Abstract
Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT(1A) partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT(1A) partial agonist pharmacological profile as well as excellent selectivity for the norepinephrine transporter over the dopamine transporter.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Adrenergic Uptake Inhibitors / chemical synthesis*
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Adrenergic Uptake Inhibitors / metabolism
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Adrenergic Uptake Inhibitors / pharmacology
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Cell Line
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Crystallography, X-Ray
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Drug Design*
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Drug Evaluation, Preclinical / methods
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Humans
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors*
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Norepinephrine Plasma Membrane Transport Proteins / metabolism
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Phenols / chemical synthesis
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Phenols / metabolism
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Phenols / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / metabolism
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Pyridines / pharmacology
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Receptor, Serotonin, 5-HT1A / metabolism
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Serotonin 5-HT1 Receptor Agonists*
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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / metabolism
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Serotonin Receptor Agonists / pharmacology
Substances
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Adrenergic Uptake Inhibitors
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Norepinephrine Plasma Membrane Transport Proteins
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Phenols
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Pyridines
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Serotonin 5-HT1 Receptor Agonists
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Serotonin Receptor Agonists
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Receptor, Serotonin, 5-HT1A
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phenoxy radical