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J Med Chem. 1996 Jan 5;39(1):143-8.

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.

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1
Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA.

Abstract

A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A 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-HT2A/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.

PMID:
8568801
DOI:
10.1021/jm950625l
[Indexed for MEDLINE]
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