Receptor Occupancy of the κ-Opioid Antagonist LY2456302 Measured with Positron Emission Tomography and the Novel Radiotracer 11C-LY2795050

@article{Naganawa2016ReceptorOO,
  title={Receptor Occupancy of the $\kappa$-Opioid Antagonist LY2456302 Measured with Positron Emission Tomography and the Novel Radiotracer 11C-LY2795050},
  author={Mika Naganawa and Gemma L. Dickinson and Ming-Qiang Zheng and Shannan Henry and François Vandenhende and Jennifer Wright Witcher and Robert L. Bell and Nabeel B. Nabulsi and Shu-Fei Lin and Jim R Ropchan and Alexander Neumeister and Mohini Ranganathan and Johannes T. Tauscher and Yiyun Huang and Richard E. Carson},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  year={2016},
  volume={356},
  pages={260 - 266}
}
The κ-opioid receptor (KOR) is thought to play an important therapeutic role in a wide range of neuropsychiatric and substance abuse disorders, including alcohol dependence. LY2456302 is a recently developed KOR antagonist with high affinity and selectivity and showed efficacy in the suppression of ethanol consumption in rats. This study investigated brain penetration and KOR target engagement after single oral doses (0.5–25 mg) of LY2456302 in 13 healthy human subjects. Three positron emission… 

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