PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 12959268-10 1993 Formation of 5-O-desmethylomeprazole was inhibited by both R, S-mephenytoin and quinidine, indicating that both S-mephenytoin hydroxylase and CYP2D6 may mediate this reaction in human liver microsomes and in vivo. Quinidine 80-89 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 142-148 8013282-3 1994 The cytochrome P-450 (CYP) 2D6 inhibitor quinidine (1 microM) reduced the hydroxylation of tropisetron (67%) and ondansetron (18%). Quinidine 41-50 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-30 8242617-12 1993 By contrast, the CYP2D6-selective inhibitor quinidine did not affect either microsomal activity, while anti-CYP2A antibodies had only a modest inhibitory effect. Quinidine 44-53 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 17-23 8272795-3 1993 The influence of naloxone and quinidine (a selective P450DB1 or CAP2D6 inhibitor) on tramadol effect was investigated crossover and double-blind vs placebo in healthy subjects. Quinidine 30-39 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 53-60 8272795-13 1993 Quinidine blockade of tramadol myosis suggests that the mu agonist component of tramadol effect results from its O-demethylation by the polymorphic P450DB1 enzyme. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 148-155 7693389-7 1993 However, over the first hour after dosing, the extensive metabolizers reported more "good opiate effects" and fewer "bad opiate effects" than poor metabolizers and extensive metabolizers in whom CYP2D6 was inhibited by quinidine. Quinidine 219-228 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 195-201 8272570-6 1993 Prior administration of quinidine produced a large reduction in the metabolic oxidation of trimipramine with CYP2D6 while prior administration of quinine had no effect. Quinidine 24-33 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 109-115 8323546-4 1993 Quinidine, a selective inhibitor of CYP2D6, suppressed the ring-hydroxylase activities of CZ and FZ. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 36-42 8371133-6 1993 As reported previously, RS-mexiletine disposition was altered by a genetically determined (PM) or drug-induced (quinidine) decrease in CYP2D6 activity. Quinidine 112-121 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 135-141 2312782-1 1990 Quinidine has been reported to be a potent inhibitor of a specific isozyme of cytochrome P-450 (P-450db 1) that is responsible for the metabolism of a select group of drugs. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-105 8100167-0 1993 Quinidine inhibition of debrisoquine S(+)-4- and 7-hydroxylations in Chinese of different CYP2D6 genotypes. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 90-96 8100167-5 1993 The inhibition of CYP2D6 by quinidine was also investigated. Quinidine 28-37 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 18-24 8100167-12 1993 This study shows that the cytochrome P450 catalysing the 4- and 7-hydroxylations of debrisoquine in Chinese EM has the same properties (product stereoselectivity and inhibition by quinidine) as the CYP2D6 in Caucasian EM. Quinidine 180-189 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 198-204 8485585-7 1993 h2D6v2 microsomes were capable of metabolizing NNK and NNK metabolism and mutagenicity were markedly inhibited by the addition of quinidine, a CYP2D6 inhibitor. Quinidine 130-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 143-149 8276051-5 1993 The enzyme catalysing bupranolol metabolism was CYP2D6: microsomes from a liver with the genetic enzyme deficiency did not metabolize bupranolol; in microsomes from livers containing the enzyme and 10 microM bupranolol, 5 microM quinidine caused a 72% inhibition of bupranolol metabolism. Quinidine 229-238 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 48-54 1623898-1 1992 We have studied the hypoalgesic effect of codeine (100 mg) after blocking the hepatic O-demethylation of codeine to morphine via the sparteine oxygenase (CYP2D6) by quinidine (200 mg). Quinidine 165-174 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 154-160 1761076-0 1991 Quinidine but not quinine inhibits in man the oxidative metabolic routes of methoxyphenamine which involve debrisoquine 4-hydroxylase. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-133 1761076-3 1991 The oxidative routes of methoxyphenamine metabolisms which had been previously shown to involve debrisoquine 4-hydroxylase, namely O-demethylation and 5-hydroxylation were both significantly inhibited by quinidine in the 12 extensive metabolizers. Quinidine 204-213 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-122 7835228-7 1994 MP metabolism studies were also conducted with CYP2D6 microsomes in the presence of quinidine and quinine. Quinidine 84-93 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 47-53 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). Quinidine 77-86 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 2775304-0 1989 The specificity of inhibition of debrisoquine 4-hydroxylase activity by quinidine and quinine in the rat is the inverse of that in man. Quinidine 72-81 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-59 2775304-1 1989 The kinetics of inhibition of debrisoquine 4-hydroxylase activity by quinidine and quinine in rat and human liver microsomes have been compared. Quinidine 69-78 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 30-56 2775304-2 1989 Quinidine is a potent inhibitor of debrisoquine 4-hydroxylase activity of human liver (IC50: 3.6 microM). Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 35-61 2775304-7 1989 Inhibition of debrisoquine 4-hydroxylase activity by both quinine and quinidine in human and rat liver is competitive. Quinidine 70-79 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-40 2775304-10 1989 Although both quinidine and quinine are competitive inhibitors of debrisoquine 4-hydroxylase activity in rat and man, their potency is reversed. Quinidine 14-23 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 66-92 32198085-10 2020 Quinidine, a competitive CYP2D6 inhibitor, demonstrated protection on enzymes against the NOT-induced inactivation, but such protection was not found in incubation systems fortified with glutathione or catalase/superoxide dismutase. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 25-31 33641805-7 2021 In canine and feline microsomes, the formation rate of demethyl-cimicoxib, a phase 1 metabolite, was decreased in presence of quinidine, a specific human cytochrome P450 (CYP)2D6 inhibitor. Quinidine 126-135 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 154-178 29773554-8 2018 Quinidine as a competitive inhibitor of CYP2D6 slowed down the inactivation by NC. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 40-46 31925778-7 2020 The model was further challenged with simulations of oxycodone DDI with CYP3A4 inhibitors ketoconazole and itraconazole, CYP3A4 inducer rifampicin and CYP2D6 inhibitor quinidine. Quinidine 168-177 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 31113867-5 2019 Our results reveal that activity and respiration in mouse brain mitochondrial complex I are significantly affected by these toxins in WT mice but remain unchanged in Cyp2d6 locus knockout mice, indicating a possible role of CYP2D6 in the metabolism of these compounds both in vivo and in vitro These metabolic effects were minimized in the presence of two CYP2D6 inhibitors, quinidine and ajmalicine. Quinidine 375-384 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 224-230 30058787-4 2018 The cytochrome P450 (human hepatic cytochrome [CYP]) 2D6 inhibitor quinidine reduced in vitro hydroxylation of ondansetron, which indicates the important role of CYP2D6 in ondansetron metabolism. Quinidine 67-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 162-168 31730751-9 2019 The use of potent pan-CYP4 inhibitor HET0016, the specific CYP2D6 inhibitor quinidine, or both confirmed major contributions of CYP4- and CYP2D6-mediated metabolism in the microsomal disappearance of BACs. Quinidine 76-85 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 59-65 30368994-8 2019 Quinidine, a competitive inhibitor of CYP2D6, attenuated the CHE-mediated enzyme inactivation, while glutathione and catalase/superoxide dismutase did not markedly ameliorate the inhibitory effect. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 38-44 26325084-9 2015 Quinidine, a known inhibitor of CYP2D6, was used as a reference. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 32-38 27756789-6 2017 Coincubation with quinidine, a CYP2D6 inhibitor, ablated endoxifen generation by hCYP2D6 MLMs. Quinidine 18-27 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 31-37 27756789-6 2017 Coincubation with quinidine, a CYP2D6 inhibitor, ablated endoxifen generation by hCYP2D6 MLMs. Quinidine 18-27 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 81-88 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%. Quinidine 43-52 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 56-62 25417051-7 2016 All MDD showed inhibition against CYP2D6 activity and most of them in the range of the clinically relevant CYP2D6 inhibitors quinidine and fluoxetine. Quinidine 125-134 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 34-40 25417051-7 2016 All MDD showed inhibition against CYP2D6 activity and most of them in the range of the clinically relevant CYP2D6 inhibitors quinidine and fluoxetine. Quinidine 125-134 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-113 28478356-3 2017 METHODS: The current study is a phase IIa open label clinical trial examining the efficacy and tolerability of a combination of dextromethorphan (DM) and the CYP2D6 enzyme inhibitor quinidine (Q) in patients with TRD. Quinidine 182-191 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 158-164 28520381-5 2012 In addition, a number of drugs inhibit CYP2D6 activity, such as quinidine, fluoxetine, paroxetine, and propafenone. Quinidine 64-73 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 26452722-11 2016 Similarly, quinidine-mediated CYP2D6 inhibition reduced clearance of dextromethorphan and desipramine by 71 and 22%, respectively. Quinidine 11-20 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 30-36 26325084-12 2015 Inhibition of CYP2D6 enzyme with Quinidine increased in a linear dose-related fashion from -7.07% at 2.06 nM to 84.05% at 500 nM. Quinidine 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 24166670-6 2013 RESULTS: From the reaction phenotyping studies, it was shown that the metabolism of BI 11634 in HLM was inhibited by ketoconazole and quinidine, well-accepted specific inhibitors of CYP3A4 and CYP2D6, respectively. Quinidine 134-143 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 193-199 25719307-3 2015 The phenomenon of phenocopy with regard to CYP2D6 was first described when Danish patients changed phenotype from extensive to poor metabolizers during treatment with quinidine. Quinidine 167-176 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 43-49 25619394-7 2015 The metabolism of TEST and DEM in HepG2 cells was dose-dependently inhibited by the specific CYP3A4 inhibitor ketoconazole and CYP2D6 inhibitor quinidine. Quinidine 144-153 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 127-133 25475885-8 2015 Mirtazapine clearance in pooled human liver microsomes was inhibited by quinidine (a CYP2D6 inhibitor), ketoconazole (a CYP3A inhibitor), and in combination with risperidone and duloxetine, possible coadministered medicines. Quinidine 72-81 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 85-91 25222611-6 2014 The inhibition effect of quinidine on CYP2D6 catalyze-cycle was also investigated. Quinidine 25-34 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 38-44 27957038-0 2014 Cytochrome P450-2D6 Genotype Definition May Improve Therapy for Paroxysmal Atrial Fibrillation A Case of Syncope Following "Pill-in-the-Pocket" Quinidine plus Propafenone. Quinidine 144-153 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-19 23258538-8 2013 These studies show for the first time that dopaminergic neurons expressing mitochondrial CYP2D6 are fully capable of activating the pro-neurotoxin MPTP and inducing neuronal damage, which is effectively prevented by the CYP2D6 inhibitor quinidine. Quinidine 237-246 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 89-95 23258538-8 2013 These studies show for the first time that dopaminergic neurons expressing mitochondrial CYP2D6 are fully capable of activating the pro-neurotoxin MPTP and inducing neuronal damage, which is effectively prevented by the CYP2D6 inhibitor quinidine. Quinidine 237-246 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 220-226 24166670-12 2013 The specificity of quinidine as a CYP2D6 inhibitor is questionable as it can also significantly inhibit CYP3A4-mediated metabolism of some compounds. Quinidine 19-28 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 34-40 22459173-0 2012 Binding of quinidine radically increases the stability and decreases the flexibility of the cytochrome P450 2D6 active site. Quinidine 11-20 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 92-111 22688609-8 2012 Inhibition of CYP2D6 (by quinidine) reduced formation of 7-hydroxy-N-desalkylquetiapine by 81%, whereas the CYP3A4 inhibitor ketoconazole inhibited formation of N-desalkylquetiapine sulfoxide and M3 by 65 and 34%, respectively. Quinidine 25-34 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 22459173-5 2012 While the unliganded CYP2D6 is compressible, quinidine binding significantly rigidifies the CYP2D6 active site. Quinidine 45-54 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 92-98 23340533-7 2013 RESULTS: Quinidine was effective in inhibiting CYP2D6 activity, with 2-fold reduction of DM to DOR biotransformation clearance, prolonged DM half-life, and increased DM systemic availability. Quinidine 9-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 47-53 23340533-11 2013 CONCLUSION: CYP2D6 inhibition by quinidine influenced the pre-emptive analgesic effectiveness of DM confirming that CYP2D6 phenotypic switch increases the neuromodulatory effect of oral dextromethorphan. Quinidine 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 12-18 22459173-2 2012 Here, we present a combined experimental and computational study on the compressibility and flexibility of unliganded and quinidine-bound CYP2D6. Quinidine 122-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 22459173-4 2012 We identified sharp differences between ligand-free and quinidine-bound CYP2D6 forms in compressibility, flexibility parameters and active site solvation. Quinidine 56-65 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 72-78 21842479-2 2012 Recombinant human CYP3A4 and CYP2D6 enzymes were used and the activities were expressed by the metabolism of testosterone and dextromethorphan with ketoconazole and quinidine as positive inhibitor controls, respectively. Quinidine 165-174 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 29-35 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. Quinidine 13-22 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 74-80 21508180-4 2012 Throughout the study (follow-up, 199 +- 155 days), quinidine successfully inhibited CYP2D6: propafenone concentrations were 3 times higher in patients receiving quinidine (1033 +- 611 ng/mL vs 328 +- 229 ng/mL; P < .001). Quinidine 51-60 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 84-90 21508180-7 2012 Thus, chronic inhibition of CYP2D6 is achievable with low-dose quinidine in humans. Quinidine 63-72 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 28-34 22675558-8 2012 Moreover, quinidine, a potent inhibitor of human CYP2D6, only inhibited the bufuralol 1"-hydroxylation activity of CYP2D49 to a negligible degree. Quinidine 10-19 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 21976621-11 2012 Finally, the magnitude of in vivo CYP2D6 DDIs caused by quinidine was predicted using desipramine, dextromethorphan, and metoprolol. Quinidine 56-65 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 34-40 20388857-6 2010 MDMA metabolism by CYP2D6 significantly increased cytotoxicity, which was counteracted by CYP2D6 inhibition by quinidine. Quinidine 111-120 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 19-25 21679153-6 2011 Tyramine elimination rates were inhibited by quinidine and significantly correlated with bufuralol 1"-hydroxylation activities (a CYP2D6 marker). Quinidine 45-54 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 130-136 21722088-10 2011 Impurities with potent CYP2D6 inhibition, such as quinidine, can significantly decrease the apparent IC(50) value for the mixture. Quinidine 50-59 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 23-29 20388857-6 2010 MDMA metabolism by CYP2D6 significantly increased cytotoxicity, which was counteracted by CYP2D6 inhibition by quinidine. Quinidine 111-120 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 90-96 20590587-11 2010 Blocking CYP2D6 (with quinidine) reduced oxymorphone and noroxymorphone C(max) by 40% and 80%, and increased noroxycodone AUC(infinity) by 70%. Quinidine 22-31 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 9-15 20373255-3 2010 AVP-923 consists of a combination of the NMDA antagonist/sigma1 receptor agonist dextromethorphan hydrobromide (DM) and the cytochrome P450 2D6 (CYP2D6) enzyme inhibitor quinidine sulfate (Q). Quinidine 170-187 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 145-151 20345925-6 2010 CYP2D6 metabolized 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin and the CYP2D6-specific inhibitor quinidine (1 microM) blocked 96 +/- 1% of this metabolism, indicating that CYP2D6 is functional in this cell line. Quinidine 122-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 20345925-6 2010 CYP2D6 metabolized 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin and the CYP2D6-specific inhibitor quinidine (1 microM) blocked 96 +/- 1% of this metabolism, indicating that CYP2D6 is functional in this cell line. Quinidine 122-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-102 20345925-6 2010 CYP2D6 metabolized 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin and the CYP2D6-specific inhibitor quinidine (1 microM) blocked 96 +/- 1% of this metabolism, indicating that CYP2D6 is functional in this cell line. Quinidine 122-131 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-102 20345925-7 2010 Treatment of cells with CYP2D6 inhibitors (quinidine, propanolol, metoprolol or timolol) at varying concentrations significantly increased the neurotoxicity caused by 1-methyl-4-phenylpyridinium (MPP+) at 10 and 25 microM by between 9 +/- 1 and 22 +/- 5% (P < 0.01). Quinidine 43-52 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 24-30 19230594-5 2008 The formation of AS2036313-00, and YM-394111 or YM-394112 was inhibited by quinidine and ketoconazole with Ki values of 140 and 0.24 microM, respectively, which indicates that YM758 metabolism may be affected by coadministration of strong CYP2D6 and 3A4 inhibitors in vivo, given the clinical plasma concentrations of quinidine and ketoconazole. Quinidine 75-84 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 239-245 19444798-7 2009 The method has been successfully applied for the in vitro inhibition of metabolism of dextromethorphan by CYP2D6 and CYP3A4 using known inhibitors of CYPs such as quinidine and verapamil. Quinidine 163-172 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 106-112 19428327-6 2009 In addition, inhibition studies towards MBDB biotransformation using the CYP2D6 selective inhibitor quinidine confirmed the dominant role of this polymorphic isozyme in total MBDB metabolism. Quinidine 100-109 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 73-79 18938231-6 2008 For comparison, the K(i) values for quinidine and fluoxetine were 0.0092 and 8.2microM using recombinant CYP2D6 and 0.019 and 0.93microM using HLM. Quinidine 36-45 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 105-111 19000552-2 2008 The pharmacokinetics of pactimibe and its pharmacologically inactive plasma metabolite, R-125528, of which the main clearance pathway is CYP2D6, was affected by coadministration of quinidine. Quinidine 181-190 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 137-143 20041473-2 2010 This study examined whether pharmacological inhibition of CYP2D6 activity with quinidine would mimic the genetic mutation and thus also alter the psychoactive effects of DM. Quinidine 79-88 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 58-64 18026129-7 2008 This work has led directly to the successful design of CYP2D6 mutants with novel activity-including creating a testosterone hydroxylase, converting quinidine from inhibitor to substrate, creating a diclofenac hydroxylase and creating a dextromethorphan O-demethylase. Quinidine 148-157 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-61 18448569-11 2008 Moreover, the f(m CYP2D6) of R-125528 estimated to be almost 1 would well explain the accumulation of R-125528 observed with the quinidine treatment. Quinidine 129-138 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 18-24 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 237-246 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 237-246 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 237-246 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 407-416 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 407-416 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 18238857-8 2008 In contrast to CYP3A4-dependent bioactivation of trazodone itself, formation of M4 was mediated specifically by CYP2D6, as evidenced by cDNA-expressed CYP2D6-catalyzing formation of M4 from m-CPP, strong inhibition of formation of M4 by quinidine, a specific CYP2D6 inhibitor, in both incubations of trazodone and m-CPP with human liver microsomes, and concentration-dependent inhibition of M4 formation by quinidine. Quinidine 407-416 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 18356267-2 2008 Significant differences in IC(50,u) values between enzyme sources were observed for quinidine (0.02 microM in recombinant CYP2D6 versus 0.5 microM in hepatocytes) and propafenone (0.02 versus 4.1 microM). Quinidine 84-93 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 122-128 18346782-1 2008 3D-models were created and refined for CYP2D6 and for its complexes with ajmalicine and quinidine. Quinidine 88-97 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 78-87 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 190-196 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 78-87 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 250-256 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 78-87 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 250-256 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 265-274 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 190-196 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 265-274 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 250-256 18346782-3 2008 The results suggested that the experimental binding values of ajmalicine- and quinidine-like inhibitors better fit with the energetic terms derived from their interaction with structures of CYP2D6 obtained by, respectively, optimizing the ajmalicine/CYP2D6 and the quinidine/CYP2D6 complexes, rather than exploiting the 3D-strucure of the enzyme not subjected to a ligand-induced conformational change. Quinidine 265-274 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 250-256 17431033-8 2007 The CYP2D6 inhibitor quinidine proved a potent competitive inhibitor of timolol metabolism, with an in vitro K(i) value of 0.08 microM. Quinidine 21-30 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 17962373-5 2008 At 1 microM MPBP, the chemical inhibitors quinidine (CYP2D6), fluconazole (CYP2C19), and alpha-naphthoflavone (CYP1A2) reduced metabolite formation in pooled HLM by 83, 53, and 47%, respectively, and at 50 microM MPBP by 41, 47, and 45%, respectively. Quinidine 42-51 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 53-59 18974610-6 2008 In addition, the method was applied to the CYP2D6-mediated desipramine-quinidine interaction: the predicted 6.4-fold increase of desipramine AUC by quinidine was consistent with the observed 6.7-fold increase of AUC in the clinical drug-drug interaction study. Quinidine 71-80 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 43-49 18974610-6 2008 In addition, the method was applied to the CYP2D6-mediated desipramine-quinidine interaction: the predicted 6.4-fold increase of desipramine AUC by quinidine was consistent with the observed 6.7-fold increase of AUC in the clinical drug-drug interaction study. Quinidine 148-157 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 43-49 18445989-9 2008 Quinidine (1 microM) completely inhibited the metabolism of enclomiphene by all the EM livers and by recombinant CYP2D6 (p<0.001, one way ANOVA). Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 113-119 17881661-4 2007 Its formation was inhibited in human microsomes only by quinidine, a CYP2D6 inhibitor. Quinidine 56-65 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 69-75 16763018-2 2006 The reliability of the selective CYP2D6 inhibitor quinidine was evaluated in a retrospective analysis using a standardized approach that avoids laboratory-to-laboratory variation. Quinidine 50-59 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-39 17409567-4 2007 Quinidine, a CYP2D6 selective inhibitor, was applied to investigate its effect on biotransformation. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 13-19 17409567-5 2007 The concentration of quinidine was 4-folds higher than that of dextromethorphan and the yield of dextrorphan was reduced by 84%, which proved there was drug metabolism enzyme similar to CYP2D6 in C. blakesleeana AS 3.153. Quinidine 21-30 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 186-192 17484519-4 2007 The formation of fluvoxamino alcohol from fluvoxamine in pooled human liver microsomes was significantly inhibited by quinidine, a relatively specific CYP2D6 inhibitor, with a Ki value of 2.2 microM, whereas other several relatively specific CYP inhibitors did not inhibit the formation of fluvoxamino alcohol. Quinidine 118-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 17364883-12 2007 After the treatment with quinidine, a specific inhibitor of human CYP2D6, the area under the curve (AUC) of a CYP2D6 metabolite, 4"-hydroxydebrisoquin, was significantly decreased in the chimeric mice but not in the control mice. Quinidine 25-34 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 66-72 17364883-12 2007 After the treatment with quinidine, a specific inhibitor of human CYP2D6, the area under the curve (AUC) of a CYP2D6 metabolite, 4"-hydroxydebrisoquin, was significantly decreased in the chimeric mice but not in the control mice. Quinidine 25-34 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 110-116 16763018-6 2006 An estimate of the fraction metabolized by CYP2D6 in microsomes was derived from the rate constant determined with and without 1 microM quinidine for 11 substrates. Quinidine 136-145 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 43-49 16595712-9 2006 Quinidine and ketoconazole, potent inhibitors to CYP2D6 and CYP3A4, respectively, did not show strong inhibition toward Cyp2d22-mediated dextromethorphan O- or N-demethylation. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 16162505-0 2005 Why is quinidine an inhibitor of cytochrome P450 2D6? Quinidine 7-16 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-52 16472104-8 2006 However, after co-administration of drugs such as quinidine, propafenone and thioridazine (potent inhibitors of CYP2D6), the NE-100 AUC(oral) ratios predicted from the dispersion model was much greater than those from well-stirred model. Quinidine 50-59 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 16162505-7 2005 We have now examined the effect of mutations of these residues on interactions of the enzyme with the prototypical CYP2D6 inhibitor, quinidine. Quinidine 133-142 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 115-121 15619261-2 2005 Quinidine (a specific inhibitor of CYP2D6) did not markedly affect the metabolism of perospirone, whereas quercetin (an inhibitor of CYP2C8) and ketoconazole (an inhibitor of CYP3A4) caused a decrease in the metabolism with human liver microsomes in a concentration dependent fashion. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 35-41 16192109-3 2005 The contributions of CYP2D6 to the primary metabolisms of the substrates were estimated from the quinidine-mediated inhibition of their depletion rate constants in human hepatocytes and liver microsomes. Quinidine 97-106 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 21-27 16019948-7 2005 The CYP2D6-specific chemical inhibitor quinidine (3 microM) significantly (p<0.001) inhibited di-HO-PPP formation by 75.8%+/-1.7% (mean+/-standard error of the mean) in incubation mixtures with HLM and 2 microM MDPPP. Quinidine 39-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 15183128-9 2004 A known inhibitor of CYP2D6, quinidine, effectively inhibited the BF 1"-hydroxylation activities in liver microsomal fractions prepared from KYU- and KAU-marmosets. Quinidine 29-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 21-27 15507542-6 2005 This catalytic activity was >95% inhibited by quinidine, a CYP2D6 inhibitor. Quinidine 49-58 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 15342614-2 2004 To find out whether quinidine (Q), a CYP2D6 inhibitor, could elevate and prolong DM plasma profiles, 2 multiple-dose studies identified the lowest oral dose of Q that could be used in a fixed combination with 3 doses of DM. Quinidine 20-29 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 37-43 15537169-4 2004 Quinidine (a selective inhibitor of CYP2D6) inhibited the O-demethylation of DMAE in pooled human microsomes by 86%, while selective inhibitors for other forms of CYP did not show any appreciable effect. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 36-42 16680870-8 2004 Preincubation of human liver microsomes with cimetidine and NADPH did not increase the inhibitory potency of cimetidine; however, preincubation with recombinant CYP2D6 resulted in enzyme inactivation that could be attenuated by the CYP2D6 inhibitor quinidine. Quinidine 249-258 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 161-167 15039299-9 2004 Quinidine inhibition showed that CYP2D6 is the high affinity enzyme for O-demethylation with a mean K(m) of 130 +/- 33 microM and a V(max) that ranged from 89 to 356 pmol/mg/min. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-39 14998425-9 2004 Hydromorphone formation was inhibited by quinidine (a selective inhibitor of CYP2D6 activity), and monoclonal antibodies specific to CYP2D6. Quinidine 41-50 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 77-83 14563706-4 2004 In rat brain microsomes, these activities were not inhibited by anti-P450c21 antibodies, but they were effectively inhibited by the CYP2D-specific chemical inhibitor quinidine and by anti-CYP2D4 antibodies. Quinidine 166-175 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 132-137 14555336-11 2003 The CYP2D6 specific chemical inhibitor quinidine (3 microM) significantly (p<0.0001) inhibited HO-PPP formation by 91.8 +/- 0.5% (mean +/- SEM) in incubation mixtures with HLM and 2 microM MOPPP. Quinidine 39-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 14985146-11 2004 The CYP2D6-specific chemical inhibitor quinidine (1 and 3 microM) significantly inhibited 4-HO-PP formation by 71.9 +/- 4.8% and by 98.5% +/- 0.5%, respectively, in incubation mixtures with pHLM and 200 microM MeOPP. Quinidine 39-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 12695349-1 2003 The effects of microsomal concentration on the inhibitory potencies of four compounds--fluoxetine, quinidine, imipramine, and ezlopitant--on heterologously expressed recombinant CYP2D6-catalyzed bufuralol 1"-hydroxylase activity were determined. Quinidine 99-108 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 178-184 12867484-10 2003 Incubation of 2 microM MPPP with 3 microM of the CYP2D6-specific inhibitor quinidine resulted in significant (p < 0.01) turnover inhibition (11.8 +/- 1.6% of control). Quinidine 75-84 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 12433806-6 2002 quinidine, a CYP2D6-specific inhibitor, inhibited (-)-OSU6162 N-depropylation, whereas other p450 enzyme-specific substrates/inhibitors did not significantly inhibit this activity; 3). Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 13-19 12642457-6 2003 In their study, they have also demonstrated that quinidine inhibits both CYP2D6- and CYP1A1-mediated debrisoquine 4-hydroxylation. Quinidine 49-58 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 73-79 11689122-5 2001 In incubations containing either pooled microsomes or recombinant CYP2D6, [(14)C]dextromethorphan O-demethylase activity was inhibited in the presence of quinidine (IC(50) = 1.0 microM and 20 nM, respectively). Quinidine 154-163 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 66-72 12167559-7 2002 In incubations with human liver microsomes, quinidine, an inhibitor of CYP2D6, demonstrated little inhibition of metabolite formation while ketoconazole, an inhibitor of CYP3A, demonstrated almost complete inhibition. Quinidine 44-53 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 71-77 12006904-5 2002 Two weeks of baseline monitoring were followed by 8 weeks of daily treatment with fluoxetine or quinidine (two potent CYP2D6 inhibitors) or placebo. Quinidine 96-105 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 118-124 12006904-8 2002 Quinidine > fluoxetine > placebo inhibited CYP2D6 as reflected in the change of the O-demethylation of dextromethorphan, a specific CYP2D6 probe. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 12006904-8 2002 Quinidine > fluoxetine > placebo inhibited CYP2D6 as reflected in the change of the O-demethylation of dextromethorphan, a specific CYP2D6 probe. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 12023534-5 2002 Additionally and surprisingly, this reaction was also inhibited by quinidine and quinine, with respective IC(50) values of 1.38 +/- 0.10 and 3.31 +/- 0.14 microM, compared with those for CYP2D6 debrisoquine 4-hydroxylase of 0.018 +/- 0.05 and 3.75 +/- 2.07 microM, respectively. Quinidine 67-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 187-193 12023534-5 2002 Additionally and surprisingly, this reaction was also inhibited by quinidine and quinine, with respective IC(50) values of 1.38 +/- 0.10 and 3.31 +/- 0.14 microM, compared with those for CYP2D6 debrisoquine 4-hydroxylase of 0.018 +/- 0.05 and 3.75 +/- 2.07 microM, respectively. Quinidine 67-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 194-220 11994058-7 2002 In CYP2D6 poor metabolizers, systemic exposure was greater after chlorpheniramine alone than in extensive metabolizers, and administration of quinidine resulted in a slight increase in CLoral. Quinidine 142-151 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 3-9 11454734-9 2001 Tramadol metabolism in human liver microsomes to M1 and M2 was markedly inhibited by the CYP2D6 inhibitor quinidine and the CYP3A4 inhibitor troleandomycin, respectively. Quinidine 106-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 89-95 12235248-5 2002 In inhibition studies, quinidine, a known CYP2D6 inhibitor, markedly inhibited BF 1"-hydroxylation in the fractions of human liver microsomes that showed the CYP2D6-type selectivity. Quinidine 23-32 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 42-48 12235248-5 2002 In inhibition studies, quinidine, a known CYP2D6 inhibitor, markedly inhibited BF 1"-hydroxylation in the fractions of human liver microsomes that showed the CYP2D6-type selectivity. Quinidine 23-32 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 158-164 11825096-8 2002 Lack of morphine formation from codeine as a result of CYP2D6 inhibition by quinidine results in an almost complete loss of the analgesic effects of codeine. Quinidine 76-85 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-61 11560868-5 2001 The formation of (+)-9-hydroxyrisperidone was strongly inhibited by quinidine, a potent CYP2D6 inhibitor, whereas ketoconazole, a CYP3A4 inhibitor, strongly inhibited the formation of (-)-9-hydroxyrisperidone. Quinidine 68-77 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 11560869-4 2001 This metabolite was also formed by cDNA expressed CYP2D6, and the reaction in human liver microsomes was inhibited by quinidine. Quinidine 118-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 50-56 11519155-3 2001 The elimination of TCAs is impaired by CYP2D6 inhibitors such as quinidine. Quinidine 65-74 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 11408374-5 2001 In pooled human liver microsomes, formation of both metabolites was partially inhibited by both quinidine and ketoconazole, suggesting that CYP2D6 and CYP3A enzymes are involved in the metabolism of CJ-12,458. Quinidine 96-105 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 140-146 11353755-6 2001 Addition of quinidine, a reversible inhibitor of CYP2D6, to a preincubation mixture consisting of SCH 66712, HL microsomes, or Supersomes and NADPH partially protected CYP2D6 from inactivation. Quinidine 12-21 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 11353755-6 2001 Addition of quinidine, a reversible inhibitor of CYP2D6, to a preincubation mixture consisting of SCH 66712, HL microsomes, or Supersomes and NADPH partially protected CYP2D6 from inactivation. Quinidine 12-21 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 168-174 11334347-7 2001 The CYP2D6 inhibition assay has been validated using quinidine as a known selective inhibitor of the isoform. Quinidine 53-62 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 11556126-7 2001 (3-[m-(1-piperidinylmethyl)-phenoxy]propionic acid) and M-3 (m-(1-piperidinylmethyl) phenol) formation from M-5 were inhibited by quinidine and anti-CYP2D6 serum. Quinidine 130-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 149-155 11266079-9 2001 Quinidine inhibited bufuralol 1"-hydroxylation in liver microsomes, particularly at low substrate concentrations, in individuals with CYP2D6*1/*1, and 1/1*2, but not those with CYP2D6*4/*4 and very slightly in individuals with CYP2D6*10B/*10B. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 134-140 10945865-5 2000 Significant correlations were noted between propranolol 4-hydroxylation and ethoxyresorufin-O-deethylation (marker of CYP1A2 activity), with marked improvement in the correlations when CYP2D6-mediated propranolol 4-hydroxylation was inhibited with quinidine. Quinidine 248-257 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 185-191 11432537-8 2001 Quinidine is a potent inhibitor of CYP2D6, but it appears that this enzyme does not mediate the metabolism of any other antimalarial agent. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 35-41 11113407-3 2000 Low-dose quinidine may promote the efficacy of propafenone by inhibiting its degradation through the cytochrome P450 pathway (CYP2D6). Quinidine 9-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 126-132 10924511-6 2000 Tolterodine inhibited the microsomal 25-hydroxylation, whereas quinidine, an inhibitor of CYP2D6, did not markedly inhibit the reaction. Quinidine 63-72 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 90-96 11061580-6 2000 RESULTS: Quinidine selectively and almost completely inhibited the activity of CYP2D6 from day 3 through day 28 without affecting any other enzymes. Quinidine 9-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 11061580-8 2000 The quinidine/rifampin combination resulted in selective CYP2D6 inhibition and induction of all other enzymes evaluated over this time period, suggesting that predictable complex interactions occur with the drug combination. Quinidine 4-13 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 57-63 10997938-7 2000 These data were corroborated with the examination of the effects of CYP-specific inhibitors quinidine (CYP2D6), sulfaphenazole (CYP2C9), and ketoconazole (CYP3A4) on fluoxetine N-demethylation in pooled human liver microsomes. Quinidine 92-101 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 103-109 10950860-5 2000 The M1 formation from R(+)-cibenzoline was highly correlated with bufuralol 1"-hydroxylation and CYP2D6 content and was inhibited by quinidine, a potent inhibitor of CYP2D6. Quinidine 133-142 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 97-103 10950860-5 2000 The M1 formation from R(+)-cibenzoline was highly correlated with bufuralol 1"-hydroxylation and CYP2D6 content and was inhibited by quinidine, a potent inhibitor of CYP2D6. Quinidine 133-142 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 166-172 10806376-9 2000 The reaction was sensitive to inhibition by the CYP2D6-selective inhibitors quinidine, quinine, lobeline and norfluoxetine, whereas chemical inhibitors selective for other CYP isoforms failed to affect the reaction. Quinidine 76-85 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 48-54 10996483-4 2000 Compared to control incubations (no inhibitor) where cholinesterase activity was inhibited to between 1 and 4% of control levels, incorporation of the CYP2D6 inhibitor quinidine into the microsomal incubation resulted in cholinesterase activity of 50% for parathion, 38% for diazinon and 30% for chlorpyrifos. Quinidine 168-177 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 10381752-3 1999 Quinidine, a CYP 3A4 substrate commonly used as a selective in vitro inhibitor of CYP 2D6, was found to markedly increase the rate of meloxicam hydroxylation during in vitro experiments with human liver microsomes. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 82-89 10821163-3 2000 The results indicate that sulphaphenazole, quinidine and alpha-naphthoflavone are selective inhibitors of CYP2C9 (IC50 = 0.5-0.7 microM), CYP2D6 (0.3-0.4 microM) and CYP1A (0.05-5 microM) respectively on the basis of the IC50, which are much lower than those of other P450 isoforms (> 10-fold). Quinidine 43-52 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 10677595-4 2000 Inhibition studies using ketoconazole, furafylline, sulfaphenazole, omeprazole and quinidine suggested that CYP3A4 is the isoform responsible for this reaction whereas CYP1A2, CYP2C9, CYP2C19 and CYP2D6 do not seem to be involved. Quinidine 83-92 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 196-202 10901285-5 2000 Quinidine (an inhibitor of CYP2D6) completely inhibited while alpha-naphthoflavone (an inhibitor of CYP1A2) marginally inhibited the chlorpromazine 7-hydroxylase activity in a human liver microsomal sample showing high CYP2D6 activity. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 27-33 10901285-5 2000 Quinidine (an inhibitor of CYP2D6) completely inhibited while alpha-naphthoflavone (an inhibitor of CYP1A2) marginally inhibited the chlorpromazine 7-hydroxylase activity in a human liver microsomal sample showing high CYP2D6 activity. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 219-225 10510150-1 1999 AIMS: To test the hypothesis that inhibition of cytochrome P450 2D6 (CYP2D6) by quinidine increases the antitussive effect of dextromethorphan (DEX) in an induced cough model. Quinidine 80-89 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 48-67 10510150-1 1999 AIMS: To test the hypothesis that inhibition of cytochrome P450 2D6 (CYP2D6) by quinidine increases the antitussive effect of dextromethorphan (DEX) in an induced cough model. Quinidine 80-89 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 69-75 10510150-4 1999 RESULTS: Inhibition of CYP2D6 by quinidine caused a significant increase in the mean ratio of DEX to dextrorphan (DEX:DOR) plasma AUC(96) (0.04 vs 1.81, P<0.001). Quinidine 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 23-29 10421620-7 1999 The enzyme activity was significantly (p <.01) and stereoselectively inhibited by CYP2D1 inhibitors quinine and quinidine (not by CYP2C or CYP3A inhibitors), and by anti-CYP2D6 peptide antiserum (not by anti-CYP2C, -CYP2B, or -CYP3A antibodies). Quinidine 115-124 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 173-179 10803680-6 2000 Treatment of blood cultures with 25 microM diethyldithiocarbamate (DDC), a specific CYP2E1 inhibitor, or 0.5 microM quinidine, a specific CYP2D6 inhibitor, simultaneously with NNK, significantly decreased NNK-induced chromosome aberration. Quinidine 116-125 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 10671914-0 2000 Inhibition of debrisoquine hydroxylation with quinidine in subjects with three or more functional CYP2D6 genes. Quinidine 46-55 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 98-104 10671914-1 2000 AIMS: To study whether the CYP2D6 capacity in ultrarapid metabolizers of debrisoquine due to duplication/multiduplication of a functional CYP2D6 gene, can be "normalised" by low doses of the CYP2D6 inhibitor quinidine and whether this is dose-dependent. Quinidine 208-217 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 27-33 10671914-1 2000 AIMS: To study whether the CYP2D6 capacity in ultrarapid metabolizers of debrisoquine due to duplication/multiduplication of a functional CYP2D6 gene, can be "normalised" by low doses of the CYP2D6 inhibitor quinidine and whether this is dose-dependent. Quinidine 208-217 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 10671914-1 2000 AIMS: To study whether the CYP2D6 capacity in ultrarapid metabolizers of debrisoquine due to duplication/multiduplication of a functional CYP2D6 gene, can be "normalised" by low doses of the CYP2D6 inhibitor quinidine and whether this is dose-dependent. Quinidine 208-217 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 10671914-8 2000 A dose-effect relationship could be established for quinidine with regard to the inhibitory effect on CYP2D6 activity. Quinidine 52-61 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 102-108 10671914-11 2000 CONCLUSIONS: A dose-effect relationship could be established for quinidine inhibition of CYP2D6 in ultrarapid metabolizers. Quinidine 65-74 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 89-95 10671914-12 2000 The clinical use of low doses of quinidine as an inhibitor of CYP2D6 might be considered in ultrarapid metabolizers taking CYP2D6 metabolized drugs rather than giving increased doses of the drug. Quinidine 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 10671914-12 2000 The clinical use of low doses of quinidine as an inhibitor of CYP2D6 might be considered in ultrarapid metabolizers taking CYP2D6 metabolized drugs rather than giving increased doses of the drug. Quinidine 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 123-129 10671914-13 2000 Normalizing the metabolic capacity of CYP2D6, by giving a low dose of quinidine, may solve the problem of "treatment resistance" caused by ultrarapid metabolism. Quinidine 70-79 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 38-44 10354960-4 1999 The high-affinity component (Km 1.3 +/- 0.4 microM, n = 11 livers) was selectively inhibited by the CYP 2D6 inhibitor quinidine, whereas the CYP3A4 inhibitor ketoconazole selectively inhibited the low-affinity component (K(m) 24.4 +/- 7 microM, n = 11 livers). Quinidine 118-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 100-107 10418968-11 1999 Furafylline, sulfaphenazole, quinidine, and ketoconazole were found to be specific inhibitors of CYP1A2, CYP2C9, CYP2D6, and CYP3A4, respectively. Quinidine 29-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 113-119 9929520-8 1999 Quinidine almost completely inhibited the CYP2D6-mediated de-esterification at the concentration of 1 x 10(-6) M. Ketoconazole and troleandomycin inhibited the CYP3A4-mediated reaction in a dose-related manner. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 42-48 10219965-14 1999 Quinidine, an inhibitor of human CYP2D6, had little effect on these latter activities in human hepatic microsomes. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-39 10702886-12 1999 Hence, quinidine effectively converted extensive metabolisers of CYP2D6 to poor metabolisers of CYP2D6. Quinidine 7-16 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 65-71 10048600-8 1999 This observation is confirmed by the findings that both quinidine (inhibitor of CYP2D6) and ketoconazole (inhibitor of CYP3A4) can inhibit the formation of 9-hydroxyrisperidone. Quinidine 56-65 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 80-86 10702886-0 1999 Inhibition of CYP2D6 by quinidine and its effects on the metabolism of cilostazol. Quinidine 24-33 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 10702886-12 1999 Hence, quinidine effectively converted extensive metabolisers of CYP2D6 to poor metabolisers of CYP2D6. Quinidine 7-16 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-102 10702886-13 1999 The 21-day washout period was adequate to have complete recovery from quinidine inhibition of CYP2D6. Quinidine 70-79 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 94-100 10702886-19 1999 CONCLUSIONS: Administration of quinidine sulfate 200 mg profoundly inhibited CYP2D6-mediated metabolism. Quinidine 31-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 77-83 10702886-20 1999 The effects of quinidine inhibition of CYP2D6 metabolism were completely reversible during the 21-day washout period. Quinidine 15-24 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 9806111-15 1998 EMs, but not PMs, are susceptible to drug interactions between mexiletine and drugs that inhibit CYP2D6 (e.g. quinidine). Quinidine 110-119 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 97-103 9836023-7 1998 Finally, when the specific CYP2D6 inhibitor quinidine was preincubated with either human liver microsomes or cells expressing human CYP2D6, there was a concentration-dependent decrease in the production of OH-mCPP. Quinidine 44-53 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 27-33 9836023-7 1998 Finally, when the specific CYP2D6 inhibitor quinidine was preincubated with either human liver microsomes or cells expressing human CYP2D6, there was a concentration-dependent decrease in the production of OH-mCPP. Quinidine 44-53 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 132-138 9871425-4 1998 The aim of this study was to evaluate the role of oxymorphone in mediating the opioid effects of oxycodone by means of blocking CYP2D6 with quinidine. Quinidine 140-149 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 128-134 9721180-9 1998 The human CYP2D6-specific inhibitor quinidine and the rat CYP2D1-specific inhibitor quinine were both shown to be inhibitors of bufuralol 1"-hydroxylase activity for dog liver microsomes, CYP2D15 WT2, and the CYP2D15 V1 variant with nearly equal potency. Quinidine 36-45 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 10-16 8528270-10 1995 Similar Ki values (within a factor of three) were observed for perhexiline and (R,S)-propranolol while quinidine and dextromethorphan were 8.5-fold and 21-fold more effective inhibitors of CYP2D6-Val relative to CYP2D6-Met. Quinidine 103-112 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 189-195 9731719-12 1998 They also suggest that the Ghanaians have an additional unidentified allele(s) with altered substrate specificity and quinidine sensitivity which is currently genotyped as CYP2D6*1. Quinidine 118-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 172-178 9131945-6 1997 The addition of quinidine, a selective inhibitor of CYP2D6, along with triacetyloleandomycin and sulphaphenazole produced an additional decrease in the rate of NT formation in all but the PM liver, but did not completely eliminate the reaction. Quinidine 16-25 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 52-58 9041677-4 1997 When the metabolism of AMI by CYP2D6 was repeated in the presence of quinidine, none of the metabolites, 10-hydroxy-AMI, NT and 10-hydroxy-NT, was formed. Quinidine 69-78 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 30-36 8877032-5 1996 N-desisopropylpropranolol formation inhibitable by quinidine was highly correlated with specific CYP2D6 activity, as measured by the alpha-hydroxylation of metoprolol (rs = 0.90; P < 0.001). Quinidine 51-60 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 97-103 8819299-8 1996 Sulphaphenazole, 7,8-benzoflavone, quinidine and troleandomycin were selective inhibitors of the CYP2C subfamily (except CYP2C19), the CYP1A subfamily, CYP2D6 and the CYP3A subfamily respectively. Quinidine 35-44 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 152-158 8801060-13 1996 In contrast, amiodarone (IC50, 25 microM) and flecainide (49 microM) inhibited CYP2C9 and quinidine (0.26 microM), and flecainide (0.44 microM) inhibited CYP2D6. Quinidine 90-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 154-160 8861656-4 1996 The involvement of CYP2D6 in drug metabolism was assessed by inhibition studies using quinidine (5 mu M), a specific inhibitor of human CYP2D6, as well as by incubating compounds with microsomes prepared from cells transfected with cDNA encoding human CYP2D6. Quinidine 86-95 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 19-25 8820420-8 1996 Quinidine competitively inhibited the formation of hydroxybupranolol, with Ki values of 5 nM in expressed CYP2D6 and 14.05 nM in human liver (L-1). Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 106-112 8615885-9 1996 Quinidine (5 microm), a CYP2D6 inhibitor, inhibited the formation of DCL approximately 20% when added to microsomal incubations of loratadine at concentrations of 7-35 microM. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 24-30 8531125-7 1995 Similarly, CYP 2D6 inactivation also was prevented by quinidine, a specific competitive inhibitor of this isoform. Quinidine 54-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 11-18 9352574-5 1997 Additional experiments demonstrated that the formation rate of N-hydroxyprocainamide by CYP2D6 enriched microsomes was decreased from 45 +/- 4% to 93 +/- 1% by quinidine at concentrations ranging from 30 nM to 100 microM (all p < 0.05 vs control) and by approximately 75% by antibodies directed against CYP2D6. Quinidine 160-169 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 9352574-5 1997 Additional experiments demonstrated that the formation rate of N-hydroxyprocainamide by CYP2D6 enriched microsomes was decreased from 45 +/- 4% to 93 +/- 1% by quinidine at concentrations ranging from 30 nM to 100 microM (all p < 0.05 vs control) and by approximately 75% by antibodies directed against CYP2D6. Quinidine 160-169 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 306-312 9256169-6 1997 The binding of [3H]GBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine). Quinidine 119-128 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 32-38 9256169-6 1997 The binding of [3H]GBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine). Quinidine 119-128 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 32-37 9264312-8 1997 This reaction was negligible in CYP2D6-deficient liver microsomes, was inhibited stereoselectively by the quinidine/quinine enantiomer pair, and was cosegregated with dextromethorphan O-demethylation (r = 0.975). Quinidine 106-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 32-38 9149373-4 1997 A number of typical CYP2D6 substrates are shown to fit the putative active site of the enzyme, as can the specific inhibitor quinidine. Quinidine 125-134 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 20-26 9037249-7 1997 The proportion of activity inhibited by quinidine correlated positively with total microsomal tamoxifen 4-hydroxylation activity (rs = 0.89, P < 0.01), indicating a major involvement of CYP2D6 in this reaction. Quinidine 40-49 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 189-195 8946477-3 1996 The promethazine hydroxylase in human liver microsomes was inhibited by SKF-525A, propranolol, sparteine, quinidine and anti-CYP2D6 serum suggesting involvement of a P450 related to CYP2D6. Quinidine 106-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 182-188 8627546-6 1996 Yeast microsomes containing heterologously expressed CYP2D6 N-demethylated MPTP (Km = 39 microM), and there was a high correlation between the quinidine-inhibitable N-demethylation of MPTP (50 microM) (0.7-91%, mean 44%, of total activity) and the alpha-hydroxylation of metoprolol in microsomes from 11 human livers (rs = 0.92; P < .001). Quinidine 143-152 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 53-59 8866916-6 1996 The 1"-hydroxylation of bufuralol, form selective for CYP2D6, was competitively inhibited by olanzapine (Ki = 89 microM), clozapine (Ki = 19 microM), and quinidine (Ki = 0.03 microM). Quinidine 154-163 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 8820427-7 1996 During inhibition of CYP2D6-mediated metabolism with quinidine, S-metoprolol areas under the concentration vs. time curves were 2515 +/- 749 and 2719 +/- 742 in White and Black subjects, respectively. Quinidine 53-62 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 21-27 8706777-2 1996 We studied the ability of quinidine, which is a potent inhibitor of CYP2D6, to penetrate the blood brain barrier and its possible impact on codeine O-demethylation in CNS. Quinidine 26-35 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 68-74 8845855-8 1995 Examples of potent inhibitors of CYP2D6 are quinidine, some selective serotonin reuptake inhibitors and some neuroleptics. Quinidine 44-53 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 33-39 7593709-6 1995 Pretreatment of these subjects with 100 mg of quinidine, a selective inhibitor of CYP2D6, significantly suppressed the formation of dextrorphan and elevated the concentrations of dextromethorphan (t1/2, 16.4 hours). Quinidine 46-55 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 82-88 8528270-10 1995 Similar Ki values (within a factor of three) were observed for perhexiline and (R,S)-propranolol while quinidine and dextromethorphan were 8.5-fold and 21-fold more effective inhibitors of CYP2D6-Val relative to CYP2D6-Met. Quinidine 103-112 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 212-218 7720517-7 1995 Substances known to interact with CYP2C (sulfaphenazole, mephenytoin, and tolbutamide) and with CYP2D6 (bufuralol and quinidine) did not specifically inhibit the metabolism of budesonide. Quinidine 118-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-102 7720520-5 1995 The probes sulfaphenazole (CYP2C9) and quinidine (CYP2D6) selectively inhibited tolbutamide methylhydroxylation and bufuralol 1"-hydroxylation, respectively. Quinidine 39-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 50-56 8582470-1 1995 Quinidine is a very potent inhibitor of CYP2D6, but the role of the enzyme in the biotransformation of quinidine has only been investigated in a single in vitro study and in two small in vivo experiments, with contradictory results. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 40-46 8582470-2 1995 The present investigation was designed to present definite evaluation of whether quinidine is metabolised by CYP2D6. Quinidine 81-90 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 109-115 8080088-5 1994 Furthermore, the O-demethylase activity in a panel of microsomes prepared from a series of human livers was significantly correlated with the immunochemically determined levels of CYP2D6 protein (r = 0.925, p < 0.001), and was inhibited (> 89%) by quinidine and lobeline. Quinidine 254-263 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 180-186 7895609-8 1994 Quinidine, a specific inhibitor of CYP2D6, inhibited propranolol 4- and 5-hydroxylase activities selectively and in a concentration-dependent manner. Quinidine 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 35-41 7951142-4 1994 The bunitrolol 4-hydroxylase activity was significantly inhibited by quinidine, a selective inhibitor for CYP2D6. Quinidine 69-78 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 106-112