Characterisation of Ca(2+)-dependent inwardly rectifying K+ currents in HeLa cells

Pflugers Arch. 1995 Jun;430(2):168-80. doi: 10.1007/BF00374647.

Abstract

The whole-cell configuration of the patch-clamp technique was used to examine K+ currents in HeLa cells. Under quasi-physiological ionic gradients, using an intracellular solution containing 10(-7) mol/l free Ca2+, mainly outward currents were observed. Large inwardly rectifying currents were elicited in symmetrical 145 mmol/l KCl. Replacement of all extracellular K+ by isomolar Na+, greatly decreased inward currents and shifted the reversal potential as expected for K+ selectivity. The inwardly rectifying K+ currents exhibited little or no apparent voltage dependence within the range of from -120 mV to 120 mV. A square-root relationship between chord conductance and [K+] at negative potentials could be established. The inwardly rectifying nature of the currents was unaltered after removal of intracellular Mg2+ and chelation with ATP and ethylenediaminetetraacetic acid (EDTA). Permeability ratios for other monovalent cations relative to K+ were: K+ (1.0) > Rb+ (0.86) > Cs+ (0.12) > Li (0.08) > Na+ (0.03). Slope conductance ratios measured at -100 mV were: Rb+ (1.66) > K+ (1.0) > Na+ (0.09) > Li (0.08) > Cs+ (0.06). K+ conductance was highly sensitive to intracellular free Ca2+ concentration. The relationship between conductance at 0 mV and Ca2+ concentration was well described by a Hill expression with a dissociation constant, KD, of 70 nmol/l and a Hill coefficient, n, of 1.81. Extracellular Ba2+ blocked the currents in a concentration- and voltage-dependent manner. The dependence of the KD for the blockade was analysed using a Woodhull-type treatment, locating the ion interaction site at 19% of the distance across the electrical field of the membrane and a KD (0 mV) of 7 mmol/l. Tetraethylammonium and 4-aminopyridine were without effect whilst quinine and quinidine blocked the currents with concentrations for half-maximum effects equal to 7 mumol/l and 3.5 mumol/l, respectively. The unfractionated venom of the scorpion Leiurus quinquestriatus (LQV) blocked the K+ currents of HeLa cells. The toxins apamin and scyllatoxin had no detectable effect whilst charybdotoxin, a component of LQV, blocked in a voltage-dependent manner with half-maximal concentrations of 40 nmol/l at -120 mV and 189 nmol/l at 60 mV; blockade by charybdotoxin accounts for the effect of LQV. Application of ionomycin (5-10 mumol/l), histamine (1 mmol/l) or bradykinin (1-10 mumol/l) to cells dialysed with low-buffered intracellular solutions induced K+ currents showing inward rectification and a lack of voltage dependence.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / pharmacology
  • Barium / pharmacology
  • Bradykinin / pharmacology
  • Calcium / pharmacology*
  • Cations, Monovalent
  • Cell Membrane Permeability
  • Charybdotoxin
  • Edetic Acid / pharmacology
  • Electric Conductivity
  • HeLa Cells
  • Histamine / pharmacology
  • Humans
  • Magnesium / pharmacology
  • Patch-Clamp Techniques
  • Potassium / metabolism*
  • Potassium / pharmacology
  • Potassium Channels / physiology*
  • Potassium Channels, Inwardly Rectifying*
  • Quinidine / pharmacology
  • Quinine / pharmacology
  • Scorpion Venoms / pharmacology
  • Tetraethylammonium
  • Tetraethylammonium Compounds / pharmacology

Substances

  • Cations, Monovalent
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • Scorpion Venoms
  • Tetraethylammonium Compounds
  • Charybdotoxin
  • Barium
  • Tetraethylammonium
  • Histamine
  • Adenosine Triphosphate
  • Edetic Acid
  • Quinine
  • Magnesium
  • Quinidine
  • Potassium
  • Bradykinin
  • Calcium