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

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.

Bioorg Med Chem Lett ; 22(23): 7219-22, 2012 Dec 01.

Article in English | MEDLINE | ID: mdl-23084899

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.

Subject(s)

Dopamine Uptake Inhibitors/chemistry , Tetrahydroisoquinolines/chemistry , Dopamine Plasma Membrane Transport Proteins/antagonists & inhibitors , Dopamine Plasma Membrane Transport Proteins/metabolism , Dopamine Uptake Inhibitors/chemical synthesis , Dopamine Uptake Inhibitors/metabolism , Kinetics , Norepinephrine Plasma Membrane Transport Proteins/antagonists & inhibitors , Norepinephrine Plasma Membrane Transport Proteins/metabolism , Protein Binding , Serotonin Plasma Membrane Transport Proteins/chemistry , Serotonin Plasma Membrane Transport Proteins/metabolism , Selective Serotonin Reuptake Inhibitors/chemical synthesis , Selective Serotonin Reuptake Inhibitors/chemistry , Selective Serotonin Reuptake Inhibitors/metabolism , Structure-Activity Relationship , Tetrahydroisoquinolines/chemical synthesis , Tetrahydroisoquinolines/metabolism

ABSTRACT

Subject(s)

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