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Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Jia Zhou, Rong He, Kenneth M Johnson, Yanping Ye, Alan P Kozikowski
Journal of medicinal chemistry 2004 Nov 18
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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.
Citation
Jia Zhou, Rong He, Kenneth M Johnson, Yanping Ye, Alan P Kozikowski.
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Journal of medicinal chemistry.
2004 Nov 18;47(24):5821-4
Mesh Tags
Animals
Benzhydryl Compounds
Biological Availability
Cocaine
Dopamine Plasma Membrane Transport Proteins
Drug Design
In Vitro Techniques
Ligands
Membrane Glycoproteins
Membrane Transport Modulators
Membrane Transport Proteins
Modafinil
Motor Activity
Nerve Endings
Nerve Tissue Proteins
Norepinephrine Plasma Membrane Transport Proteins
Piperidines
Rats
Serotonin Plasma Membrane Transport Proteins
Symporters
Synaptosomes
Substances
Benzhydryl Compounds
Dopamine Plasma Membrane Transport Proteins
Ligands
Membrane Glycoproteins
Membrane Transport Modulators
Membrane Transport Proteins
Nerve Tissue Proteins
Norepinephrine Plasma Membrane Transport Proteins
Piperidines
Serotonin Plasma Membrane Transport Proteins
Slc6a2 protein, rat
Slc6a3 protein, rat
Slc6a4 protein, rat
Symporters
methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate
Cocaine
Modafinil
PMID: 15537337
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