[Biotransformation and excretion of Z-2-amino-5-chlorobenzophenoneamidinohydrazone].
After i.v., p.o. and i.p. administration of 14C-labeled Z-2-amino-5-chlorobenzophenoneamidinohydrazone (1) to male Wistar rats the total radioactivity 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 faeces. 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 to 8. With regard to the results of high resolution mass spectrometry, UV, TLC and the hydrolyzability using beta-glucuronidase we can conclude 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.
Borchert
H H
HH
Fachbereich Pharmazie, Humboldt-Universität zu Berlin.
Schieweck
A
A
Franke
P
P
Morgenroth
U
U
Joram
U
U
D000284:Administration, Oral; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001577:Benzophenones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001711:Biotransformation; D002855:Chromatography, Thin Layer; D005243:Feces / Q000737:chemistry; D006835:Hydrazones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D008297:Male; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013056:Spectrophotometry, Ultraviolet
D000889:Anti-Arrhythmia Agents; D001577:Benzophenones; D006835:Hydrazones; C080444:(Z)-2-amino-5-chlorobenzophenonamidinohydrazone acetate
Biotransformation und Ausscheidung von Z-2-Amino-5-chlorbenzophenonamidinohydrazon.