PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 10078840-6 1999 Furafylline, sulphaphenazole, omeprazole, quinidine and ketoconazole were identified as specific markers for the respective CYP1A2 (IC50 = 6 microM), CYP2C9 (0.7 microM), CYP2C19 (6 microM), CYP2D6 (0.02 microM) and CYP3A4 (0.2 microM) inhibition screens. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 124-130 9431831-7 1997 Ketoconazole, an inhibitor of CYP3A4, inhibited competitively CPHP formation (Ki=0.1 microM), whereas sulphaphenazole (CYP2C9), furafylline (CYP1A2) and quinidine (CYP2D6) gave only little inhibition (IC50 > 100 microM). furafylline 128-139 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 141-147 9884161-3 1998 Selective inhibitors-4-methylpyrazole (CYP2E1), furafylline (CYP1A2), and troleandomycin (CYP3A4)-also decreased microsomal ethanol oxidation in the livers of 18 organ donors. furafylline 48-59 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 61-67 9585555-0 1998 Mechanism-based inactivation of human cytochrome P450 1A2 by furafylline: detection of a 1:1 adduct to protein and evidence for the formation of a novel imidazomethide intermediate. furafylline 61-72 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 38-57 9491822-5 1998 RESULTS: Furafylline was a potent, selective inhibitor of phenacetin O-deethylation (CYP1A2-mediated) in human liver microsomes (IC50 = 0.48 microM), but inhibited both phenacetin O-deethylation and tolbutamide 4-hydroxylation (CYP2C9-mediated) at equimolar concentrations in rat liver microsomes (IC50 = 20.8 and 24.0 microM respectively). furafylline 9-20 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 85-91 9825830-7 1998 Sulphaphenazole (CYP2C9), furafylline (CYP1A2) and quinidine and paroxetine (CYP2D6) gave only little inhibition (IC50 > 60 microM). furafylline 26-37 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 39-45 9585555-1 1998 The rapid loss of human CYP1A2 (cytochrome P450 1A2) activity caused by the 8-methylxanthine furafylline is investigated with the aim of determining whether a stable covalent adduct of the xanthine to the enzyme could be identified. furafylline 93-104 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 24-30 9585555-1 1998 The rapid loss of human CYP1A2 (cytochrome P450 1A2) activity caused by the 8-methylxanthine furafylline is investigated with the aim of determining whether a stable covalent adduct of the xanthine to the enzyme could be identified. furafylline 93-104 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 32-51 9585555-9 1998 We conclude that oxidation of the 8-methyl group of furafylline and cyclohexylline, but not their N7-methyl analogues, by CYP1A2 promotes a major fraction of the inactivating xanthines to a two electron oxidized intermediate which either terminates enzyme activity by reaction with an active site amino acid or is decomposed by reaction with the medium to give carbinol. furafylline 52-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 122-128 9435160-8 1998 7,8-Benzoflavone (5 microM) and furafylline (20 microM), two inhibitors of CYP1A2, reduced the bisallylic hydroxylation activity of adult human liver microsomes. furafylline 32-43 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 75-81 9394024-5 1997 At 5 microM of lisofylline the CYP1A2 inhibitor, furafylline, inhibited pentoxifylline formation by 58.8%, and the nonspecific CYP2E1 inhibitor, diethyldithiocarbamate, inhibited pentoxifylline formation by 21.7%. furafylline 49-60 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 31-37 8825200-7 1996 In addition, the reaction was inhibited (36-75%, N = 11 different livers) by furafylline (FURA), a CYP1A2-selective mechanism-based inhibitor. furafylline 90-94 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 99-105 9202738-3 1997 Using a potent and selective inhibitor of human CYP1A2, furafylline, we have shown that N-hydroxylation catalysed by this enzyme is the major pathway of metabolism of MeIQx and PhIP and is solely responsible for their oxidation to mutagenic species. furafylline 56-67 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 48-54 21781720-3 1996 An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. furafylline 46-57 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 96-102 8786569-7 1996 The CYP1A2 inhibitors furafylline, ellipticine and alpha-naphthoflavone were potent inhibitors of both 1-MX and 3-MX formation with more that 80% of N-demethylase activities inhibited below a concentration of 5 microM. furafylline 22-33 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 4-10 8825200-7 1996 In addition, the reaction was inhibited (36-75%, N = 11 different livers) by furafylline (FURA), a CYP1A2-selective mechanism-based inhibitor. furafylline 77-88 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 99-105 9351903-8 1997 The reaction was inhibited in presence of the potent CYP1A2 inhibitors alpha-naphthoflavone (7, 8-benzoflavone) and furafylline. furafylline 116-127 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 53-59 8975785-4 1996 Furthermore, the portion of AFBO formed in HLMs which was eliminated by furafylline, a specific mechanism-based inhibitor of CYP1A2, also followed Michaelis-Menten kinetics (Km = 32-47 microM, Vmax = 0.36-0.69 nmol/min/nmol P450). furafylline 72-83 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 125-131 8975785-11 1996 AFB1-DNA binding in control HLMs (reflecting the contribution of CYP1A2 and CYP3A4) and furafylline-pretreated microsomes (reflecting the contribution of CYP3A4 only) catalyzed the binding of 1.71 and 0.085 pmol equivalents of AFB1 to DNA, respectively, indicating that CYP1A2 was responsible for 95% of AFB1-DNA adduct formation at 0.133 microM AFB. furafylline 88-99 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 270-276 8678801-5 1996 Studies in which furafylline, a potent and selective inhibitor of human CYP1A2, was administered before ingestion of beef revealed that more than 90% of MeIQx and 70% of PhIP are N-hydroxylated in vivo, probably pre-systemically in the liver. furafylline 17-28 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 72-78 7503788-4 1995 Oxidation of O6-benzylguanine also occurred with pooled human liver microsomes and was inhibited by both furafylline and troleandomycin, selective inhibitors of CYP1A2 and CYP3A4, respectively. furafylline 105-116 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 161-167 8558417-8 1996 In contrast, the conversion of m-xylene to 2,4-dimethylphenol followed single enzyme Michaelis-Menten kinetics, was inhibited selectively by furafylline, and correlated significantly with known CYP1A2 catalyzed reactions. furafylline 141-152 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 194-200 7720520-4 1995 Furafylline was a potent, mechanism-based inhibitor for CYP1A2-mediated phenacetin O-deethylation. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 56-62 8844804-6 1995 Both N-hydroxylation and mutagenicity of the amines can be almost completely inhibited by furafylline, a potent and highly selective inhibitor of CYP1A2 in man. furafylline 90-101 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 146-152 8844810-5 1995 Experiments with furafylline, a potent and selective inhibitor of human CYP1A2, reveal that more than 90% of MeIQx and 70% of PhIP are N-hydroxylated in vivo, probably presystemically in the liver. furafylline 17-28 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 72-78 35246464-5 2022 The current study also demonstrated that selective inhibition sufficient for fm calculation was achieved by inhibitors of CYP1A2 (20 microM furafylline), CYP2C8 (40 microM montelukast), CYP2C9 (40 microM sulfaphenazole), CYP2C19 (3 microM (-)N-3-benzyl-phenobarbital) and CYP2D6 (5 microM quinidine). furafylline 140-151 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 122-128 8261468-2 1994 The inhibitory potential of furafylline in vivo was first assessed by determining its effect on clearance of phenacetin to paracetamol by the model CYP1A2-dependent O-deethylation pathway. furafylline 28-39 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 148-154 8261468-3 1994 Furafylline inhibited this reaction by > 99% in all subjects, thus demonstrating its applicability to determining the contribution of CYP1A2 to a given reaction in vivo. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 137-143 35599345-5 2022 Selective CYP inhibitor studies showed FFA metabolism partially inhibited by quinidine (CYP2D6, 48%), phencyclidine (CYP2B6, 42%), and furafylline (CYP1A2, 32%) and, to a lesser extent (<15%), by tienilic acid (CYP2C9), esomeprazole (CYP2C19), and troleandomycin (CYP3A4/5). furafylline 135-146 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 148-154 8292742-0 1993 Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline. furafylline 77-88 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 54-73 1473228-11 1992 The specific inhibitor of human CYP1A2, furafylline (5 microM) inhibited the N-hydroxylation of MeIQx by > 90%. furafylline 40-51 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 32-38 30390556-1 2019 The present study reports the in vitro studies with furafylline and troleandomycin (TAO) as specific inhibitors of activities 7-methoxyresorufin-O-demethylase (MROD) and nifedipine oxidase, catalyzed by cytochrome P450 1 A2 (CYP1 A2) and 3A4 human enzymes, respectively, in hepatic microsomes of quail, duck, turkey and chicken. furafylline 52-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 203-223 30390556-1 2019 The present study reports the in vitro studies with furafylline and troleandomycin (TAO) as specific inhibitors of activities 7-methoxyresorufin-O-demethylase (MROD) and nifedipine oxidase, catalyzed by cytochrome P450 1 A2 (CYP1 A2) and 3A4 human enzymes, respectively, in hepatic microsomes of quail, duck, turkey and chicken. furafylline 52-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 225-232 26856397-4 2016 RESULTS: Furafylline (a CYP1A2 inhibitor), quinidine (a CYP2D6 inhibitor), and heat treatment (inactivates FMO3) suppressed liver microsomal metabolic clearance of olanzapine by approximately 30%. furafylline 9-20 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 24-30 29785610-7 2018 RESULTS: Dihydralazine and furafylline displayed irreversible MDI of CYP1A2. furafylline 27-38 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 69-75 16814747-5 2006 Metabolite peak areas were substantially and significantly reduced by the CYP1A2 inhibitor furafylline and to a lesser extent by the CYP2E1 inhibitor 4-methylpyrazole. furafylline 91-102 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 74-80 23898916-10 2013 Pretreatment of hepatocytes with furafylline, a selective inhibitor of cytochrome P450 1A2, resulted in a strong diminution of DNA adducts signifying that P450 1A2 is a major P450 isoform involved in bioactivation of these procarcinogens. furafylline 33-44 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 71-90 21755496-6 2011 Treatment of Huh7-1A2-I-E cells and the Huh7-E control cells with aflatoxin B1 showed that cells with CYP1A2 expression are much more sensitive to aflatoxin B1 and the cellular toxicity of aflatoxin B1 in Huh7-1A2-I-E cells could be prevented by furafylline, a CYP1A2 inhibitor. furafylline 246-257 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 102-108 19204080-10 2009 Experiments with P450-selective chemical inhibitors and monoclonal anti-P450 antibodies showed that furafylline, a mechanism-based inhibitor CYP1A2, and anti-CYP1A2 antibody markedly inhibited 6-MNA formation, whereas inhibitors for other P450s did not show significant inhibitory effects. furafylline 100-111 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 141-147 22266842-7 2012 Furafylline, quinidine, and ketoconazole, selective inhibitors of CYP1A2, CYP2D6, and CYP3A4, respectively, inhibited 5-hydroxylorcaserin (IC(50) = 1.914 muM), 7-hydroxylorcaserin (IC(50) = 0.213 muM), and 1-hydroxylorcaserin formation (IC(50) = 0.281 muM), respectively. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 66-72 23106957-9 2012 This seems to indicate important contributions of CYP1A1 and CYP3A7 as compared to CYP1A2 and CYP3A4, respectively, because furafylline and ketokonazole are stronger inhibitors of CYP1A2 and CYP3A4 than CYP1A1 and CYP3A7, respectively. furafylline 124-135 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 83-89 23106957-9 2012 This seems to indicate important contributions of CYP1A1 and CYP3A7 as compared to CYP1A2 and CYP3A4, respectively, because furafylline and ketokonazole are stronger inhibitors of CYP1A2 and CYP3A4 than CYP1A1 and CYP3A7, respectively. furafylline 124-135 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 180-186 21726170-10 2011 Similarly, alpha-naphthoflavone (CYP1A1 inhibitor) and furafylline (CYP1A2 inhibitor) significantly decreased the formation of 4"-OH-NBL. furafylline 55-66 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 68-74 21336516-7 2011 The most selective inhibitors available are furafylline (in co-incubation and pre-incubation conditions) for CYP1A2, 2-phenyl-2-(1-piperidinyl)propane (PPP) for CYP2B6, montelukast for CYP2C8, sulfaphenazole for CYP2C9, (-)-N-3-benzyl-phenobarbital for CYP2C19 and quinidine for CYP2D6. furafylline 44-55 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 109-115 17823234-4 2007 The human liver microsomal CYP1A2 inactivation kinetics of resveratrol, oltipraz, furafylline, and dihydralazine (Fig. furafylline 82-93 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 16771648-9 2006 The spheroids responded to the inducer beta-naphthoflavone and to the inhibitor furafylline of CYP1A2. furafylline 80-91 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 95-101 15649641-11 2005 Resveratrol and furafylline exhibited dose-dependent decreases in CYP1A1 and CYP1A2 enzyme activities with IC50 values of 1.89 and 0.79 microM, respectively. furafylline 16-27 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 77-83 15766918-9 2005 Inhibitory effects of furafylline, an inhibitor of human CYP1A2, on ER O-deethylation by recombinant CYP1A2 enzymes were much lower than those of alpha-naphthoflavone, but marmoset CYP1A2 was more sensitive to furafylline than Japanese monkey CYP1A2. furafylline 22-33 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 57-63 15766918-9 2005 Inhibitory effects of furafylline, an inhibitor of human CYP1A2, on ER O-deethylation by recombinant CYP1A2 enzymes were much lower than those of alpha-naphthoflavone, but marmoset CYP1A2 was more sensitive to furafylline than Japanese monkey CYP1A2. furafylline 22-33 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 101-107 15766918-9 2005 Inhibitory effects of furafylline, an inhibitor of human CYP1A2, on ER O-deethylation by recombinant CYP1A2 enzymes were much lower than those of alpha-naphthoflavone, but marmoset CYP1A2 was more sensitive to furafylline than Japanese monkey CYP1A2. furafylline 210-221 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 57-63 15766918-9 2005 Inhibitory effects of furafylline, an inhibitor of human CYP1A2, on ER O-deethylation by recombinant CYP1A2 enzymes were much lower than those of alpha-naphthoflavone, but marmoset CYP1A2 was more sensitive to furafylline than Japanese monkey CYP1A2. furafylline 210-221 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 101-107 12867277-8 2003 Furafylline, the CYP1A2-specific inhibitor, estrogen and monoclonal antibody raised against human CYP1A2 (MAB-1A2) substantially inhibited the formation rates of mono-hydroxylated metabolites. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 17-23 15276085-6 2004 Formation of these metabolites was markedly inhibited by alpha-naphthoflavone and furafylline, two inhibitors of CYP1A2. furafylline 82-93 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 113-119 15696928-7 2004 Furafylline, the CYP1A2 specific inhibitor, estrogen, and monoclonal antibody raised against human CYP1A2 (MAB-1A2) apparently inhibited the formation of mono-hydroxylated metabolites, The IC50 of Fur for the formation of 7,3",4"-THI, 6,7,4"-THI and 7,8,4"-THI was 1.0, 0.9 and 0. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 17-23 15696928-7 2004 Furafylline, the CYP1A2 specific inhibitor, estrogen, and monoclonal antibody raised against human CYP1A2 (MAB-1A2) apparently inhibited the formation of mono-hydroxylated metabolites, The IC50 of Fur for the formation of 7,3",4"-THI, 6,7,4"-THI and 7,8,4"-THI was 1.0, 0.9 and 0. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 99-105 15279827-7 2004 When CYP selective chemical inhibitors, such as furafylline for CYP1A2 and ketoconazole for CYP3A4, were added to the reaction mixture of norharman, aniline and human microsomes, formation of APNH was decreased to 14 and 16% of the control level, respectively. furafylline 48-59 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 64-70 15537169-6 2004 Furafylline (a selective inhibitor of CYP1A2) inhibited the M-2 formation in the PM microsomes by 57%. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 38-44 12867277-8 2003 Furafylline, the CYP1A2-specific inhibitor, estrogen and monoclonal antibody raised against human CYP1A2 (MAB-1A2) substantially inhibited the formation rates of mono-hydroxylated metabolites. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 98-104 12180536-4 2002 Furafylline (CYP1A2) and sulfaphenazole (CYP2C9) inhibited the N-demethylation to a lesser extent while quinidine (CYP2D6) or troleandomycine (CYP3A4) had no effect. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 13-19 12721102-14 2003 Furafylline (a CYP1A2 inhibitor) and ketoconazole (a CYP3A4 inhibitor) significantly decreased the rate of promazine 5-sulphoxidation, while furafylline and ticlopidine (a CYP2C19 inhibitor) significantly decreased the rate of promazine N-demethylation in human liver microsomes. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 15-21 12495659-8 2003 After induction with 1,2-benzanthracene, the CYP1A1 selective inhibitor, alpha-naphthoflavone, and the CYP1A2 selective inhibitor, furafylline, effectively inhibited enzyme activities with IC(50)s of 2.4 microM and 12.8 microM, respectively, in microsomes from both trophoblasts culture systems. furafylline 131-142 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 103-109 12569440-5 2003 IC(50) values of 3.2, 1.4, 8.9, 0.2, and 0.3 microM were obtained for the standard isozyme inhibitors CYP1A2/furafylline, CYP2C9/sulfaphenazole, CYP2C19/tranylcypromine, CYP2D6/quinidine, and CYP3A4/ketoconazole, respectively, which were in good agreement with literature values. furafylline 109-120 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 102-108 12523495-8 2002 The obtained results suggest a strong inhibitory effect of perazine on human CYP1A2 activity with predicted Ki value similar to those of the known for CYP1A2 inhibitors, such as furafylline and fluvoxamine. furafylline 178-189 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 77-83 11744615-6 2002 alpha-Naphthoflavone and furafylline, which both inhibit CYP1A2, significantly inhibited the formation of JANEX-1-M in human liver microsomes. furafylline 25-36 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 57-63 15618695-6 2002 Furafylline and erythromycin, both mechanism based inhibitors, strongly inhibited CYP1A2 and CYP3A4 activity, respectively and their inhibitory effects increased depending on the preincubation time. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 82-88 11231111-6 2001 The inhibition potential of CYP1A2 has been evaluated using its selective inhibitors, alpha-naphthoflavone and furafylline. furafylline 111-122 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 28-34 11315102-15 2000 Among various CYP inhibitors tested here, 7,8-benzoflavone and furafylline, typical human CYP1A2 inhibitors, inhibited the microsomal p-hydroxylation of o-phenylphenol in human livers most potently by 70 and 50% respectively. furafylline 63-74 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 90-96 11095582-6 2000 The involvement of CYP1A2 in DMXAA metabolism by human livers was demonstrated by the following: 1) the potent inhibition of DMXAA metabolism by furafylline (k(inact) = 0.23 +/- 0.04 min(-1), K"(app) = 15.6 +/- 6.7 microM) and alpha-naphthoflavone (K(i) = 0.036 microM), but not by cimetidine, ketoconazole, tolbutamide, quinidine, chlorzoxazone, diethyldithiocarbamate, troleandomycin, and sulfaphenazole; 2) when incubated with human lymphoblastoid cell microsomes containing cDNA-expressed CYP isoenzymes, DMXAA was metabolized only by CYP1A2, with an apparent K(m) of 6.2 +/- 1.5 microM and V(max) of 0.014 +/- 0.001 nmol/min/mg, but not by CYP2A6, CYP2B6, CYP2C9 (Arg(144)), CYP2C19, CYP2D6 (Val(374)), CYP2E1, and CYP3A4; 3) a significant correlation (r = 0.90; P <.001) between 6-methylhydroxylation of DMXAA and 7-ethoxyresorufin O-deethylation; and 4) a significant correlation (r = 0.75; P <.01) between the CYP1A protein level determined by Western blots and DMXAA 6-methylhydroxylation. furafylline 145-156 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 19-25 11095582-6 2000 The involvement of CYP1A2 in DMXAA metabolism by human livers was demonstrated by the following: 1) the potent inhibition of DMXAA metabolism by furafylline (k(inact) = 0.23 +/- 0.04 min(-1), K"(app) = 15.6 +/- 6.7 microM) and alpha-naphthoflavone (K(i) = 0.036 microM), but not by cimetidine, ketoconazole, tolbutamide, quinidine, chlorzoxazone, diethyldithiocarbamate, troleandomycin, and sulfaphenazole; 2) when incubated with human lymphoblastoid cell microsomes containing cDNA-expressed CYP isoenzymes, DMXAA was metabolized only by CYP1A2, with an apparent K(m) of 6.2 +/- 1.5 microM and V(max) of 0.014 +/- 0.001 nmol/min/mg, but not by CYP2A6, CYP2B6, CYP2C9 (Arg(144)), CYP2C19, CYP2D6 (Val(374)), CYP2E1, and CYP3A4; 3) a significant correlation (r = 0.90; P <.001) between 6-methylhydroxylation of DMXAA and 7-ethoxyresorufin O-deethylation; and 4) a significant correlation (r = 0.75; P <.01) between the CYP1A protein level determined by Western blots and DMXAA 6-methylhydroxylation. furafylline 145-156 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 539-545 11315104-13 2000 The metabolism of 20 microM BFC in human liver microsomes was inhibited to 37-48% of control by 5-100 microM of the mechanism-based CYP1A2 inhibitor furafylline and to 64-69% of control by 5-100 microM of the mechanism-based CYP3A4 inhibitor troleandomycin. furafylline 149-160 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 132-138 10460803-9 1999 Dihydrodiol formation was inhibited by the CYP1A2 inhibitor furafylline. furafylline 60-71 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 43-49 10992045-5 2000 Using methylcholanthrene, CYP1A2 can be induced dramatically, and it is inhibited by furafylline, a mechanism-based inhibitor of this enzyme. furafylline 85-96 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 26-32 10727902-6 2000 The reduced metabolite of 1-nitropyrene, 1-aminopyrene, was also shown to be activated to a mutagenic metabolite by CYP1A2, using 3T3-1A2 cells in combination with a shuttle vector, and the Amestest in combination with the specific CYP1A2 inhibitor furafylline. furafylline 249-260 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 116-122 11790342-5 2000 The mammalian CYP1A2 inhibitor furafylline (50 microM-1 mM) reduced activity in the EROD, caffeine and POD assays to 65, 21 and 20% of control values in flounders and to 85, 10 and 5% of control values in eels, respectively. furafylline 31-42 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 14-20 10215755-5 1999 RESULTS: The CYP1A2 inhibitor furafylline variably inhibited (0-65%) 7-MX formation, but had no effect on other pathways. furafylline 30-41 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 13-19 10418968-11 1999 Furafylline, sulfaphenazole, quinidine, and ketoconazole were found to be specific inhibitors of CYP1A2, CYP2C9, CYP2D6, and CYP3A4, respectively. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 97-103 10553725-5 1999 Furafylline, a selective inhibitor of CYP1A2, almost completely abolished the hepatocellular metabolism of zolmitriptan and markedly inhibited formation of the N-desmethyl metabolite in microsomes. furafylline 0-11 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 38-44 10359460-5 1999 Troleandomycin (CYP3A inhibitor) and furafylline (CYP1A2 inhibitor) inhibited CLZ N-oxidation in human liver microsomes by 23.2+/-12.1% and 7.8+4.3%, respectively, whereas CLZ N-demethylation was inhibited by 17.5+/-13.9% and 25.6+/-16.5%, respectively. furafylline 37-48 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 50-56