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- W2079508770 abstract "The antioxidant properties of the active (+) and inactive (-) isomers of the calcium channel blocker nicardipine were investigated in isolated membrane, endothelial cell, and perfused rat heart preparations. Using an isolated cardiac membrane preparation exposed to exogenous free radicals, both active and inactive isomers of nicardipine displayed equipotent concentration-dependent antiperoxidative activities. With a cultured endothelial cell preparation, effects of the nicardipine isomers on free radical-induced cell injury were compared. When untreated isolated endothelial cells were exposed to an iron-catalyzed hydroxyl radical system for 30 minutes, lipid peroxidation, assayed as thiobarbituric acid reactant (TBAR) formation, occurred and cellular glutathione decreased by 43%; concomitantly, cellular viability decreased 60%. Preincubation of the endothelial cells with active or inactive isomers of nicardipine before adding free radicals resulted in a similar dose-dependent (5, 20 μM) inhibition of lipid peroxide formation, significant preservation of glutathione levels, and attenuation of the viability losses. In a perfused rat heart preparation, 40 minutes of ischemia followed by 15 minutes of reperfusion resulted in dramatic production of alkoxyl radicals, which were detected as α-phenyl-tert-butylnitrone-adducts using electron spin resonance spectroscopy. Pretreatment of the heart with 1 μM inactive nicardipine reduced the total postischemic adduct formation by 75%. Because this isomer of nicardipine is considered inactive as a calcium channel blocker, the observed endothelial cytoprotective effect and inhibition of the alkoxyl-adduct production from rat hearts must have been mediated by the agent's membrane antiperoxidative activity, which is unrelated to its calcium channel blockade ability. We suggest that such properties might potentially contribute to the clinical beneficial effects of nicardipine." @default.
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- W2079508770 title "Antioxidant properties of active and inactive isomers of nicardipine in cardiac membranes, endothelial cells, and perfused rat hearts" @default.
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