BIOTRANSFORMATION AND EXCRETION OF Z-2-AM INO-5-CHLOROBENZOPHENONEAMIDINOHYDRAZONE

After i.v., p.o. and i.p. administration of C-14-labeled Z-2-amino-5-c hlorobenzophenoneamidinohydrazone (1) to male Wistar rats the total ra dioactivity is mainly excreted via faeces (80%). Within 3 to 4 d after administration 86 to 100% of the dose have been found in urine and fa eces. Beside 1 and its E-isomer (2) we have detected in faeces of rats and rabbits the metabolites 3 (principal metabolite) and 4, in urine of rats additionally 5 and 6, and in urine of rabbits additionally 5 t o 8. With regard to the results of high resolution mass spectrometry, UV, TLC and the hydrolyzability using beta-glucuronidase we can conclu de that 3 and 4 are metabolites position isomerically hydroxylated at the unsubstituted phenyl group, 5 and 6 are the glucuronides of them, and 7 and 8 are the glucuronides of 1 and 2.