Human moricizine metabolism. I. Isolation and identification of metabolites in human urine

L. E. Richards, H. J. Pieniaszek*, S. Shatzmiller, G. O. Page, K. F. Blom, J. M. Read, A. F. Davidson, P. N. Confalone

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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-morpholinopropionyl) 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.

Original languageEnglish
Pages (from-to)217-229
Number of pages13
JournalXenobiotica
Volume27
Issue number2
DOIs
StatePublished - 1997

Fingerprint

Dive into the research topics of 'Human moricizine metabolism. I. Isolation and identification of metabolites in human urine'. Together they form a unique fingerprint.

Cite this