Abstract
A novel potent NMDA-NR2B selective antagonist without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / metabolism
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Amides / pharmacology*
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Animals
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Cell Line
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Glutathione / chemistry
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Humans
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Mice
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Molecular Structure
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Neurons / drug effects
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Neurons / metabolism
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Phenol / chemistry
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Phenols / chemistry
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Receptors, N-Methyl-D-Aspartate / metabolism*
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Structure-Activity Relationship
Substances
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Amides
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NR2B NMDA receptor
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Phenols
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Receptors, N-Methyl-D-Aspartate
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Phenol
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Glutathione