3-BENZISOTHIAZOLYLPIPERAZINE DERIVATIVES AS POTENTIAL ATYPICAL ANTIPSYCHOTIC AGENTS

A series of substituted phenethyl derivatives of 3-benzisothiazolylpip erazine incorporating potent D-2 and 5-HT2A antagonist activity was in vestigated as an approach to a novel atypical antipsychotic agent. The in vitro profile of 8e from this series is a combination of D-2 recep tor affinity comparable to the typical antipsychotic agent haloperidol and a 5-HT2A/D-2 ratio comparable to the atypical agent clozapine. In vivo 8e possesses activity consistent with an efficacious antipsychot ic agent with less tendency to induce extrapyramidal side effects in m an.