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

Authors
Journal
Life Sciences
0024-3205
Publisher
Elsevier
Publication Date
Volume
64
Issue
22
Identifiers
DOI: 10.1016/s0024-3205(99)00148-4
Keywords
  • Mu Opioid Receptor
  • Affinity Label
  • In Vitro Receptor Binding
  • Alkoxymorphinans

Abstract

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 mu 2 specificity. However, some of these ligands are able to block partially (40–60%) the high affinity (putative mu 1) opioid binding sites while all of them act as reversible ligands at the low affinity (putative mu 2) sites.

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