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

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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