κ-阿片受体
敌手
Pet成像
阿片受体
药理学
上瘾
限制
卡帕
类阿片
受体
医学
化学
心理学
神经科学
内科学
正电子发射断层摄影术
哲学
工程类
机械工程
语言学
作者
Zhengxin Cai,Songye Li,Richard Pracitto,Arturo Anadón Navarro,Anupama Shirali,Jim Ropchan,Yiyun Huang
标识
DOI:10.1021/acschemneuro.6b00268
摘要
Kappa opioid receptor (KOR) antagonists are potential drug candidates for diseases such as treatment-refractory depression, anxiety, and addictive disorders. PET imaging radiotracers for KOR can be used in occupancy study to facilitate drug development, and to investigate the roles of KOR in health and diseases. We have previously developed two 11C-labeled antagonist radiotracers with high affinity and selectivity toward KOR. What is limiting their wide applications is the short half-life of 11C. Herein, we report the synthesis of a first 18F-labeled KOR antagonist radiotracer and the initial PET imaging study in a nonhuman primate.
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