Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of health (NIH), Bethesda, MD 20892, USA.
Curr Drug Metab. 2010 Jul;11(6):483-93. doi: 10.2174/138920010791636167.
Positron emission tomography (PET) is a very sensitive molecular imaging technique that when employed with an appropriate radioligand has the ability to quantititate physiological processes in a non-invasive manner. Since the imaging technique detects all radioactive emissions in the field of view, the presence and biological activity of radiolabeled metabolites must be determined for each radioligand in order to validate the utility of the radiotracer for measuring the desired physiological process. Thus, the identification of metabolic profiles of radiolabeled compounds is an important aspect of design, development, and validation of new radiopharmaceuticals and their applications in drug development and molecular imaging. Metabolite identification for different chemical classes of radiopharmaceuticals allows rational design to minimize the formation and accumulation of metabolites in the target tissue, either through enhanced excretion or minimized metabolism. This review will discuss methods for identifying and quantitating metabolites during the pre-clinical development of radiopharmaceuticals with special emphasis on the application of LC/MS.
正电子发射断层扫描（PET）是一种非常敏感的分子成像技术，当与适当的放射性配体一起使用时，它能够以非侵入性的方式定量生理过程。由于成像技术检测视野中的所有放射性发射，因此必须确定每个放射性配体的放射性标记代谢物的存在和生物活性，以验证示踪剂用于测量所需生理过程的效用。因此，放射性化合物代谢谱的鉴定是设计、开发和验证新放射性药物及其在药物开发和分子成像中的应用的一个重要方面。不同化学类别的放射性药物的代谢产物鉴定允许通过增强排泄或最小化代谢来合理设计，以最小化目标组织中代谢物的形成和积累。本综述将讨论在放射性药物的临床前开发过程中识别和定量代谢产物的方法，特别强调 LC/MS 的应用。
