title: Synthesis and biological activity of some known and putative duloxetine metabolites.
abstract: Several putative phase I duloxetine metabolites, 4-hydroxy-, 5-hydroxy-, 6-hydroxy-, 5-hydroxy-6-methoxy-, 6-hydroxy-5-methoxy-, 5,6-dihydroxy-, and 4,6-dihydroxyduloxetine were synthesized, and their phase II metabolite as glucuronide or sulfate conjugates were also synthesized. Their in vitro binding activities were compared to that of parent compound duloxetine.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285 USA. kuo_fengjiun@lilly.com
authors.forename: F
authors.initials: F
authors.lastname: Kuo
authors.forename: T A
authors.initials: TA
authors.lastname: Gillespie
authors.forename: P
authors.initials: P
authors.lastname: Kulanthaivel
authors.forename: R J
authors.initials: RJ
authors.lastname: Lantz
authors.forename: T W
authors.initials: TW
authors.lastname: Ma
authors.forename: D L
authors.initials: DL
authors.lastname: Nelson
authors.forename: P G
authors.initials: PG
authors.lastname: Threlkeld
authors.forename: W J
authors.initials: WJ
authors.lastname: Wheeler
authors.forename: P
authors.initials: P
authors.lastname: Yi
authors.forename: M
authors.initials: M
authors.lastname: Zmijewski
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001665:Binding Sites; D003001:Cloning, Molecular; D050483:Dopamine Plasma Membrane Transport Proteins; D000068736:Duloxetine Hydrochloride; D020719:Glucuronides / Q000378:metabolism; D006801:Humans; D008562:Membrane Glycoproteins / Q000378:metabolism; D026901:Membrane Transport Proteins / Q000378:metabolism; D008956:Models, Chemical; D009419:Nerve Tissue Proteins / Q000378:metabolism; D011869:Radioligand Assay; D013431:Sulfates / Q000378:metabolism; D013876:Thiophenes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D018759:Adrenergic Uptake Inhibitors; D050483:Dopamine Plasma Membrane Transport Proteins; D020719:Glucuronides; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D013431:Sulfates; D013876:Thiophenes; D000068736:Duloxetine Hydrochloride