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furafylline  (Toronto Research Chemicals)


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    Structured Review

    Toronto Research Chemicals furafylline
    Furafylline, supplied by Toronto Research Chemicals, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/furafylline/Furafylline/pm38914316-49-98-106
    Average 92 stars, based on 1 article reviews
    furafylline - by Bioz Stars, 2026-10
    92/100 stars

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    Related Articles

    Incubation:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Blocking Assay:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Control:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Solvent:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Liquid Chromatography with Mass Spectroscopy:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Comparison:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Software:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Two Tailed Test:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Inhibition:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).

    Activity Assay:

    Article Title: Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib
    Article Snippet: Data were fit to the following equation using nonlinear regression analysis with GraphPad Prism 9.0 software to estimate the apparent K I and k inact .

    Article Title: Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions.
    Article Snippet: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor and has finished its phase II clinical trial.. The inhibition of six major cytochrome P450 enzymes (P450) (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six UDP-glucuronosyltransferases (UGT) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7) by vicagrel was evaluated using pooled human liver microsomes and specific probe substrates.. Physiology-based pharmacokinetic (PBPK) simulation was further applied to predict the in vivo drugdrug interaction (DDI) potential between vicagrel and bupropion as well as S-mephenytoin.

    Article Title: Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation
    Article Snippet: N -Desethylsunitinib (D289650), sunitinib- d 4 (S820003), and furafylline were purchased from Toronto Research Chemicals (Toronto, ON).

    Article Title: Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats.
    Article Snippet: Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity.. However, its metabolism and disposition are little known.. In this study, we investigated the metabolic characteristics of dendrobine in vitro and in rats.

    Article Title: Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol.
    Article Snippet: Furafylline, 2-phenyl-2-(1piperidinyl)propane, CYP3cide, and (1)-N-3-benzylnirvanol were purchased from Toronto Research Chemicals (Toronto, ON).



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    Chemie GmbH furafylline
    (a) Microsomal preparations of 21 heterologously expressed human CYP isoforms were incubated with 0.5 μM IMQ for 15 min at 37°C. IMQ content was determined by LC/MS. (ins. Ctrl = control insect cell preparation; n = 2). (b) Formation of monohydroxylated IMQ metabolites (RT = retention time) by four of the 21 heterologously expressed human CYP isoforms. (c) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Next, cells were treated with 0.5 μM IMQ alone and in combination with 5 μM 7-HF and 2 μM <t>furafylline</t> (Fura). After 6 hrs, monohydroxylated IMQ metabolites in the cell culture supernatants were determined by LC/MS (n = 3). (d) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Subseqeuntly, cells were treated with 1 μM granisetron alone and in combination with 5 μM 7-HF, 2 μM furafylline (Fura) and 0.5 μM IMQ. The amount of 7-hydroxylated granisetron in the cell culture supernatants was assessed after 6 hrs by LC/MS (n ≥ 4). (n.d. = not detectable; n.s. = not significant; * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.005).
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    (a) Microsomal preparations of 21 heterologously expressed human CYP isoforms were incubated with 0.5 μM IMQ for 15 min at 37°C. IMQ content was determined by LC/MS. (ins. Ctrl = control insect cell preparation; n = 2). (b) Formation of monohydroxylated IMQ metabolites (RT = retention time) by four of the 21 heterologously expressed human CYP isoforms. (c) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Next, cells were treated with 0.5 μM IMQ alone and in combination with 5 μM 7-HF and 2 μM furafylline (Fura). After 6 hrs, monohydroxylated IMQ metabolites in the cell culture supernatants were determined by LC/MS (n = 3). (d) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Subseqeuntly, cells were treated with 1 μM granisetron alone and in combination with 5 μM 7-HF, 2 μM furafylline (Fura) and 0.5 μM IMQ. The amount of 7-hydroxylated granisetron in the cell culture supernatants was assessed after 6 hrs by LC/MS (n ≥ 4). (n.d. = not detectable; n.s. = not significant; * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.005).

    Journal: Archives of toxicology

    Article Title: The Toll-like receptor agonist imiquimod is metabolized by aryl hydrocarbon receptor-regulated cytochrome P450 enzymes in human keratinocytes and mouse liver

    doi: 10.1007/s00204-019-02488-5

    Figure Lengend Snippet: (a) Microsomal preparations of 21 heterologously expressed human CYP isoforms were incubated with 0.5 μM IMQ for 15 min at 37°C. IMQ content was determined by LC/MS. (ins. Ctrl = control insect cell preparation; n = 2). (b) Formation of monohydroxylated IMQ metabolites (RT = retention time) by four of the 21 heterologously expressed human CYP isoforms. (c) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Next, cells were treated with 0.5 μM IMQ alone and in combination with 5 μM 7-HF and 2 μM furafylline (Fura). After 6 hrs, monohydroxylated IMQ metabolites in the cell culture supernatants were determined by LC/MS (n = 3). (d) HaCaT keratinocytes were pre-treated for 24 hrs with 0.5 μM BaP or solvent. Subseqeuntly, cells were treated with 1 μM granisetron alone and in combination with 5 μM 7-HF, 2 μM furafylline (Fura) and 0.5 μM IMQ. The amount of 7-hydroxylated granisetron in the cell culture supernatants was assessed after 6 hrs by LC/MS (n ≥ 4). (n.d. = not detectable; n.s. = not significant; * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.005).

    Article Snippet: Furafylline was obtained from Cayman Chemicals (Ann Arbor, MI, USA) and 7-ethoxyresorufin from Santa Cruz Biotechnology (Heidelberg, Germany).

    Techniques: Incubation, Liquid Chromatography with Mass Spectroscopy, Control, Solvent, Cell Culture