The goal of this study was to assess in human liver microsomes the inhibitory capacity of commonly used antipsychotics on the most prominent CYP450 drug metabolizing enzymes (CYP1A2, CYP2C9, CYP2D6, and CYP3A). Chlorpromazine was the only antipsychotic that inhibited CYP1A2 activity (IC50 = 9.5  μ M), whilst levomepromazine, chlorpromazine, and thioridazine significantly decreased CYP2D6-mediat...

NADPH oxidases (NOXs) constitute a family of enzymes generating reactive oxygen species (ROS) and are increasingly recognized as interesting drug targets. Here we investigated the effects of 10 phenothiazine compounds on NOX activity using an extensive panel of assays to measure production of ROS (Amplex red, WST-1, MCLA) and oxygen consumption. Striking differences between highly similar pheno...

Rapid-onset psychotic rebound is uncommon on discontinuation of most antipsychotic drugs, as might be expected for antipsychotic drugs with (hypothetically) indirect actions at their final target receptors. Rapid-onset psychosis is more common on withdrawal of clozapine, which might be expected if its action is direct. Drugs other than clozapine (notably thioridazine) may have hitherto unrecogn...

The breast cancer therapies available are insufficient, especially since first-line treatments, such as paclitaxel, result in drug resistance and their toxicity often limits concentration. Strategies like repurposing beneficial, novel treatments can emerge by drugs that interfere with the dopamine serotonin receptors, thus influence tumor growth. In this study, MTT assay was used to test effica...

We describe a method for quantitative determination of fluphenazine in human plasma, based on gas chromatography of its trimethylsilyl derivative and the use of a structurally similar internal standard. We determined its concentrations in plasma of four patients who were receiving the drug intramuscularly as its decanoate, in doses ranging from 12.5 to 250 mg; the concentrations in the plasma o...

松 木 勝彦 ・岩本 多喜男 In the preceding paper, it was shown that the rat became tolerant to some psycho tropic drugs when blockage of the conditioned avoidance response was estimated as an index of tranquillizing activity (1). In the course of these studies, a statistically signi ficant difference was obtained between male and female rats in the development of tolerance upon the repeated administration...