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ACS Chem Neurosci. 2017 Jan 18;8(1):12-16. doi: 10.1021/acschemneuro.6b00268. Epub 2016 Oct 20.

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

Author information

1
PET Center, Department of Radiology and Biomedical Imaging, Yale University , New Haven, Connecticut 06520, United States.
2
Eli Lilly and Company , Indianapolis, Indiana 46285, United States.

Abstract

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.

KEYWORDS:

Kappa opioid receptor; PET; fluorination; iodonium ylide; microfluidic; nonhuman primate

PMID:
27741398
DOI:
10.1021/acschemneuro.6b00268
[Indexed for MEDLINE]

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