Characterization of functional μ opioid receptor turnover in rat locus coeruleus: an electrophysiological and immunocytochemical study.
Autor: | Medrano MC; Department of Pharmacology, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Santamarta MT; Department of Pharmacology, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Pablos P; Department of Pharmacology, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Aira Z; Department of Neuroscience, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Buesa I; Department of Neuroscience, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Azkue JJ; Department of Neuroscience, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Mendiguren A; Department of Pharmacology, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain., Pineda J; Department of Pharmacology, Faculty of Medicine and Nursing, University of the Basque Country (UPV/EHU), Leioa, Bizkaia, Spain. |
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Jazyk: | angličtina |
Zdroj: | British journal of pharmacology [Br J Pharmacol] 2017 Aug; Vol. 174 (16), pp. 2758-2772. Date of Electronic Publication: 2017 Jul 07. |
DOI: | 10.1111/bph.13901 |
Abstrakt: | Background and Purpose: 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). Experimental Approach: 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. Key Results: 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 Conclusions and Implications: 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. (© 2017 The British Pharmacological Society.) |
Databáze: | MEDLINE |
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