Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a µ-agonist δ-antagonist and δ-inverse agonists

@article{Cheng2007OpioidLW,
  title={Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a µ-agonist $\delta$-antagonist and $\delta$-inverse agonists},
  author={K. Cheng and I. J. Kim and Mei-Jing Lee and S. Adah and Tyler J. Raymond and E. Bilsky and M. Aceto and E. May and L. Harris and A. Coop and C. Dersch and R. Rothman and A. E. Jacobson and K. Rice},
  journal={Organic and Biomolecular Chemistry},
  year={2007},
  volume={5},
  pages={1177-1190}
}
Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylethyl moiety on the nitrogen atom, were synthesized and their binding affinity to the µ-, δ-, and κ-opioid receptors was examined. The higher affinity ligands were further examined in the [35S]GTPγS assay to study their function and efficacy. 3-((1R… Expand

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