The outwardly rectifying chloride channel in rat peritoneal mast cells is regulated by serine/threonine kinases and phosphatases

Pflugers Arch. 2002 Feb;443(4):558-64. doi: 10.1007/s00424-001-0724-6. Epub 2001 Oct 2.

Abstract

A slowly activating, outwardly rectifying Cl- channel (ORCC) has been described in rat peritoneal mast cells (RPMCs). This channel is activated by intracellular application of cAMP, an effect that might be mediated by a PKA-type serine/threonine protein kinase. To test this hypothesis, whole-cell patch-clamp experiments (nystatin-perforated patch) were performed and 8-bromoadenosine 3',5'-cyclic monophosphothioate, Sp-enantiomer (Sp-8Br-cAMPS), a cell membrane-permeable activator of PKA, and three inhibitors of different serine/threonine protein phosphatases (okadaic acid, cantharidin, calyculin A), were tested. In RPMCs application of repetitive series of step hyper- and depolarizations (holding potential 0 mV, test potentials -80 to +80 mV, step size +20 mV) induced a slowly increasing, [half-maximal activation time ( t0.5) 11.0+/-1.1 min, Imax (at +80 mV) 18.7+/-3.1 pA pF-1], DIDS-sensitive, outwardly rectifying Cl- current I(Cl,OR). The activation of this current could be accelerated by Sp-8Br-cAMPS, okadaic acid or cantharidin in the extracellular solution. Co-application of Sp-8Br-cAMPS and okadaic acid increased Imax supra-additively. Calyculin A and higher concentrations of cantharidin inhibited the Cl- current via unknown mechanisms. Our findings suggest that I(Cl,OR) in RPMCs is activated by a PKA-type protein kinase, a process which is antagonized functionally by okadaic acid- and cantharidin-sensitive protein phosphatases.

MeSH terms

  • 8-Bromo Cyclic Adenosine Monophosphate / analogs & derivatives
  • 8-Bromo Cyclic Adenosine Monophosphate / pharmacology
  • Animals
  • Chloride Channels / metabolism*
  • Chlorides / metabolism
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Enzyme Inhibitors / pharmacology
  • Male
  • Marine Toxins
  • Mast Cells / enzymology*
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Okadaic Acid / pharmacology
  • Oxazoles / pharmacology
  • Patch-Clamp Techniques
  • Peritoneal Cavity / cytology
  • Phosphoric Monoester Hydrolases / metabolism*
  • Protein Serine-Threonine Kinases / metabolism*
  • Rats
  • Rats, Wistar
  • Thionucleotides / pharmacology

Substances

  • 8-bromoadenosine-3',5'-cyclic monophosphorothioate
  • Chloride Channels
  • Chlorides
  • Enzyme Inhibitors
  • Marine Toxins
  • Oxazoles
  • Thionucleotides
  • Okadaic Acid
  • 8-Bromo Cyclic Adenosine Monophosphate
  • calyculin A
  • Protein Serine-Threonine Kinases
  • Cyclic AMP-Dependent Protein Kinases
  • Phosphoric Monoester Hydrolases