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Caution with PBPK Modeling Based on the In Vitro Kinetics for Bilirubin Hepatic Uptake and Glucuronidation: Commentary on Dong et al. [PDF]
Clin Pharmacol TherMiners JO, Polasek TM.
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Glucuronidation: driving factors and their impact on glucuronide disposition
Drug Metabolism Reviews, 2017 Glucuronidation is a well-recognized phase II metabolic pathway for a variety of chemicals including drugs and endogenous substances. Although it is usually the secondary metabolic pathway for a compound preceded by phase I hydroxylation, glucuronidation alone could serve as the dominant metabolic pathway for many compounds, including some with high ...
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Effect of Glucuronides on Glucuronide Biosnthesis
European Journal of Biochemistry, 19711‐Naphthyl and phenolphthalein glucuronides were found to be potent inhibitors of p‐nitro‐phenyl glucuronide synthesis catalyzed by rat liver microsomal fraction. They did not compete with theaglycone, p‐nitrophenol, but with glucuronyl donor, UDPglucuronic acid.
O, Hänninen, J, Marniemi
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Glucuronidation of apomorphine
Life Sciences, 2000Apomorphine, a dopaminergic receptor agonist, is largely used in the therapy of Parkinson's disease. In this study, we characterized the glucuronidation of apomorphine and other catechols in rat liver and brain microsomes, using UDP-[U-14C]glucuronic acid and separation of the glucuronides formed by a thin layer chromatographic method.
R S, El-Bachá +4 more
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Xenobiotica, 1991
1. To expedite direct studies on phase II metabolites of fluphenazine, pure fluphenazine or 7-hydroxyfluphenazine were incubated with a rabbit hepatic microsomal immobilized enzyme system. After purification and recrystallization a high yield (60%) of 7-hydroxy-beta-D-O-glucuronyl-fluphenazine was obtained. 2.
C J, Jackson, J W, Hubbard, K K, Midha
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1. To expedite direct studies on phase II metabolites of fluphenazine, pure fluphenazine or 7-hydroxyfluphenazine were incubated with a rabbit hepatic microsomal immobilized enzyme system. After purification and recrystallization a high yield (60%) of 7-hydroxy-beta-D-O-glucuronyl-fluphenazine was obtained. 2.
C J, Jackson, J W, Hubbard, K K, Midha
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Drug Metabolism and Disposition, 2012
Glucuronidation reaction is catalyzed by mammalian uridine diphosphoglucuronosyl transferases by using uridine diphosphoglucuronic acid as a cosubstrate. Conjugation of glucuronic acid to nucleophilic functional groups in chemical entities results in formation of glucuronides. As anticipated, a number of nucleophilic functional groups such as hydroxyl,
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Glucuronidation reaction is catalyzed by mammalian uridine diphosphoglucuronosyl transferases by using uridine diphosphoglucuronic acid as a cosubstrate. Conjugation of glucuronic acid to nucleophilic functional groups in chemical entities results in formation of glucuronides. As anticipated, a number of nucleophilic functional groups such as hydroxyl,
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Glucuronidation and the Transport of the Glucuronide Metabolites in LLC-PK1 Cells
Molecular Pharmaceutics, 2005Formation and transport of glucuronide metabolites were studied in LLC-PK1 cells. Glucuronidation of 17beta-estradiol, 1-naphthol, mycophenolic acid, and 4-methylumbelliferone was examined in microsomes prepared from LLC-PK1 cells, human livers, human kidneys, and human intestines.
Jae H, Chang, Leslie Z, Benet
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Current Drug Metabolism, 2011
This review on isomers or acyl glucuronides (iso-glucuronides) updates earlier reviews, and attempts to place in context the advances that have been made, especially over the last 15 years. The essential chemistry behind the intramolecular acyl migration and anomerization reactions of acyl glucuronides has been appreciated for 30 years.
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This review on isomers or acyl glucuronides (iso-glucuronides) updates earlier reviews, and attempts to place in context the advances that have been made, especially over the last 15 years. The essential chemistry behind the intramolecular acyl migration and anomerization reactions of acyl glucuronides has been appreciated for 30 years.
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