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British journal of pharmacology

Characterization of functional μ opioid receptor turnover in rat locus coeruleus: an electrophysiological and immunocytochemical study.


PMID 28589556

Abstract

Regulation of μ receptor dynamics such as its trafficking is a possible mechanism underlying opioid tolerance that contributes to inefficient recycling of opioid responses. We aimed to characterize the functional turnover of μ receptors in the noradrenergic nucleus locus coeruleus (LC). We measured opioid effect by single-unit extracellular recordings of LC neurons from rat brain slices. Immunocytochemical techniques were used to evaluate μ receptor trafficking. After near-complete, irreversible μ receptor inactivation with β-funaltrexamine (β-FNA), opioid effect spontaneously recovered in a rapid and efficacious manner. In contrast, α Constitutive trafficking of μ receptors from a depletable intracellular pool (endosome) may account for its rapid and efficient functional turnover in the LC. A finely-tuned regulation of μ receptor trafficking and endosomes could explain neuroadaptive plasticity to opioids in the LC.

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