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2021
Glucuronidation catalyzed by uridine 5′-diphospho-glucuronosyltransferase (UGT) is the most common phase II metabolism. The UGTs can severely limit a drug's exposure and generate reactive metabolites, leading to toxicity. This chapter provides a brief overview of the current understanding of the UGT enzyme family, followed by various medicinal ...
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Glucuronidation catalyzed by uridine 5′-diphospho-glucuronosyltransferase (UGT) is the most common phase II metabolism. The UGTs can severely limit a drug's exposure and generate reactive metabolites, leading to toxicity. This chapter provides a brief overview of the current understanding of the UGT enzyme family, followed by various medicinal ...
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MicrosomalAcyl Glucuronidation: Enzyme-Kinetic Studies with Labile Glucuronides
Pharmacology, 1993Because of the labile nature of acyl glucuronides under physiologic conditions, metabolic rates of formation calculated using traditional methods may be confounded by concomitant rates of degradation. True metabolic formation rates may be approximated by stabilization of the metabolic product or by purifying the metabolite and calculating its ...
H, Spahn-Langguth, L 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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Intermediates for Glucuronide Synthesis: 7-Hydroxycoumarin Glucuronide
Journal of Chemical Research, 1997A convenient synthesis of the important metabolite 7-hydroxycoumarin glucuronide 3 is presented, including a first report of the β-imidate 11β, together with new preparations of the iodosugar 6 and α-imidate 11α: stability data on 11α and 11β are also given, and the importance of carefully controlled hydrolysis in the last step of the preparation of 3 ...
Richard T. Brown +2 more
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Hydrolysis of Morphine Glucuronide
Journal of Forensic Sciences, 1974Abstract In procedures requiring the quantitative analysis for total morphine in body fluids there is a need to liberate the bound drug, and for the hydrolysis of conjugates in urine there are alternative methods of acid or enzyme hydrolysis.
F, Fish, T S, Hayes
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Drug glucuronidation in humans
Pharmacology & Therapeutics, 1991Glucuronidation is a major metabolic pathway for a large number of drugs in humans. Conjugation of drugs and other chemicals with glucuronic acid is catalyzed by the multigene UDP-glucuronosyltransferase family. It is believed that a number (unspecified at present) of glucuronosyltransferase isozymes, which probably differ in terms of substrate ...
J O, Miners, P I, Mackenzie
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Morphine‐3‐glucuronide prevents tolerance to morphine‐6‐glucuronide in mice
European Journal of Pain, 1997Daily subcutaneous (s.c.) pretreatment with morphine‐3‐glucuronide (6 mg/kg) was found to reduce morphine‐6‐glucuronide (4 mg/kg s.c.)‐induced antinociception, with no decrease in the effect over 5 days. Morphine‐6‐glucuronide administration (4 mg/kg s.c.) on Day 6, without morphine‐3‐glucorinide pretreatment, results in a significant increase in ...
Faura, Clara C. +2 more
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ChemInform Abstract: Intermediates for Glucuronide Synthesis: 7‐Hydroxycoumarin Glucuronide.
ChemInform, 1998AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
R. T. BROWN +2 more
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Scintigraphic imaging with a peptide glucuronide in rabbits: 99mTc- exorphin C glucuronide
Applied Radiation and Isotopes, 2007A peptide glucuronide (Exorphin C glucuronide) was labeled with 99mTc using glucoheptonate (GH) as a bifunctional chelating agent. Scintigraphic imaging was performed in male Albino rabbits. Exorphin C glucuronide showed rapid and efficient labeling with 99mTc using glucoheptonate as a bifunctional chelate.
Unak, P. +5 more
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General Pharmacology: The Vascular System, 1998
Françoise Guéraud, Alain Paris
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Françoise Guéraud, Alain Paris
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