GIRK channel activation via adenosine or muscarinic receptors has similar effects on rat atrial electrophysiology

J Cardiovasc Pharmacol. 2013 Aug;62(2):192-8. doi: 10.1097/FJC.0b013e3182965221.

Abstract

G protein-coupled inwardly rectifying K⁺ channels (GIRK) are important in the regulation of heart rate and atrial electrophysiology. GIRK channels are activated by G protein-coupled receptors, including muscarinic M₂ receptors and adenosine A₁ receptors. The aim of this study was to characterize and compare the electrophysiological effects of acetylcholine (ACh) and adenosine on GIRK channels in rat atria. Action potential duration at 90% repolarization (APD₉₀), effective refractory period (ERP), and resting membrane potential (RMP) were investigated in isolated rat atria by intracellular recordings. Both the adenosine analog N6-cyclopentyladenosine (CPA) and ACh profoundly shortened APD₉₀ and ERP and hyperpolarized the RMP. No additive or synergistic effect of CPA and ACh coapplication was observed. To antagonize GIRK channel activation, the specific inhibitor rTertiapin Q (TTQ) was applied. The coapplication of TTQ reversed the CPA and ACh-induced effects. When TTQ was applied without exogenous receptor activator, both APD₉₀ and ERP were prolonged and RMP was depolarized, confirming a basal activity of the GIRK current. The results reveal that activation of A₁ and M₂ receptors has a profound and equal effect on the electrophysiology in rat atrium. This effect is to a major extent mediated through GIRK channels. Furthermore, these results support the notion that atrial GIRK currents from healthy hearts have a basal component and additional activation can be mediated via at least 2 different receptor mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / metabolism
  • Adenosine / metabolism
  • Adrenergic alpha-1 Receptor Agonists / pharmacology
  • Animals
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / metabolism
  • Arrhythmias, Cardiac / prevention & control*
  • Atrial Function / drug effects
  • Electrophysiological Phenomena / drug effects
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels / agonists*
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels / antagonists & inhibitors
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels / metabolism
  • Heart / drug effects*
  • In Vitro Techniques
  • Male
  • Membrane Potentials / drug effects
  • Membrane Transport Modulators / pharmacology*
  • Myocardium / metabolism*
  • Potassium Channel Blockers / pharmacology
  • Purinergic P1 Receptor Agonists / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Muscarinic M2 / agonists
  • Receptor, Muscarinic M2 / metabolism*
  • Receptors, Adrenergic, alpha-1 / metabolism*
  • Refractory Period, Electrophysiological / drug effects

Substances

  • Adrenergic alpha-1 Receptor Agonists
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • Membrane Transport Modulators
  • Potassium Channel Blockers
  • Purinergic P1 Receptor Agonists
  • Receptor, Muscarinic M2
  • Receptors, Adrenergic, alpha-1
  • Adenosine
  • Acetylcholine