Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
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Sabatucci JP, Mahaney PE, Leiter J, Johnston G, Burroughs K, Cosmi S, Zhang Y, Ho D, Deecher DC, Trybulski E
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett. 2010 May 1;20(9):2809-12. doi: 10.1016/j.bmcl.2010.03.059. Epub 2010 Mar 15.
- PubMed ID
- 20378347 [ View in PubMed]
- Abstract
A series of heterocyclic cycloalkanol ethylamines have been prepared to expand our norepinephrine reuptake inhibitor (NRI) program. Synthesis of a variety of heterocycles identified (+)-S-21, a potent NRI efficacious in an animal model for thermoregulatory dysfunction.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Desipramine Sodium-dependent noradrenaline transporter IC 50 (nM) 3.4 N/A N/A Details Duloxetine Sodium-dependent dopamine transporter IC 50 (nM) >1000 N/A N/A Details Duloxetine Sodium-dependent noradrenaline transporter IC 50 (nM) 4 N/A N/A Details Duloxetine Sodium-dependent serotonin transporter IC 50 (nM) 3 N/A N/A Details Fluoxetine Sodium-dependent serotonin transporter IC 50 (nM) 9.4 N/A N/A Details Mazindol Sodium-dependent dopamine transporter IC 50 (nM) 22.1 N/A N/A Details Venlafaxine Sodium-dependent dopamine transporter IC 50 (nM) >10000 N/A N/A Details Venlafaxine Sodium-dependent noradrenaline transporter IC 50 (nM) 535 N/A N/A Details Venlafaxine Sodium-dependent serotonin transporter IC 50 (nM) 27 N/A N/A Details