Interaction of i.v. anaesthetic agents with 5-HT3 receptors

Br J Anaesth. 1996 Feb;76(2):271-3. doi: 10.1093/bja/76.2.271.

Abstract

Using N1E-115 neuroblastoma cells as an experimental model, we have examined if four commonly used i.v. anaesthetic induction agents interact with 5-HT3 receptors. Specifically, we tested the hypothesis that the antiemetic effects of propofol may result from 5-HT3 receptor antagonism. Binding of tropisetron (a 5-HT3 selective reference compound), etomidate, ketamine, thiopentone and propofol to 5-HT3 receptors was assessed by measuring the displacement of [3H]BRL 43694 from whole N1E-115 cells. The rank order potency (Ki) was tropisetron (1.7 (SEM 0.2) nmol litre-1) >> etomidate (83.(4) mumol litre-1) > or = ketamine (97 (4) mumol litre-1) > thiopentone (177 (9) mumol litre-1) > propofol (819 (171) mumol litre-1). With the exception of thiopentone these effects were outside the clinical range and suggest that anaesthetic agents are unlikely to interact directly with 5-HT3 receptors, and that other mechanism(s) must underlie the antiemetic effects of propofol.

MeSH terms

  • Anesthetics, Intravenous / metabolism*
  • Animals
  • Antiemetics / metabolism
  • Binding, Competitive
  • Dose-Response Relationship, Drug
  • Etomidate / metabolism
  • Granisetron / metabolism
  • Indoles / metabolism
  • Ketamine / metabolism
  • Mice
  • Propofol / metabolism
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / metabolism
  • Thiopental / metabolism
  • Tropisetron
  • Tumor Cells, Cultured

Substances

  • Anesthetics, Intravenous
  • Antiemetics
  • Indoles
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Ketamine
  • Tropisetron
  • Thiopental
  • Granisetron
  • Propofol
  • Etomidate