Identification of trimoprostil metabolites excreted in rat bile formed by oxidation and taurine conjugation.
14C-Trimoprostil was administered iv and orally to male rats. Radioactivity was excreted mainly via the feces after both routes of drug administration. Bile duct-cannulated rats excreted an average of 76% of an iv dose in the bile within 6 hr after dosing. Four biliary metabolites were isolated by HPLC and identified by proton NMR spectroscopy and mass spectrometry. These metabolites were taurine conjugates of: trimoprostil (approximately 11% of dose), 5,6-dihydro-2,3-dinor trimoprostil (approximately 5% of dose), 3,4-dehydro trimoprostil (less than 5% of dose) and 5,6-dihydro-2,3,4,5-tetranor trimoprostil (less than 5% of dose).
Kolis
S J
SJ
Postma
E J
EJ
Williams
T H
TH
Sasso
G J
GJ
D000818:Animals; D001646:Bile / Q000378:metabolism*; D001711:Biotransformation; D015232:Dinoprostone / Q000031:analogs & derivatives*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008657:Metabolic Clearance Rate; D010084:Oxidation-Reduction; D011459:Prostaglandins E, Synthetic / Q000378:metabolism*; D051381:Rats; D013654:Taurine / Q000378:metabolism
D011459:Prostaglandins E, Synthetic; D013654:Taurine; C038879:trimoprostil; D015232:Dinoprostone