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  • Title: 3-substituted-1,2-benzisoxazoles: novel antipsychotic agents.
    Author: Davis L, Effland RC, Klein JT, Dunn RW, Geyer HM, Petko WW.
    Journal: Drug Des Discov; 1992 Feb; 8(3):225-40. PubMed ID: 1356026.
    Abstract:
    A series of 3-substituted-6-fluoro-1,2-benzisoxazoles (II) was synthesized and evaluated for potential antipsychotic activity. Many of the compounds displayed potent antipsychotic-like activity in the apomorphine induced climbing in mice (CMA) or spiroperidol binding assays, and compound 42 (HRP 392, 1-[3-(6-fluoro-1,2-benzisoxazol-3-yl)propyl]-4-(2-methoxyphenyl) piperazine) was selected for more detailed antipsychotic evaluation in a battery of preclinical assays. The results of these studies suggests that 42 is a potential antipsychotic drug with less propensity for EPS than some standard neuroleptics in monkeys. The compound was advanced for toxicological evaluation.
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