Slow modal gating of single G protein-activated K+ channels expressed in Xenopus oocytes

J Physiol. 2000 May 1;524 Pt 3(Pt 3):737-55. doi: 10.1111/j.1469-7793.2000.00737.x.

Abstract

The slow kinetics of G protein-activated K+ (GIRK) channels expressed in Xenopus oocytes were studied in single-channel, inside-out membrane patches. Channels formed by GIRK1 plus GIRK4 subunits, which are known to form the cardiac acetylcholine (ACh)-activated GIRK channel (KACh), were activated by a near-saturating dose of G protein betagamma subunits (Gbetagamma; 20 nM). The kinetic parameters of the expressed GIRK1/4 channels were similar to those of cardiac KACh. GIRK1/4 channels differed significantly from channels formed by GIRK1 with the endogenous oocyte subunit GIRK5 (GIRK1/5) in some of their kinetic parameters and in a 3-fold lower open probability, Po. The unexpectedly low Po (0.025) of GIRK1/4 was due to the presence of closures of hundreds of milliseconds; the channel spent approximately 90 % of the time in the long closed states. GIRK1/4 channels displayed a clear modal behaviour: on a time scale of tens of seconds, the Gbetagamma-activated channels cycled between a low-Po mode (Po of about 0.0034) and a bursting mode characterized by an approximately 30-fold higher Po and a different set of kinetic constants (and, therefore, a different set of channel conformations). The available evidence indicates that the slow modal transitions are not driven by binding and unbinding of Gbetagamma. The GTPgammaS-activated Galphai1 subunit, previously shown to inhibit GIRK channels, substantially increased the time spent in closed states and apparently shifted the channel to a mode similar, but not identical, to the low-Po mode. This is the first demonstration of slow modal transitions in GIRK channels. The detailed description of the slow gating kinetics of GIRK1/4 may help in future analysis of mechanisms of GIRK gating.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Cloning, Molecular
  • Female
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • GTP-Binding Protein alpha Subunits, Gi-Go / metabolism
  • Gene Expression / physiology
  • Guanosine 5'-O-(3-Thiotriphosphate) / pharmacology
  • Ion Channel Gating / drug effects
  • Ion Channel Gating / physiology*
  • Kinetics
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Myocardium / chemistry
  • Oocytes / physiology
  • Patch-Clamp Techniques
  • Plasmids
  • Potassium Channels / genetics*
  • Potassium Channels / metabolism*
  • Potassium Channels, Inwardly Rectifying*
  • RNA, Messenger / pharmacology
  • Receptors, Muscarinic / genetics
  • Receptors, Muscarinic / metabolism
  • Xenopus laevis

Substances

  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • RNA, Messenger
  • Receptors, Muscarinic
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • GTP-Binding Protein alpha Subunits, Gi-Go