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

被引：24

作者：

Cai, Zhengxin ^{[1
]}

Li, Songye ^{[1
]}

Pracitto, Richard ^{[1
]}

Navarro, Antonio ^{[2
]}

Shirali, Anupama ^{[1
]}

Ropchan, Jim ^{[1
]}

Huang, Yiyun ^{[1
]}

机构：

[1] Yale Univ, Dept Radiol & Biomed Imaging, PET Ctr, New Haven, CT 06520 USA

[2] Eli Lilly & Co, Indianapolis, IN 46285 USA

来源：

ACS CHEMICAL NEUROSCIENCE | 2017年 / 8卷 / 01期

关键词：

Kappa opioid receptor; PET; fluorination; nonhuman primate; iodonium ylide; microfluidic; TEST-RETEST REPRODUCIBILITY; SELECTIVE ANTAGONIST; LATE-STAGE; IN-VIVO; RADIOTRACER; SINGLE; RADIOFLUORINATION; AGONIST; C-11-LY2795050; LY2456302;

D O I：

10.1021/acschemneuro.6b00268

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 C-11-labeled antagonist radiotracers with high affinity and selectivity toward KOR. What is limiting their wide applications is the short half-life of (11)-IC. Herein, we report the synthesis of a first F-18-labeled KOR antagonist radiotracer and the initial PET imaging study in a nonhuman primate.

引用

页码：12 / 16

页数：5

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