PMID: 10781289Apr 26, 2000Paper

Intravenous anesthetics differentially modulate ligand-gated ion channels

Anesthesiology
P Flood, M D Krasowski

Abstract

Heteromeric neuronal nicotinic acetylcholine receptors (nAChRs) are potently inhibited by volatile anesthetics, but it is not known whether they are affected by intravenous anesthetics. Ketamine potentiates gamma-aminobutyric acid type A (GABAA) receptors at high concentrations, but it is unknown whether there is potentiation at clinically relevant concentrations. Information about the effects of intravenous anesthetics with different behavioral profiles on specific ligand-gated ion channels may lead to hypotheses as to which ion channel effect produces a specific anesthetic behavior. A heteromeric nAChR composed of alpha4 and beta4 subunits was expressed heterologously in Xenopus laevis oocytes. Using the two-electrode voltage clamp technique, peak ACh-gated current was measured before and during application of ketamine, etomidate, or thiopental. The response to GABA of alpha1beta2gamma2s GABAA receptors expressed in human embryonic kidney cells and Xenopus oocytes was compared with and without coapplication of ketamine from 1 microm to 10 mm. Ketamine caused potent, concentration-dependent inhibition of the alpha4beta4 nAChR current with an IC50 of 0.24 microm. The inhibition by ketamine was use-dependent; the antagonist was ...Continue Reading

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Citations

Oct 2, 2003·European Journal of Pharmacology·Mahsa Hadipour-Jahromy, Stephen Daniels
Jul 27, 2001·Brain Research Bulletin·O MameliF Sanna Randaccio
Feb 19, 2002·Brain Research Bulletin·Edömer TassonyiDaniel Bertrand
Nov 20, 2001·Current Opinion in Pharmacology·S A Thompson, K Wafford
Jun 10, 2010·Journal of the American Chemical Society·Hansjörg JerabekThomas Stockner
Jul 12, 2008·International Anesthesiology Clinics·Christa J Van DortRalph Lydic
Jun 6, 2009·European Journal of Anaesthesiology·Andrea Kopp LugliChristoph H Kindler
Nov 1, 2011·The Journal of Pharmacology and Experimental Therapeutics·Yuri A BlednovR Adron Harris
Mar 27, 2001·Annual Review of Pharmacology and Toxicology·T YamakuraR A Harris
Jul 23, 2005·Anesthesia and Analgesia·Julia O UdeskyPamela Flood
Mar 23, 2006·Anesthesia and Analgesia·Toshihiko MitsuyoEarl Carstens
Oct 24, 2006·Anesthesia and Analgesia·Yasumasa TanifujiJames M Sonner
Nov 29, 2007·Anesthesia and Analgesia·Andrea ParisPeter H Tonner
Aug 21, 2008·Anesthesia and Analgesia·Edmond I EgerJames M Sonner
Feb 4, 2006·American Journal of Veterinary Research·Alonso G P GuedesElaine P Rudé
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
Apr 20, 2002·Anesthesiology·Pamela Flood, Kristen M Coates
Aug 31, 2013·Journal of Clinical Anesthesia·Michael G FitzsimonsKeith H Baker
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Mar 8, 2006·The International Journal of Biochemistry & Cell Biology·Hugo R AriasCecilia Bouzat
Aug 30, 2005·Trends in Pharmacological Sciences·Hugh C HemmingsNeil L Harrison

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