Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with μ- opioid receptor in rat brain and CHO-μ/1 cell line

Mariana Spetea, Ferenc Ötvös, Géza Tóth, Thi M.D. Nguyen, Peter W. Schiller, Zvi Vogel, Anna Borsodi

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

Opioid receptor binding properties of [3H]Tyr-D-Ala-Phe-Phe-NH2 (TAPP) were characterized in rat brain and Chinese hamster ovary (CHO) cells expressing the rat μ-receptor. In rat brain, [3H]TAPP labeled a single class of opioid sites with a dissociation constant (K(d)) of 0.31 nM and maximal number of binding sites (B(max)) of 119 fmol/mg protein. In CHO-μ/l cell membranes, the K(d) and B(max) values were 0.78 nM and 1806 fmol/mg protein, respectively. Binding to rat brain was demonstrated to be pharmacologically identical to that obtained with CHO-μ/l cell membranes and modulated by Na+ ions and guanine nucleotides. The high affinity and selectivity of [3H]TAPP together with its low non-specific binding make this radioligand a useful tool for labeling the native and cloned μ-opioid receptor.

Original languageEnglish
Pages (from-to)1091-1098
Number of pages8
JournalPeptides
Volume19
Issue number6
DOIs
Publication statusPublished - Jun 1 1998

Keywords

  • CHO-μl cell line
  • Opioid receptors
  • Radioligand binding
  • Rat brain
  • [H]TAPP
  • μ-Opioid agonist peptides

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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