Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital

Eur J Pharmacol. 2007 Nov 14;573(1-3):60-4. doi: 10.1016/j.ejphar.2007.07.009. Epub 2007 Jul 13.

Abstract

The actions of intravenous anaesthetics on 5-HT(3AB) receptors have not been studied. Using oocyte electrophysiology, the effects of etomidate, propofol, and pentobarbital on human 5-HT(3A) and 5-HT(3AB) receptors were studied and compared. Inhibition of peak currents by all three compounds in both receptor subtypes was anaesthetic concentration-dependant and non-competitive. Because the half-maximal inhibitory concentrations for etomidate, propofol and pentobarbital in 5-HT(3A) and 5-HT(3AB) receptors were all above their respective anaesthetic concentrations, the results of our study suggest that neither 5-HT(3) receptor subtype contributes to the anaesthetic actions of etomidate, propofol or pentobarbital.

Publication types

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

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Electrophysiology / methods
  • Etomidate / pharmacology*
  • Female
  • Humans
  • Hypnotics and Sedatives / pharmacology
  • Membrane Potentials / drug effects
  • Microinjections
  • Oocytes / drug effects
  • Oocytes / metabolism
  • Oocytes / physiology
  • Pentobarbital / pharmacology*
  • Propofol / pharmacology*
  • Protein Isoforms / genetics
  • Protein Isoforms / physiology
  • RNA / administration & dosage
  • RNA / genetics
  • Receptors, Serotonin, 5-HT3 / genetics
  • Receptors, Serotonin, 5-HT3 / physiology*
  • Xenopus laevis

Substances

  • Hypnotics and Sedatives
  • Protein Isoforms
  • Receptors, Serotonin, 5-HT3
  • RNA
  • Pentobarbital
  • Propofol
  • Etomidate