Type 2 ryanodine receptors are highly sensitive to alcohol

FEBS Lett. 2014 May 2;588(9):1659-65. doi: 10.1016/j.febslet.2014.03.005. Epub 2014 Mar 12.

Abstract

Exposure to ethanol levels reached in circulation during alcohol intoxication (>10mM) constricts cerebral arteries in rats and humans. Remarkably, targets and mechanisms underlying this action remain largely unidentified. Artery diameter is regulated by myocyte Ca(2+) sparks, a vasodilatory signal contributed to by type 2 ryanodine receptors (RyR2). Using laser confocal microscopy in rat cerebral arteries and bilayer electrophysiology we unveil that ethanol inhibits both Ca(2+) spark and RyR2 activity with IC50<20 mM, placing RyR2 among the ion channels that are most sensitive to ethanol. Alcohol directly targets RyR2 and its lipid microenvironment, leading to stabilization of RyR2 closed states.

Keywords: Alcohol; Cerebral artery smooth muscle; Lipid bilayer electrophysiology; Ryanodine receptor.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alcoholic Intoxication / physiopathology
  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Signaling / drug effects*
  • Central Nervous System Depressants / pharmacology
  • Cerebral Arteries / drug effects
  • Cerebral Arteries / physiopathology
  • Ethanol / pharmacology*
  • HEK293 Cells
  • Humans
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Ion Channel Gating / drug effects
  • Male
  • Protein Stability
  • Rats
  • Rats, Sprague-Dawley
  • Ryanodine Receptor Calcium Release Channel / metabolism*

Substances

  • Calcium Channel Blockers
  • Central Nervous System Depressants
  • Ryanodine Receptor Calcium Release Channel
  • Ethanol