[Biotransformation and pharmacokinetics of mesoionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443). Studies on its biotransformation in rats].
The metabolism of the antiepileptic mesoionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443) was investigated after p.o. application in rats. The main metabolite was benzoic acid, besides the unchanged material and hippuric acid the spasmodically compounds N-methyl-benzamide and mesionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-one were detectable. In-vitro experiments could be demonstrated that LU 2443 was not demethylated by biochemical oxidation, and LU 2443 was also very stable against metabolizing influences by enteric bacteria.
D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism*; D001565:Benzoates / Q000378:metabolism; D001711:Biotransformation; D003640:Dealkylation; D005243:Feces / Q000032:analysis; D006626:Hippurates / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D051381:Rats; D013830:Thiadiazoles / Q000378:metabolism*
D000927:Anticonvulsants; D001565:Benzoates; D006626:Hippurates; D013830:Thiadiazoles; C036262:Lu 2443; C030514:hippuric acid
Biotransformation und Pharmakokinetik von mesoionischem Didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidin-2-thion (LU 2443). Untersuchungen zur Biotransformation an Ratten.