Abstract
A series of 3alpha-(4-substituted)nortropane-2beta-carboxylic acid methyl esters was synthesized and evaluated for the ability to inhibit radioligand binding at the dopamine, serotonin, and norepinephrine transporters. 3alpha-(4-Methylphenyl)nortropane-2beta-carboxylic acid methyl ester (4c) was found to be selective and highly potent for the norepinephrine transporter (NET) relative to the dopamine and serotonin transporters.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Carboxylic Acids / chemical synthesis*
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Carboxylic Acids / chemistry*
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Carboxylic Acids / pharmacology
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Carrier Proteins / metabolism*
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Cocaine / pharmacology
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Dopamine Plasma Membrane Transport Proteins
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Membrane Glycoproteins / metabolism
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Membrane Transport Proteins*
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Molecular Conformation
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Molecular Structure
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Nerve Tissue Proteins*
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Norepinephrine Plasma Membrane Transport Proteins
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Nortropanes / chemical synthesis*
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Nortropanes / metabolism*
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Nortropanes / pharmacology
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Protein Binding
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Radioligand Assay
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Serotonin Plasma Membrane Transport Proteins
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Structure-Activity Relationship
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Symporters*
Substances
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3-(4-Methylphenyl)nortropane-2-carboxylic acid methyl ester
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Carboxylic Acids
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Norepinephrine Plasma Membrane Transport Proteins
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Nortropanes
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Serotonin Plasma Membrane Transport Proteins
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Symporters
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Cocaine