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Monday, May 4, 2020 | History

2 edition of In vitro metabolism and covalent binding of furazolidone. found in the catalog.

In vitro metabolism and covalent binding of furazolidone.

Lynn Elizabeth Witherow

In vitro metabolism and covalent binding of furazolidone.

by Lynn Elizabeth Witherow

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Published by University of Manchester in Manchester .
Written in English


Edition Notes

Thesis (Ph.D.), - University of Manchester, Department of Pharmacy.

ContributionsUniversity of Manchester. Department of Pharmacy.
The Physical Object
Pagination229p.
Number of Pages229
ID Numbers
Open LibraryOL16573049M

Protocols of in vitro protein covalent binding studies in liver. Lévesque JF(1), Day SH, Jones AN. Author information: (1)Department of Drug Metabolism and Pharmacokinetics, Merck Frosst Centre for Therapeutic Research, Kirkland, QC, Canada. [email protected] by: 2. Furazolidone is active in vitro against Campylobacter jejuni, Enterobacter aerogenes, Escherichia coli, Proteus species, Salmonella species, Shigella species, and staphylococci. However, clinical studies on the effectiveness of furazolidone in some types of bacterial diarrhea have been inconclusive or conflicting. {01} {02} {25} {26}.

Following incubation of [14C]neratinib in control human plasma at 37°C for 6 hours, about 60% to 70% of the radioactivity was not extractable, due to covalent binding to albumin. In this study, factors that could potentially affect the covalent binding of neratinib to plasma proteins, specifically to Cited by: Abstract. Phencyclidine (PCP) is a drug of abuse which may produce, in some users, a persistent schizophreniform psychosis. The possibility that long term effects of PCP are mediated by metabolic activation of the parent compound to reactive species is consistent with the demonstration of metabolism-dependent covalent binding of radiolabeled PCP in vivo and in vitro to .

Studies undertaken using radiolabelled furazolidone have demonstrated the covalent binding of residues of the drug to cellular protein in vivo.A portion of these bound residues and those formed by furaltadone, a related nitrofuran drug, possess intact side-chains, 3-aminooxazolidinone (AOZ) and 5-morpholinomethylaminooxazolidinone (AMOZ), respectively. Nitrofurantoin is a synthetic derivative of imidazolidinedione, Nitrofurantoin inhibits bacterial DNA, RNA, and cell wall protein ted by bacterial flavoproteins to intermediates that inactivate bacterial ribosomal proteins, Nitrofurantoin is used prophylactically as a urinary anti-infective agent against most gram-positive and gram-negative organisms and for long-term.


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In vitro metabolism and covalent binding of furazolidone by Lynn Elizabeth Witherow Download PDF EPUB FB2

In vitro covalent binding assessments of drugs have been useful in providing retrospective insights into the association between drug metabolism and a resulting toxicological response.

On the basis of these studies, it has been advocated that in vitro covalent binding to liver microsomal proteins in the presence and the absence of NADPH be used routinely to screen drug by: This proton at 8 also coupled with the doublet at b Coupling was proved by using spin decoupling methods.

In vitro metabolism of furazolidone The in vitro aerobic metabolism of furazolidone by liver microsomes from 3MC-induced male rats is characterized by rapid conversion of the parent by: Pelkonen, Effects of microsomal enzyme inducers in vivo and inhibitors in vitro on the covalent binding of benzo(a)pyrene metabolites to DNA catalyzed by liver microsomes from genetically responsive and nonresponsive mice, by: In vitro covalent binding studies in which xenobiotics are shown to undergo metabolism-dependent covalent binding to macromolecules have been commonly used to shed light on the biochemical mechanisms of xenobiotic-induced toxicity.

In this paper, 18 drugs (nine hepatotoxins and nine nonhepatotoxins) were tested for their proclivity to demonstrate metabolism-dependent covalent binding Cited by: In vitro covalent binding studies in which xenobiotics are shown to undergo metabolism-dependent covalent binding to macromolecules have been commonly used to shed light on the biochemical mechanisms of xenobiotic-induced toxicity.

The bioactivation is generally considered to be related to drug toxicity, although mechanism involved in the toxicity induced by the adduct is largely undefined. 20 In vitro covalent protein binding (CPB) study offers direct evidence of covalent binding of drug to proteins and is commonly used to measure bioactivation and assess potential toxicity risk in humans.

21,22 Radiolabeling a drug provides a convenient way to measure the metabolism Cited by: 1. Covalent protein binding Bioactivation Reactive intermediate Idiosyncratic toxicity Drug metabolism Hepatocytes Microsomes Radiolabeled compound Cytochrome P This is a preview of subscription content, log in to check by: 2.

Abstract. It has become increasingly evident that many chemically inert foreign compounds are converted in the body to chemically reactive metabolites that react with a number of substances in tissues and thereby cause changes which result in various toxicites including cancer, mutagenesis, cellular necrosis, immunological reactions, blood dyscrasias, and fetal damage (1–11).

In vitro, some work has focused on the role of esterases in the detoxication process (Jao et al., a,b; Soderlund and Casida, ; White et al., ). Furthermore, during metabolism, covalent binding has been found to exist between the metabolites and the microsomal protein of rat liver (Ueda et al., b; Gray et al., ).Cited by: In Vitro Drug Metabolism.

Covalent binding studies provide the most quantitative data which can be used for decision making, appreciating that there are caveats of extrapolating from in vitro.

The binding of 3H acetaminophen to hepatic microsomes was studied in vitro. Binding of 3H acetaminophen to rat and mouse microsomal protein was linear with time and with protein concentration. In Vivo and in Vitro Metabolic Studies of Furazolidone: A Risk Evaluation. Drug Metabolism Reviews: Vol.

22, No.pp. Cited by: During metabolism, a considerable amount of material (% of total metabolites) became covalently bound to microsomal protein. This covalent binding could be inhibited by addition of glutathione, which also resulted in an almost complete shift from non-polar to water-soluble by: Toxicology Letters, 30 () Eisevier TOXLett.

EFFECT OF ETHANOL ON THE IN VIVO COVALENT BINDING AND IN VITRO METABOLISM OF AFLATOXIN Bi IN RATS (Aflatoxin B|; ethanol; covalent adducts; metabolism) CHAIVAT TOSKULKAO* and THIRAYUDH GLINSUKON Department of Physiology, Faculty of Science, Mahidol University, Rama VI Road, Bangkok Cited by:   Each volume of Methods in Toxicology is available in case binding for the library and Wire-O-binding for the laboratory.

About the Book: Concurrent with the development of biological systems for in vitro toxicologic investigations (Volume 1A-In Vitro Biological Systems), techniques have evolved to detect and evaluate the diverse effects Book Edition: 1.

Correlation of metabolism, covalent binding and toxicity for a series of bromobenzene derivatives using rat liver slices in vitro. Fisher R(1), Brendel K, Hanzlik RP. Author information: (1)Department of Pharmacology, University of Arizona, Tucson Cited by: Benchmarking in Vitro Covalent Binding Burden As a Tool To Assess Potential Toxicity Caused by Nonspecific Covalent Binding of Covalent Drugs.

() Can in vitro metabolism. In vitro metabolism of furazolidone (N-(5-nitrofurfuryliden)aminooxazolidone) was investigated by using milk xanthine oxidase and rat liver g supernatant. A new type of reduction product was isolated as 1 of the main metabolites from the incubation mixture and it was tentatively identified as 2,3-dihydrocyanomethylhydroxylnitro-1a,2-di(2-oxo-oxazolidinyl)imino methyl.

Purchase Microsomes, Drug Oxidations and Chemical Carcinogenesis V2 - 1st Edition. Print Book & E-Book. ISBNBook Edition: 1. Covalent binding to proteins was also determined to check the presence and activity of enzymatic systems in subcellular compartments other than microsomes, e.g., nuclei.

In experiments with cyclophosphamide as substrate it was shown that nuclear enzymatic activities might well be responsible for drug covalent binding to by: 6. The gastrointestinal fate of protein-bound residues of the model compound furazolidone (FZD) was investigated in vitro and ex vivo. Protein-bound residues were generated in rat liver microsomes, isolated by solvent extraction and digested with % hydrochloric acid and Pronase E.

by: 9.Abstract. The hepatotoxicity of bromobenzene (1) has been associated with its metabolic activation and the subsequent covalent binding of a reactive metabolite, presumably its 3,4-oxide, to liver macromolecules (Reid and Krishna, ).In view of the presumed non-enzymatic nature of the covalent binding step, it was hypothesized that modulation of the reactivity of the metabolite through the Cited by: 7.Recently, a number of pharmaceutical companies have utilized in vitro (and in vivo) screens for covalent binding [75].Although a strong case can be made for the role of bioactivation and covalent binding in the toxicity of many drugs, e.g., [58], exactly what the impact of these screens has been is not easy to l recent studies have involved analyses of the covalent binding of.