Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics

@article{Li2019DevelopmentAI,
  title={Development and In Vivo Evaluation of a $\kappa$-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics},
  author={Songye Li and Ming-Qiang Zheng and Mika Naganawa and Sujin Kim and Hong Gao and Michael Kapinos and David C Labaree and Yiyun Huang},
  journal={The Journal of Nuclear Medicine},
  year={2019},
  volume={60},
  pages={1023 - 1030}
}
Studies have shown κ-opioid receptor (KOR) abnormalities in addictive disorders, other central nervous system diseases, and Alzheimer’s disease. We have developed the first set of agonist 11C-GR103545 and antagonist 11C-LY2795050 radiotracers for PET imaging of KOR in humans. Nonetheless, 11C-GR103545 displays protracted uptake kinetics and is not an optimal radiotracer. Here, we report the development and evaluation of 11C-methyl-(R)-4-(2-(3,4-dichlorophenyl)acetyl)-3-((diethylamino)methyl… 

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