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  • Title: Interaction of [D-Pen2,D-Pen5]enkephalin and [D-Ala2,Glu4]deltorphin with delta-opioid receptor subtypes in vivo.
    Author: Vanderah T, Takemori AE, Sultana M, Portoghese PS, Mosberg HI, Hruby VJ, Haaseth RC, Matsunaga TO, Porreca F.
    Journal: Eur J Pharmacol; 1994 Feb 03; 252(2):133-7. PubMed ID: 8157053.
    Abstract:
    The interaction of [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2,Glu4]deltorphin with delta-opioid receptor subtypes was investigated. Pretreatment of mice with the delta 1-opioid receptor antagonist, [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., delta 1-opioid receptors blocked), DPDPE was able to significantly antagonize the antinociceptive effects of [D-Ala2,Glu4]deltorphin. Pretreatment of mice with the delta 2-opioid receptor antagonist, naltrindole-5'-isothiocyanate (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., delta 2-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 delta 2-opioid receptor in vivo, and that neither agonist nor antagonist actions can be demonstrated at delta 1-opioid receptors for this peptide. In contrast, under appropriate conditions, DPDPE can be shown to interact with both delta 1- and delta 2-opioid receptor subtypes; DPDPE may have limited efficacy (i.e., is a partial agonist) at the delta 2-opioid receptor.
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