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3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents

Harry R. Howard,* John A. Lowe, III,* Thomas F. Seeger, Patricia A. Seymour, Stevin H. Zorn, Patrick R. Maloney, Frank E. Ewing, Michael E. Newman, Anne W. Schmidt, Jerome S. Furman, Gwendolyn L. Robinson, Elisa Jackson, Celeste Johnson, and Jean Morrone

Central Research Division, Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340

J. Med. Chem., 1996, 39 (1), pp 143–148

DOI: 10.1021/jm950625l

Publication Date (Web): January 5, 1996

In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.

Abstract

A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D₂ and 5-HT_2A antagonist activity was investigated as an approach to a novel atypical antipsychotic agent. The in vitro profile of 8e from this series is a combination of D₂ receptor affinity comparable to the typical antipsychotic agent haloperidol and a 5-HT_2A/D₂ ratio comparable to the atypical agent clozapine. In vivo 8e possesses activity consistent with an efficacious antipsychotic agent with less tendency to induce extrapyramidal side effects in man.

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Published In Issue January 05, 1996
Received August 22, 1995

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Article

3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents

Abstract

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Recommend & Share

Related Content

Effect of Linking Bridge Modifications on the Antipsychotic Profile of Some Phthalimide and Isoindolinone Derivatives

Recent Progress in Development of Dopamine Receptor Subtype-Selective Agents: Potential Therapeutics for Neurological and Psychiatric Disorders

1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents

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