N-Alkyl derivatives of (.+-.)-.alpha.-methyldopamine

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 anima...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1979-08, Vol.22 (8), p.901-907
Main Authors: Cannon, Joseph G, Perez, Zurilma, Long, John Paul, Rusterholz, David B, Flynn, Jan R, Costall, Brenda, Fortune, David H, Naylor, Robert J
Format: Article
Language:English
Subjects:
Animals
Cats
Deoxyepinephrine - analogs & derivatives
Deoxyepinephrine - chemical synthesis
Deoxyepinephrine - pharmacology
Dogs
Dopamine - analogs & derivatives
Heart Rate - drug effects
Humans
In Vitro Techniques
Injections
Mice
Motor Activity - drug effects
Myocardial Contraction - drug effects
Nucleus Accumbens
Rats
Stereotyped Behavior - drug effects
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00194a003