Tsukada Hideo
Central Research Laboratory, Hamamatsu Photonics K. K., Hamamatsu, Japan.
Nihon Shinkei Seishin Yakurigaku Zasshi. 2011 Nov;31(5-6):231-7.
Positron emission tomography (PET) is a sophisticated method for the quantitative and noninvasive imaging of biological functions by monitoring the delivery of tracers labeled with positron emitters (1C, 'aN, '"O, and 8F). The distribution and kinetic patterns of a labeled compound in relation to the specific biomolecule in the target tissue are assumed to reflect specific biological functions in the living body. A wide variety of labeled compounds as molecular probes have been developed to measure biochemical and physiological parameters, such as blood flow, glucose and oxygen metabolism, protein synthesis, and neurotransmitter receptor functions. Recently, PET has gradually been introduced into the research field of drug development both in pre-clinical and clinical stages. In the present chapter, the applications of animal PET with small animals (rats and mice) and non-human primates in drug development in the pre-clinical stage will be discussed based on our own experiences. In the course of drug development, the pre-clinical studies with experimental animals are indispensable, and these studies are expected to provide useful information to facilitate the development of drug candidates with more efficacy and fewer adverse effects in the clinical stage with
正电子发射断层扫描(PET)是一种通过监测用正电子发射体(11C、13N、15O和18F)标记的示踪剂的输送情况,对生物功能进行定量和非侵入性成像的精密方法。假定标记化合物在靶组织中相对于特定生物分子的分布和动力学模式反映了活体中的特定生物功能。已经开发出各种各样的标记化合物作为分子探针,用于测量生化和生理参数,如血流量、葡萄糖和氧代谢、蛋白质合成以及神经递质受体功能。最近,PET已逐渐被引入临床前和临床阶段的药物研发领域。在本章中,将根据我们自己的经验,讨论小动物(大鼠和小鼠)和非人灵长类动物PET在临床前阶段药物研发中的应用。在药物研发过程中,用实验动物进行临床前研究是必不可少的,这些研究有望提供有用信息,以便在临床阶段促进开发出疗效更高、副作用更少的候选药物。