Human Liver Microsomes
Glucuronidation of 6 alpha hydroxy bile acids by human liver microsomes
... The glucuronidation of 6-hydroxylated bile acids by human liver microsomes has been studied in vitro; for comparison, several major bile acids lacking a 6-hydroxyl group were also investigated. ...
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Genetic predisposition to the metabolism of irinotecan (CPT 11) Role of uridine diphosphate glucuronosyltransferase isoform 1A1 in the glucuronidation of its active metabolite (SN 38) in human liver microsomes
... An in vitro study investigating UGT1A1 activity and geno- type in human liver microsomes is in progress. A phase I clinical trial is being initiated to investigate the relationship between UGT1A1 ...
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In-vitro assessment of CYP3A4 and CYPC29 inhibition potential of Lupeol using human liver microsomes
... Lupeol (purity 99 %) was purchased from Natural Remedies Private Limited, Bangalore, India. Ketoconazole, Sulfaphenazole, Diclofenac, and Testosterone were received as gift Samples from CIPLA (Patalganga Panvel, ...
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Inhibitory effect study of calf thymus DNA on catalytic activity of CYP450 enzyme in human liver microsomes
... five human liver CYP isoforms, CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 have been confirmed to be the most relevant isozymes in the metabolism of clinically commonly used drugs [3, ...
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Hemodialysis does not alter in vitro hepatic CYP3A4 and CYP2D6 metabolic activity in uremic serum
... in microsomes because microsomes also lack ...using human liver microsomes and the probes, midazolam and dextromethorphan, to test the hypothesis that acute clearance of uremic toxins ...
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<p>Metabolic Stability Assessment of New PARP Inhibitor Talazoparib Using Validated LC–MS/MS Methodology: In silico Metabolic Vulnerability and Toxicity Studies</p>
... method was 5 – 500 ng/mL (r 2 ≥ 0.999) in the human liver microsomes (HLMs) matrix. Different parameters were calculated to con fi rm the method sensitivity (limit of quanti fi ca- tion was 2.0 ng/mL), ...
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Identification and mechanistic study of novel drug metabolites by LC MS
... A compound series in an early drug discovery programme formed unusual methanol adducts post incubation in human liver microsomes.. The work undertaken in this thesis revealed the generat[r] ...
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In vitro and in vivo evaluation of CYP1a interaction potential of terminalia arjuna bark
... and human liver ...rat liver microsomes while 30.0, 29.7 and 39.0 µg/ml in human liver microsomes, respectively for ...rat liver microsomes and human ...
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<p>Metabolic Stability Assessment of Larotrectinib Using Liquid Chromatography Tandem Mass Spectrometry</p>
... Results and Discussion: The linearity range of the established method was 5 – 500 ng/mL (r 2 ≥ 0.9999) in the human liver microsomes (HLMs) matrix. Various parameters were calculated to validate the ...
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Nitrosamines and oesophageal cancer. A study of factors influencing the distribution and metabolism of nitrosamines and the enzymes responsible for their activation
... rat liver microsomes (Raunio, 1988), so the coumarin metabolism is carried out by a P450 which is not closely related to mouse ...rat liver (Soucek, ...to human P450 2A6 (Gonzalez, 1992), but ...
240
Original Article Human UDP-glucuronosyltransferase 1A1, 1A7, 1A8, 1A9 and 1A10 are mainly responsible for icariside II-7- O-glucuronidation
... involving human UDP-glucuronosyltransferases (UGTs) remains ...by human liver microsomes (HLM) and human intestine microsomes (HIM) with the intrinsic clearance (CL int ) values ...
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Inhibitory effect of celecoxib on agomelatine metabolism in vitro and in vivo
... Recombinant human CYP2C9 and cytochrome b5 were kind gifts from Beijing Hospital (Beijing, ...Pooled human liver microsomes (HLMs) from donors were purchased from Gentest (Woburn, MA, ...
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Construction of a novel quinoxaline as a new class of Nrf2 activator
... HLM: human liver microsomes; RLM: rat liver microsomes; MLM: mouse liver microsomes; DMEM: Dublecco’s modified eagle medium; FBS: fetal bovine serum; MTT: ...
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The Effect of Inducers and Inhibitors of Monooxygenase on the Activity Nitrergic System in the Microsomes in the Ischemic Liver
... DOI: 10.9734/JAMMR/2018/41216 Editor(s): (1) Dr. Kate S Collison, Department of Cell Biology, King Faisal Specialist Hospital & Research Centre, Saudi Arabia. (2) Dr. Chan-Min Liu, School of Life Science, Xuzhou ...
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An investigation into the contribution of flavin containing monooxygenases to the development and prevention of thiourea-induced pulmonary toxicity in the rat
... both liver and lungs, followed after 2 d by an elevation of non-protein sulphydryl levels above the reference levels reported in literature: rats challenged with ANTU 48 h after phorone administration showed ...
228
Characteristics of intracellular Ca<sup>2+</sup> signals consisting of two successive peaks in hepatocytes during liver regeneration after 70% partial hepatectomy in rats
... of microsomes prepared from 70% PH rats and ALT values at 24 hours after CCl 4 administration immediately after 70% PH, their levels recovered temporarily to the control levels at day 4, returned to the decreased ...
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Triptolide Induces hepatotoxicity via inhibition of CYP450s in Rat liver microsomes
... However, the underlying mechanisms of TP-induced toxicity mediated by the CYP450 family have not been well delineated. Since abnormal drug metabolism by CYP450s also plays an important role in the hepatotox- icity, the ...
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TRANSCORTIN: A CORTICOSTEROID BINDING PROTEIN OF PLASMA V IN VITRO INHIBITION OF CORTISOL METABOLISM
... liver homogenates or microsomes to reduce the cortisol molecule efficiently in the presence of transcortin either in concentrated form or in transcortin-rich plasma points to the ability[r] ...
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Observations on the factors that control the generation of triiodothyronine from thyroxine in rat liver and the nature of the defect induced by fasting
... Studies were performed to explore the mechanism underlying the impaired generation of 125-I-3,5,3'-triiodothyronine (T3) from 125I-thyroxine (T4) (T3-neogenesis)) in preparations of liver from rats fasted for 48 h ...
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Effect of MRP2 and MRP3 Polymorphisms on Anastrozole Glucuronidation and MRP2 and MRP3 Gene Expression in Normal Liver Samples
... Briefly, human liver specimens (n=102) were obtained from the Cooperative Human Tissue Network ...All liver specimens were from Caucasian donors ranging in age from 26 to 102 years, with 54 ...
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