Abstract
A novel 6,14-epoxymorphinan benzamide derivative (NS22) was synthesized, which showed opioid kappa receptor agonistic activity in the [(35)S]GTPgammaS binding assay. The antinociceptive effect of NS22 was evaluated in the tail-flick and the hot-plate test. This compound showed a potent antinociceptive activity in mice by s.c. administration, which was attenuated with nor-BNI (selective opioid kappa receptor antagonist).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics / pharmacology
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Animals
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Benzamides / chemical synthesis*
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Benzamides / pharmacology
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Hydrogen Bonding
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Injections, Subcutaneous
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Ions
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Ligands
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Mice
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Models, Biological
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Models, Chemical
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Morphinans / chemical synthesis*
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Morphinans / chemistry
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Morphinans / pharmacology
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Protein Binding
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Receptors, Opioid, kappa / chemistry
Substances
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Analgesics
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Benzamides
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Ions
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Ligands
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Morphinans
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NS22 compound
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Receptors, Opioid, kappa
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Guanosine 5'-O-(3-Thiotriphosphate)