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

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.

• Authors: A Bianchetti, A Giudice, N Picerno, P Carminati
• Journal: Life sciences (Life Sci) 1982 Nov 15-22 Vol. 31 Issue 20-21 Pg. 2261-4 ISSN: 0024-3205 [Print] Netherlands
• PMID: 6186879 (Publication Type: Journal Article)

Chemical References

• Levallorphan
• Morphine
• Oxymorphone
• Hydromorphone

Topics

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