In vivo biotransformation and biliary excretion of 1-14C-acrylonitrile in rats.

1-14C-Acrylonitrile (VCN) was give orally to rats, 27% of the given dose was excreted in bile in 6 h. When 1-14C-VCN was given to overnight fasted or cobaltous chloride treated rats, a significant increase in the biliary excretion occurred. Pretreatment of rats with phenobarbital produced no change, while diethyl maleate pretreatment significantly decreased the portion of the dose excreted in bile in 6 h. Four metabolites of 1-14C-VCN have been isolated from the collected bile, and characterized. The two major biliary metabolites were found to be glutathione (GSH) conjugates of VCN, indicating the importance of GSH in VCN biotransformation.