Characterization of functional μ opioid receptor turnover in rat locus coeruleus: an electrophysiological and immunocytochemical study.
After near-complete, irreversible μ receptor inactivation with β–funaltrexamine (β-FNA), opioid effect spontaneously recovered in a rapid and efficaciousmanner. In contrast, α2-adrenoceptor-mediated effect hardly recovered after receptor inactivation with the irreversible antagonist EEDQ. When the r...
| Autores: | , , , , , , , |
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| Tipo de recurso: | artículo |
| Fecha de publicación: | 2017 |
| País: | España |
| Institución: | Universidad del País Vasco |
| Repositorio: | Addi. Archivo Digital para la Docencia y la Investigación |
| OAI Identifier: | oai:addi.ehu.eus:10810/74905 |
| Acceso en línea: | http://hdl.handle.net/10810/74905 |
| Access Level: | acceso abierto |
| Palabra clave: | opioid tolerance μ receptors noradrenergic nucleus locus coeruleus |
| Sumario: | After near-complete, irreversible μ receptor inactivation with β–funaltrexamine (β-FNA), opioid effect spontaneously recovered in a rapid and efficaciousmanner. In contrast, α2-adrenoceptor-mediated effect hardly recovered after receptor inactivation with the irreversible antagonist EEDQ. When the recovery of opioid effect was tested after various inactivating time schedules, we found that the longer the β-FNA pre exposure, the less efficient and slower the functional μ receptor turnover became. Interestingly, μ receptor turnover was slower when β-FNA challenge was repeated in the same cell, indicating constitutive μ receptor recycling by trafficking from a depletable pool. Double immunocytochemistry confirmed the constitutive nature of μ receptor trafficking from a cytoplasmic compartment. The μ receptor turnover was slowed down when LC neuron calcium- or firing-dependent processes were prevented or vesicular protein trafficking was blocked by a low temperature or transport inhibitor. |
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