Sulfhydryl modification inhibits K+ (M) current with kinetics close to acetylcholine in rodent NG108-15 cells

Neurosci Res. 1997 Jan;27(1):35-44. doi: 10.1016/s0168-0102(96)01130-3.

Abstract

The effects of sulfhydryl reagents on M-type voltage-dependent potassium currents (IK(M)) were examined in NG108-15 cells transformed to express ml muscarinic acetylcholine receptors (mAChRs), a NGPM1-27 clone. Focal application of glutathione at millimolar concentrations dissolved in acidic solutions caused a transient inward current in NGPM1-27 cells at holding potentials of -30mV, associated with an inhibition of IK(M). The glutathione-induced response was mimicked by cysteine. These effects were also reproduced by superfusion with micromolar concentrations of HgCl2, AgNO3, N-methylmaleimide and p-chloromercuribenzoic acid (pCMB), agents which target protein thiols. Glutathione, HgCl2, AgNO3 and pCMB inhibited the peak conductance of IK(M) without shifting the half activating voltage (V1/2), which was comparable to the acetylcholine (ACh)-induced response. The voltage dependence of time constants for IK(M) deactivation in sulfhydryl reagent-, ACh- and non-treated cells resembled, but differed from that in Ba(2+)-treated cells. These results reveal that there is an accessible cysteine moiety, but not a disulfide bond, either on the M channel protein itself or on a protein directly involved in agonist-M channel coupling.

MeSH terms

  • Acetylcholine / pharmacology*
  • Animals
  • Cysteine / pharmacology
  • Glioma
  • Glutathione / analogs & derivatives
  • Glutathione / pharmacology
  • Glutathione Disulfide
  • Glycine / pharmacology
  • Hybrid Cells
  • Kinetics
  • Membrane Potentials / drug effects
  • Mercuric Chloride / pharmacology
  • Mice
  • Neuroblastoma
  • Potassium Channels / drug effects
  • Potassium Channels / physiology*
  • Rats
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic / biosynthesis
  • Receptors, Muscarinic / drug effects
  • Receptors, Muscarinic / physiology
  • Recombinant Proteins / drug effects
  • Recombinant Proteins / metabolism
  • Silver Nitrate / pharmacology
  • Sulfhydryl Reagents / pharmacology*
  • Transfection

Substances

  • Potassium Channels
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic
  • Recombinant Proteins
  • Sulfhydryl Reagents
  • Mercuric Chloride
  • Silver Nitrate
  • Glutathione
  • Cysteine
  • Acetylcholine
  • Glycine
  • Glutathione Disulfide