PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 16272957-0 2005 Interaction magnitude, pharmacokinetics and pharmacodynamics of ticlopidine in relation to CYP2C19 genotypic status. Ticlopidine 64-75 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 91-98 16272957-1 2005 OBJECTIVES: The aim of this study was to investigate the impact of CYP2C19 polymorphism on the extent of the interaction and on the pharmacokinetics and pharmacodynamics of ticlopidine. Ticlopidine 173-184 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 67-74 16272957-9 2005 CONCLUSIONS: Ticlopidine is a potent inhibitor for CYP2C19 and may be associated with the phenocopy when CYPC19 substrates are co-administered to EMs. Ticlopidine 13-24 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 51-58 16272957-10 2005 Whether and to what extent CYP2C19 would be involved in the metabolism of ticlopidine remain unanswered from the present in-vivo study. Ticlopidine 74-85 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-34 11764927-1 2001 Mechanism-based inactivation of CYP 2C19 by ticlopidine. Ticlopidine 44-55 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 32-40 15155554-7 2004 In addition to CYP2B6, ticlopidine also inhibited both mephenytoin 4-hydroxylation (CYP2C19) (IC(50), 2.7 microM) and dextromethorphan O-demethylation (CYP2D6) (IC(50), 4.4 microM). Ticlopidine 23-34 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 84-91 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. Ticlopidine 157-168 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 172-179 11580286-0 2001 Ticlopidine as a selective mechanism-based inhibitor of human cytochrome P450 2C19. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 62-82 15056479-4 2004 alpha-Naphthoflavone (a CYP1A2 inhibitor) and ketoconazole (a CYP3A4 inhibitor) significantly decreased the rate of perazine 5-sulphoxidation, while ticlopidine (a CYP2C19 inhibitor) strongly reduced the rate of perazine N-demethylation in human liver microsomes. Ticlopidine 149-160 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 164-171 14977868-8 2004 Ticlopidine, a CYP2C19 mechanism-based inhibitor, inhibited disulfoton sulfoxidation by CYP2C19 (IC50 after coincubation, 43.5 microM; IC50 after preincubation, 4.3 microM) and also in HLMs. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 15-22 14977868-8 2004 Ticlopidine, a CYP2C19 mechanism-based inhibitor, inhibited disulfoton sulfoxidation by CYP2C19 (IC50 after coincubation, 43.5 microM; IC50 after preincubation, 4.3 microM) and also in HLMs. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 88-95 14563790-4 2004 Both clopidogrel and ticlopidine inhibited CYP2B6 with highest potency and CYP2C19 with lower potency. Ticlopidine 21-32 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 75-82 11580286-1 2001 Experiments using recombinant yeast-expressed human liver cytochromes P450 confirmed previous literature data indicating that ticlopidine is an inhibitor of CYP 2C19. Ticlopidine 126-137 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 157-165 11580286-2 2001 The present studies demonstrated that ticlopidine is selective for CYP 2C19 within the CYP 2C subfamily. Ticlopidine 38-49 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 67-75 11580286-3 2001 UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. Ticlopidine 53-64 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 82-90 11580286-3 2001 UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. Ticlopidine 53-64 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 128-136 11580286-3 2001 UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. Ticlopidine 103-114 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 82-90 11580286-3 2001 UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. Ticlopidine 103-114 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 128-136 11580286-5 2001 Ticlopidine is oxidized by CYP 2C19 with formation of two major metabolites, the keto tautomer of 2-hydroxyticlopidine (1) and the dimers of ticlopidine S-oxide (TSOD) (V(max) = 13 +/- 2 and 0.4 +/- 0.1 min(-1)). Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-35 11580286-6 2001 During this oxidation, CYP 2C19 was inactivated; the rate of its inactivation was time and ticlopidine concentration dependent. Ticlopidine 91-102 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 23-31 11580286-8 2001 It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. Ticlopidine 59-70 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-35 11580286-8 2001 It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. Ticlopidine 59-70 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 127-135 11580286-8 2001 It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. Ticlopidine 193-204 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-35 11580286-8 2001 It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. Ticlopidine 193-204 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 127-135 11580286-10 2001 The effects of ticlopidine on CYP 2C19 are very analogous with those previously described for the inactivation of CYP 2C9 by tienilic acid. Ticlopidine 15-26 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 30-38 11580286-11 2001 This suggests that a similar electrophilic intermediate, possibly a thiophene S-oxide, is involved in the inactivation of CYP 2C19 and CYP 2C9 by ticlopidine and tienilic acid, respectively. Ticlopidine 146-157 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 122-130 11580286-13 2001 Importantly, ticlopidine is the first selective mechanism-based inhibitor of human liver CYP 2C19 and should be a new interesting tool for studying the topology of the active site of CYP 2C19. Ticlopidine 13-24 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 89-97 11580286-13 2001 Importantly, ticlopidine is the first selective mechanism-based inhibitor of human liver CYP 2C19 and should be a new interesting tool for studying the topology of the active site of CYP 2C19. Ticlopidine 13-24 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 183-191 11181505-9 2001 The metabolic activities of CYP2C9 and CYP2C19 were confirmed by inhibition by sulfaphenazole for CYP2C9 and ticlopidine for CYP2C19. Ticlopidine 109-120 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 39-46 11181505-9 2001 The metabolic activities of CYP2C9 and CYP2C19 were confirmed by inhibition by sulfaphenazole for CYP2C9 and ticlopidine for CYP2C19. Ticlopidine 109-120 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 125-132 10460802-7 1999 Ticlopidine, a potent inhibitor of CYP2C19 and CYP2D6, inhibited bufuralol 1"-hydroxylation by each of these enzymes equipotently. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 35-42 10497136-8 1999 We have shown that ticlopidine is a potent inhibitor of CYP2C19 (IC(50) = 4. Ticlopidine 19-30 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 56-63 10759690-0 2000 In vitro inhibition of the cytochrome P450 (CYP450) system by the antiplatelet drug ticlopidine: potent effect on CYP2C19 and CYP2D6. Ticlopidine 84-95 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 114-121 10759690-5 2000 RESULTS: TCL was a potent, competitive inhibitor of CYP2C19 (Ki = 1.2 +/- 0.5 microM) and of CYP2D6 (Ki = 3.4 +/- 0.3 microM). Ticlopidine 9-12 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 52-59 10759690-8 2000 CONCLUSIONS: TCL appears to be a broad-spectrum inhibitor of the CYP isoforms, but clinically significant adverse drug interactions are most likely with drugs that are substrates of CYP2C19 or CYP2D6. Ticlopidine 13-16 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 182-189 10613611-9 1999 The results are consistent with previous human liver microsome findings that ticlopidine is a potent inhibitor of CYP2C19, a P450 isozyme that is significantly responsible for phenytoin metabolism. Ticlopidine 77-88 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 114-121 9390115-0 1997 Ticlopidine inhibition of phenytoin metabolism mediated by potent inhibition of CYP2C19. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 80-87 10233213-11 1999 CONCLUSIONS: These findings suggest that ticlopidine inhibited the in vivo activity of CYP2C19, but not, or to a lesser extent CYP3 A4, and that the magnitude of inhibition by ticlopidine is related to the in vivo activity of CYP2C19 before inhibition. Ticlopidine 41-52 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 87-94 10233213-11 1999 CONCLUSIONS: These findings suggest that ticlopidine inhibited the in vivo activity of CYP2C19, but not, or to a lesser extent CYP3 A4, and that the magnitude of inhibition by ticlopidine is related to the in vivo activity of CYP2C19 before inhibition. Ticlopidine 41-52 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 226-233 10233213-11 1999 CONCLUSIONS: These findings suggest that ticlopidine inhibited the in vivo activity of CYP2C19, but not, or to a lesser extent CYP3 A4, and that the magnitude of inhibition by ticlopidine is related to the in vivo activity of CYP2C19 before inhibition. Ticlopidine 176-187 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 87-94 10233213-11 1999 CONCLUSIONS: These findings suggest that ticlopidine inhibited the in vivo activity of CYP2C19, but not, or to a lesser extent CYP3 A4, and that the magnitude of inhibition by ticlopidine is related to the in vivo activity of CYP2C19 before inhibition. Ticlopidine 176-187 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 226-233 10233213-0 1999 Ticlopidine decreases the in vivo activity of CYP2C19 as measured by omeprazole metabolism. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 46-53 10233213-1 1999 AIMS: To examine the effect of ticlopidine administration on the activities CYP2C19 and CYP3 A in vivo using omeprazole as a model substrate. Ticlopidine 31-42 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 76-83 9390115-4 1997 Using human liver microsomes, we showed that ticlopidine is a potent inhibitor of cytochrome P450 2C19, with an estimated inhibition constant (Ki) of 3.7 +/- 0.2 mumol/L. Ticlopidine 45-56 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 82-102 9390115-6 1997 These data suggest that, in this patient, phenytoin toxicity was caused by inhibition of CYP2C19 by ticlopidine, and the data emphasize the importance of CYP2C19 in the metabolism of phenytoin. Ticlopidine 100-111 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 89-96 19845434-0 2009 Comparison of mechanism-based inhibition of human cytochrome P450 2C19 by ticlopidine, clopidogrel, and prasugrel. Ticlopidine 74-85 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 50-70 28737446-13 2018 Ticlopidine is a time-dependent inhibitor of both CYP2B6 and CYP2C19 that can inhibit the bupropion metabolism by 50-60%. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 61-68 24855828-5 2014 Both ticlopidine and fluvoxamine were competitive inhibitors of CYP2C19. Ticlopidine 5-16 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 64-71 23474500-4 2013 Specific mammalian inhibitors were used as diagnostic tools for related activities of CYP1A (alpha-naphthoflavone; alphaNF), CYP2B6 and CYP2C19 (ticlopidine) and CYP3A4 (ketoconazole). Ticlopidine 145-156 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 136-143 22652334-3 2012 To distinguish reversible MDI from mechanism-based inhibition (MBI), R-fluoxetine and ticlopidine were used as positive inhibitors for reversible MDI and MBI of CYP2C19, respectively. Ticlopidine 86-97 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 161-168 22652334-4 2012 R-fluoxetine and ticlopidine inhibited CYP2C19 activity, as determined using S-mephenytoin as a substrate, and caused 8.7- and 2.3-fold IC(50) shifts, respectively, after pre-incubation. Ticlopidine 17-28 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 39-46 21148250-8 2011 The recombinant human CYP2C19 inactivation kinetics of isoniazid, ticlopidine, and tranylcypromine were evaluated, and their key kinetic parameters were measured from the same experiment. Ticlopidine 66-77 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 22-29 27386066-2 2016 It seems that methadone as CYP2C19 inhibitor affects ticlopidine activity in vivo. Ticlopidine 53-64 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-34 21178986-0 2011 Differential impacts of CYP2C19 gene polymorphisms on the antiplatelet effects of clopidogrel and ticlopidine. Ticlopidine 98-109 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 24-31 21178986-6 2011 Ticlopidine may be an effective therapeutic option for CYP2C19 PMs. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 55-62 19948947-7 2010 Knowledge of the CYP-dependent formation of ticlopidine and clopidogrel thiolactones helps explain some of the observed drug-drug interactions with these molecules and, more important, the role of CYP2C19 genetic polymorphism on the pharmacokinetics of and pharmacodynamic response to clopidogrel. Ticlopidine 44-55 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 197-204 19845434-1 2009 Mechanism-based inhibition of CYP2C19 in human liver microsomes by the thienopyridine antiplatelet agents clopidogrel, prasugrel and their thiolactone metabolites was investigated by determining the time- and concentration-dependent inhibition of the activity of S-mephenytoin 4"-hydroxylase as typical CYP2C19 activity and compared with ticlopidine and its metabolite. Ticlopidine 338-349 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 30-37 19845434-2 2009 Clopidogrel was shown to be a mechanism-based inhibitor of CYP2C19 with the inactivation kinetic parameters, k(inact) and K(I), equal to 0.0557 min(-1) and 14.3 microM, respectively, as well as ticlopidine (0.0739 min(-1) and 3.32 microM, respectively). Ticlopidine 194-205 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 59-66 19845434-3 2009 The thiolactone metabolite of ticlopidine and clopidogrel inhibited CYP2C19 only in a concentration-dependent manner. Ticlopidine 30-41 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 68-75 19144769-4 2009 In this study, we compared fluoxetine, its (R)- and (S)-enantiomers, ticlopidine, and S-benzylnirvanol as potential time-dependent inhibitors of human liver microsomal CYP2C19. Ticlopidine 69-80 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 168-175 17332142-7 2007 In HLMs, analysis of the two-enzyme kinetics in the presence of P450 isozyme-selective chemical inhibitors (ticlopidine for CYP2C19, sulfaphenazole for CYP2C9, and furafylline for CYP1A2) indicated that CYP2C19 was the high affinity component and CYP2C9 was the low affinity component. Ticlopidine 108-119 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 124-131 19122335-2 2008 Ticlopidine and clopidogrel inhibited CYP2B6 with IC(50) values of 0.0517+/-0.0323 microM and 0.0182+/-0.0069 microM, respectively, and inhibited CYP2C19 with IC(50) values of 0.203+/-0.124 microM and 0.524+/-0.160 microM, respectively. Ticlopidine 0-11 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 146-153 18474675-2 2008 Mechanism-based CYP2B6 inhibitors (i.e., clopidogrel, ticlopidine, and triethylenethiophoramide) significantly inhibited the formation of M1 from sibutramine and M2 from M1, respectively; in contrast, no effect was observed when using potent inhibitors of eight P450 isozymes (CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A). Ticlopidine 54-65 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 309-316 17307149-2 2007 In order to gain insights for developing personalized drugs, the 3D (dimensional) structure of CYP2C19 has been developed based on the crystal structure of CYP2C9 (PDB code 1R90), and its structure-activity relationship with the ligands of CEC, Fluvoxamine, Lescol, and Ticlopidine investigated through the structure-activity relationship approach. Ticlopidine 270-281 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 95-102