N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole

Bioorg Med Chem Lett. 2000 Nov 6;10(21):2449-51. doi: 10.1016/s0960-894x(00)00479-0.

Abstract

The position of the indole in the indolomorphinans, which includes the delta opioid antagonist naltrindole, is considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be mu preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands.

MeSH terms

  • Analgesics / chemical synthesis
  • Analgesics / chemistry
  • Analgesics / metabolism
  • Analgesics / pharmacology
  • Animals
  • Mice
  • Molecular Structure
  • Morphine / chemical synthesis*
  • Morphine / chemistry
  • Morphine / metabolism*
  • Morphine / pharmacology
  • Morphine Derivatives
  • Naltrexone / analogs & derivatives*
  • Naltrexone / chemistry
  • Naltrexone / metabolism
  • Naltrexone / pharmacology
  • Narcotic Antagonists / chemical synthesis*
  • Narcotic Antagonists / chemistry
  • Narcotic Antagonists / metabolism*
  • Narcotic Antagonists / pharmacology
  • Pain Measurement
  • Receptors, Opioid, mu / metabolism*

Substances

  • Analgesics
  • Morphine Derivatives
  • N-Cyclohexylethyl-N-noroxymorphindole
  • Narcotic Antagonists
  • Receptors, Opioid, mu
  • Naltrexone
  • Morphine
  • naltrindole