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methapyrilene and Acute Liver Injury, Drug-Induced

methapyrilene has been researched along with Acute Liver Injury, Drug-Induced in 16 studies

Methapyrilene: Histamine H1 antagonist with sedative action used as a hypnotic and in allergies.
methapyrilene : A member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group.

Research Excerpts

ExcerptRelevanceReference
"Methapyrilene, [N,N-dimethyl-N'-pyridyl-N'(2-thienylmethyl)-1,2-ethanediamine] (MP) was withdrawn from, clinical use due to reported periportal hepatic necrosis and hepatocarcinogenicity in the rat, via S-oxidation of the thiophene group."7.75Functional and toxicological consequences of metabolic bioactivation of methapyrilene via thiophene S-oxidation: Induction of cell defence, apoptosis and hepatic necrosis. ( Antoine, DJ; Benson, CA; Foster, J; Graham, EE; Hirst, CM; Kenna, JG; Mercer, AE; Park, BK; Regan, SL; Williams, DP, 2009)
"Methapyrilene, [N,N-dimethyl-N'-pyridyl-N'(2-thienylmethyl)-1,2-ethanediamine] (MP) was withdrawn from, clinical use due to reported periportal hepatic necrosis and hepatocarcinogenicity in the rat, via S-oxidation of the thiophene group."3.75Functional and toxicological consequences of metabolic bioactivation of methapyrilene via thiophene S-oxidation: Induction of cell defence, apoptosis and hepatic necrosis. ( Antoine, DJ; Benson, CA; Foster, J; Graham, EE; Hirst, CM; Kenna, JG; Mercer, AE; Park, BK; Regan, SL; Williams, DP, 2009)
"Administration of high doses of the histamine antagonist methapyrilene to rats causes periportal liver necrosis."3.73Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat. ( Craig, A; Holmes, E; Jackson, D; Nicholson, J; Nickson, J; Orton, T; Rowlinson, R; Sidaway, J; Tonge, R; Wilson, I, 2006)
" Methapyrilene, a known hepatotoxin was dosed daily over 14-days at doses of 30 and 80mg/kg, followed by a recovery phase of 10days."1.46Quantitative targeted bile acid profiling as new markers for DILI in a model of methapyrilene-induced liver injury in rats. ( Ellinger-Ziegelbauer, H; Ernst, R; Herrmann, A; Keck, M; Mally, A; Pavkovic, M; Riefke, B; Slopianka, M, 2017)
" The method was successfully applied to the determination of OA in samples obtained following the chronic administration of the rat hepatotoxin methapyrilene, where plasma OA concentrations were observed to show a weak negative correlation with those of established liver injury biomarkers such as aspartate aminotransferase (AST)."1.37HPLC-MS/MS methods for the quantitative analysis of ophthalmic acid in rodent plasma and hepatic cell line culture medium. ( Geenen, S; Kenna, JG; Kolaja, KL; Michopoulos, F; Westerhoff, HV; Wilson, I, 2011)
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."1.36Developing structure-activity relationships for the prediction of hepatotoxicity. ( Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010)
" In the middle dose groups (30 mg/kg MP), no apparent changes were noted in blood biochemical data by single dosing or repeated dosing up to one week, and no obvious histopathological changes were observed except a slight hypertrophy in the hepatocytes."1.35Gene expression profiling of methapyrilene-induced hepatotoxicity in rat. ( Hirode, M; Kiyosawa, N; Miyagishima, T; Mizukawa, Y; Nagao, T; Omura, K; Ono, A; Shimizu, T; Uehara, T; Urushidani, T, 2008)
"Methapyrilene treatment alone specifically decreased microsomal enzyme activity markers for CYP2C11, CYP3A, and CYP2A and pretreatment with all the hepatic enzyme-inducing agents specifically prevented the loss of CYP2C11."1.30Effects of induction and inhibition of cytochromes P450 on the hepatotoxicity of methapyrilene. ( Cottrell, S; Powell, CJ; Ratra, GS, 1998)

Research

Studies (16)

TimeframeStudies, this research(%)All Research%
pre-19901 (6.25)18.7374
1990's1 (6.25)18.2507
2000's5 (31.25)29.6817
2010's9 (56.25)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Greene, N1
Fisk, L1
Naven, RT1
Note, RR1
Patel, ML1
Pelletier, DJ1
Ekins, S1
Williams, AJ1
Xu, JJ1
Dawson, S1
Stahl, S2
Paul, N1
Barber, J1
Kenna, JG5
Liu, Z1
Shi, Q1
Ding, D1
Kelly, R1
Fang, H1
Tong, W1
Warner, DJ1
Chen, H1
Cantin, LD1
Walker, CL1
Noeske, T1
Slopianka, M1
Herrmann, A1
Pavkovic, M1
Ellinger-Ziegelbauer, H1
Ernst, R1
Mally, A1
Keck, M1
Riefke, B1
Leitch, AC1
Probert, PME1
Shayman, JA1
Meyer, SK1
Kass, GEN1
Wright, MC1
Braeuning, A1
Oberemm, A1
Heise, T1
Gundert-Remy, U1
Hengstler, JG1
Lampen, A1
Mercer, AE1
Regan, SL1
Hirst, CM2
Graham, EE2
Antoine, DJ1
Benson, CA1
Williams, DP2
Foster, J1
Park, BK2
Geenen, S1
Michopoulos, F1
Kolaja, KL1
Westerhoff, HV1
Wilson, I2
O'Brien, PJ1
Slaughter, MR1
Polley, SR1
Kramer, K1
Craig, A1
Sidaway, J1
Holmes, E1
Orton, T1
Jackson, D1
Rowlinson, R1
Nickson, J1
Tonge, R1
Nicholson, J1
Uehara, T1
Kiyosawa, N1
Hirode, M1
Omura, K1
Shimizu, T1
Ono, A1
Mizukawa, Y1
Miyagishima, T1
Nagao, T1
Urushidani, T1
Walsh, RJ1
Maggs, JL1
Martin, S1
Wild, MJ1
Wilson, ID1
Harding, JR1
Peter, RM1
Ratra, GS1
Cottrell, S1
Powell, CJ1
Graichen, ME1
Neptun, DA1
Dent, JG1
Popp, JA1
Leonard, TB1

Other Studies

16 other studies available for methapyrilene and Acute Liver Injury, Drug-Induced

ArticleYear
Developing structure-activity relationships for the prediction of hepatotoxicity.
    Chemical research in toxicology, 2010, Jul-19, Volume: 23, Issue:7

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Humans; Structure-Activity Relationship;

2010
A predictive ligand-based Bayesian model for human drug-induced liver injury.
    Drug metabolism and disposition: the biological fate of chemicals, 2010, Volume: 38, Issue:12

    Topics: Bayes Theorem; Chemical and Drug Induced Liver Injury; Humans; Ligands

2010
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:1

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters

2012
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
    PLoS computational biology, 2011, Volume: 7, Issue:12

    Topics: Animals; Anti-Infective Agents; Anti-Inflammatory Agents; Chemical and Drug Induced Liver Injury; Da

2011
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:12

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters

2012
Quantitative targeted bile acid profiling as new markers for DILI in a model of methapyrilene-induced liver injury in rats.
    Toxicology, 2017, 07-01, Volume: 386

    Topics: Animals; Bile Acids and Salts; Biomarkers; Chemical and Drug Induced Liver Injury; Chromatography, L

2017
B-13 progenitor-derived hepatocytes (B-13/H cells) model lipid dysregulation in response to drugs and chemicals.
    Toxicology, 2017, 07-01, Volume: 386

    Topics: Animals; Benzoates; Benzylamines; Cell Line; Chemical and Drug Induced Liver Injury; Dose-Response R

2017
In vitro proteomic analysis of methapyrilene toxicity in rat hepatocytes reveals effects on intermediary metabolism.
    Archives of toxicology, 2019, Volume: 93, Issue:2

    Topics: Animals; Cell Culture Techniques; Chemical and Drug Induced Liver Injury; Computational Biology; Gen

2019
Functional and toxicological consequences of metabolic bioactivation of methapyrilene via thiophene S-oxidation: Induction of cell defence, apoptosis and hepatic necrosis.
    Toxicology and applied pharmacology, 2009, Sep-15, Volume: 239, Issue:3

    Topics: Animals; Apoptosis; Blotting, Western; Cell Survival; Cells, Cultured; Chemical and Drug Induced Liv

2009
HPLC-MS/MS methods for the quantitative analysis of ophthalmic acid in rodent plasma and hepatic cell line culture medium.
    Journal of pharmaceutical and biomedical analysis, 2011, Apr-05, Volume: 54, Issue:5

    Topics: Animals; Biomarkers; Cell Line; Chemical and Drug Induced Liver Injury; Chromatography, High Pressur

2011
Advantages of glutamate dehydrogenase as a blood biomarker of acute hepatic injury in rats.
    Laboratory animals, 2002, Volume: 36, Issue:3

    Topics: Acute Disease; Alkaline Phosphatase; Animals; Aspartate Aminotransferases; Biomarkers; Chemical and

2002
Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat.
    Journal of proteome research, 2006, Volume: 5, Issue:7

    Topics: Animals; Chemical and Drug Induced Liver Injury; Dose-Response Relationship, Drug; Gene Expression R

2006
Gene expression profiling of methapyrilene-induced hepatotoxicity in rat.
    The Journal of toxicological sciences, 2008, Volume: 33, Issue:1

    Topics: Alanine Transaminase; Animals; Apoptosis; Aspartate Aminotransferases; Cell Cycle; Chemical and Drug

2008
Identification of the thiophene ring of methapyrilene as a novel bioactivation-dependent hepatic toxicophore.
    The Journal of pharmacology and experimental therapeutics, 2008, Volume: 326, Issue:2

    Topics: Animals; Cell Survival; Cells, Cultured; Chemical and Drug Induced Liver Injury; Chromatography, Hig

2008
Effects of induction and inhibition of cytochromes P450 on the hepatotoxicity of methapyrilene.
    Toxicological sciences : an official journal of the Society of Toxicology, 1998, Volume: 46, Issue:1

    Topics: Animals; Body Weight; Chemical and Drug Induced Liver Injury; Cytochrome P-450 Enzyme Inhibitors; Cy

1998
Effects of methapyrilene on rat hepatic xenobiotic metabolizing enzymes and liver morphology.
    Fundamental and applied toxicology : official journal of the Society of Toxicology, 1985, Volume: 5, Issue:1

    Topics: Alanine Transaminase; Aminopyridines; Animals; Bile Acids and Salts; Bile Ducts; Chemical and Drug I

1985