Development and in vitro characterization of a novel bifunctional μ-agonist/δ-antagonist opioid tetrapeptide.

@article{Purington2011DevelopmentAI,
  title={Development and in vitro characterization of a novel bifunctional μ-agonist/δ-antagonist opioid tetrapeptide.},
  author={Lauren C. S. Purington and Katarzyna Sobczyk-Kojiro and Irina D. Pogozheva and John R. Traynor and Henry I. Mosberg},
  journal={ACS chemical biology},
  year={2011},
  volume={6 12},
  pages={1375-81}
}
The development of tolerance to and dependence on opioid analgesics greatly reduces their long-term usefulness. Previous studies have demonstrated that co-administration of a μ-opioid receptor (MOR) agonist and δ-opioid receptor (DOR) antagonist can decrease MOR agonist-induced tolerance and dependence development after chronic exposure. Clinically, a single ligand displaying multiple efficacies (e.g., MOR agonism concurrently with DOR antagonism) would be of increased value over two drugs… CONTINUE READING

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