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- W2083485457 abstract "The antinociceptive potency and receptor affinity of several optically active aromatic mono- and di-oxygenated N-methylmorphinans and N-methylmorphinan-6-ones, prepared from natural morphine, were determined. Thus, in order of antinociceptive potency, 4-methoxy-N-methylmorphinan-6-one ≈ 3,4-dimethoxy-N-methylmorphinan-6-one ≈ 3,4-dimethoxy-N-methylmorphinan > 4-methoxy-N-methylmorphinan ≈ 4-acetoxy-N-methylmorphinan-6-one > 4-acetoxy-N-methylmorphinan ≈ 4-hydroxy-N-methylmorphinan-6-one ≈ 4-hydroxy-N-methylmorphinan. The 4-hydroxy compounds were slightly less potent than morphine, and the 4-methoxy and 3,4-dimethoxy compounds were found to have three times the potency of morphine. 4-Methoxy-N-methylmorphinan-6-one showed an opiate receptor affinity one-third that of morphine; this is a remarkably high affinity for a non-phenolic compound." @default.
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- W2083485457 date "1981-07-22" @default.
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- W2083485457 title "Structure-Activity Relationships of Oxygenated Morphinans. I. 4-Mono- and 3,4-dimethoxy-N-methylmorphinans and -N-methyl-morphinan-6-ones with unusually high antinociceptive potency. Preliminary communication" @default.
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- W2083485457 doi "https://doi.org/10.1002/hlca.19810640506" @default.
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