Chlorpromazine, haloperidol, fluphenazine, clozapine, risperidone, quetiapine, olanzapine, ziprasidone, and aripiprazole are antipsychotics commonly used in psychiatric medicine. Approximately one third...Full Text Available
Objective: A growing body of data from genetic, immunological and clinical studies indicates an involvement of the immune system in the pathophysiology of schizophrenia and suggests that the modulation of the cytokine system by antipsychotics may be one cause for the improvement of psychotic symptoms. However, the influence of the typical antipsychotics chlorpromazine and haloperidol, and the effect of typical and atypical antipsychotics on the TSST-1-stimulated blood cell secretion of cytokines, and specifically the interleukin (IL)-17 production have not been studied so far, although IL-17 is a leading pro-inflammatory cytokine. Method: We measured levels of IL-1@b, IL-2, IL-4, IL-6, IL-17 and tumor necrosis factor-@a (TNF-@a) in stimulated blood of 10 healthy female subjects in a whole ...
Three regio-isomers of N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, IBP, were prepared and evaluated for their sigma affinities. All three isomers (2, 3, and 4-substituted) showed high affinities for sigma-1 receptors in guinea pig brain membranes (Ki - 1.64 nM, 3.02 nM, 1.70 nM respectively) against ["3H]-(+)-pentazocine, a sigma-1 selective ligand. 2-IBP and 4-IBP showed modest affinities for sigma-2 sites in rat liver (Ki = 29.6 nM. 25.2 nM respectively) against ["3H]DTG in the presence of dextrallorphan to mask sigma-1 sites. The homologous competition binding studies of 4-["1"2"5I]BP in MCF-7 human breast tumor cells showed high affinity dose-dependent binding. Competition binding studies with haloperidol and DTG also showed a high affinity binding (Ki = 4.6 nM, 60 nM respectively), demonstrating the sigma specificity. The saturation binding (Scatchard analysis) of ["3H]DTG with MCF-7 cell membrane preparations gave Kd of 24.54 nM and a Bmax of 2071 fmol/mg ...