5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone: a long-lasting mu-opioid receptor antagonist devoid of agonist properties

Eur J Pharmacol. 1993 Jan 5;230(1):129-30. doi: 10.1016/0014-2999(93)90423-f.

Abstract

5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone (MET-CAMO) suppressed morphine-induced antinociception but had no effect on antinociception mediated by delta- or kappa-opioid receptors after a single i.c.v. 1-nmol injection from 8 to 72 h before testing. MET-CAMO had no agonist effects in the mouse tail-flick assay in doses up to 100 nmol. MET-CAMO is the first N-methylated morphine derivative which shows such long-lasting mu-selective opioid receptor antagonism with no agonistic properties.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Analgesics / pharmacology
  • Animals
  • Hydromorphone / analogs & derivatives*
  • Hydromorphone / pharmacology
  • Injections, Intraventricular
  • Mice
  • Morphine / antagonists & inhibitors
  • Morphine / pharmacology
  • Pain Measurement / drug effects
  • Reaction Time / drug effects
  • Receptors, Opioid, mu / antagonists & inhibitors*
  • Receptors, Opioid, mu / drug effects

Substances

  • Analgesics
  • Receptors, Opioid, mu
  • 5-methyl-14-(4-nitrocinnamoylamino)-7,8-dihydromorphinone
  • Morphine
  • Hydromorphone