N-Phenethyl Substitution in 14-Methoxy-N-methylmorphinan-6-ones Turns Selective µ Opioid Receptor Ligands into Dual µ/δ Opioid Receptor Agonists

Autor: Dumitrascuta, Maria, Bermudez, Marcel, Ben Haddou, Tanila, Guerrieri, Elena, Schläfer, Lea, Ritsch, Andreas, Hosztafi, Sandor, Lantero, Aquilino, Kreutz, Christoph, Massotte, Dominique, Schmidhammer, Helmut, Wolber, Gerhard, Spetea, Mariana

Publikováno v: Scientific Reports, Vol 10, Iss 1, Pp 1-12 (2020)
Scientific Reports
Scientific Reports, Nature Publishing Group, 2020, 10 (1), ⟨10.1038/s41598-020-62530-w⟩

Morphine and structurally-derived compounds are µ opioid receptor (µOR) agonists, and the most effective analgesic drugs. However, their usefulness is limited by serious side effects, including dependence and abuse potential. The N-substituent in m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::1b9f2c809866bebddf78298a937e3f5d
http://link.springer.com/article/10.1038/s41598-020-62530-w

Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14-O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives

Autor: Spetea, Mariana, Rief, Silvia B., Haddou, Tanila Ben, Fink, Monika, Kristeva, Elka, Mittendorfer, Harald, Haas, Stefanie, Hummer, Nora, Follia, Valeria, Guerrieri, Elena, Asim, Muhammad Faheem, Sturm, Sonja, Schmidhammer, Helmut

Publikováno v: Journal of Medicinal Chemistry

Herein, the synthesis and pharmacological characterization of an extended library of differently substituted N-methyl-14- O-methylmorphinans with natural and unnatural amino acids and three dipeptides at position 6 that emerged as potent μ/δ opioid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::911aa4dc168a0f80e0e5ce84acbb7c38
http://europepmc.org/articles/PMC6348443

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Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14‑O‑Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.

Autor: Spetea, Mariana, Rief, Silvia B., Haddou, Tanila Ben, Fink, Monika, Kristeva, Elka, Mittendorfer, Harald, Haas, Stefanie, Hummer, Nora, Follia, Valeria, Guerrieri, Elena, Asim, Muhammad Faheem, Sturm, Sonja, Schmidhammer, Helmut

Publikováno v: Journal of Medicinal Chemistry; 2/24/2019, Vol. 62 Issue 3, p641-653, 13p