Position 6 of the morphinan skeleton plays a key role in the -opioid receptor (MOR) activity in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N-methylmorphinan-6-ones 1−4 on ligand−MOR interaction, signaling, and antinociception. While 6-desoxo compounds 1a, 2a, and 4a show similar profiles to their 6-keto counterparts, the 6-desoxo-14-benzyloxy substituted 3a displays significantly increased MOR binding and agonist potency and a distinct binding mode compared with its analogue 3.
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent Opioid Receptor Agonists
Posted by
Maria Dumitrascuta
on 12 09 2020
Related content
03 10 2022
< 1 minute
Calculate on the cloud
In order to increase the flexibility, access and integrability, Calculators and Predictors have...
12 05 2022
< 1 minute
Coupling stabilizers open KV1-type potassium channels
ABSTRACT: The opening and closing of voltage-gated ion channels are regulated by voltage sensors...
13 11 2021
< 1 minute
Cheminfo Stories 2021 Virtual UGM | Boost analytical experiments with phys-chem properties
TRY CHEMICALIZE Log in for videos & slides
13 11 2021
< 1 minute
Cheminfo Stories 2021 Virtual UGM | Enhancing Sibylla’s innovative drug discovery platform with ChemAxon
Sibylla's innovative pharmacological platform is aimed at discovering new drugs for untreatable...