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