Opioid peptide receptor studies. 1. Identification of a novel δ-opioid receptor binding site in rat brain membranes

Xian Yuan Cha, Heng Xu, Kenner C. Rice, Frank Porreca, Josephine Lai, Subramaniam Ananthan, Richard B. Rothman

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

Our laboratory was among the first to propose the existence of δ receptor subtypes: a δ site thought to be associated with a μ-δ-opioid receptor complex termed the δcx binding site and δ site not associated with the μ-δ-opioid receptor complex, termed the δncx site. In previous studies, we assayed the δcx site with [3H][d-Ala2,d-Leu5]enkephalin using rat brain membranes depleted of δncx sites by pretreatment with the site-directed acylating agent, (+)-trans-SUPERFIT. In the present study, we investigated, using (+)-trans-SUPERFIT-pretreated membranes, the possibility of heterogeneity of the δcx binding site. Two sites were resolved: the δcx-1 site at which μ ligands are potent noncompetitive inhibitors and δ ligands are weak competitive inhibitors, and the δcx-2 site has a δ-like ligand-selectivity profile, several experiments distinguished it from the δncx site. Two lines of evidence suggest that the δncx site corresponds to the cloned δ receptor. One, the δ receptor was cloned from the NG108-15 cell line, and this receptor, like the δncx binding site, irreversibly binds SUPERFIT and (+)-trans-SUPERFIT. Secondly, administration of δ-antisense DNA selectively decreases δncx binding. Viewed collectively, the major finding of this study is the discovery of a novel SUPERFIT-insensitive and δ-antisense-insensitive δcx-2 binding site.

Original languageEnglish (US)
Pages (from-to)191-198
Number of pages8
JournalPeptides
Volume16
Issue number2
DOIs
StatePublished - 1995

Fingerprint

Peptide Receptors
Opioid Peptides
Opioid Receptors
Rats
Brain
Binding Sites
Membranes
Ligands
Antisense DNA
Enkephalins
Cells
3-methylfentanyl isothiocyanate
Cell Line
Experiments

Keywords

  • Antisense DNA
  • Deltorphin
  • Opioid receptors
  • SUPERFIT
  • δ Receptor

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Opioid peptide receptor studies. 1. Identification of a novel δ-opioid receptor binding site in rat brain membranes. / Cha, Xian Yuan; Xu, Heng; Rice, Kenner C.; Porreca, Frank; Lai, Josephine; Ananthan, Subramaniam; Rothman, Richard B.

In: Peptides, Vol. 16, No. 2, 1995, p. 191-198.

Research output: Contribution to journalArticle

Cha, Xian Yuan ; Xu, Heng ; Rice, Kenner C. ; Porreca, Frank ; Lai, Josephine ; Ananthan, Subramaniam ; Rothman, Richard B. / Opioid peptide receptor studies. 1. Identification of a novel δ-opioid receptor binding site in rat brain membranes. In: Peptides. 1995 ; Vol. 16, No. 2. pp. 191-198.
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