Opioid peptide receptor studies. 9. Identification of a novel non-μ- non-δ-like opioid peptide binding site in rat brain

N. I. Qing, X. U. Heng, John S. Partilla, Kenner C. Rice, Dorota Matecka, Silvia N. Calderon, Frank Porreca, Josephine Lai, Helmut Schmidhammer, Roland Krassnig, Richard B. Rothman

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

Quantitative binding studies resolved two high-affinity [3H][D-Ala2,D- Leu5]enkephalin binding sites in rat brain membranes depleted of μ binding sites by pretreatment with the irreversible agent BIT. - The two binding sites had lower (δ(nc-x), Ki = 96.6 nM) and higher ({dncx-1) , Ki = 1.55 nM) affinity for DPDPE. The ligand-selectivity profile of the δ(ncx-1) site was that of a classic δ binding site. The ligand-selectivity profile of the δ(ncx-2) site was neither μ- or δ-like. The Ki values of selected agents for the δ(ncx-2) site were: [pCl]DPDPE (3.9 nM), DPLPE (140 nM), and DAMGO (2.6 nM), under these assay conditions, [3H][D-Ala2,D-Leu5]enkephalin binding to the cells expressing the cloned μ receptor is very low and pretreatment of cell membranes with BIT almost completely inhibits [3H]DAMGO and [3H][D-Ala2,D-Leu5]enkephalin binding. Intracerebroventricular administration of antisense DNA to the cloned delta receptor selectively decreased [3H][D-Ala2,D-Leu5]enkephalin binding to the δ(ncx-1) site. Administration of buprenorphine to rats 24 h prior to preparation of membranes differentially affected μ, δ(ncx-1), and δ(ncx-2) binding sites. Viewed collectively, these studies have identified a novel non-μ- non-δ- like binding site in rat brain.

Original languageEnglish (US)
Pages (from-to)1079-1090
Number of pages12
JournalPeptides
Volume19
Issue number6
DOIs
StatePublished - Jun 1 1998

Keywords

  • Acetalin
  • Antisense DNA
  • Delta receptors
  • Ligand binding
  • Opiate receptors

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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