title: Effect of deuteration on the metabolism and clearance of some pharmacologically active compounds--synthesis and in vitro metabolism of deuterated derivatives of dronedadrone.
abstract: The synthesis and in vitro metabolism studies of a family of specifically deuterated derivatives of dronedarone are described. Metabolic stability and clearance of the parent compound are not sensitive to deuterium substitution, irrespective of the position of the heavy label.
authors.affiliation: Isotope Chemistry and Metabolite Synthesis, DSAR-DD, Sanofi R&D, 1 Avenue Pierre Brossolette, 91380, Chilly-Mazarin, France.
authors.forename: Joseph
authors.initials: J
authors.lastname: Schofield
authors.forename: Denis
authors.initials: D
authors.lastname: Brasseur
authors.forename: Béatrice
authors.initials: B
authors.lastname: de Bruin
authors.forename: Thierry
authors.initials: T
authors.lastname: Vassal
authors.forename: Sylvie
authors.initials: S
authors.lastname: Klieber
authors.forename: Catherine
authors.initials: C
authors.lastname: Arabeyre
authors.forename: Martine
authors.initials: M
authors.lastname: Bourrié
authors.forename: Freddy
authors.initials: F
authors.lastname: Sadoun
authors.forename: Gérard
authors.initials: G
authors.lastname: Fabre
mesh_terms: D000638:Amiodarone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D060326:Chemistry Techniques, Synthetic; D003903:Deuterium / Q000737:chemistry*; D000077764:Dronedarone; D022781:Hepatocytes / Q000378:metabolism; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D003903:Deuterium; D000077764:Dronedarone; D000638:Amiodarone
keywords: antiarrhythmic; deuterium; deuterium labelling; in vitro metabolism; isotope effect; stable labelled synthesis