PET Center, the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310009, China.
Department of Chemistry, Zhejiang University, Hangzhou 310058, China.
J Zhejiang Univ Sci B. 2019;20(11):865-867. doi: 10.1631/jzus.B1900535.
Positron emission tomography (PET) is a powerful non-invasive molecular imaging technique for the early detection, characterization, and "real-time" monitoring of disease, and for investigating the efficacy of drugs (Phelps, 2000; Ametamey et al., 2008). The development of molecular probes bearing short-lived positron-emitting radionuclides, such as F (half-life 110 min) or C (half-life 20 min), is crucial for PET imaging to collect in vivo metabolic information in a time-efficient manner (Deng et al., 2019). In this regard, one of the main challenges is rapid synthesis of radiolabeled probes by introducing the radionuclides into pharmaceuticals as soon as possible before injection for a PET scan. Although many potential PET probes have been discovered, only a handful can satisfy the demand for a highly efficient synthesis procedure that achieves radiolabeling and delivery for imaging within 1-2 radioisotope half-lives. Only a few probes, such as 2-deoxy-2-[F]fluoro-D-glucose (F-FDG) and [F]fluorodopa, are routinely produced on a commercial scale for daily clinical diagnosis (Grayson et al., 2018; Carollo et al., 2019).
正电子发射断层扫描(PET)是一种强大的非侵入性分子成像技术,可用于早期检测、特征描述和疾病的“实时”监测,并用于研究药物的疗效(Phelps,2000;Ametamey 等人,2008)。携带短寿命正电子发射放射性核素的分子探针的开发对于 PET 成像至关重要,这样可以有效地收集体内代谢信息(Deng 等人,2019)。在这方面,主要挑战之一是通过在注射用于 PET 扫描之前尽快将放射性核素引入药物中,快速合成放射性标记探针。尽管已经发现了许多潜在的 PET 探针,但只有少数能够满足高效合成程序的需求,该程序能够在 1-2 个放射性核素半衰期内实现放射性标记和成像。只有少数探针,如 2-脱氧-2-[F]氟-D-葡萄糖(F-FDG)和[F]氟多巴,才能在商业规模上常规生产,用于日常临床诊断(Grayson 等人,2018;Carollo 等人,2019)。