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Characterization of aldo-keto reductase 1C subfamily members encoded in two rat genes (akr1c19 and RGD1564865). Relationship to 9-hydroxyprostaglandin dehydrogenase.
Arch Biochem Biophys
March 2021
Faculty of Engineering, Gifu University, Gifu, 501-1193, Japan.
Rat genes, akr1c19 and RGD1564865, encode members (R1C19 and 20HSDL, respectively) of the aldo-keto reductase (AKR) 1C subfamily, whose functions, however, remain unknown. Here, we show that recombinant R1C19 and 20HSDL exhibit NAD-dependent dehydrogenase activity for prostaglandins (PGs) with 9α-hydroxy group (PGF, its 13,14-dihydro- and 15-keto derivatives, 9α,11β-PGF and PGD). 20HSDL oxidized the PGs with much lower K (0.
View Article and Find Full Text PDFA simple in vitro model to study the stability of acylglucuronides.
J Pharmacol Toxicol Methods
April 2007
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
Introduction: Compounds containing the carboxylic functional group (e.g. non-steroidal anti-inflammatory drugs) can be metabolized to form acylglucuronides.
View Article and Find Full Text PDFIn vitro and in vivo studies on acyl-coenzyme A-dependent bioactivation of zomepirac in rats.
Chem Res Toxicol
November 2005
Department of Analytical Chemistry, The Danish University of Pharmaceutical Sciences, DK-2100 Copenhagen, Denmark.
Zomepirac [ZP, 5-(chlorobenzoyl)-1,4-dimethylpyrrole-2-acetic acid] was withdrawn from the market because of unpredictable allergic reactions that may have been caused by ZP-protein adducts formed by reaction of the reactive acyl glucuronide of ZP (ZP-O-G) with endogenous proteins. To test the hypothesis that the reactive ZP acyl coenzyme A thioester (ZP-CoA) was formed and potentially could contribute to formation of ZP-protein adducts, we investigated the acyl CoA-dependent metabolism of ZP in freshly isolated rat hepatocytes (1 mM) and in vivo (100 mg ZP/kg, ip) in rat livers (2 h after dose administration), rat bile (0-4 h), and rat urine (0-24 h). ZP-CoA was detected in freshly isolated hepatocytes and in vivo in rat livers by LC/MS/MS.
View Article and Find Full Text PDFChemical and immunochemical comparison of protein adduct formation of four carboxylate drugs in rat liver and plasma.
Chem Res Toxicol
October 1996
Department of Medicine, University of Queensland, Brisbane, Australia.
Carboxylate drugs usually form acyl glucuronide conjugates as major metabolites. These electrophilic metabolites are reactive, capable of undergoing hydrolysis, rearrangement, and covalent binding reactions to proteins. The last-mentioned property has the potential to initiate immune and other toxic responses in vivo.
View Article and Find Full Text PDFExamining product risk in context. Market withdrawal of zomepirac as a case study.
JAMA
October 1993
Department of Social Medicine, Harvard Medical School, Boston, MA 02215.
Objective: To examine changes in the prescribing of analgesics after the market entry and subsequent withdrawal of zomepirac sodium, a nonsteroidal anti-inflammatory drug (NSAID), following repeated reports of zomepirac-related deaths.
Design: To evaluate this natural quasi experiment, we conducted time-series analyses to compare prescribing in two cohorts of primary care physicians from July 1980 through September 1983.
Setting: Study physicians provided outpatient pharmaceutical care to patients enrolled in the New Jersey Medicaid program.
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