Differential effects of volatile and intravenous anesthetics on the activity of human TASK-1

Am J Physiol Cell Physiol. 2007 Oct;293(4):C1319-26. doi: 10.1152/ajpcell.00100.2007. Epub 2007 Aug 15.

Abstract

Volatile anesthetics have been shown to activate various two-pore (2P) domain K(+) (K(2P)) channels such as TASK-1 and TREK-1 (TWIK-related acid-sensitive K(+) channel), and mice deficient in these channels are resistant to halothane-induced anesthesia. Here, we investigated whether K(2P) channels were also potentially important targets of intravenous anesthetics. Whole cell patch-clamp techniques were used to determine the effects of the commonly used intravenous anesthetics etomidate and propofol on the acid-sensitive K(+) current in rat ventricular myocytes (which strongly express TASK-1) and selected human K(2P) channels expressed in Xenopus laevis oocytes. In myocytes, etomidate decreased both inward rectifier K(+) (K(ir)) current (I(K1)) and acid-sensitive outward K(+) current at positive potentials, suggesting that this drug may inhibit TASK channels. Indeed, in addition to inhibiting guinea pig Kir2.1 expressed in oocytes, etomidate inhibited human TASK-1 (and TASK-3) in a concentration-dependent fashion. Propofol had no effect on human TASK-1 (or TASK-3) expressed in oocytes. Moreover, we showed that, similar to the known effect of halothane, sevoflurane and the purified R-(-)- and S-(+)-enantiomers of isoflurane, without stereoselectivity, activated human TASK-1. We conclude that intravenous and volatile anesthetics have dissimilar effects on K(2P) channels. Human TASK-1 (and TASK-3) are insensitive to propofol but are inhibited by supraclinical concentrations of etomidate. In contrast, stimulatory effects of sevoflurane and enantiomeric isoflurane on human TASK-1 can be observed at clinically relevant concentrations.

MeSH terms

  • Anesthetics, Inhalation / pharmacology*
  • Anesthetics, Intravenous / pharmacology*
  • Animals
  • Arachidonic Acids / pharmacology
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Etomidate / pharmacology
  • Halothane / pharmacology
  • Humans
  • Hydrogen-Ion Concentration
  • Isoflurane / pharmacology
  • Membrane Potentials / drug effects
  • Methyl Ethers / pharmacology
  • Myocytes, Cardiac / cytology
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / physiology
  • Nerve Tissue Proteins / genetics
  • Nerve Tissue Proteins / physiology*
  • Oocytes / drug effects
  • Oocytes / metabolism
  • Oocytes / physiology
  • Patch-Clamp Techniques
  • Potassium / metabolism
  • Potassium Channel Blockers / pharmacology
  • Potassium Channels, Tandem Pore Domain / genetics
  • Potassium Channels, Tandem Pore Domain / physiology*
  • Propofol / pharmacology
  • RNA, Complementary / genetics
  • Rats
  • Sevoflurane
  • Xenopus laevis

Substances

  • Anesthetics, Inhalation
  • Anesthetics, Intravenous
  • Arachidonic Acids
  • Methyl Ethers
  • Nerve Tissue Proteins
  • Potassium Channel Blockers
  • Potassium Channels, Tandem Pore Domain
  • RNA, Complementary
  • methanandamide
  • potassium channel subfamily K member 3
  • Sevoflurane
  • Isoflurane
  • Potassium
  • Halothane
  • Propofol
  • Etomidate