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Opioid receptor internalization contributes to dermorphin-mediated antinociception.

T A Macey1, S L Ingram, E N Bobeck

  • 1Department of Psychology, Washington State University Vancouver, 14204 NE Salmon Creek Avenue, Vancouver, WA 98686, USA.

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|April 17, 2010
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Summary

Opioid receptor internalization is crucial for antinociception. Blocking mu-opioid receptor (MOPr) internalization in the ventrolateral periaqueductal gray (vlPAG) reduces pain relief, indicating internalization is key for opioid signaling.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Opioid administration into the ventrolateral periaqueductal gray (vlPAG) induces antinociception via mu-opioid receptors (MOPrs).
  • Limited MOPr internalization by low-efficacy agonists suggests internalization and signaling may be independent processes.

Purpose of the Study:

  • To investigate the role of MOPr internalization in mediating antinociception induced by opioid microinjection into the vlPAG.
  • To determine if opioid receptor signaling leading to antinociception is dependent on receptor internalization.

Main Methods:

  • Utilized awake, behaving rats for experiments.
  • Employed microinjection of a fluorescently labeled dermorphin analog (DERM-A594) into the vlPAG.
  • Administered irreversible opioid antagonist (beta-chlornaltrexamine), internalization blockers (dynamin-DN, ConA), and GABA(A) antagonist (bicuculline).

Main Results:

  • Microinjected DERM-A594 produced both antinociception and MOPr internalization in the vlPAG.
  • Opioid receptor antagonist and internalization blockers significantly reduced DERM-A594-induced antinociception and internalization.
  • Blocking internalization decreased the potency of dermorphin-induced antinociception but did not affect bicuculline-induced antinociception.

Conclusions:

  • Opioid receptor-mediated antinociception in the vlPAG is dependent on MOPr internalization.
  • These findings indicate that key aspects of opioid signaling require receptor internalization.