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• W2005382267 endingPage "328" @default.
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• W2005382267 abstract "1 . Whole-cell patch-clamp method was applied to single smooth muscle cells freshly isolated from the rat inferior vena cava. 2 . Depolarizing pulses, applied from a holding potential of − 90 mV, activated both Na+ and Ca2+ channels. The fast Na+ current was inhibited by nanomolar concentrations of tetrodotoxin (TTX). The slow Ba2+ current (measured in 5 mm Ba2+ solution) was inhibited by Cd2+ and modulated by dihydropyridine derivatives. When the cells were held at a holding potential of −80 mV, racemic Bay K 8644 increased the Ba2+ current (ED50 = 10 nm) while racemic isradipine inhibited the current (IC50 = 21 nm). 3 . The voltage-dependency of isradipine blockade was assessed by determining the steady-state availability of the Ca2+ channels. From the shift of the inactivation curve in the presence of isradipine, we calculated a dissociation constant of 1.11 nm for inactivated Ca2+ channels. Scatchard plots of the specific binding of (+)-[3H]-isradipine obtained in intact strips incubated in 5.6 mm or 135 mm K+ solutions confirmed the voltage-dependency of isradipine binding. 4 . Specific binding of (+)-[3H]-isradipine was completely displaced by unlabelled (±)-isradipine, with an IC50 of 15.1 nm. This value is similar to the IC50 for inhibition of the Ba2+ current (21 nm) in cells maintained at a holding potential of −80 mV. 5 . Bay K 8644 had no effects on the Ba2+ current kinetics during a depolarizing test pulse. The steady-state inactivation-activation curves of Ba2+ current were not significantly shifted along the voltage axis. 6 . The present data suggest the existence of two distinct dihydropyridine binding sites which can be bound preferentially by agonist or antagonist derivatives." @default.
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• W2005382267 date "1992-02-01" @default.
• W2005382267 modified "2023-09-26" @default.
• W2005382267 title "Effect of dihydropyridines on calcium channels in isolated smooth muscle cells from rat vena cava" @default.
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• W2005382267 doi "https://doi.org/10.1111/j.1476-5381.1992.tb14253.x" @default.
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