PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 17908053-5 2007 Some cholinesterase inhibitors (tacrine, donepezil, galantamine) are metabolized via CYP-related enzymes, especially CYP2D6, CYP3A4, and CYP1A2. Tacrine 32-39 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 137-143 17823102-5 2007 The primary pharmacokinetic interactions with smoking occur with drugs that are CYP1A2 substrates, such as caffeine, clozapine, fluvoxamine, olanzapine, tacrine, and theophylline. Tacrine 153-160 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 80-86 10613616-12 1999 This interaction between tacrine and HRT involves reduced metabolic conversion of tacrine to its main metabolite 1-hydroxytacrine by CYP1A2 during the first-pass phase. Tacrine 25-32 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 133-139 14533945-6 2003 The principal proven clinically relevant drug interactions involve tacrine and drugs metabolised by the cytochrome P450 (CYP) 1A2 enzyme, as well as tacrine or donepezil and antipsychotics (which results in the appearance of parkinsonian symptoms). Tacrine 67-74 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 104-129 12162759-7 2002 Tacrine is metabolised by hepatic cytochrome P450 (CYP) 1A2, and donepezil and galantamine are metabolised by CYP3A4 and CYP2D6. Tacrine 0-7 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-59 17166674-1 2007 Controversial results about the involvement of CYP 1A2 and oxidative stress in tacrine-induced hepatotoxicity have been described by the different research groups. Tacrine 79-86 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 47-54 17166674-6 2007 The fact that fluvoxamine, a potent cytochrome P450 (CYP) 1A2 inhibitor, reduced tacrine toxicity and the expression of the CYP 1A2 gene was maintained in gel entrapped hepatocytes, but not in hepatocyte monolayers, could illustrate a close association between CYP 1A2 expression levels and tacrine toxicity. Tacrine 291-298 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 124-131 16128905-1 2005 The cytochrome P450 enzyme CYP1A2 mediates the rate-limiting step in the metabolism of many drugs including theophylline, clozapine, and tacrine as well as in the bioactivation of procarcinogens. Tacrine 137-144 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 10613616-12 1999 This interaction between tacrine and HRT involves reduced metabolic conversion of tacrine to its main metabolite 1-hydroxytacrine by CYP1A2 during the first-pass phase. Tacrine 82-89 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 133-139 10456487-1 1999 OBJECTIVE: In vitro studies have shown that tacrine is metabolized by cytochrome P4501A2 (CYP1A2). Tacrine 44-51 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 70-88 10594467-1 1999 AIMS: The aim of the present study was to examine the CYP1A2 substrate tacrine as a possible alternative to caffeine for assessing CYP1A2 activity in vivo. Tacrine 71-78 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 54-60 10594467-1 1999 AIMS: The aim of the present study was to examine the CYP1A2 substrate tacrine as a possible alternative to caffeine for assessing CYP1A2 activity in vivo. Tacrine 71-78 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 131-137 10456487-1 1999 OBJECTIVE: In vitro studies have shown that tacrine is metabolized by cytochrome P4501A2 (CYP1A2). Tacrine 44-51 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 90-96 10456487-3 1999 The aim of this study was to establish whether the potent CYP1A2 inhibitor fluvoxamine in clinically relevant doses could inhibit tacrine metabolism. Tacrine 130-137 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 58-64 9868741-1 1998 The selective serotonin re-uptake inhibitor, fluvoxamine, is a very potent inhibitor of CYP1A2, and accordingly causes pharmacokinetic interactions with drugs metabolised by CYP1A2, such as caffeine, theophylline, imipramine, tacrine and clozapine. Tacrine 226-233 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9868741-1 1998 The selective serotonin re-uptake inhibitor, fluvoxamine, is a very potent inhibitor of CYP1A2, and accordingly causes pharmacokinetic interactions with drugs metabolised by CYP1A2, such as caffeine, theophylline, imipramine, tacrine and clozapine. Tacrine 226-233 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 174-180 9764962-0 1998 Caffeine based measures of CYP1A2 activity correlate with oral clearance of tacrine in patients with Alzheimer"s disease. Tacrine 76-83 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 9764962-1 1998 AIMS: To study the potential utility of caffeine based probes of CYP1A2 enzyme activity in predicting the pharmokinetics of tacrine in patients with Alzheimer"s disease. Tacrine 124-131 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 65-71 9764962-5 1998 CONCLUSIONS: These observations support a central role for CYP1A2 in the in vivo disposition of tacrine and the potential for drug interactions when tacrine treated patients receive known inducers or inhibitors of this enzyme. Tacrine 96-103 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 59-65 9764962-5 1998 CONCLUSIONS: These observations support a central role for CYP1A2 in the in vivo disposition of tacrine and the potential for drug interactions when tacrine treated patients receive known inducers or inhibitors of this enzyme. Tacrine 149-156 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 59-65 8675160-2 1996 Recent studies using human liver microsomes have suggested that a single liver enzyme, cytochrome P450 1A2 (CYP1A2), catalyzes the major route of metabolism and elimination of tacrine, and also catalyzes the pathway(s) involved in the generation of reactive metabolites capable of covalent protein binding and cytotoxicity. Tacrine 176-183 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 87-106 10022747-0 1998 Use of heterologously expressed human cytochrome P450 1A2 to predict tacrine-fluvoxamine drug interaction in man. Tacrine 69-76 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 38-57 10022747-2 1998 In vitro metabolism of tacrine (a CYP1A2 probe) in the presence and absence of fluvoxamine, a CYP1A2 inhibitor, was investigated in human liver mircrosomes and with different rH-CYP. Tacrine 23-30 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-40 10022747-4 1998 The extent of tacrine metabolism inhibition procured by fluvoxamine with rH-CYP1A2, was compared with previous results observed in man. Tacrine 14-21 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 76-82 10022747-7 1998 Using the Km, Vmax and Ki determined with rH-CYP1A2, we calculated that fluvoxamine produced an inhibition of 1-, 2- and 4-hydroxytacrine formation rate of 91, 87 and 88%, respectively, in the range of tacrine and fluvoxamine concentrations observed in man. Tacrine 130-137 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 45-51 9065747-3 1997 THA-induced toxicity may be related to a metabolic pathway implicating cytochrome P450 1A2 (CYP1A2). Tacrine 0-3 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 71-90 9065747-3 1997 THA-induced toxicity may be related to a metabolic pathway implicating cytochrome P450 1A2 (CYP1A2). Tacrine 0-3 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 92-98 9065747-4 1997 The purpose of this study was to clarify the role of the metabolic conversion of THA by CYP1A2 in the cytotoxicity of THA. Tacrine 81-84 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9065747-4 1997 The purpose of this study was to clarify the role of the metabolic conversion of THA by CYP1A2 in the cytotoxicity of THA. Tacrine 118-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9453170-1 1997 It has been suggested that tacrine (THA) induced hepatotoxicity was related to its metabolic pathway involving cytochrome P4501A2 (CYP1A2). Tacrine 27-34 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 111-129 9453170-1 1997 It has been suggested that tacrine (THA) induced hepatotoxicity was related to its metabolic pathway involving cytochrome P4501A2 (CYP1A2). Tacrine 27-34 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 131-137 9209244-0 1997 Influence of the CYP1A2 inhibitor fluvoxamine on tacrine pharmacokinetics in humans. Tacrine 49-56 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 17-23 9209244-1 1997 OBJECTIVE: Tacrine is extensively metabolized by cytochrome P4501A2 (CYP1A2). Tacrine 11-18 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 49-67 9209244-1 1997 OBJECTIVE: Tacrine is extensively metabolized by cytochrome P4501A2 (CYP1A2). Tacrine 11-18 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 69-75 9209244-2 1997 Fluvoxamine, a potent CYP1A2 inhibitor, may be coadministered with tacrine. Tacrine 67-74 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 22-28 8675160-2 1996 Recent studies using human liver microsomes have suggested that a single liver enzyme, cytochrome P450 1A2 (CYP1A2), catalyzes the major route of metabolism and elimination of tacrine, and also catalyzes the pathway(s) involved in the generation of reactive metabolites capable of covalent protein binding and cytotoxicity. Tacrine 176-183 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 108-114 8675160-3 1996 Because CYP1A2 activity has been shown to vary up to 60-fold among patients, we proposed that a convenient measure of CYP1A2 activity, the [(13)C 3-methyl] caffeine breath test (CBT), might be clinically useful in identifying patients most susceptible to tacrine liver toxicity. Tacrine 255-262 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 118-124 8675160-12 1996 However, the correlation we observed between CBT results and tacrine blood levels is the first evidence supporting a critical role for CYP1A2 activity in the disposition of the drug in vivo. Tacrine 61-68 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 135-141 8565783-0 1995 Determination of human hepatic cytochrome P4501A2 activity in vitro use of tacrine as an isoenzyme-specific probe. Tacrine 75-82 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 31-49 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). Tacrine 48-55 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 123-141 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). Tacrine 48-55 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 143-149 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). Tacrine 57-91 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 123-141 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). Tacrine 57-91 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 143-149 8565783-2 1995 In this study, the use of tacrine as a specific substrate to measure CYP1A2 activity in vitro was investigated. Tacrine 26-33 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 69-75 8565783-4 1995 Initially, the percentage conversion of tacrine to stable metabolites (i.e. 1-, 2-, 4-, and 7-hydroxytacrine) at a single time point was correlated with levels of CYP1A2 apoprotein. Tacrine 40-47 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 163-169 8565783-14 1995 It is concluded, therefore, that tacrine is a valuable probe for the determination of human hepatic CYP1A2 activity in vitro. Tacrine 33-40 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 100-106 24910237-3 2014 The metabolic pathways examined were the CYP1A2-catalyzed tacrine 1-hydroxylation, CYP2B6-catalyzed bupropion hydroxylation, CYP2C8-catalyzed amodiaquine N-deethylation, CYP2C9- catalyzed diclofenac 4"-hydroxylation, CYP2D6-catalyzed dextromethorphan O-demethylation, and CYP3A4-catalyzed midazolam 1"-hydroxylation. Tacrine 58-65 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 41-47 33397254-2 2021 CYP1A2 metabolises many clinical drugs, such as phenacetin, caffeine, clozapine, tacrine, propranolol, and mexiletine. Tacrine 81-88 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 0-6 28400237-3 2017 However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2. Tacrine 9-16 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 174-180 28400237-6 2017 The hepatotoxic potential of tacrine derivatives was evaluated using recombinant cytochrome (CYP) P450 CYP1A2 and CYP3A4 enzymes. Tacrine 29-36 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 103-109 7656503-12 1995 In vitro metabolism studies have demonstrated the importance of cytochrome P450 (CYP1A2) in the biotransformation of tacrine to 1-, 2-, 4- and 7-hydroxylated metabolites. Tacrine 117-124 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 81-87 7946932-7 1994 Using cytochrome P450 isoform specific inhibitors CYP1A2 was identified as the major enzyme involved in all routes of THA metabolism. Tacrine 118-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 50-56 8347124-17 1993 Enoxacin, a specific inhibitor of cytochrome P450 1A2 significantly inhibited all routes of THA metabolism. Tacrine 92-95 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-53 19754423-5 2009 Typical CYP1A2 substrates generally contain planar ring that can fit the narrow and planar active site of the enzyme, such as propranolol, clozapine, guanabenz, flutamide, imatinib, thalidomide, carbamazepine, lidocaine, theophylline, tacrine, tizanidine, zolpidem, riluzole, zileuton, and leflunomide. Tacrine 235-242 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 8-14 19961320-1 2010 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). Tacrine 114-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 19702529-1 2009 CYP1A2 is one of the major CYPs in human liver ( approximately 13%) and metabolises a variety of clinically important drugs, such as clozapine, lidocaine, theophylline, tacrine, and leflunomide. Tacrine 169-176 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 0-6 19590965-1 2009 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a variety of clinically important drugs (e.g., clozapine, tacrine, tizanidine, and theophylline), a number of procarcinogens (e.g. benzo[a]pyrene and aflatoxin B(1)), and several important endogenous compounds (e.g. steroids and arachidonic acids). Tacrine 127-134 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 18634893-3 2008 METHODS: The assay consisted of human liver microsomes and a cocktail of probe substrates metabolized by the five major CYP isoforms (tacrine for CYP1A2, diclofenac for CYP2C9, (S)-mephenytoin for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4). Tacrine 134-141 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 146-152 18584988-3 2008 The 384-well assay used human liver microsomes in conjunction with a cocktail of probe substrates metabolized by the five major CYPs (tacrine for CYP1A2, diclofenac for CYP2C9, (S)-mephenytoin for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4). Tacrine 134-141 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 146-152 18573860-9 2008 In conclusion, tacrine, ethoxyresorufin, and phenacetin are probe substrates for CYP1A2 not only in humans but also in dogs. Tacrine 15-22 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 81-87