Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.

@article{Botros1989OpioidAA,
  title={Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.},
  author={Sanaa Botros and Andrzej Wojciech Lipkowski and David L. Larson and Peter A. Stark and Akihiro Takemori and Philip S. Portoghese},
  journal={Journal of medicinal chemistry},
  year={1989},
  volume={32 9},
  pages={2068-71}
}
A series of beta-naltrexamine and beta-oxymorphamine derivatives that contain ionizable moieties coupled to the 6 beta-amino group were synthesized in an effort to develop antagonists and agonists that have negligible access into the central nervous system (CNS). Among the beta-naltrexamine derivatives 1-7, all displayed partial agonism on the guinea pig ileal longitudinal muscle preparation except for aspartyl derivative 6, which was a full agonist with activity in the range of morphine. The… CONTINUE READING

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