Interaction of [d-Pen2, d-Pen5]enkephalin and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes in vivo

T. Vanderah, A. E. Takemori, M. Sultana, P. S. Portoghese, H. I. Mosberg, V. J. Hruby, R. C. Haaseth, T. O. Matsunaga, F. Porreca

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52 Scopus citations

Abstract

The interaction of [d-Pen2, d-Pen5]enkephalin (DPDPE) and [d-Ala2, Glu4]deltorphin with δ-opioid receptor subtypes was investigated. Pretreatment of mice with the δ1-opioid receptor antagonists, [d-Ala2, Leu5, Cys6]enkephalin (DALCE), produced a virtually complete antagonism of the antinociceptive actions of DPDPE, but had no effect on those of [d-Ala2, Glu4]deltorphin. In DALCE pretreated mice (i.e., δ1-opioid receptors blocked), DPDPE was able to significantly antagonize the antinociceptive effects of [d-Ala2, Glu4]deltorphin. Pretreatment of mice with the δ2-opioid receptor antagonist, na naltrindole-5′-isothiocynate (5′-NTII) produced a virtually complete antagonism of the antinociceptive effects of [d-Ala2, Glu4]deltorphin, but had no effect on the antinociception produced by DPDPE. In 5′-NTII pretreated mice (i.e., δ2-opioid receptors blocked), [d-Ala2, Glu4]deltorphin had no effect on the antinociception produced by DPDPE. These data suggest that [d-Ala2, Glu4]deltorphin is highly selective for the δ2-opioid receptor in vivo, and that neither agonist nor antagonist actions can be demonstrated at δ1-opioid receptors for this peptide. In contrast, under appropriate conditions, DPDPE can be shown to interact with both δ1- and δ2-opioid receptor subtypes; DPDPE may have limited efficacy (i.e., is a partial agonist) at the δ2-opioid receptor.

Original languageEnglish (US)
Pages (from-to)133-137
Number of pages5
JournalEuropean Journal of Pharmacology
Volume252
Issue number2
DOIs
StatePublished - Feb 3 1994

Keywords

  • (Mouse)
  • Antinociception
  • DPDPE ([d-Pen, d-Pen]enkephalin)
  • Opioid
  • [d-Ala, Glu]Deltorphin
  • δ-Opioid receptor subtype

ASJC Scopus subject areas

  • Pharmacology

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