Document Detail

Analysis of the effects of anesthetics and ethanol on mu-opioid receptor.
MedLine Citation:
PMID:  20379080     Owner:  NLM     Status:  MEDLINE    
G protein-coupled receptors, in particular, Ca(2+)-mobilizing G(q)-coupled receptors have been reported to be targets for anesthetics. Opioids are commonly used analgesics in clinical practice, but the effects of anesthetics on the opioid mu-receptors (muOR) have not been systematically examined. We report here an electrophysiological assay to analyze the effects of anesthetics and ethanol on the functions of muOR in Xenopus oocytes expressing a muOR fused to chimeric Galpha protein G(qi5) (muOR-G(qi5)). Using this system, the effects of halothane, ketamine, propofol, and ethanol on the muOR functions were analyzed. In oocytes expressing muOR-G(qi5), the( )muOR agonist DAMGO ([D-Ala(2),N-MePhe(4),Gly-ol]-enkephalin) elicited Ca(2+)-activated Cl(-) currents in a concentration-dependent manner (EC(50) = 0.24 microM). Ketamine, propofol, halothane, and ethanol themselves did not elicit any currents in oocytes expressing muOR-G(qi5), whereas ketamine and ethanol inhibited the DAMGO-induced Cl(-) currents at clinically equivalent concentrations. Propofol and halothane inhibited the DAMGO-induced currents only at higher concentrations. These findings suggest that ketamine and ethanol may inhibit muOR functions in clinical practice. We propose that the electrophysiological assay in Xenopus oocytes expressing muOR-G(qi5) would be useful for analyzing the effects of anesthetics and analgesics on opioid receptor function.
Kouichiro Minami; Yuka Sudo; Seiji Shiraishi; Masanori Seo; Yasuhito Uezono
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-02
Journal Detail:
Title:  Journal of pharmacological sciences     Volume:  112     ISSN:  1347-8648     ISO Abbreviation:  J. Pharmacol. Sci.     Publication Date:  2010  
Date Detail:
Created Date:  2010-04-28     Completed Date:  2010-08-12     Revised Date:  2011-06-20    
Medline Journal Info:
Nlm Unique ID:  101167001     Medline TA:  J Pharmacol Sci     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  424-31     Citation Subset:  IM    
Department of Anesthesiology and Critical Care Medicine, Jichi Medical University, Japan.
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MeSH Terms
Analgesics, Opioid / pharmacology
Anesthetics / pharmacology*
Chloride Channels / drug effects
Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / pharmacology
Ethanol / pharmacology*
Halothane / pharmacology
Ketamine / pharmacology
Propofol / pharmacology*
Receptors, Opioid, mu / drug effects*
Xenopus laevis
Reg. No./Substance:
0/Analgesics, Opioid; 0/Anesthetics; 0/Chloride Channels; 0/Receptors, Opioid, mu; 100929-53-1/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; 151-67-7/Halothane; 2078-54-8/Propofol; 64-17-5/Ethanol; 6740-88-1/Ketamine

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