Metabolism of Benthiocarb (4-Chlorobenzyl N, N-Diethylthiolcarbamate) in Mice

抄録

Benthiocarb labeled at benzyl methylene group with carbon-14 was synthesized and studied on the distribution, excretion and metabolism in white mice. Benthiocarb was rapidly translocated into organs after oral administration. Radioactive substances were also rapidly eliminated mainly into urine, slightly into feces and little into expiration. Major metabolites in urine were identified as 4-chlorohippuric and 4-chlorobenzoic acids, and small amounts of glucuronides of the latter acid and 4-chlorobenzyl alcohol were detected. Benthiocarb was degraded in liver homogenates, in which the microsomal fraction showed the largest activity, and the degradation was accelerated by reduced NADP as the cofactor for the reaction. N-Desethylbenthiocarb, bis(4-chlorobenzyl) mono- and di-sulfides, and 4-chlorobenzoic acid were identified in the incubation mixture of the liver homogenates. The main metabolic pathway in mice seemed to be as follows; parent benthiocarb and/or the N-desethylbentiocarb were hydrolyzed, and the produced 4-chlorobenzylmercaptan presumed to be oxidized finally to 4-chlorobenzoic acid, which then conjugated with glycine to produce 4-chlorohippuric acid.