2,2,2-trichloroethanol activates a nonclassical potassium channel in cerebrovascular smooth muscle and dilates the middle cerebral artery

J Pharmacol Exp Ther. 2010 Mar;332(3):803-10. doi: 10.1124/jpet.109.162313. Epub 2009 Dec 2.

Abstract

Trichloroacetaldehyde monohydrate [chloral hydrate (CH)] is a sedative/hypnotic that increases cerebral blood flow (CBF), and its active metabolite 2,2,2-trichloroethanol (TCE) is an agonist for the nonclassical two-pore domain K(+) (K(2P)) channels TREK-1 and TRAAK. We sought to determine whether TCE dilates cerebral arteries in vitro by activating nonclassical K(+) channels. TCE dilated pressurized and perfused rat middle cerebral arteries (MCAs) in a manner consistent with activation of nonclassical K(+) channels. Dilation to TCE was inhibited by elevated external K(+) but not by an inhibitory cocktail (IC) of classical K(+) channel blockers. Patch-clamp electrophysiology revealed that, in the presence of the IC, TCE increased whole-cell currents and hyperpolarized the membrane potential of isolated MCA smooth muscle cells. Heating increased TCE-sensitive currents, indicating that the activated channel was thermosensitive. Immunofluorescence in sections of the rat MCA demonstrated that, like TREK-1, TRAAK is expressed in the smooth muscle of cerebral arteries. Isoflurane did not, however, dilate the MCA, suggesting that TREK-1 was not functional. These data indicate that TCE activated a nonclassical K(+) channel with the characteristics of TRAAK in rat MCA smooth-muscle cells. Stimulation of K(+) channels such as TRAAK in cerebral arteries may therefore explain in part how CH/TCE increases CBF.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Ethylene Chlorohydrin / analogs & derivatives*
  • Ethylene Chlorohydrin / pharmacology
  • Hypnotics and Sedatives / pharmacology*
  • Immunohistochemistry
  • In Vitro Techniques
  • Isoflurane / pharmacology
  • Male
  • Membrane Potentials / drug effects
  • Middle Cerebral Artery / drug effects*
  • Middle Cerebral Artery / physiology
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / physiology
  • Patch-Clamp Techniques
  • Potassium Channels / agonists
  • Potassium Channels / biosynthesis
  • Potassium Channels / physiology*
  • Rats
  • Rats, Long-Evans
  • Vasodilator Agents / pharmacology*

Substances

  • Hypnotics and Sedatives
  • Kcnk18 protein, rat
  • Kcnk4 protein, rat
  • Potassium Channels
  • Vasodilator Agents
  • Ethylene Chlorohydrin
  • 2,2,2-trichloroethanol
  • Isoflurane