Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital.
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.
Department of Anaesthesia and Critical Care, University Hospital Giessen-Marburg GmbH, Marburg Campus, Baldingerstrasse, 35033 Marburg, Germany. ruesch@staff.uni-marburg.de
Dirk
D
Rüsch
Hans A
HA
Braun
Hinnerk
H
Wulf
Anika
A
Schuster
Douglas E
DE
Raines
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology / Q000379:methods; D005045:Etomidate / Q000494:pharmacology*; D005260:Female; D006801:Humans; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D008564:Membrane Potentials / Q000187:drug effects; D008845:Microinjections; D009865:Oocytes / Q000187:drug effects / Q000378:metabolism / Q000502:physiology; D010424:Pentobarbital / Q000494:pharmacology*; D015742:Propofol / Q000494:pharmacology*; D020033:Protein Isoforms / Q000235:genetics / Q000502:physiology; D012313:RNA / Q000008:administration & dosage / Q000235:genetics; D044406:Receptors, Serotonin, 5-HT3 / Q000235:genetics / Q000502:physiology*; D014982:Xenopus laevis
D006993:Hypnotics and Sedatives; D020033:Protein Isoforms; D044406:Receptors, Serotonin, 5-HT3; D012313:RNA; D010424:Pentobarbital; D015742:Propofol; D005045:Etomidate