The present study shows the factors that modulate the photodamage promoted by phenothiazines. Cytochrome c was irradiated with UV light for 120 min, over a pH range from 4.0 to 8.0, in the absence and in the presence of different concentrations of thioridazine (TR) and fluphenazine (FP). In the absence of phenothiazines, the maximal rate of a Soret band blue shift (nm/min) from 409 to 406 nm wa...

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...

The reaction between phenothiazine and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) in the presence of p-toluenesulfonic acid in chloroform was investigated by potentiometry, voltammetry and spectrophotometry, and the reaction pathways were proposed. The conditions for the oxidimetric titration of phenothiazines with a standard chloroform solution of DDQ were optimized and the potentiometric...

The presented review is devoted to analytical applications of reactions of Fe(III) and K(3)[Fe(CN)(6)] with 2,10-disubstituted phenothiazines (PT). It was found that iron(III) and hexacyanoferrate(III) ions in acidic media easily oxidized PT with the formation of colored oxidation products. This property has been exploited for spectrophotometric determination of iron(III) ions and phenothiazine...

The antischizophrenic activity of phenothiazine drugs and their tendency to elicit extrapyramidal symptoms are thought to involve blockade of synaptic dopamine receptors in the brain. Space filling molecular models show how favorable Van der Waal's interactions between the side chain amino of phenothiazines and the 2-substituent on ring A can promote a conformation mimicking dopamine. These Van...

High osmolarity and glucose deprivation cause rapid shutdowns of both actin polarization and translation initiation in yeast. Like these stresses, administration of local anesthetics and of antipsychotic phenothiazines caused similar responses. All these drugs have amphiphilic structures and formed emulsions and permeabilized the cell membrane, indicating that they have the same features as a s...

Cancer is, despite rapid progress in development of new targeted therapies, still mainly treated with surgery, chemotherapy and/or radiation therapy. The last two mentioned conventional therapies often meet general obstacles such as normal cell toxicity and tumour cell resistance. Further efforts are, hence, required to increase efficacy of both radiotherapy and chemotherapy in order to increas...

A high-performance liquid chromatographic method has been developed for the simultaneous analysis of the 12 phenothiazines (chlorpromazine, fluphenazine, levomepromazine, perazine, perphenazine, prochlorperazine, profenamine, promethazine, propericiazine, thioproperazine, thioridazine and trifluoperazine) in human serum using HPLC/UV. The separation was achieved using a C(18) reversed-phase col...

The actions of the phenothiazines chlorpromazine, prochlorperazine, and trifluoperazine were studied on the acetylcholine receptor-ionic channel complex of frog and rat skeletal muscle and of Torpedo californica to determine their role in pharmacological desensitization and their interactions with different states of the receptor-ionic channel complex. The phenothiazines depressed the peak ampl...