title: Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect.
abstract: The major human metabolite of atomoxetine (4-hydroxyatomoxetine) was tested against a panel of receptors and enzymes, and was found to interact with the mu, delta, and kappa-opioid receptors based upon studies involving both binding and functional assays. 4-hydroxyatomoxetine was determined to be a partial agonist of the kappa-opioid receptor.
authors.affiliation: Drug Discovery, Johnson and Johnson Pharmaceutical, Research and Development, Spring House, PA 19477-0776, USA. ccreight@prdus.jnj.com
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Creighton
authors.forename: Kris
authors.initials: K
authors.lastname: Ramabadran
authors.forename: Patrick E
authors.initials: PE
authors.lastname: Ciccone
authors.forename: Jingchun
authors.initials: J
authors.lastname: Liu
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Orsini
authors.forename: Allen B
authors.initials: AB
authors.lastname: Reitz
mesh_terms: D000069445:Atomoxetine Hydrochloride; D001289:Attention Deficit Disorder with Hyperactivity / Q000188:drug therapy; D006801:Humans; D011437:Propylamines / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D017473:Receptors, Opioid, kappa / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D011437:Propylamines; D017473:Receptors, Opioid, kappa; D000069445:Atomoxetine Hydrochloride