Pharmacological actions of levallorphan allyl bromide (CM 32191), a new peripheral narcotic antagonist.
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.
D000818:Animals; D001681:Biological Assay; D003248:Constipation / Q000503:physiopathology*; D005260:Female; D004091:Hydromorphone / Q000031:analogs & derivatives / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D007977:Levallorphan / Q000494:pharmacology*; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects*; D010111:Oxymorphone / Q000494:pharmacology; D013329:Structure-Activity Relationship
D007977:Levallorphan; D009020:Morphine; D010111:Oxymorphone; D004091:Hydromorphone