Role of receptor kinase in short-term desensitization of cardiac muscarinic K+ channels expressed in Chinese hamster ovary cells

J Physiol. 1998 Mar 1;507 ( Pt 2)(Pt 2):325-34. doi: 10.1111/j.1469-7793.1998.325bt.x.

Abstract

1. The cardiac muscarinic receptor-K+ channel system was reconstructed in Chinese hamster ovary (CHO) cells by transfecting the cells with the various components of the system. The activity of the muscarinic K+ channel was measured with the cell-attached configuration of the patch clamp technique. 2. In CHO cells transfected with the channel (Kir3.1/Kir3.4), receptor (hm2) and receptor kinase (GRK2), on exposure to agonist, there was a decline in channel activity as a result of desensitization, similar to that in atrial cells. 3. Whereas the desensitization was almost abolished by not transfecting with the receptor kinase or by transfecting with a mutant receptor lacking phosphorylation sites, it was only reduced (by approximately 39%) by transfecting with a mutant receptor kinase with little/kinase activity. 4. These results suggest that the receptor kinase is responsible for desensitization of the muscarinic K+ channel and that this involves phosphorylation-dependent and -independent mechanisms.

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Electric Stimulation
  • Electrophysiology
  • Heart / drug effects*
  • Heart Atria / cytology
  • Membrane Potentials / physiology
  • Muscarinic Antagonists / pharmacology*
  • Myocardium / metabolism
  • Patch-Clamp Techniques
  • Potassium Channel Blockers*
  • Rats
  • Receptor Protein-Tyrosine Kinases / metabolism*
  • Receptors, Muscarinic / drug effects*
  • Transfection

Substances

  • Muscarinic Antagonists
  • Potassium Channel Blockers
  • Receptors, Muscarinic
  • Receptor Protein-Tyrosine Kinases