Novel 18F-Labeled κ-Opioid Receptor Antagonist as PET Radiotracer: Synthesis and In Vivo Evaluation of 18F-LY2459989 in Nonhuman Primates

  title={Novel 18F-Labeled $\kappa$-Opioid Receptor Antagonist as PET Radiotracer: Synthesis and In Vivo Evaluation of 18F-LY2459989 in Nonhuman Primates},
  author={Songye Li and Zhengxin Cai and Ming-Qiang Zheng and Daniel Holden and Mika Naganawa and Shu-Fei Lin and Jim R Ropchan and David C Labaree and Michael Kapinos and Teresa Lara-Jaime and Antonio Navarro and Yiyun Huang},
  journal={The Journal of Nuclear Medicine},
  pages={140 - 146}
The κ-opioid receptor (KOR) has been implicated in depression, addictions, and other central nervous system disorders and, thus, is an important target for drug development. We previously developed several 11C-labeled PET radiotracers for KOR imaging in humans. Here we report the synthesis and evaluation of 18F-LY2459989 as the first 18F-labeled KOR antagonist radiotracer in nonhuman primates and its comparison with 11C-LY2459989. Methods: The novel radioligand 18F-LY2459989 was synthesized by… 

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