Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans

Krisztina Monory, Elisabeth Greiner, Nana Sartania, László Sallai, Yves Pouille, Helmut Schmidhammer, Jacques Hanoune, Anna Borsodi

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Abstract

Several hydrazone, oxime, carbazone and semicarbazone derivatives of 14- alkoxycodeinones and 14-alkoxydihydrocodeinones were synthesised [1] and characterised in in vitro radioligand binding assays in rat brain membrane preparations. The tested compounds show the highest affinity for the mu opioid binding sites and most of them have agonist character. Subtype analysis of the binding shows mu2 specificity. However, some of these ligands are able to block partially (40-60%) the high affinity (putative mu1) opioid binding sites while all of them act as reversible ligands at the low affinity (putative mu2) sites.

Original languageEnglish
Pages (from-to)2011-2020
Number of pages10
JournalLife Sciences
Volume64
Issue number22
DOIs
Publication statusPublished - Apr 23 1999

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Keywords

  • Affinity label
  • Alkoxymorphinans
  • In vitro receptor binding
  • Mu opioid receptor

ASJC Scopus subject areas

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

Cite this

Monory, K., Greiner, E., Sartania, N., Sallai, L., Pouille, Y., Schmidhammer, H., Hanoune, J., & Borsodi, A. (1999). Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans. Life Sciences, 64(22), 2011-2020. https://doi.org/10.1016/S0024-3205(99)00148-4