title: Human moricizine metabolism. I. Isolation and identification of metabolites in human urine.
abstract: 1. Using synthetic standards and/or spectral data, seven moricizine metabolites were structurally identified in human urine. Two novel metabolites were identified as phenothiazine-2-carbamic acid and ethyl [10-(3-aminopropionyl) phenothiazin-2-yl] carbamate. Two novel human moricizine metabolites, 2-amino-10-(3-morpholino-propionyl) phenothiazine, a previously identified dog metabolite, and 2-aminophenothiazine, a previously identified rat metabolite, were also identified. Three additional human metabolites, phenothiazine-2-carbamic acid ethyl ester sulphoxide (P2CAEES), moricizine sulphoxide, and ethyl ¿10-[N-(2'-hydroxyethyl)3-aminopropionyl] phenothiazin-2-yl¿ carbamate, all previously described in the literature, were observed. 2. Both 2-amino-10-(3-morpholinopropionyl) phenothiazine and ethyl [10-(3-aminopropionyl) phenothiazin-2-yl] carbamate, and possibly ethyl ¿10-[N-(2'-hydroxyethyl) 3-aminopropionyl]phenothiazin-2-yl¿ carbamate, possess the structural characteristics thought to be necessary for class 1 antiarrhythmic activity.
authors.affiliation: DuPont Merck Pharmaceutical Co., Stine-Haskell Research Center, Newark, USA.
authors.forename: L E
authors.initials: LE
authors.lastname: Richards
authors.forename: H J
authors.initials: HJ
authors.lastname: Pieniaszek
authors.forename: S
authors.initials: S
authors.lastname: Shatzmiller
authors.forename: G O
authors.initials: GO
authors.lastname: Page
authors.forename: K F
authors.initials: KF
authors.lastname: Blom
authors.forename: J M
authors.initials: JM
authors.lastname: Read
authors.forename: A F
authors.initials: AF
authors.lastname: Davidson
authors.forename: P N
authors.initials: PN
authors.lastname: Confalone
mesh_terms: D000328:Adult; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000378:metabolism*; D005260:Female; D006801:Humans; D008297:Male; D015394:Molecular Structure; D016293:Moricizine / Q000008:administration & dosage / Q000378:metabolism*; D011355:Prodrugs / Q000008:administration & dosage / Q000378:metabolism*
chemical_list: D000889:Anti-Arrhythmia Agents; D011355:Prodrugs; D016293:Moricizine