Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.

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Hudson S, Kiankarimi M, Eccles W, Mostofi YS, Genicot MJ, Dwight W, Fleck BA, Gogas K, Wade WS

Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. doi: 10.1016/j.bmcl.2008.07.050. Epub 2008 Jul 17.

PubMed ID

18667309 [ View in PubMed

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Abstract

The design, synthesis and SAR of a series of heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. As racemates, the best compounds compare favorably with atomoxetine (IC(50)'s<10 nM) in potency at the transporter.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Fluoxetine	Sodium-dependent serotonin transporter	IC 50 (nM)	47	N/A	N/A	Details