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. 1996 Jan 5;39(1):143-8.
doi: 10.1021/jm950625l.

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents

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3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents

H R Howard et al. J Med Chem. .

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.

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