectrum. With the application of this tracer in neuroendocrine tumor imaging, improved radiosyntheses have been developed. Among these, the no-carrier-added nucleophilic introduction of fluorine-18, especially, has gained increasing attention as it gives [(18)F]F-DOPA in higher specific activities and shorter reaction times by less intricate synthesis protocols. The nucleophilic syntheses which were developed recently are able to provide [(18)F]F-DOPA by automated syntheses in very high specific activities, radiochemical yields, and enantiomeric purities. This review summarizes the developments in the field of [(18)F]F-DOPA syntheses using electrophilic synthesis pathways as well as recent developments of nucleophilic syntheses of [(18)F]F-DOPA and compares the different synthesis strategies regarding the accessibility and applicability of the products for human in vivo PET tumor imaging.
多年来,[(18)F]F-DOPA的主要应用是对神经精神疾病、运动障碍和脑恶性肿瘤进行PET成像。然而,最近的研究结果表明,这种示踪剂在对神经内分泌肿瘤、嗜铬细胞瘤和胰腺腺癌等其他恶性疾病进行成像时效果非常好,从而扩大了其应用范围。随着这种示踪剂在神经内分泌肿瘤成像中的应用,已经开发出了改进的放射性合成方法。其中,特别是无载体添加的氟-18亲核引入法,因其通过不太复杂的合成方案以更高的比活度和更短的反应时间得到[(18)F]F-DOPA而受到越来越多的关注。最近开发的亲核合成方法能够通过自动化合成以非常高的比活度、放射化学产率和对映体纯度提供[(18)F]F-DOPA。本文综述了使用亲电合成途径的[(18)F]F-DOPA合成领域的进展以及[(18)F]F-DOPA亲核合成的最新进展,并比较了不同合成策略在产品用于人体PET肿瘤成像的可及性和适用性方面的差异。