Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
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.
Mesh Terms:
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, Motor Activity, Nerve Endings, Nerve Tissue Proteins, Norepinephrine Plasma Membrane Transport Proteins, Piperidines, Rats, Serotonin Plasma Membrane Transport Proteins, Symporters, Synaptosomes
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, Motor Activity, Nerve Endings, Nerve Tissue Proteins, Norepinephrine Plasma Membrane Transport Proteins, Piperidines, Rats, Serotonin Plasma Membrane Transport Proteins, Symporters, Synaptosomes
J. Med. Chem.
Date: Nov. 18, 2004
PubMed ID: 15537337
View in: Pubmed Google Scholar
Download Curated Data For This Publication
178148
Switch View:
- Chemical Interactions 1