3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents
Journal of Medicinal Chemistry1996Vol. 39(1), pp. 143–148
Citations Over TimeTop 10% of 1996 papers
Harry Howard, John Lowe, Thomas Seeger, Patricia A. Seymour, Stevin H. Zorn, Patrick Maloney, Frank E. Ewing, Michael E. Newman, Anne W. Schmidt, Jerome S. Furman, Gwendolyn L. Robinson, Elisa R. Jackson, Celeste Johnson, Jean Morrone
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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