Abstract
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.
MeSH terms
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Animals
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Crystallography, X-Ray
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Dopamine Plasma Membrane Transport Proteins / drug effects
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Dopamine Plasma Membrane Transport Proteins / metabolism
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Half-Life
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / pharmacology*
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Humans
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Indicators and Reagents
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Models, Molecular
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Molecular Conformation
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Norepinephrine / metabolism
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Rats
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Receptors, Histamine H3 / drug effects*
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Selective Serotonin Reuptake Inhibitors / chemical synthesis*
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Selective Serotonin Reuptake Inhibitors / pharmacokinetics
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin Plasma Membrane Transport Proteins / drug effects
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Serotonin Plasma Membrane Transport Proteins / metabolism
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis*
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Tetrahydroisoquinolines / pharmacokinetics
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Tetrahydroisoquinolines / pharmacology*
Substances
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Dopamine Plasma Membrane Transport Proteins
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Histamine Antagonists
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Indicators and Reagents
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Receptors, Histamine H3
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Serotonin Plasma Membrane Transport Proteins
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Serotonin Uptake Inhibitors
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Tetrahydroisoquinolines
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Norepinephrine