1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents

The design and synthesis of a series of potential atypical antipsychotic agents based on the structure of 1-naphthylpiperazine are described. The incorporation of dopamine antagonist activity into the parent structure was achieved with heterocyclic surrogates for the catechol moiety of dopamine. Com...

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Veröffentlicht in:	Journal of medicinal chemistry 1991-06, Vol.34 (6), p.1860-1866
Hauptverfasser:	Lowe, John A, Seeger, Thomas F, Nagel, Arthur A, Howard, Harry R, Seymour, Patricia A, Heym, James H, Ewing, Frank E, Newman, Michael E, Schmidt, Anne W
Format:	Artikel
Sprache:	eng
Schlagworte:	8-Hydroxy-2-(di-n-propylamino)tetralin Amphetamines - pharmacology Animals Antipsychotic Agents Apomorphine - pharmacology Autoradiography Behavior, Animal - drug effects Dopamine Antagonists Haloperidol - pharmacology Ketanserin - metabolism Locomotion - drug effects Male Piperazines - pharmacology Prazosin - metabolism Rats Rats, Inbred Strains Structure-Activity Relationship Tetrahydronaphthalenes - metabolism
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Zusammenfassung:	The design and synthesis of a series of potential atypical antipsychotic agents based on the structure of 1-naphthylpiperazine are described. The incorporation of dopamine antagonist activity into the parent structure was achieved with heterocyclic surrogates for the catechol moiety of dopamine. Compound 4b from this series showed a biochemical profile that translated to behavioral activity in the rat predictive of an antipsychotic agent with a low propensity to cause extrapyramidal side effects in man.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00110a016