4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors

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 rep...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-12, Vol.22 (23), p.7219-7222
Main Authors: 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.
Format: Article
Language:English
Subjects:
ADHD
Biological and medical sciences
DAT
Depression
Dopamine
Dopamine Plasma Membrane Transport Proteins - antagonists & inhibitors
Dopamine Plasma Membrane Transport Proteins - metabolism
Dopamine reuptake inhibitor
Dopamine Uptake Inhibitors - chemical synthesis
Dopamine Uptake Inhibitors - chemistry
Dopamine Uptake Inhibitors - metabolism
Dual dopamine and norepinephrine reuptake inhibitors
Kinetics
Medical sciences
NET
norepinephrine
Norepinephrine Plasma Membrane Transport Proteins - antagonists & inhibitors
Norepinephrine Plasma Membrane Transport Proteins - metabolism
Norepinephrine reuptake inhibitor
Pharmacology. Drug treatments
Protein Binding
Serotonin Plasma Membrane Transport Proteins - chemistry
Serotonin Plasma Membrane Transport Proteins - metabolism
Serotonin Uptake Inhibitors - chemical synthesis
Serotonin Uptake Inhibitors - chemistry
Serotonin Uptake Inhibitors - metabolism
Structure-Activity Relationship
structure-activity relationships
tetrahydroisoquinolines
Tetrahydroisoquinolines - chemical synthesis
Tetrahydroisoquinolines - chemistry
Tetrahydroisoquinolines - metabolism
transporters
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.09.050