4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors

…, AS Vellekoop, AM Klos, PJ Crocker, C Hassler…

Index: Pechulis, Anthony D.; Beck, James P.; Curry, Matt A.; Wolf, Mark A.; Harms, Arthur E.; Xi, Ning; Opalka, Chet; Sweet, Mark P.; Yang, Zhicai; Vellekoop, A. Samuel; Klos, Andrew M.; Crocker, Peter J.; Hassler, Carla; Laws, Mia; Kitchen, Douglas B.; Smith, Mark A.; Olson, Richard E.; Liu, Shuang; Molino, Bruce F. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7219 - 7222

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Citation Number: 7

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.