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

  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},
  • 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
    73 Citations
    Morphine‐6β‐glucuronide has a higher efficacy than morphine as a mu‐opioid receptor agonist in the rat locus coeruleus
    • 26
    • Highly Influenced
    Opioid Partial Agonist Effects of 3-O-Methylnaltrexone in Rhesus Monkeys
    • 5
    • PDF
    Morphine‐6‐glucuronide: Actions and mechanisms
    • 70
    High levels of morphine-6-glucuronide in street heroin addicts
    • 31
    Functional blockade of opioid analgesia by orphanin FQ/nociceptin.
    • 53
    Repeated Exposures to Heroin and/or Cadmium Alter the Rate of Formation of Morphine Glucuronides in the Rat
    • 23
    • PDF


    Pharmacological characterization of morphine-6 beta-glucuronide, a very potent morphine metabolite.
    • 362
    Pharmacodynamics of subcutaneously administered diacetylmorphine, 6-acetylmorphine and morphine in mice.
    • J. Umans, C. Inturrisi
    • Chemistry, Medicine
    • The Journal of pharmacology and experimental therapeutics
    • 1981
    • 116
    Morphine-6-glucuronide, a potent mu agonist.
    • 352
    Analgesic effect of morphine glucuronides.
    • 357
    The Pharmacokinetics of Heroin in Patients with Chronic Pain
    • 221