Abstract
[4-(Phenoxy)pyridine-3-yl]methylamines are disclosed as a new series of selective noradrenaline reuptake inhibitors (NRI). Structure-activity relationships established that potent NRI activity could be achieved by appropriate substitution at the 2-position of the phenoxy ring. Compound 31 demonstrated potent NRI activity combined with good selectivity over serotonin and dopamine reuptake and no significant off-target pharmacology.
MeSH terms
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Adrenergic Uptake Inhibitors / chemical synthesis
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Adrenergic Uptake Inhibitors / pharmacology*
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Animals
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Biological Transport
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Caco-2 Cells
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Cytochrome P-450 Enzyme Inhibitors
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Dopamine / metabolism
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Dopamine Uptake Inhibitors / pharmacology
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Ether-A-Go-Go Potassium Channels / metabolism
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Extracellular Fluid / drug effects
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Hepatocytes / drug effects
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Hepatocytes / metabolism
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Humans
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Methylamines / chemical synthesis
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Methylamines / pharmacology*
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Microdialysis
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Molecular Structure
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Norepinephrine / antagonists & inhibitors*
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Prefrontal Cortex / drug effects
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Pyridines / chemical synthesis
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Pyridines / pharmacology*
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Rats
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Selective Serotonin Reuptake Inhibitors / pharmacology
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Serotonin / metabolism
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Structure-Activity Relationship
Substances
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Adrenergic Uptake Inhibitors
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Cytochrome P-450 Enzyme Inhibitors
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Dopamine Uptake Inhibitors
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Ether-A-Go-Go Potassium Channels
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KCNH1 protein, human
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Methylamines
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Pyridines
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Serotonin Uptake Inhibitors
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Serotonin
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Dopamine
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Norepinephrine