Agonist-specific regulation of mu-opioid receptor desensitization and recovery from desensitization

Molecular Pharmacology
Michael S Virk, John T Williams

Abstract

Agonist-selective actions of opioids on the desensitization of mu-opioid receptors (MORs) have been well characterized, but few if any studies have examined agonist-dependent recovery from desensitization. The outward potassium current induced by several opioids was studied using whole-cell voltage-clamp recordings in locus ceruleus neurons. A brief application of the irreversible opioid antagonist beta-chlornaltrexamine (beta-CNA) was applied immediately after treatment of slices with saturating concentrations of opioid agonists. This approach permitted the measurement of desensitization and recovery from desensitization using multiple opioid agonists, including [Met](5)enkephalin (ME), [d-Ala(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin (DAMGO), etorphine, fentanyl, methadone, morphine, morphine-6-glucuronide, oxycodone, and oxymorphone. The results indicate that desensitization protects receptors from irreversible antagonism with beta-CNA. The amount of desensitization was measured as the decrease in current during a 10-min application of a saturating agonist concentration and was a good predictor of the extent of receptor protection from irreversible inactivation with beta-CNA. After desensitization with ME or DAMGO and treatment w...Continue Reading

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Citations

Aug 27, 2010·The Journal of Pharmacology and Experimental Therapeutics·Leon W FyfeSusan L Ingram
Jul 10, 2008·Molecular Pharmacology·Seksiri ArttamangkulJohn T Williams
Nov 25, 2011·Molecular Pharmacology·Seksiri ArttamangkulJohn T Williams
May 4, 2012·Molecular Pharmacology·Guadalupe RiveroEamonn Kelly
Aug 24, 2012·Molecular Pharmacology·Erica S Levitt, John T Williams
Jan 17, 2013·Pharmacological Reviews·John T WilliamsMacdonald J Christie
Jun 6, 2009·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Michael S VirkJohn T Williams
Mar 1, 2013·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·William T BirdsongJohn T Williams
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