4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.

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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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
DuloxetineSodium-dependent noradrenaline transporterKi (nM)5.97N/AN/ADetails
NomifensineSodium-dependent dopamine transporterKi (nM)84N/AN/ADetails
NomifensineSodium-dependent noradrenaline transporterKi (nM)23N/AN/ADetails
NomifensineSodium-dependent serotonin transporterKi (nM)2057N/AN/ADetails