Binding properties of the pure opioid antagonist [3H](N-propyl)-noroxymorphone in rat brain membranes.

G. Tóth, S. Benyhe, S. Hosztafi, A. Borsodi

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

(-)[N-(propyl)-14-OH-dihydromorphinan-6-one] = (N-propyl)-noroxymorphone and its multiple tritiated form (molar activity: 126 Ci/mmol; 1 Ci = 37 GBq) was synthesized. According to our knowledge this specific radioactivity exceeds all of the commercially available [3H]opioid ligands. The ligand was found to be a pure opioid antagonist in receptor binding assays performed with rat brain membranes. Scatchard analysis of equilibrium binding isotherms revealed one high affinity (Kd approximately 4 nM) binding site. Reversibility, stereospecificity and opioid nature of the binding was confirmed by ligand binding experiments. Because of its antagonist character combined with high specific radioactivity the ligand might be a useful tool in characterizing and purifying opioid receptors.

Original languageEnglish
Pages (from-to)327-335
Number of pages9
JournalNeurobiology (Budapest, Hungary)
Volume1
Issue number4
Publication statusPublished - 1993

ASJC Scopus subject areas

  • Neuroscience(all)

Fingerprint Dive into the research topics of 'Binding properties of the pure opioid antagonist [3H](N-propyl)-noroxymorphone in rat brain membranes.'. Together they form a unique fingerprint.

  • Cite this