title: 4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
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.
authors.affiliation: AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA.
authors.forename: Anthony D
authors.initials: AD
authors.lastname: Pechulis
authors.forename: James P
authors.initials: JP
authors.lastname: Beck
authors.forename: Matt A
authors.initials: MA
authors.lastname: Curry
authors.forename: Mark A
authors.initials: MA
authors.lastname: Wolf
authors.forename: Arthur E
authors.initials: AE
authors.lastname: Harms
authors.forename: Ning
authors.initials: N
authors.lastname: Xi
authors.forename: Chet
authors.initials: C
authors.lastname: Opalka
authors.forename: Mark P
authors.initials: MP
authors.lastname: Sweet
authors.forename: Zhicai
authors.initials: Z
authors.lastname: Yang
authors.forename: A Samuel
authors.initials: AS
authors.lastname: Vellekoop
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Klos
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Crocker
authors.forename: Carla
authors.initials: C
authors.lastname: Hassler
authors.forename: Mia
authors.initials: M
authors.lastname: Laws
authors.forename: Douglas B
authors.initials: DB
authors.lastname: Kitchen
authors.forename: Mark A
authors.initials: MA
authors.lastname: Smith
authors.forename: Richard E
authors.initials: RE
authors.lastname: Olson
authors.forename: Shuang
authors.initials: S
authors.lastname: Liu
authors.forename: Bruce F
authors.initials: BF
authors.lastname: Molino
mesh_terms: D050483:Dopamine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D018765:Dopamine Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D007700:Kinetics; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D011485:Protein Binding; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors; D050484:Norepinephrine Plasma Membrane Transport Proteins; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; D044005:Tetrahydroisoquinolines