title: Synthesis and activity of a new class of dual acting norepinephrine and serotonin reuptake inhibitors: 3-(1H-indol-1-yl)-3-arylpropan-1-amines.
abstract: Compounds with a combination of norepinephrine and serotonin reuptake inhibition have been approved in the US and Europe for a number of indications, including major depressive disorder and pain disorders such as diabetic neuropathy and fibromyalgia. Efforts to design selective norepinephrine reuptake inhibitors based on SAR from the aryloxypropanamine series of monoamine reuptake inhibitors have led to the identification of a potent new class of dual acting norepinephrine and serotonin reuptake inhibitors, namely the 3-(1H-indol-1-yl)-3-arylpropan-1-amines.
authors.affiliation: Chemical and Screening Sciences, Discovery Medicinal Chemistry, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. mahanep@wyeth.com
authors.forename: Paige E
authors.initials: PE
authors.lastname: Mahaney
authors.forename: An T
authors.initials: AT
authors.lastname: Vu
authors.forename: Casey C
authors.initials: CC
authors.lastname: McComas
authors.forename: Puwen
authors.initials: P
authors.lastname: Zhang
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Nogle
authors.forename: William L
authors.initials: WL
authors.lastname: Watts
authors.forename: Ani
authors.initials: A
authors.lastname: Sarkahian
authors.forename: Liza
authors.initials: L
authors.lastname: Leventhal
authors.forename: Nicole R
authors.initials: NR
authors.lastname: Sullivan
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Uveges
authors.forename: Eugene J
authors.initials: EJ
authors.lastname: Trybulski
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D001679:Biogenic Amines / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor / Q000187:drug effects; D002822:Choriocarcinoma / Q000188:drug therapy / Q000473:pathology; D050483:Dopamine Plasma Membrane Transport Proteins / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D009638:Norepinephrine / Q000037:antagonists & inhibitors*; D010920:Placenta / Q000187:drug effects / Q000378:metabolism; D011437:Propylamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012701:Serotonin / Q000737:chemistry*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D018759:Adrenergic Uptake Inhibitors; D001679:Biogenic Amines; D050483:Dopamine Plasma Membrane Transport Proteins; D007211:Indoles; D009638:Norepinephrine; D011437:Propylamines; D012701:Serotonin; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; C493230:SLC6A4 protein, human