Emetic activity of N-substituted norapomorphines.
Norapomorphine and ten of its N-substituted derivatives were prepared by modifications of procedures described earlier. In a dog emesis test the N-ethyl and N-n-propyl compounds had minimum effective doses of 0.00025 and 0.0005 mg/kg, respectively, when administered iv, sc, or im. In a modified Irwin mouse profile screen the minimum effective iv dose was 0.013 mg/kg for the N-ethyl and 0.0024 mg/kg for the N-n-propyl compound; percutaneous absorption was also observed in mice. All compounds examined caused the stereotyped apomorphine behavior syndrome but hypotensive effects were not serious.
D000818:Animals; D001058:Apomorphine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D003864:Depression, Chemical; D004285:Dogs; D004639:Emetics / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D000882:Haplorhini; D006801:Humans; D008297:Male; D051379:Mice; D013239:Stereotyped Behavior / Q000187:drug effects; D013268:Stimulation, Chemical
D004639:Emetics; D001058:Apomorphine