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No evidence for G-protein-coupled epsilon receptor in the brain of triple opioid receptor knockout mouse

Academic Article
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Overview

authors

  • Contet, Candice
  • Matifas, A.
  • Kieffer, B. L.

publication date

  • 2004

journal

  • European Journal of Pharmacology  Journal

abstract

  • Pharmacological approaches have defined the epsilon receptor as a beta-endorphin-preferring opioid receptor, described in rat vas deferens and in brain of several species. Only three opioid receptors-mu, delta and kappa-have been cloned and the existence of this additional subtype as a distinct protein remains controversial. Recently, the mouse brain epsilon receptor was detected in a G protein activation assay, as mediating residual beta-endorphin activity following pharmacological blockade of mu, delta and kappa receptors. To clarify whether this site is independent from mu, delta and kappa receptors, we performed beta-endorphin-induced [(35)S]GTPgammaS binding using mice lacking these three receptors (triple knockout mice). We tested both pons-medulla and whole brain preparations. beta-Endorphin strongly stimulated [(35)S]GTPgammaS binding in wild-type membranes but had no detectable effect in membranes from triple knockout mice. We conclude that the brain epsilon site involves mu, delta and/or kappa receptors, possibly coupled to nonclassical G proteins.

subject areas

  • Animals
  • Binding, Competitive
  • Brain
  • Female
  • GTP-Binding Proteins
  • Humans
  • In Vitro Techniques
  • Male
  • Medulla Oblongata
  • Mice
  • Mice, Knockout
  • Pons
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • beta-Endorphin
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Research

keywords

  • [S-35]GTP gamma S binding
  • epsilon receptor
  • knockout mice
  • opioid receptor
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Identity

International Standard Serial Number (ISSN)

  • 0014-2999

Digital Object Identifier (DOI)

  • 10.1016/j.ejphar.2004.03.056

PubMed ID

  • 15178356
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Additional Document Info

start page

  • 131

end page

  • 136

volume

  • 492

issue

  • 2-3

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