1996•Journal of Medicinal ChemistryOpen access
3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents
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
Open full text 90 citations
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.