HUMAN MORICIZINE METABOLISM .1. ISOLATION AND IDENTIFICATION OF METABOLITES IN HUMAN URINE

1. Using synthetic standards and/or spectral data, seven moricizine me tabolites were structurally identified in human urine. Two novel metab olites were identified as phenothiazine-2-carbamic acid and ethyl [10- (3-aminopropionyl) phenothiazin-2-yl] carbamate. Two novel human moric izine metabolites, 2-amino-10-(3-morpholinopropionyl) phenothiazine, a previously identified dog metabolite, and 2-aminophenothiazine, a pre viously identified rat metabolite, were also identified. Three additio nal human metabolites, phenothiazine-2-carbamic acid ethyl ester sulph oxide (P2CAEES), moricizine sulphoxide, and ethyl {10-[N-(2'-hydroxyet hyl)3-aminopropionyl] phenothiazin-2-yl} carbamate, all previously des cribed in the literature, were observed. 2. Both 2-amino-10-(3-morphol inopropionyl) phenothiazine and ethyl [10-(3-aminopropionyl) phenothia zin-2-yl] carbamate, and possibly ethyl 2'-hydroxyethl)3-aminopropiony l]phenothiazin-2-yl} carbamate, possess the structural characteristics thought to be necessary for class 1 antiarrhythmic activity.