In vivo metabolism of ethyl-1- 14C- N,N-di- n-propylthiolcarbamate in rats

Abstract

A study of the metabolism of ethyl-1- 14C- N,N-di- n-propylthiolcarbamate (EPTC) in adult female rats following oral doses, ranging from 0.6 to 103 mg, was carried out. Results revealed that increasing the dose led to a decrease in 14CO 2 output with a corresponding increase in urinary excretion of radioactivity. Generally, 14CO 2 elimination was completed within 15 hr for lower doses, but extended to approximately 35 hr for higher doses. The time for complete urinary elimination of radioactivity was likewise extended. The pattern of 14CO 2 elimination was changed from a single peaked pattern with lower doses to multiple peaked ones with higher doses. Paper chromatography and radioautography revealed six major radioactive metabolites in the urine. The relative amounts of these metabolites changed with the dose. One of the major metabolites was identified as urea. Attempts to isolate the individual metabolites through ion exchange column chromatography or extraction with organic solvents have not been successful. These procedures, as well as elution of metabolites from the paper strips, demonstrated the labile nature of three major metabolites.