title: Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
abstract: A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, La Jolla, CA 92121, USA. jkeith@prdus.jnj.com
authors.forename: John M
authors.initials: JM
authors.lastname: Keith
authors.forename: Leslie A
authors.initials: LA
authors.lastname: Gomez
authors.forename: Ann J
authors.initials: AJ
authors.lastname: Barbier
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Jamin D
authors.initials: JD
authors.lastname: Boggs
authors.forename: Brian
authors.initials: B
authors.lastname: Lord
authors.forename: Curt
authors.initials: C
authors.lastname: Mazur
authors.forename: Leah
authors.initials: L
authors.lastname: Aluisio
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier; D006634:Histamine H1 Antagonists / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology*; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000187:drug effects*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D006634:Histamine H1 Antagonists; D011759:Pyrrolidines; D018100:Receptors, Histamine H3; D050486:Serotonin Plasma Membrane Transport Proteins; D044005:Tetrahydroisoquinolines