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, A. Borsodi

Research output: Contribution to journalArticle

47 Citations (Scopus)

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

Fingerprint

Semicarbazones
Hydrazones
Oximes
Opioid Analgesics
Binding Sites
Ligands
Derivatives
Radioligand Assay
Rats
Assays
Brain
Membranes

Keywords

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

ASJC Scopus subject areas

  • Pharmacology

Cite this

Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans. / Monory, Krisztina; Greiner, Elisabeth; Sartania, Nana; Sallai, László; Pouille, Yves; Schmidhammer, Helmut; Hanoune, Jacques; Borsodi, A.

In: Life Sciences, Vol. 64, No. 22, 23.04.1999, p. 2011-2020.

Research output: Contribution to journalArticle

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, vol. 64, no. 22, pp. 2011-2020. https://doi.org/10.1016/S0024-3205(99)00148-4
Monory, Krisztina ; Greiner, Elisabeth ; Sartania, Nana ; Sallai, László ; Pouille, Yves ; Schmidhammer, Helmut ; Hanoune, Jacques ; Borsodi, A. / Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans. In: Life Sciences. 1999 ; Vol. 64, No. 22. pp. 2011-2020.
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