Pharmacological actions of levallorphan allyl bromide (CM 32191), a new peripheral narcotic antagonist

Life Sci. 1982 Nov;31(20-21):2261-4. doi: 10.1016/0024-3205(82)90133-3.

Abstract

A dissociation of the effects of the newly synthesized quaternary ammonium narcotic antagonist, levallorphan allyl bromide (CM 32191) on morphine-induced analgesia and constipation in the mouse is reported. CM 32191 behaved as a pure morphine antagonist on the "in vitro" preparation of longitudinal muscle of guinea-pig ileum and antagonized dose-dependently the peripherally mediated morphine constipation (ID50:15.6 mg/kg) without significantly affecting morphine analgesia (ID50: greater than 80 mg/kg). Its peripheral selectivity was greater than that of another quaternary ammonium compound, N-methyl naloxone. It is proposed as a useful pharmacological tool to differentiate the peripherally mediated from the centrally mediated effects of opioids.

MeSH terms

  • Animals
  • Biological Assay
  • Constipation / physiopathology*
  • Female
  • Hydromorphone / analogs & derivatives
  • Hydromorphone / pharmacology
  • Ileum / drug effects
  • Ileum / physiology
  • Levallorphan / pharmacology*
  • Mice
  • Morphine / pharmacology
  • Muscle Contraction / drug effects*
  • Oxymorphone / pharmacology
  • Structure-Activity Relationship

Substances

  • Levallorphan
  • Morphine
  • Oxymorphone
  • Hydromorphone