摘要
正电子发射型计算机断层显像技术(positron emission tomography,PET)在中枢神经系统(CNS)药物研发中发挥重要作用。PET可以定量研究CNS药物在脑组织体液中的生物分布,药代动力学,与靶点相互作用,提供药物浓度与受体占有率的定量关系。本综述总结了PET在CNS药物研发中的定量分析手段,包括药代动力学分析以及受体占有率分析中常用的方法与数学公式。同时,本综述也总结了PET在CNS新药研发中的应用,为后续CNS的新药研发提供新的思路与方向。
Positron emission tomography(PET)now plays an important role in the research and development(R&D)of central nervous system(CNS)drugs.PET could characterize the biodistribution,pharmacokinetics,and receptor binding of CNS drugs quantitatively.The present review summarized the quantitative methods of PET used in the pharmacokinetics and receptor occupancy analysis of CNS drugs.Moreover,the present review listed various applications of PET supporting R&D of CNS drugs,which could provide a new direction for the R&D of CNS drugs.
作者
李思泽
黄琪
武晓捷
王少楠
管一晖
谢芳
张菁
LI Size;HUANG Qi;WU Xiaojie;WANG Shaonan;GUAN Yihui;XIE Fang;ZHANG Jing(Phase I Clinical Research Center,Huashan Hospital,Fudan University,Shanghai 200040,China;Department of Nuclear Medicine&PET Center,Huashan Hospital,Fudan University,Shanghai 200235,China;National Center for Neurological Disorders(Huashan),Shanghai 200040,China;Translational Medicine&Clinical Pharmacology,Boehringer Ingelheim,The Chinese Market,Shanghai 200040,China;Institue of Antibiotics,Huashan Hospital,Fudan University,Shanghai 200040,China)
出处
《中国临床药理学与治疗学》
CAS
CSCD
北大核心
2024年第3期316-327,共12页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
科技部“重大新药创制”科技重大专项(2017ZX09304005)。
关键词
正电子发射型计算机断层扫描
中枢神经系统
新药研发
药代动力学
受体占有率
positron emission tomography
central nervous system
the research and development of new drugs
pharmacokinetics
receptor occupancy
