Citatepine is an antagonist of dopamine receptors. It attenuated dopamine-agonist induced behavioral stimulation (stereotypies in rats or climbing in mice). The compound displayed preferential action on hippocampal DA receptors as compared to the striatum. In addition, it shows antihistaminergic, antiserotonergic, anticholinergic and adrenolytic effects. The drug was investigated in the clinic for the treatment of schizophrenia. It was expected that this drug would show an antipsychotic efficacy in doses not causing extrapyramidal side-effects. This expectation has not been fulfilled.