3‐Methoxynaltrexone, a selective heroin/morphine‐6β‐glucuronide antagonist

@article{Brown19973MethoxynaltrexoneAS,
  title={3‐Methoxynaltrexone, a selective heroin/morphine‐6β‐glucuronide antagonist},
  author={George P Brown and K. Yang and M. King and Grace C Rossi and L. Leventhal and Albert J. Chang and Gavril W. Pasternak},
  journal={FEBS Letters},
  year={1997},
  volume={412}
}
  • George P Brown, K. Yang, +4 authors Gavril W. Pasternak
  • Published 1997
  • Medicine, Biology
  • FEBS Letters
  • Recent work has suggested that heroin and morphine‐6β‐glucuronide (M6G) both act through a novel mu opioid receptor subtype distinct from those mediating morphine's actions. This very high affinity 3H‐M6G site is selectively competed by 3‐methoxynaltrexone. In vivo, 3‐methoxynaltrexone (2.5 ng, i.c.v.) selectively antagonizes the analgesic actions of heroin and M6G without interfering with mu (morphine and [d‐Ala2,MePhe4,Gly(ol)5]enkephalin), delta ([d‐Pen2,d‐Pen5]enkephalin), kappa1 (U50,488H… CONTINUE READING
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