PMID: 9523815Apr 2, 1998Paper

Stereoselective effects of etomidate optical isomers on gamma-aminobutyric acid type A receptors and animals

Anesthesiology
S L TomlinN P Franks

Abstract

The intravenous anesthetic etomidate is optically active and exists in two mirror-image enantiomeric forms. However, although the R(+) isomer is used as a clinical anesthetic, quantitative information on the relative potencies of the R(+) and S(-) isomers is lacking. These data could be used to test the relevance of putative molecular targets. The anesthetic concentrations for a half-maximal effect (EC50) needed to induce a loss of righting reflex in tadpoles (Rana temporaria) were determined for both etomidate enantiomers. The effects of the isomers on gamma-aminobutyric acid (GABA)-induced currents in stably transfected mouse fibroblast cells was also investigated using the patch-clamp technique. In addition, the effects of the isomers on a lipid chain-melting phase transition were determined. The EC50 concentrations for general anesthesia for the R(+) and S(-) isomers were 3.4 +/- 0.1 microM and 57 +/- 1 microM, with slopes of n = 1.9 +/- 0.1 and n = 2.9 +/- 0.2, respectively. The R(+) isomer was also much more effective than the S(-) isomer at potentiating GABA-induced currents, although the degree of stereoselectivity varied with anesthetic concentration. R(+) etomidate potentiated the GABA-induced currents by increasing t...Continue Reading

References

May 1, 1978·European Journal of Pharmacology·S RyderA J Trevor
Oct 15, 1978·Experientia·R H Evans, R G Hill
Jul 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·K L HadinghamP J Whiting
Jan 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·G W MossW R Lieb
Aug 1, 1983·Journal of Neurochemistry·R ThyagarajanM K Ticku
Apr 1, 1983·British Journal of Anaesthesia·B S HebronS J Mather
Sep 1, 1983·Pharmacotherapy·J L Giese, T H Stanley
Oct 1, 1982·Anesthesiology·P R Andrews, L C Mark
Dec 9, 1982·Nature·N P Franks, W R Lieb
Jul 1, 1983·Anesthesia and Analgesia·R J FragenN J Caldwell
Feb 17, 1994·Nature·N P Franks, W R Lieb
Jul 1, 1993·British Journal of Anaesthesia·N P Franks, W R Lieb
Feb 1, 1995·British Journal of Pharmacology·P Charlesworth, C D Richards
Sep 22, 1994·European Journal of Pharmacology·G S LyskoR A Ferrone
Jul 1, 1994·British Journal of Pharmacology·A C HallN P Franks
Apr 1, 1996·British Journal of Pharmacology·A JenkinsW R Lieb
Feb 1, 1996·British Journal of Anaesthesia·B L Appadu, D G Lambert
Dec 1, 1996·British Journal of Pharmacology·M P MasciaR A Harris
Oct 6, 1997·Proceedings of the National Academy of Sciences of the United States of America·D BelelliP J Whiting

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Citations

Sep 16, 1999·Cellular and Molecular Life Sciences : CMLS·M D Krasowski, N L Harrison
Jan 8, 2011·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Stuart A Forman, Keith W Miller
Dec 22, 1999·Trends in Pharmacological Sciences·D BelelliJ J Lambert
Jul 20, 2002·Progress in Neurobiology·Esa R KorpiHartmut Lüddens
Feb 27, 1999·Toxicology Letters·N P Franks, W R Lieb
Jun 8, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Qing C MengRoderic G Eckenhoff
Apr 22, 2008·Nature Reviews. Neuroscience·Nicholas P Franks
Jul 12, 2008·International Anesthesiology Clinics·Jonathan D Reasor, Gina R Poe
Jun 6, 2009·European Journal of Anaesthesiology·Andrea Kopp LugliChristoph H Kindler
Mar 27, 2001·Annual Review of Pharmacology and Toxicology·T YamakuraR A Harris
Jul 20, 2012·Critical Care : the Official Journal of the Critical Care Forum·Gordon Flynn, Yahya Shehabi
Feb 1, 2013·Critical Care : the Official Journal of the Critical Care Forum·Rile GeDouglas E Raines
Sep 15, 2010·Critical Care : the Official Journal of the Critical Care Forum·Robert Dickinson, Nicholas P Franks
Mar 23, 2006·Anesthesia and Analgesia·Toshihiko MitsuyoEarl Carstens
Nov 26, 2009·Anesthesia and Analgesia·Yun WengJames M Sonner
Feb 22, 2012·Anesthesia and Analgesia·James R TrudellM Bruce Maciver
Nov 21, 2014·BMC Pharmacology & Toxicology·Robert J Brosnan, Trung L Pham
Nov 15, 2006·Journal of Clinical Monitoring and Computing·Leslie C Jameson, Tod B Sloan
May 23, 2012·Current Opinion in Anaesthesiology·Edward J Bertaccini, James R Trudell
Nov 20, 2001·Current Opinion in Pharmacology·S A Thompson, K Wafford
Oct 4, 2006·Current Opinion in Anaesthesiology·J G Bovill
Apr 2, 1998·Anesthesiology·N L Harrison
Sep 2, 2000·Anesthesiology·R DickinsonN P Franks
Feb 10, 1999·Anesthesiology·A JenkinsW R Lieb
Dec 23, 2015·Anesthesiology·Ervin PejoDouglas E Raines
Nov 23, 2005·Journal of Neurochemistry·Nathalie BoulineauErwin Sigel
Jan 13, 2006·British Journal of Pharmacology·Nicholas P Franks
Aug 26, 2010·British Journal of Pharmacology·P-L Chau
Mar 5, 2014·Acta Anaesthesiologica Scandinavica·G ErdoesB Eberle

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