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

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

SUBMITTER: Virk MS 

PROVIDER: S-EPMC3640555 | biostudies-literature | 2008 Apr

REPOSITORIES: biostudies-literature