Fluorine-18-Labeled Antagonist for PET Imaging of Kappa Opioid Receptors

详细信息    查看全文

• 作者：Zhengxin Cai ; Songye Li ; Richard Pracitto ; Antonio Navarro ; Anupama Shirali ; Jim Ropchan ; Yiyun Huang
• 刊名：ACS Chemical Neuroscience
• 出版年：2017
• 出版时间：January 18, 2017
• 年：2017
• 卷：8
• 期：1
• 页码：12-16
• 全文大小：320K
• ISSN：1948-7193

文摘

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.