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Abstract

In vitro incorporation of tranquilizer phenazepam in a concentration of 10(-13) M into membrane fraction from mouse brain produced a prooxidant effect. In concentrations of 10(-5)-10(-9) and 10(-15)-10(-17) M this agent possessed antioxidant activity. Phenazepam significantly decreased the maximum rate of enzymatic reactions (10(-5) and 10(-15) M) and Michaelis constant (10(-5) M) for acetylcholinesterase. Incorporation of phenazepam in ultralow doses into membrane modified its lipid components (estimated by lipid peroxidation) and functional state, and this effect was comparable with the influence of this substance in standard doses. This probably contributes to the physiological effect of ultralow doses of phenazepam in.

Hybrid antioxidants

“…The anticholinesterase activity of ichphans was assessed with regard to soluble and membrane-bound acetylcholinesterase (AChE) of human blood erythrocytes; it was determined from the inhibition constants and influence on the enzyme efficacy. All ichphans behaved as reversible inhibitors of AChE [31][32][33][34].…”

“…The type of inhibition depends on the alkyl substituent. Although, for the substances studied, the inhibiting effect for the membrane-bound enzyme is by an order of magnitude lower than that for soluble AChE, in both cases, similar relations exist between the structure and inhibiting activity of the compounds [31][32][33][34].…”

Free Radical Oxidation in Rat Brain during Chronic Stress and Pharmacological Regulation of This Process

“…Antioxidant activity of these drugs was confirmed in numerous experimental and clinical studies [2,6[. There is strong evidence that several antioxidant drugs have psychotropic activity [4].…”

Changes in the structure and functions of membranes in erythrocytes and Ehrlich ascites carcinoma cells under the influence of a new generation hybrid antioxidant IKhFAN-10

“…IKhFANs, derivatives of phenosan [β-4-hydroxy-(3,5-ditert-butyl-4-hydroxyphenyl) potassium propionate], consist of the AO part, choline residue responsible for anticholinesterase activity, and fatty acid fragment modulating membrane viscosity and promoting to permeation through the blood-brain barrier. IKhFANs have high AO activity and serve as cholinesterase inhibitors in human erythrocytes [5]. Here we studied the effects of IKhFAN-10 on membranes.…”