Several hydrazone, oxime, carbazone and semicarbazone derivatives of 14- alkoxycodeinones and 14-alkoxydihydrocodeinones were synthesised  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.
- Affinity label
- In vitro receptor binding
- Mu opioid receptor
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Pharmacology, Toxicology and Pharmaceutics(all)