4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
Article Details
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Pechulis AD, Beck JP, Curry MA, Wolf MA, Harms AE, Xi N, Opalka C, Sweet MP, Yang Z, Vellekoop AS, Klos AM, Crocker PJ, Hassler C, Laws M, Kitchen DB, Smith MA, Olson RE, Liu S, Molino BF
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
Bioorg Med Chem Lett. 2012 Dec 1;22(23):7219-22. doi: 10.1016/j.bmcl.2012.09.050. Epub 2012 Sep 25.
- PubMed ID
- 23084899 [ View in PubMed]
- Abstract
Novel 4-phenyl tetrahydroisoquinolines that inhibit both dopamine and norepinephrine transporters were designed and prepared. In this Letter, we describe the synthesis, in vitro activity and associated structure-activity relationships of this series. We also report the ex vivo NET occupancy of a representative compound, 41.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Duloxetine Sodium-dependent noradrenaline transporter Ki (nM) 5.97 N/A N/A Details Nomifensine Sodium-dependent dopamine transporter Ki (nM) 84 N/A N/A Details Nomifensine Sodium-dependent noradrenaline transporter Ki (nM) 23 N/A N/A Details Nomifensine Sodium-dependent serotonin transporter Ki (nM) 2057 N/A N/A Details