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• W2158839757 abstract "A novel 6,14-epoxymorphinan benzamide derivative (NS22) that was previously reported showed opioid κ receptor agonistic activity and analgesic activity. The unsatisfactory κ selectivity of NS22 led us to synthesize its derivatives to improve the opioid κ receptor selectivity and the agonist activity. In the course of SAR of the various derivatives, 17-benzyl-6,14-epoxymorphinan derivatives (KNT-33, 53, 55, 80, 90, 133) were found to show high selectivities and affinities for the opioid κ receptor. In addition, KNT-33, 53, 55 showed dose-dependent analgesic effects in acetic acid writhing tests. Therefore, 17-benzyl substituents may play an important role for developing κ selectivity." @default.
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• W2158839757 date "2011-02-01" @default.
• W2158839757 modified "2023-09-25" @default.
• W2158839757 title "Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies" @default.
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• W2158839757 doi "https://doi.org/10.1016/j.bmc.2010.12.035" @default.
• W2158839757 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21256034" @default.
• W2158839757 hasPublicationYear "2011" @default.
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