Abstract
A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, mu opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective mu opioid receptor antagonist, which interacts selectively with mu peripheral receptors.
MeSH terms
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Administration, Oral
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Animals
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Cell Membrane / metabolism
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Central Nervous System / drug effects*
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Chromatography, High Pressure Liquid
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Diprenorphine / metabolism
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Gastrointestinal Transit / drug effects
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Humans
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Loperamide / pharmacology
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Mice
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / pharmacology*
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Receptors, Opioid, delta / antagonists & inhibitors*
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Receptors, Opioid, delta / metabolism
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Receptors, Opioid, kappa / antagonists & inhibitors*
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Receptors, Opioid, kappa / metabolism
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Receptors, Opioid, mu / antagonists & inhibitors*
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Receptors, Opioid, mu / metabolism
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Structure-Activity Relationship
Substances
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OPRM1 protein, human
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Piperidines
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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Diprenorphine
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Guanosine 5'-O-(3-Thiotriphosphate)
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alvimopan
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Loperamide