From the Selective Serotonin Transporter Inhibitor Citalopram to the Selective Norepinephrine Transporter Inhibitor Talopram: Synthesis and Structure−Activity Relationship Studies
| Autor: | Kristian Strømgaard, Jonas N. N. Eildal, Jacob Andersen, Anders S. Kristensen, Benny Bang-Andersen, Anne Marie Jørgensen, Morten Jørgensen |
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| Rok vydání: | 2008 |
| Předmět: |
Blood Platelets
Citalopram In Vitro Techniques Cell Line Norepinephrine (medication) Structure-Activity Relationship chemistry.chemical_compound Talopram mental disorders Drug Discovery medicine Animals Humans Serotonin transporter Benzofurans Serotonin Plasma Membrane Transport Proteins Norepinephrine Plasma Membrane Transport Proteins Propylamines biology Chemistry Brain Recombinant Proteins Rats Norepinephrine transporter Biochemistry biology.protein Catecholamine Molecular Medicine Serotonin Reuptake inhibitor Selective Serotonin Reuptake Inhibitors Synaptosomes medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 51:3045-3048 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm701602g |
| Popis: | Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity. |
| Databáze: | OpenAIRE |
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