Abstract
After intravenous dosage in dogs, the major portion of the xanthine oxidase inhibitor, 3-(4-pyrimidinyl)-5-(4-pynidyl)-1,2,4-triazole, is excreted in bile as a polar conjugate refractory to µ-glucuronidase, sulfatase, µ-glycosidase and nucleoside phosphorylase. High resolution mass spectrometry. nuclear magnetic resonance, absorption and fluorescence spectra, and identification of chemical hydrolysis produets of recrystallized conjugate have established its structure as the N-(1)-µ-D-glucopyranoside. The same conjugate is a sigificant component of renal and biliary elimination in the rat and monkey as well. These constitute the first reported instance of N-glucosylation as a detoxification mechanism in mammals.
Footnotes
- Received February 26, 1974.
- Accepted May 21, 1974.
- © 1974 by The Williams & Wilkins Co.
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