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Ren Fail
December 2021
Department of Anatomy, and Laboratory of Neuroscience and Tissue Engineering, Basic Medical College, Chongqing Medical University, Chongqing, China.
Background: End-stage renal disease (ESRD) is the final stage during the development of renal failure. Depression is the most common psychiatric disorder in patients with ESRD, which in turn aggravates the progression of renal failure, however, its underlying mechanism remains unclear. This study aimed to reveal the pathogenesis and to discover novel peripheral biomarkers for ESRD patients with depression through metabolomic analysis.
View Article and Find Full Text PDFDrug Metab Dispos
September 1997
Immunoscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
An in vitro glucuronidation assay was used to optimize a series of N-hydroxyurea-containing 5-lipoxygenase inhibitors for metabolic stability. The glucuronidation of these compounds in cynomolgus monkey microsomes followed Michaelis-Menten kinetics allowing calculation of V(max) and K(M). The V(max) values ranged from 0.
View Article and Find Full Text PDFJ Clin Pharmacol
May 1997
Abbott Laboratories, Chicago, Illinois, USA.
The pharmacokinetics of zileuton and its conjugated metabolites were evaluated in patients with chronic renal impairment. Five healthy volunteers (creatinine clearance > 90 mL/min), five patients with renal failure requiring hemodialysis, six with mild (creatinine clearance, 60-90 mL/min), eight with moderate (creatinine clearance, 30-59 mL/min), and six with severe (creatinine clearance < 30 mL/min) renal impairment participated in the study. Zileuton was well tolerated by all participants including those with severe renal impairment and those receiving hemodialysis.
View Article and Find Full Text PDFJ Med Chem
November 1995
Abbott Laboratories, Immunoscience Research, Illinois 60064, USA.
Structure-activity optimization of inhibitory potency and duration of action of N-hydroxyurea containing 5-lipoxygenase inhibitors was conducted. The lipophilic heteroaryl template and the link group connecting the template to the N-hydroxyurea pharmacophore were modified. Inhibition of 5-lipoxygenase was evaluated in vitro in a human whole blood assay.
View Article and Find Full Text PDFJ Pharmacol Exp Ther
February 1995
Immunosciences Research Area, Abbott Laboratories, Abbott Park, Illinois.
As in vitro glucuronidation assay and several biochemical assays were utilized to discover potent new N-hydroxyurea-containing 5-lipoxygenase inhibitors with long durations of action. The best of these, A-78773, is a racemic mixture of two enantiomers. These enantiomers were purified and the R(+)-enantiomer A-79175 was found to be superior to the S(-)-enantiomer with respect to in vitro metabolism and duration of action in the monkey.
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