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Summary
Novelty: Novel benzodioxan derivatives useful as antipsychotic and anxiolytic agents are disclosed. The compounds are useful in the treatment of a variety of CNS disorders, such as depression, schizophrenia and paranoia.
Biology: The affinity of the compounds for the dopamine D2 receptor and the serotonin 5-HT1A receptor were determined according to the methods of Fields (Brain Res. (1977) 136:578) and Hall (J. Neurochem. (1985) 44:1685). One compound gave 83% inhibition for D2 binding and 100% inhibition for 5-HT1A binding at 0.1 μM.
Chemistry: Syntheses of the compounds are described in nine examples. N-Methyl-[2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]-amino]ethyltricyclo[3 .3.1.1 (3,7)]-decane-1-carboxamide is one of nine specifically claimed compounds.
Structure: 