FYX-051, a Xanthine Oxidoreductase Inhibitor, Induces Nephropathy in Rats, but not in Monkeys
نویسندگان
چکیده
منابع مشابه
FYX-051: a novel and potent hybrid-type inhibitor of xanthine oxidoreductase.
4-[5-(Pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile (FYX-051) is a potent inhibitor of bovine milk xanthine oxidoreductase (XOR). Steady-state kinetics study showed that it initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previ...
متن کاملCrystal structures of mammalian xanthine oxidoreductase bound with various inhibitors: allopurinol, febuxostat, and FYX-051.
Xanthine oxidoreductase (XOR) catalyzes the reaction of hypoxanthine to xanthine and of xanthine to uric acid. Inhibitors of XOR can thus decrease the concentration of uric acid in serum. Crystal structures of XOR bound with various inhibitors reveal that inhibitors can be categorized into three types, i.e. mechanism-based, structure-based, and hybrid types.
متن کاملCharacterization of N-glucuronidation of 4-(5-pyridin-4-yl-1H-[1,2,4]triazol-3-yl) pyridine-2-carbonitrile (FYX-051): a new xanthine oxidoreductase inhibitor.
In humans, orally administered 4-(5-pyridin-4-yl-1H-[1,2,4]triazol-3-yl) pyridine-2-carbonitrile (FYX-051) is excreted mainly as triazole N(1)- and N(2)-glucuronides in urine. It is important to determine the enzyme(s) that catalyze the metabolism of a new drug to estimate individual differences and/or drug-drug interactions. Therefore, the characterization and mechanism of these glucuronidatio...
متن کاملMechanism of Urinary Bladder Carcinogenesis Induced by a Xanthine Oxidoreductase Inhibitor, in Rats
© 2013 Ashizawa and Shimo, licensee InTech. This is an open access chapter distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/3.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Mechanism of Urinary Bladder Carcinogenesis Induced by a Xanthine Oxidoreductase...
متن کاملCatechol-o-methyltransferase inhibitor tolcapone improves learning and memory in naïve but not in haloperidol challenged rats
Objective(s): Dopamine plays an important role in cognitive functions. Inhibition of the dopamine-degrading enzyme catechol-O-methyltransferase (COMT) may have beneficial effects. Our aim was to assess the effect of COMT inhibitor tolcapone (TCP) on learning and memory in naïve and haloperidol-challenged rats.Materials and Methods: Male ...
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ژورنال
عنوان ژورنال: Toxicologic Pathology
سال: 2009
ISSN: 0192-6233,1533-1601
DOI: 10.1177/0192623309332995