title: N-Alkyl derivatives of (+/-)-alpha-methyldopamine.
abstract: A series of N-alkylated alpha-methyldopamine derivatives has been prepared for comparison of their biological effects with those of semirigid dopamine congeners derived from 2-aminotetralin systems. All of the alpha-methyldopamine derivatives were inert as dopaminergic agonists in a variety of animal assays, both centrally and peripherally, although certain compounds produced powerful and prolonged locomotor hyperactivity on intra-accumbens injection in mice, by indirect mechanism(s). A rationalization, based upon conformational analysis, is presented for the lack of direct dopaminergic agonist activity of alpha-methyldopamine derivatives.
mesh_terms: D000818:Animals; D002415:Cats; D003846:Deoxyepinephrine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004285:Dogs; D004298:Dopamine / Q000031:analogs & derivatives*; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007267:Injections; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D009714:Nucleus Accumbens; D051381:Rats; D013239:Stereotyped Behavior / Q000187:drug effects
chemical_list: D003846:Deoxyepinephrine; D004298:Dopamine