Slide-binding characterization and autoradiographic localization of delta opioid receptors in rat and mouse brains with the tetrapeptide antagonist [3H]TIPP

Lidia Bakota, Judit Szikra, Geza Toth, Karoly Gulya

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Slide-binding and autoradiographic studies were performed on cryostat sections from brains of adult Sprague-Dawley rats and BALB C mice to describe the binding characteristics of the tetrapeptide [3H]TIPP, an antagonist with high specificity and affinity for the delta opioid receptors. Steady-state binding of [3H]TIPP to cryostat sections of brain paste was reached in 120- 180 min of incubation. Specific [3H]TIPP binding resulted in maximal numbers of binding sites (B(max)) of 15.59 and 23.91 fmol/mg protein, and dissociation constants (K(d)) of 0.46 and 0.85 nM for rat and mouse brain paste sections, respectively. TIPP displayed the highest affinity for delta opioid receptors in inhibiting specific [3H]TIPP binding, with IC50 values of 0.82 nM and 0.14 nM in rat and mouse brain sections, respectively. While DPDPE was also effective in displacing the specific binding of [3H]TIPP (IC50 = 3.18 ± 0.53 nM and 0.63 ± 0.42 nM in rat and mouse brain paste sections, respectively), other subclass-selective or nonopioid ligands were much less effective, or ineffective. Autoradiographic localization of [3H]TIPP binding revealed the characteristic distribution of delta opioid receptors in both species. In consequence of its antagonistic nature, and of its unnatural amino acid residue, which makes this ligand more resistant to biodegradation, [3H]TIPP is a superior ligand for evaluation of the binding characteristics and autoradiogaphic distribution of the delta opioid receptors.

Original languageEnglish
Pages (from-to)1377-1385
Number of pages9
JournalLife Sciences
Volume63
Issue number15
DOIs
Publication statusPublished - Sep 4 1998

Keywords

  • Autoradiography
  • Delta opioid antagonist
  • Delta opioid receptor
  • Slide- binding

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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