Metabolism of thymoxamine. III. Structure elucidation of the metabolites and interspecies comparison.
The structures of six metabolites were elucidated using rat urine after intragastric administration of 14C-thymoxamine by means of enzyme incubations, mass spectrometry and synthesis of metabolites: desacetylthymoxamine, N-demethyl-desacetylthymoxamine, the corresponding sulfates and glucuronides. The nature of the conjugates was confirmed by biosynthesis, i.e., co-administration of unlabelled thymoxamine and 35S-sulfate or 14C-glucose. The system high performance liquid chromatography-radioactivity detection was used for interspecies comparison. All biotransformation pathways are seen in rat and man. In dog and cat demethylation is a very minor reaction. Glucuronidation is not observed in the cat.
Vollmer
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von Hodenberg
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D000818:Animals; D001711:Biotransformation; D002415:Cats; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D003640:Dealkylation; D004285:Dogs; D005260:Female; D005965:Glucuronates / Q000378:metabolism; D008297:Male; D013948:Moxisylyte / Q000378:metabolism*; D051381:Rats; D013045:Species Specificity; D013464:Sulfuric Acids / Q000378:metabolism
D005965:Glucuronates; D013464:Sulfuric Acids; D013948:Moxisylyte