Pharmacological Conversion of a Cardiac Inward Rectifier into an Outward Rectifier Potassium Channel

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Pharmacological Conversion of a Cardiac Inward Rectifier into an Outward Rectifier Potassium Channel.

Potassium (K(+)) channels are crucial for determining the shape, duration, and frequency of action-potential firing in excitable cells. Broadly speaking, K(+) channels can be classified based on whether their macroscopic current outwardly or inwardly rectifies, whereby rectification refers to a change in conductance with voltage. Outwardly rectifying K(+) channels conduct greater current at dep...

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A conductance maximum observed in an inward-rectifier potassium channel

One prediction of a multi-ion pore is that its conductance should reach a maximum and then begin to decrease as the concentration of permeant ion is raised equally on both sides of the membrane. A conductance maximum has been observed at the single-channel level in gramicidin and in a Ca(2+)-activated K+ channel at extremely high ion concentration (> 1,000 mM) (Hladky, S. B., and D. A. Haydon. ...

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Time-dependent Outward Currents through the Inward Rectifier Potassium Channel IRK1

Outward currents through the inward rectifier K+ channel contribute to repolarization of the cardiac action potential. The properties of the IRK1 channel expressed in murine fibroblast (L) cells closely resemble those of the native cardiac inward rectifier. In this study, we added Mg2+ (0.44-1.1 mM) or putrescine (approximately 0.4 mM) to the intracellular milieu where endogenous polyamines rem...

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Spermine Block of the Strong Inward Rectifier Potassium Channel Kir2.1

Inward rectification in strong inward rectifiers such as Kir2.1 is attributed to voltage-dependent block by intracellular polyamines and Mg(2+). Block by the polyamine spermine has a complex voltage dependence with shallow and steep components and complex concentration dependence. To understand the mechanism, we measured macroscopic Kir2.1 currents in excised inside-out giant patches from Xenop...

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Revisit of the Cardiac Inward Rectifier Potassium Current IK1

Inward rectifier potassium currents are present in different types of cells. In the heart, the inward rectifier potassium current IK1 plays a crucial role in maintaining cardiac resting membrane potential and excitability. It is generally believed that the strong inward rectification of cardiac IK1 channels makes it conduct substantial current near the resting potential but carry little or no c...

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ژورنال

عنوان ژورنال: Molecular Pharmacology

سال: 2016

ISSN: 0026-895X,1521-0111

DOI: 10.1124/mol.116.104950