Life sciences (1973), 1999, Vol.64 (22), p.2011-2020
1999
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- Autor(en) / Beteiligte
- Titel
- Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans
- Ist Teil von
- Life sciences (1973), 1999, Vol.64 (22), p.2011-2020
- Ort / Verlag
- Netherlands: Elsevier Inc
- Erscheinungsjahr
- 1999
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0024-3205eISSN: 1879-0631DOI: 10.1016/S0024-3205(99)00148-4Titel-ID: cdi_proquest_miscellaneous_69829375
- Format
- –
- Schlagworte
- affinity label, Affinity Labels, alkoxymorphinans, Animals, Brain - metabolism, in vitro receptor binding, In Vitro Techniques, Kinetics, Morphinans - chemical synthesis, Morphinans - chemistry, Morphinans - metabolism, mu opioid receptor, Naloxone - metabolism, Narcotic Antagonists - metabolism, Oxycodone - analogs & derivatives, Oxycodone - metabolism, Rats, Rats, Wistar, Receptors, Opioid - agonists, Receptors, Opioid - metabolism, Receptors, Opioid, delta - agonists, Receptors, Opioid, delta - antagonists & inhibitors, Receptors, Opioid, delta - metabolism, Receptors, Opioid, kappa - agonists, Receptors, Opioid, kappa - antagonists & inhibitors, Receptors, Opioid, kappa - metabolism, Receptors, Opioid, mu - agonists, Receptors, Opioid, mu - antagonists & inhibitors, Receptors, Opioid, mu - metabolism, Structure-Activity Relationship