title: Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
abstract: A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mletavic@prdus.jnj.com
authors.forename: Michael A
authors.initials: MA
authors.lastname: Letavic
authors.forename: John M
authors.initials: JM
authors.lastname: Keith
authors.forename: Jill A
authors.initials: JA
authors.lastname: Jablonowski
authors.forename: Emily M
authors.initials: EM
authors.lastname: Stocking
authors.forename: Leslie A
authors.initials: LA
authors.lastname: Gomez
authors.forename: Kiev S
authors.initials: KS
authors.lastname: Ly
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Miller
authors.forename: Ann J
authors.initials: AJ
authors.lastname: Barbier
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonaventure
authors.forename: Jamin D
authors.initials: JD
authors.lastname: Boggs
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Kirsten L
authors.initials: KL
authors.lastname: Miller
authors.forename: Brian
authors.initials: B
authors.lastname: Lord
authors.forename: Heather M
authors.initials: HM
authors.lastname: McAllister
authors.forename: D J
authors.initials: DJ
authors.lastname: Tognarelli
authors.forename: Jiejun
authors.initials: J
authors.lastname: Wu
authors.forename: Marta C
authors.initials: MC
authors.lastname: Abad
authors.forename: Carsten
authors.initials: C
authors.lastname: Schubert
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D050483:Dopamine Plasma Membrane Transport Proteins / Q000187:drug effects / Q000378:metabolism; D006207:Half-Life; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D009638:Norepinephrine / Q000378:metabolism; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000187:drug effects / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; D006633:Histamine Antagonists; D007202:Indicators and Reagents; D009638:Norepinephrine; D018100:Receptors, Histamine H3; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; D044005:Tetrahydroisoquinolines