Development of ^(18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

作     者：Peter Brust Jrg van den Hoff Jrg Steinbach 

作者机构：Helmholtz-Zentrum Dresden-RossendorfInstitute of Radiopharmaceutical Cancer ResearchPermoserstrasse 15Leipzig04318Germany 

出 版 物：《Neuroscience Bulletin》 (神经科学通报（英文版）)

年 卷 期：2014年第30卷第5期

页      面：777-811页

核心收录：

学科分类：0831[工学-生物医学工程（可授工学、理学、医学学位）] 100207[医学-影像医学与核医学] 1006[医学-中西医结合] 1002[医学-临床医学] 1001[医学-基础医学(可授医学、理学学位)] 08[工学] 1010[医学-医学技术（可授医学、理学学位）] 100106[医学-放射医学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：ShanghaiInstitutesforBiologicalSciences CASandSpringer-VerlagBerlinHeidelberg2014 

主　　题：Alzheimer's disease autoradiography blood-brain barrier brain tumor cholinergic system kinetic modeling metabolism molecular imaging neurodegeneration positron emission tomography precursor psychiatric disorder radiotracer sigma receptor 

摘      要：Positron emission tomography （PET） is an in vivo molecular imaging tool which is widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases. PET uses biomolecules as probes which are labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiotracers. Fluorine-18 is a radionuclide routinely used in the radiolabeling of neuroreceptor ligands for PET because of its favorable half-life of 109.8 min. The delivery of such radiotracers into the brain provides images of transport, metabolic, and neurotransmission processes on the molecular level. After a short introduction into the principles of PET, this review mainly focuses on the strategy of radiotracer development bridging from basic science to biomedical application. Successful radiotracer design as described here provides molecular probes which not only are useful for imaging of human brain diseases, but also allow molecular neuroreceptor imaging studies in various small-animal models of disease, including genetically- engineered animals. Furthermore, they provide a powerful tool for in vivo pharmacology during the process of pre-clinical drug development to identify new drug targets, to investigate pathophysiology, to discover potential drug candidates, and to evaluate the pharmacokinetics and pharmacodynamics of drugs in vivo.