Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
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Wu D, Pontillo J, Ching B, Hudson S, Gao Y, Fleck BA, Gogas K, Wade WS
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. doi: 10.1016/j.bmcl.2008.05.057. Epub 2008 May 20.
- PubMed ID
- 18550369 [ View in PubMed]
- Abstract
The design, synthesis, and SAR of a series of ring-constrained norepinephrine reuptake inhibitors are described. A substantially rigid inhibitor with potent functional activity at the transporter (IC(50)=8 nM) was used to develop a model for the distance and orientation of key features necessary for interaction with the norepinephrine transporter (NET).
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Atomoxetine Sodium-dependent noradrenaline transporter IC 50 (nM) 5 N/A N/A Details Atomoxetine Sodium-dependent serotonin transporter IC 50 (nM) 180 N/A N/A Details Fluoxetine Sodium-dependent serotonin transporter IC 50 (nM) 47 N/A N/A Details