Duration of Action of a Broad Range of Selective κ-Opioid Receptor Antagonists Is Positively Correlated with c-Jun N-Terminal Kinase-1 Activation

  title={Duration of Action of a Broad Range of Selective $\kappa$-Opioid Receptor Antagonists Is Positively Correlated with c-Jun N-Terminal Kinase-1 Activation},
  author={Erica Melief and Mayumi Miyatake and F. Ivy Carroll and Cécile Béguin and William A. Carlezon and Bruce M. Cohen and Sarah Grimwood and Charles Mitch and Linda M. Rorick-Kehn and Charles Chavkin},
  journal={Molecular Pharmacology},
  pages={920 - 929}
The κ-opioid receptor is a widely expressed G-protein-coupled receptor that has been implicated in biological responses to pain, stress, anxiety, and depression, and its potential as a therapeutic target in these syndromes is becoming increasingly apparent. However, the prototypical selective κ-opioid antagonists have very long durations of action that have been attributed to c-Jun N-terminal kinase (JNK) 1 activation in vivo. To test generality of this proposed noncompetitive mechanism, we… 

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