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  • 1,4-dihydropyridines  (1)
  • Ba2+  (1)
  • Channel block  (1)
  • 1
    ISSN: 1432-2013
    Schlagwort(e): Smooth muscle ; Ba2+ ; TEA ; Ca2+-activated K+ channels ; Patchclamp ; Channel block
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The interaction of Ba2+ and TEA with Ca2+-activated K+ channels was studied in isolated membrane patches of cells from longitudinal jejunal smooth muscle of rabbit and from guinea-pig small mesenteric artery (100 μm external diameter). Ba2+ applied from the inside of the membrane did not reduce unit current, except at high concentrations, but channels failed to open for long periods (s). This effect became much stronger when the potential gradient was in a direction driving Ba2+ into the channel and was reduced by increasing K+ ion concentration on the outside of the membrane. These results are consistent with Ba2+ entering the open channel and blocking at a site most of the way through the channel bore. In contrast, TEA and procaine dose-dependently reduced unit current amplitude at all patch potentials and slightly increased mean open time. Their effects were not detectably voltage-dependent and could be explained by TEA and procaine blocking the open channel with a timecourse that was faster than the frequency response of the recording system. The lack of appreciable voltage-dependence suggests that TEA and procaine bind to a site near to the inner mouth of the channel.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 1432-2013
    Schlagwort(e): concentration-jump technique ; patch-clamp technique ; single smooth muscle cell ; 1,4-dihydropyridines
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The actions of nifedipine or BAY K 8644 were studied on barium currents recorded from single, collagenase- and elastase-dispersed, smooth muscle cells from the rabbit ear artery using the whole-cell configuration of the patch-clamp technique. Nifedipine (3μM) caused a reduction in the barium current (IBa) evoked by steps to potentials positive of-10mV. This was characterized by a pronounced ‘initial’ block, an increase in the rate of current decay during the voltage-clamp step, but by no increase in block if pulses were repeated every 600ms. Rapid extracellular application of nifedipine (1μM) during the sustained current component (using a new concentration-jump technique) was found to have no effect on IBa over 4s at +20mV, but after returning to the holding potential (-60mV) for 10s, sustained IBa was subsequently abolished. BAY K 8644 (1μM) increased IBa at all potentials, and on rapid application during the sustained current component markedly potentiated IBa. The results suggest that nifedipine binds with high affinity to the closed, available state of the Ca++ channels but they do not suggest binding to the open or inactivated states. The effect of BAY K 8644 is consistent with high affinity binding to the open or inactivated and to the closed, available states.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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