Abstract
Some piperidine-based nocaine/modafinil hybrid ligands have been designed, synthesized, and found to display an improved potency at all three monoamine transporters and particularly for DAT and/or NET. Some highly active and selective monoamine transporter inhibitors with low nanomolar to subnanomolar potency were identified. Ligands of this type may find important applications as positron emission tomography imaging tools and in the treatment of central nervous system disorders such as depression and sleep apnea.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzhydryl Compounds / chemical synthesis*
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Benzhydryl Compounds / chemistry
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Benzhydryl Compounds / pharmacology
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Biological Availability
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Cocaine / pharmacology
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Dopamine Plasma Membrane Transport Proteins
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Drug Design
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In Vitro Techniques
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Ligands
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Membrane Glycoproteins / antagonists & inhibitors*
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Membrane Transport Modulators*
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Membrane Transport Proteins / antagonists & inhibitors*
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Modafinil
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Motor Activity / drug effects
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Nerve Endings / drug effects
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Nerve Endings / metabolism
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Nerve Tissue Proteins / antagonists & inhibitors*
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Norepinephrine Plasma Membrane Transport Proteins
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology
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Rats
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Serotonin Plasma Membrane Transport Proteins
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Symporters / antagonists & inhibitors*
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Synaptosomes / drug effects
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Synaptosomes / metabolism
Substances
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Benzhydryl Compounds
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Dopamine Plasma Membrane Transport Proteins
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Ligands
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Membrane Glycoproteins
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Membrane Transport Modulators
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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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Piperidines
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Serotonin Plasma Membrane Transport Proteins
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Slc6a2 protein, rat
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Slc6a3 protein, rat
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Slc6a4 protein, rat
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Symporters
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methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate
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Cocaine
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Modafinil