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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. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Anthony D Pechulis, James P Beck, Matt A Curry, Mark A Wolf, Arthur E Harms, Ning Xi, Chet Opalka, Mark P Sweet, Zhicai Yang, A Samuel Vellekoop, Andrew M Klos, Peter J Crocker, Carla Hassler, Mia Laws, Douglas B Kitchen, Mark A Smith, Richard E Olson, Shuang Liu, Bruce F Molino. 4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors. Bioorganic & medicinal chemistry letters. 2012 Dec 1;22(23):7219-22

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PMID: 23084899

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