title: 1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors.
abstract: Further exploration around the recently disclosed potent triple re-uptake inhibitor 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane led to the identification of a new series of potent triple re-uptake inhibitors endowed with good developability characteristics. The insertion of a further aryl moiety into the template allowed the 'titration' of the SERT/NET/DAT ratio leading to the identification of further tools in this important area.
authors.affiliation: GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fabrizio.micheli@aptuit.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Paolo
authors.initials: P
authors.lastname: Cavanni
authors.forename: Michela
authors.initials: M
authors.lastname: Bettati
authors.forename: Giorgio
authors.initials: G
authors.lastname: Bonanomi
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Elettra
authors.initials: E
authors.lastname: Fazzolari
authors.forename: Carla
authors.initials: C
authors.lastname: Marchioro
authors.forename: Maja
authors.initials: M
authors.lastname: Roscic
authors.forename: Luca
authors.initials: L
authors.lastname: Tarsi
authors.forename: Filippo
authors.initials: F
authors.lastname: Visentini
authors.forename: Laura
authors.initials: L
authors.lastname: Zonzini
authors.forename: Angela
authors.initials: A
authors.lastname: Worby
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001372:Aza Compounds / Q000737:chemistry; D001643:Bridged Bicyclo Compounds / Q000737:chemistry; D050483:Dopamine Plasma Membrane Transport Proteins / Q000737:chemistry / Q000378:metabolism; D018765:Dopamine Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006536:Heptanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000737:chemistry / 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* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D018759:Adrenergic Uptake Inhibitors; D001372:Aza Compounds; D001643:Bridged Bicyclo Compounds; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors; D006536:Heptanes; D050484:Norepinephrine Plasma Membrane Transport Proteins; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors