Výsledky vyhledávání - "Tienilic acid"

Reaction Phenotyping of Low-Turnover Compounds in Long-Term Hepatocyte Cultures Through Persistent Selective Inhibition of Cytochromes P450

Autor: Sheri Smith, Donald J. Tweedie, Karsten Menzel, Bennett Ma, Michael J. Lyman

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 49(11)

Recognizing the challenges of determining the relative contribution of different drug metabolizing enzymes to the metabolism of slowly metabolized compounds, a cytochrome P450 reaction phenotyping (CRP) method using cocultured human hepatocytes (HEPA

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0947ba45d4662d8ceb71fc0fcc46cfd
https://pubmed.ncbi.nlm.nih.gov/34407991

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Akademický článek

Human Anti-Endoplasmic Reticulum Autoantibodies Appearing in a Drug-Induced Hepatitis are Directed against a Human Liver Cytochrome P-450 that Hydroxylates the Drug

Autor: Dansette, P. M., Mansuy, D., Kiffel, L., Finck, M., Amar, C., Leroux, J. P., Homberg, J. C.

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America, 1987 Jan . 84(2), 551-555.

Externí odkaz: https://www.jstor.org/stable/29052

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An automated cocktail method for in vitro assessment of direct and time-dependent inhibition of nine major cytochrome P450 enzymes - application to establishing CYP2C8 inhibitor selectivity

Autor: Mikko Niemi, Mikko Neuvonen, Janne T. Backman, Terhi Launiainen, Anne M. Filppula, Jani Katajamäki, Helinä Kahma, Aleksi Tornio, Laura Aurinsalo, Jenni Viinamäki, Marie-Noëlle Paludetto

Publikováno v: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 162

We developed an in vitro high-throughput cocktail assay with nine major drug-metabolizing CYP enzymes, optimized for screening of time-dependent inhibition. The method was applied to determine the selectivity of the time-dependent CYP2C8 inhibitors g

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cae6ebf48a5c802fc4670cefc2ee5b2
https://pubmed.ncbi.nlm.nih.gov/33753217

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In Vitro Approaches for Studying the Inhibition of Drug-Metabolizing Enzymes and Identifying the Drug-Metabolizing Enzymes Responsible for the Metabolism of Drugs (Reaction Phenotyping) with Emphasis on Cytochrome P450

Autor: Andrew Parkinson, Etsuko Usuki, Brian W. Ogilvie, Phyllis Yerino

Publikováno v: Drug-Drug Interactions ISBN: 9780429131967

Victims are those drugs whose clearance is predominantly determined by a single route of elimination, such as metabolism by a single cytochrome P450 (CYP) enzyme. This chapter focuses on in vitro reaction phenotyping and CYP inhibition. A wide range

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::619c8ec61412d5171b542eaf065ff119
https://doi.org/10.1201/9780429131967-7

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Development of a rapid profiling method for the analysis of polar analytes in urine using HILIC–MS and ion mobility enabled HILIC–MS

Autor: Lauren Mullin, Paul D. Rainville, Robert S. Plumb, Ian D. Wilson, Garth L. Maker, Robert D. Trengove, Lee A. Gethings, Muireann Coen, Adam King

Publikováno v: Metabolomics

Introduction As large scale metabolic phenotyping is increasingly employed in preclinical studies and in the investigation of human health and disease the current LC–MS/MS profiling methodologies adopted for large sample sets can result in lengthy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ed38c47c609b3427ba4b5397d615e53
http://europepmc.org/articles/PMC6342856

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Paraoxonase-1 (PON1) inhibition by tienilic acid produces hepatic injury: Antioxidant protection by fennel extract and whey protein concentrate

Autor: Fathia A. Mannaa, Khaled G. Abdel-Wahhab, Heba Fawzi

Publikováno v: Pathophysiology. 23:19-25

This study evaluated the effect of whey protein concentrate (WPC) or fennel seed extract (FSE) on paraoxonase-1 activity (PON1) and oxidative stress in liver of tienilic acid (TA) treated rats. Six groups of rats were treated for six weeks as follows

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23fd9c7007648430580070347d1c4742
https://doi.org/10.1016/j.pathophys.2015.10.002

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Capillary ultra performance liquid chromatography-tandem mass spectrometry analysis of tienilic acid metabolites in urine following intravenous administration to the rat

Autor: Ian D. Wilson, Robert S. Plumb, Isobelle Grant, Muireann Coen, Paul D. Rainville, Giorgis Isaac, Adam King

Capillary scale (100 mm × 150 μm id) UPLC/MS/MS, performed using reversed-phase gradient chromatography on sub 2 μm particles, has been successfully employed for the characterization of the metabolites of the drug tienilic acid (TA) excreted via t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a068892df2949439c652ba83d77902b
http://hdl.handle.net/10044/1/62157

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Analysis of the Metabolic Pathway of Bosentan and of the Cytotoxicity of Bosentan Metabolites Based on a Quantitative Modeling of Metabolism and Transport in Sandwich-Cultured Human Hepatocytes

Autor: Ken-ichi Nunoya, Angelina Yukiko Staub, Takeo Nakanishi, Naomi Kaneko, Ikumi Tamai, Norikazu Matsunaga, Haruo Imawaka

Publikováno v: Drug Metabolism and Disposition. 44:16-27

To quantitatively understand the events in the human liver, we modeled a hepatic disposition of bosentan and its three known metabolites (Ro 48-5033, Ro 47-8634, and Ro 64-1056) in sandwich-cultured human hepatocytes based on the known metabolic path

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74fcf44eb7d14a74e0cbdb5d737e2637
https://doi.org/10.1124/dmd.115.067074

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Significantly Different Covalent Binding of Oxidative Metabolites, Acyl Glucuronides, and S-Acyl CoA Conjugates Formed from Xenobiotic Carboxylic Acids in Human Liver Microsomes

Autor: Katarina Breitholtz, Ulrik Jurva, Lars Weidolf, Malin Darnell, Emre M. Isin

Publikováno v: Chemical Research in Toxicology. 28:886-896

Xenobiotic carboxylic acids may be metabolized to oxidative metabolites, acyl glucuronides, and/or S-acyl-CoA thioesters (CoA conjugates) in vitro, e.g., in hepatocytes, and in vivo. These metabolites can potentially be reactive species and bind cova

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d2872e73a7979df2304aac357c0dfca
https://doi.org/10.1021/tx500514z

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