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Synergistic antinociceptive actions and tolerance development produced by morphine-fentanyl coadministration: correlation with _-opioid receptor internalization
dc.creator | Silva-Moreno, Arturo | |
dc.creator | González-Espinosa, Claudia | |
dc.creator | León-Olea, Martha | |
dc.creator | Cruz, Silvia L. | |
dc.date.accessioned | 2017-06-30T02:06:09Z | |
dc.date.available | 2017-06-30T02:06:09Z | |
dc.date.issued | 2012 | es_ES |
dc.identifier | 1526 | es_ES |
dc.identifier.issn | 0014-2999 | es_ES |
dc.identifier.uri | http://repositorio.inprf.gob.mx/handle/123456789/6205 | |
dc.identifier.uri | https://doi.org/10.1016/j.ejphar.2011.10.034 | es_ES |
dc.language.iso | eng | es_ES |
dc.relation | 674 (2-3) 239-247 p. | es_ES |
dc.relation | versión del editor | es_ES |
dc.rights | acceso cerrado | es_ES |
dc.title | Synergistic antinociceptive actions and tolerance development produced by morphine-fentanyl coadministration: correlation with _-opioid receptor internalization | es_ES |
dc.type | article | es_ES |
dc.contributor.affiliation | Departamento de Farmacobiología, Cinvestav, Sede Sur. Calzada de Tenorios # 235, Col. Granjas Coapa, México DF, 14330, México. | es_ES |
dc.contributor.email | slcruz@cinvestav.mx | es_ES |
dc.relation.jnabreviado | EUR J PHARMACOL | es_ES |
dc.relation.journal | European Journal of Pharmacology | es_ES |
dc.identifier.place | Países Bajos | es_ES |
dc.date.published | 2012 | es_ES |
dc.identifier.organizacion | Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz | es_ES |
dc.identifier.eissn | 1879-0712 | es_ES |
dc.identifier.doi | 10.1016/j.ejphar.2011.10.034 | es_ES |
dc.description.month | Ene | es_ES |
dc.description.abstractotrodioma | It has been described that coadministration of opioids with low doses of other analgesics can reduce adverse effects and increase antinociception, but combinations of two _-opioid receptor agonists have been poorly explored. The objective of this work was threefold: 1) to evaluate the antinociceptive combination of i.c.v. morphine and fentanyl at different doses; 2) to compare the antinociception produced by acute or repeated administration of an effective morphine dose (1 _g) alone, or combined with a low fentanyl dose (1 ng); and 3) to correlate these effects with _-opioid receptor internalization in periaqueductal gray matter and locus coeruleus. Antinociception was evaluated by the tail-flick test and receptor internalization was analyzed by confocal microscopy in Wistar rats. Drug interactions were examined by administering combinations of opioids in 1:3, 1:1 and 3:1 ratios of their respective ED(50) fractions. For tolerance and internalization studies, animals were i.c.v. injected only once (acute treatment) or twice a day until five administrations were completed. Our results show that morphine and fentanyl have synergistic effects. The combination of 1 ng fentanyl with 1 _g morphine increases the magnitude and duration of antinociception not only after a single injection, but also after five administrations when tolerance develops to morphine alone. Increased and long-lasting antinociception correlates positively with increased _-arrestin 2 activity and _-opioid receptor internalization in periaqueductal gray matter and locus coeruleus. These results suggest that combined administration of morphine and fentanyl increases long-lasting antinociception and _-arrestin 2 signaling contributes to the combination effects | es_ES |
dc.subject.ko | Analgesics, Opioid | es_ES |
dc.subject.ko | administration & dosage | es_ES |
dc.subject.ko | Analgesics, Opioid | es_ES |
dc.subject.ko | pharmacology | es_ES |
dc.subject.ko | Animals | es_ES |
dc.subject.ko | Arrestins | es_ES |
dc.subject.ko | metabolism | es_ES |
dc.subject.ko | Dose-Response Relationship, Drug | es_ES |
dc.subject.ko | Drug Synergism | es_ES |
dc.subject.ko | Drug Tolerance | es_ES |
dc.subject.ko | Endocytosis | es_ES |
dc.subject.ko | drug effects | es_ES |
dc.subject.ko | Fentanyl | es_ES |
dc.subject.ko | administration & dosage | es_ES |
dc.subject.ko | Fentanyl | es_ES |
dc.subject.ko | pharmacology | es_ES |
dc.subject.ko | Locus Coeruleus | es_ES |
dc.subject.ko | drug effects | es_ES |
dc.subject.ko | Locus Coeruleus | es_ES |
dc.subject.ko | metabolism | es_ES |
dc.subject.ko | Male | es_ES |
dc.subject.ko | Morphine | es_ES |
dc.subject.ko | administration & dosage | es_ES |
dc.subject.ko | Morphine | es_ES |
dc.subject.ko | pharmacology | es_ES |
dc.subject.ko | Nociception | es_ES |
dc.subject.ko | drug effects | es_ES |
dc.subject.ko | Periaqueductal Gray | es_ES |
dc.subject.ko | drug effects | es_ES |
dc.subject.ko | Periaqueductal Gray | es_ES |
dc.subject.ko | metabolism | es_ES |
dc.subject.ko | Rats | es_ES |
dc.subject.ko | Rats, Wistar | es_ES |
dc.subject.ko | Receptors, Opioid, mu | es_ES |
dc.subject.ko | agonists | es_ES |
dc.subject.ko | Receptors, Opioid, mu | es_ES |
dc.subject.ko | metabolism | es_ES |
dc.subject.ko | Analgesics, Opioid | es_ES |
dc.subject.ko | Arrestins | es_ES |
dc.subject.ko | Receptors, Opioid, mu | es_ES |
dc.subject.ko | beta-arrestin | es_ES |
dc.subject.ko | Fentanyl | es_ES |
dc.subject.ko | Morphine | es_ES |
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