δ-Opioid receptor binding in mouse brain: Evidence for heterogeneous binding sites

M. Sofuoglu, P. S. Portoghese, A. E. Takemori

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39 Scopus citations

Abstract

In this study we investigated the characteristics of binding sites with which δ opioid receptor agonists interact in homogenates of mouse brain using Krebs-HEPES medium. [3H][D-Ser2, Leu5, Thr6]enkephalin (DSLET), [3H][D-Ala2, D-Leu5]enkephalin (DADLE) and [3H][D-Pen2, D-Pen5]enkephalin (DPDPE) were used to label δ opioid binding sites. The analyses of the saturation binding data of these ligands (Scatchard plots) gave best fits to single rather than multiple site models. The binding capacity (Bmax) labelled [3H]DSLET was found to be significantly greater than those of [3H]DADLE and [3H]DPDPE in brains of mice. Naltriben (the benzofuran analogue of natrindole) was equally effective in competing for [3H]DSLET, [3H]DPDPE and [3H]DADLE binding sites. On the other hand, DADLE was significantly more potent in competing for [3H]DADLE and [3H]DPDPE binding sites than for [3H]DSLET binding sites. Also DPDPE was more potent in competing for the binding sites of [3]DADLE and [3H]DPDPE than for those of [3DSLET. DSLET was found to be equipotent in competing for [3H]DSLET, [3H]DPDPE and [3H]DADLE binding sites. These results suggest a heterogeneity of δ opioid receptors which may be explained possibly by the existence of δ opioid receptor subtypes.

Original languageEnglish (US)
Pages (from-to)273-277
Number of pages5
JournalEuropean Journal of Pharmacology
Volume216
Issue number2
DOIs
StatePublished - Jun 5 1992

Bibliographical note

Funding Information:
This investigation was supported by U.S. Public Health Service Grants from the National Institute on Drug Abuse. Studies in this report were carried out in accordance with the Declaration of Helsinki and/or with the guide for the care and use of laboratory animals as adopted and promulgated by the National Institutes of Health.

Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.

Keywords

  • DADLE (D-Ala, D-Leu]enkephalin)
  • DPDPE ([D-Pen, D-Pen]enkephalin)
  • DSLET ([D-Ser, Leu, Thr]enkephalin)
  • Naltriben
  • δ-Opioid receptor subtypes

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