LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders

@article{RorickKehn2014LY2456302IA,
  title={LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders},
  author={Linda M. Rorick-Kehn and Jeffrey M. Witkin and Michael A. Statnick and Elizabeth Lutz Eberle and Jamie H. McKinzie and Steven D. Kahl and Beth M. Forster and C. K. Lin B. K. L. So J. N. S. Leung H. K. Wong and Xia Li and Robert S Crile and David B Shaw and Allison E. Sahr and Benjamin L. Adams and Steven Quimby and Nuria D{\'i}az and Alma Guadalupe Rojo Jimenez and Concepci{\'o}n Pedregal and Charles Mitch and Kelly L. Knopp and Wesley H. Anderson and Jeffrey W. Cramer and David L Mckinzie},
  journal={Neuropharmacology},
  year={2014},
  volume={77},
  pages={131-144}
}

• Linda M. Rorick-Kehn, Jeffrey M. Witkin, +19 authors David L Mckinzie
• Published 2014 in Neuropharmacology
• DOI:10.1016/j.neuropharm.2013.09.021

Kappa opioid receptors and their endogenous neuropeptide ligand, dynorphin A, are densely localized in limbic and cortical areas comprising the brain reward system, and appear to play a key role in modulating stress and mood. Growing literature indicates that kappa receptor antagonists may be beneficial in the treatment of mood and addictive disorders. However, existing literature on kappa receptor antagonists has used extensively JDTic and nor-BNI which exhibit long-lasting pharmacokinetic… CONTINUE READING

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