Synthesis and Evaluation of 11C-LY2795050 as a κ-Opioid Receptor Antagonist Radiotracer for PET Imaging

@article{Zheng2013SynthesisAE,
  title={Synthesis and Evaluation of 11C-LY2795050 as a $\kappa$-Opioid Receptor Antagonist Radiotracer for PET Imaging},
  author={Ming-Qiang Zheng and Nabeel B. Nabulsi and Su Jin Kim and Giampaolo Tomasi and Shu-Fei Lin and Charles Mitch and Steven Quimby and Vanessa N. Barth and Karen Rash and John Masters and Antonio Navarro and Eric Seest and Evan D. Morris and Richard E. Carson and Yiyun Huang},
  journal={The Journal of Nuclear Medicine},
  year={2013},
  volume={54},
  pages={455 - 463}
}
Kappa-opioid receptors (KOR) are believed to be involved in the pathophysiology of depression, anxiety disorders, drug abuse, and alcoholism. To date, only 1 tracer, the KOR agonist 11C-GR103545, has been reported to be able to image KOR in primates. The goal of the present study was to synthesize the selective KOR antagonist 11C-LY2795050 and evaluate its potential as a PET tracer to image KOR in vivo. Methods: The in vitro binding affinity of LY2795050 was measured in radioligand competition… 

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