PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 17322140-2 2007 In human liver microsomes, the mean 50% inhibitory concentrations (IC(50)) for PJ and GFJ versus CYP3A (triazolam alpha-hydroxylation) were 0.61% and 0.55%, (v/v) respectively, without preincubation of inhibitor with microsomes. Triazolam 104-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 18076219-19 2008 Dosage adjustments may be required for drugs that are substrates of CYP3A4 (e.g. ciclosporin, triazolam) and CYP2C19 enzymes (e.g. diazepam, phenytoin) when administered with armodafinil. Triazolam 94-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 17523050-7 2007 Testosterone 2alpha- and 16alpha-hydroxylation reactions were conducted primarily by CYP2C11, and midazolam 4-hydroxylation and triazolam 1"-hydroxylation were preferentially catalyzed by CYP3A1/2, but specificity was otherwise generally poor. Triazolam 128-137 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 188-196 17178770-9 2007 The mutants also greatly decreased the metabolism of testosterone, erythromycin, nevirapine, and triazolam relative to those activities of CYP3A7 wild-type enzyme. Triazolam 97-106 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 139-145 15470333-9 2004 Estimates of CYP3A-mediated extraction by the intestine and liver indicated approximately equal contributions by both organs but larger values for midazolam than for triazolam, and these differences accounted for the differences in oral bioavailability, 30% +/- 13% versus 55% +/- 20%, respectively. Triazolam 166-175 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-18 17204458-0 2007 Theoretical calculation of triazolam hydroxylation and endogenous steroid inhibition in the active site of CYP3A4. Triazolam 27-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 17204458-2 2007 CYP3A4 produced more 4-hydroxytriazolam than alpha-hydroxytriazolam at concentrations of more than 60 muM triazolam, and different steroids had different inhibitory effects on the system. Triazolam 30-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 16251267-6 2006 With triazolam, relative rCBF of the left orbital basal forebrain decreased more during stage 2 than slow wave sleep, whereas absolute CBF of the occipital cortex and cerebral white matter remained constant. Triazolam 5-14 CCAAT enhancer binding protein zeta Homo sapiens 26-29 16251267-7 2006 During triazolam-induced stage 2 sleep, absolute CBF of the cerebral white matter correlated more strongly to both MAP and Paco2 than during placebo sleep and also correlated more strongly to both MAP and Paco2 than absolute CBF of the occipital cortex. Triazolam 7-16 CCAAT enhancer binding protein zeta Homo sapiens 49-52 16251267-7 2006 During triazolam-induced stage 2 sleep, absolute CBF of the cerebral white matter correlated more strongly to both MAP and Paco2 than during placebo sleep and also correlated more strongly to both MAP and Paco2 than absolute CBF of the occipital cortex. Triazolam 7-16 CCAAT enhancer binding protein zeta Homo sapiens 225-228 16251267-8 2006 In the frontal white matter, during triazolam-induced stage 2 sleep compared to wakefulness, absolute CBF was significantly better correlated to MAP, but not to Paco2. Triazolam 36-45 CCAAT enhancer binding protein zeta Homo sapiens 102-105 16251267-9 2006 During triazolam-induced stage 2, the cerebral white matter may receive a modulated CBF regulation having the strengthened relationship of Paco2 to CBF and, more locally, the frontal white matter may depend precariously on CBF regulation. Triazolam 7-16 CCAAT enhancer binding protein zeta Homo sapiens 84-87 16251267-9 2006 During triazolam-induced stage 2, the cerebral white matter may receive a modulated CBF regulation having the strengthened relationship of Paco2 to CBF and, more locally, the frontal white matter may depend precariously on CBF regulation. Triazolam 7-16 CCAAT enhancer binding protein zeta Homo sapiens 148-151 16251267-9 2006 During triazolam-induced stage 2, the cerebral white matter may receive a modulated CBF regulation having the strengthened relationship of Paco2 to CBF and, more locally, the frontal white matter may depend precariously on CBF regulation. Triazolam 7-16 CCAAT enhancer binding protein zeta Homo sapiens 148-151 15764714-5 2005 CYP3A inhibition was tested using triazolam hydroxylation in human liver microsomes (HLM). Triazolam 34-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 15863898-5 2005 Nicardipine strongly inhibited two-pathways of triazolam hydroxylation both catalyzed by CYP3A4. Triazolam 47-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 15386482-4 2004 The three compounds were also evaluated as potential inhibitors of human CYP3A based on an in vitro model using triazolam hydroxylation by human liver microsomes as an index reaction. Triazolam 112-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-78 15470333-12 2004 CONCLUSION: Despite alprazolam, midazolam, and triazolam having markedly different pharmacokinetic characteristics, statistically significant correlations were present between the oral and systemic clearances of the 3 drugs, consistent with a major involvement of CYP3A in their metabolism and elimination. Triazolam 47-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 264-269 15482640-5 2004 In rats treated with MPS, an in-situ efflux experiment using rhodamine-123 demonstrated that the reverse transport function of P-glycoprotein (P-gp) in the small intestine was significantly enhanced, although there was no significant increase in the intestinal microsomal activity of triazolam alpha- and 4-hydroxylation, metabolic probes for CYP3A. Triazolam 284-293 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 127-141 15482640-5 2004 In rats treated with MPS, an in-situ efflux experiment using rhodamine-123 demonstrated that the reverse transport function of P-glycoprotein (P-gp) in the small intestine was significantly enhanced, although there was no significant increase in the intestinal microsomal activity of triazolam alpha- and 4-hydroxylation, metabolic probes for CYP3A. Triazolam 284-293 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 143-147 15258104-0 2004 Interaction of triazolam and ketoconazole in P-glycoprotein-deficient mice. Triazolam 15-24 phosphoglycolate phosphatase Mus musculus 45-59 15258104-1 2004 The role of P-glycoprotein (P-gp) on the distribution of the benzodiazepine triazolam (TRZ) and the azole antifungal agent ketoconazole (KET), and on the TRZ-KET interaction, was studied using mdr1a(-) or mdr1a/b(-/-) mice (P-gp-deficient mice) and matched controls. Triazolam 76-85 phosphoglycolate phosphatase Mus musculus 12-26 15258104-1 2004 The role of P-glycoprotein (P-gp) on the distribution of the benzodiazepine triazolam (TRZ) and the azole antifungal agent ketoconazole (KET), and on the TRZ-KET interaction, was studied using mdr1a(-) or mdr1a/b(-/-) mice (P-gp-deficient mice) and matched controls. Triazolam 76-85 phosphoglycolate phosphatase Mus musculus 28-32 15258104-1 2004 The role of P-glycoprotein (P-gp) on the distribution of the benzodiazepine triazolam (TRZ) and the azole antifungal agent ketoconazole (KET), and on the TRZ-KET interaction, was studied using mdr1a(-) or mdr1a/b(-/-) mice (P-gp-deficient mice) and matched controls. Triazolam 87-90 phosphoglycolate phosphatase Mus musculus 12-26 15258104-1 2004 The role of P-glycoprotein (P-gp) on the distribution of the benzodiazepine triazolam (TRZ) and the azole antifungal agent ketoconazole (KET), and on the TRZ-KET interaction, was studied using mdr1a(-) or mdr1a/b(-/-) mice (P-gp-deficient mice) and matched controls. Triazolam 87-90 phosphoglycolate phosphatase Mus musculus 28-32 15099443-6 2004 On the other hand, MP inhibited the CYP3A-mediated triazolam hydroxylations in a concentration-dependent manner. Triazolam 51-60 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 36-41 15129163-4 2004 Triazolam also slowed the decay of spontaneous inhibitory synaptic currents, reduced the amplitude of fEPSPs elicited during a theta burst and reduced the magnitude of LTP in hippocampal CA1 neurones in vitro. Triazolam 0-9 carbonic anhydrase 1 Homo sapiens 187-190 14742746-2 2004 The biotransformation of triazolam to its primary hydroxylated products, 4-OH-TRZ (triazolam) and alpha-OH-TRZ, was used as a marker of CYP3A activity in rat liver and intestine. Triazolam 25-34 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 136-141 15370962-0 2004 Role of CYP3A enzymes in the biotransformation of triazolam in rat liver. Triazolam 50-59 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 8-13 12814972-1 2003 Midazolam, triazolam (TRZ), testosterone, and nifedipine have all been widely used as probes for in vitro metabolism of CYP3A. Triazolam 11-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-125 14985144-7 2004 Compared with vehicle control, CYP3A activity in liver microsomes (intrinsic clearance for triazolam hydroxylation in vitro) was increased by a factor of 2-4 by RIT, and by 10-14-fold by DEX. Triazolam 91-100 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 31-36 12814972-1 2003 Midazolam, triazolam (TRZ), testosterone, and nifedipine have all been widely used as probes for in vitro metabolism of CYP3A. Triazolam 22-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-125 12814972-3 2003 Recombinant CYP3A4 and CYP3A5 (rCYP3A4 and rCYP3A5) both produced 1-OH and 4-OH metabolites from midazolam and triazolam, 6 beta-hydroxytestosterone from testosterone, and oxidized nifedipine from nifedipine. Triazolam 111-120 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 12814972-3 2003 Recombinant CYP3A4 and CYP3A5 (rCYP3A4 and rCYP3A5) both produced 1-OH and 4-OH metabolites from midazolam and triazolam, 6 beta-hydroxytestosterone from testosterone, and oxidized nifedipine from nifedipine. Triazolam 111-120 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 23-29 12814972-10 2003 Thus, CYP3A4 and CYP3A5 both contribute to midazolam, triazolam, testosterone, and nifedipine biotransformation in HLMs, with CYP3A5 being metabolically less active than CYP3A4 in general. Triazolam 54-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 12814972-10 2003 Thus, CYP3A4 and CYP3A5 both contribute to midazolam, triazolam, testosterone, and nifedipine biotransformation in HLMs, with CYP3A5 being metabolically less active than CYP3A4 in general. Triazolam 54-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 17-23 11158730-14 2001 Inhibition of one or both CYP2C19 and CYP3A isoforms is the likely mechanism by which INH slows the elimination of coadministered drugs, including phenytoin, carbamazepine, diazepam, triazolam, and primidone. Triazolam 183-192 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 26-33 12724045-5 2003 At 250 microM triazolam (the CYP3A index substrate), the mean (+/- s.e., n = 4) IC50 versus triazolam alpha-hydroxylation (where IC50 is the concentration producing a 50% decrement in reaction velocity) was 7.3 (+/- 0.5) microM. Triazolam 14-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-34 12724045-5 2003 At 250 microM triazolam (the CYP3A index substrate), the mean (+/- s.e., n = 4) IC50 versus triazolam alpha-hydroxylation (where IC50 is the concentration producing a 50% decrement in reaction velocity) was 7.3 (+/- 0.5) microM. Triazolam 92-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-34 12537513-14 2003 The only substantive interactions observed were with ethinylestradiol and triazolam, apparently through induction of CYP3A4, primarily in the gastrointestinal system. Triazolam 74-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 12404077-0 2002 Selective antagonism of the ataxic effects of zolpidem and triazolam by the GABAA/alpha1-preferring antagonist beta-CCt in squirrel monkeys. Triazolam 59-68 gamma-aminobutyric acid (GABA) A receptor, subunit gamma 1 Mus musculus 76-81 12404077-0 2002 Selective antagonism of the ataxic effects of zolpidem and triazolam by the GABAA/alpha1-preferring antagonist beta-CCt in squirrel monkeys. Triazolam 59-68 t-complex protein 1 Mus musculus 116-119 11823757-10 2002 Therefore significant metabolic drug-drug interactions are most likely to occur with compounds (such as triazolam) that undergo significant gastrointestinal CYP3A4/5-mediated first-pass metabolism. Triazolam 104-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-163 12751920-14 2003 While triazolam and midazolam are biotransformed almost entirely via CYP3A4, the newer hypnosedatives are biotransformed by several CYP isozymes in addition to CYP3A4, resulting in CYP3A4 inhibitors and inducers having a lesser effect on their biotransformation. Triazolam 6-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 12751920-14 2003 While triazolam and midazolam are biotransformed almost entirely via CYP3A4, the newer hypnosedatives are biotransformed by several CYP isozymes in addition to CYP3A4, resulting in CYP3A4 inhibitors and inducers having a lesser effect on their biotransformation. Triazolam 6-15 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 69-72 11981598-0 2002 Role of GABAA/benzodiazepine receptors containing alpha 1 and alpha 5 subunits in the discriminative stimulus effects of triazolam in squirrel monkeys. Triazolam 121-130 adrenoceptor alpha 1D Homo sapiens 50-69 12579961-0 2002 [Identification of estazolam, alprazolam and triazolam in human urine by LC/MSn]. Triazolam 45-54 moesin Homo sapiens 76-79 12579961-1 2002 AIM: To investigate the fragmentation behavior of triazolobenzodiazepines and to develop a specific, sensitive and rapid LC/MSn assay for simultaneous determination of estazolam, alprazolam and triazolam in human urine. Triazolam 194-203 moesin Homo sapiens 124-127 11414684-1 2001 The inhibition of CYP3A4-mediated oxidation of triazolam and testosterone was assessed in the presence of a selection of known CYP3A4 substrates and inhibitors. Triazolam 47-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-24 11414684-4 2001 In additional studies, residual CYP3A4 activity toward testosterone and triazolam hydroxylation was measured after pretreatment with the CYP3A4 mechanism based inhibitor, midazolam. Triazolam 72-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 11158730-14 2001 Inhibition of one or both CYP2C19 and CYP3A isoforms is the likely mechanism by which INH slows the elimination of coadministered drugs, including phenytoin, carbamazepine, diazepam, triazolam, and primidone. Triazolam 183-192 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 10935688-10 2000 The findings are consistent with the complete dependence of triazolam clearance on CYP3A activity, compared with the partial dependence of zolpidem clearance on CYP3A. Triazolam 60-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-88 11124232-7 2001 To explain these kinetic observations, a two-site binding model is proposed in which triazolam is hypothesized to bind within the CYP3A4 active site in spatially distinct orientations, which may lead to the formation of either the 1"-hydroxytriazolam or 4-hydroxytriazolam. Triazolam 85-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 10997940-3 2000 In addition, an investigation of MgCl(2) effects on CYP3A4-mediated metabolism of triazolam revealed that 10 mM MgCl(2) increased the apparent K(m) of triazolam 4-hydroxylation from 83 to 173 microM and reduced the V(max) for the reaction from 3.4 to 2.4 min(-1). Triazolam 82-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 10997940-3 2000 In addition, an investigation of MgCl(2) effects on CYP3A4-mediated metabolism of triazolam revealed that 10 mM MgCl(2) increased the apparent K(m) of triazolam 4-hydroxylation from 83 to 173 microM and reduced the V(max) for the reaction from 3.4 to 2.4 min(-1). Triazolam 151-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 10952482-1 2000 OBJECTIVE: Biotransformation of triazolam to its alpha-hydroxy and 4-hydroxy metabolites by human liver microsomes in vitro was used as an index of human cytochrome P450 3A (CYP3A) activity. Triazolam 32-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-172 10952482-1 2000 OBJECTIVE: Biotransformation of triazolam to its alpha-hydroxy and 4-hydroxy metabolites by human liver microsomes in vitro was used as an index of human cytochrome P450 3A (CYP3A) activity. Triazolam 32-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-179 11124232-0 2001 Triazolam substrate inhibition: evidence of competition for heme-bound reactive oxygen within the CYP3A4 active site. Triazolam 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 10773013-9 2000 The complete dependence of triazolam clearance on CYP3A activity, as opposed to the mixed CYP participation in zolpidem clearance, may explain the differing sex effects on clearance of the two compounds. Triazolam 27-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-55 10640299-1 2000 Midazolam (MDZ) and triazolam (TRZ) hydroxylation, reactions considered to be cytochrome P-4503A (CYP3A)-mediated in humans, were examined in mouse and human liver microsomes. Triazolam 20-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-103 10870985-0 2000 Prediction of in vivo interaction between triazolam and erythromycin based on in vitro studies using human liver microsomes and recombinant human CYP3A4. Triazolam 42-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 10870985-1 2000 PURPOSE: To quantitatively predict the in vivo interaction between triazolam and erythromycin, which involves mechanism-based inhibition of CYP3A4, from in vitro studies using human liver microsomes (HLM) and recombinant human CYP3A4 (REC). Triazolam 67-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 10870985-1 2000 PURPOSE: To quantitatively predict the in vivo interaction between triazolam and erythromycin, which involves mechanism-based inhibition of CYP3A4, from in vitro studies using human liver microsomes (HLM) and recombinant human CYP3A4 (REC). Triazolam 67-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 227-233 10870985-1 2000 PURPOSE: To quantitatively predict the in vivo interaction between triazolam and erythromycin, which involves mechanism-based inhibition of CYP3A4, from in vitro studies using human liver microsomes (HLM) and recombinant human CYP3A4 (REC). Triazolam 67-76 zinc finger DHHC-type palmitoyltransferase 2 Homo sapiens 235-238 10870985-2 2000 METHODS: HLM or REC was preincubated with erythromycin in the presence of NADPH and then triazolam was added. Triazolam 89-98 zinc finger DHHC-type palmitoyltransferase 2 Homo sapiens 16-19 10870985-8 2000 Based on the kinetic parameters obtained using HLM and REC, the AUCpo of triazolam was predicted to increase 2.0- and 2.6-fold, respectively, following oral administration of erythromycin (333 mg t.i.d. Triazolam 73-82 zinc finger DHHC-type palmitoyltransferase 2 Homo sapiens 55-58 10870985-10 2000 CONCLUSIONS: In vivo interaction between triazolam and erythromycin was successfully predicted from in vitro data based on a PBPK model involving a mechanism-based inhibition of CYP3A4. Triazolam 41-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 178-184 10640299-1 2000 Midazolam (MDZ) and triazolam (TRZ) hydroxylation, reactions considered to be cytochrome P-4503A (CYP3A)-mediated in humans, were examined in mouse and human liver microsomes. Triazolam 31-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-103 10546924-0 1999 Mibefradil but not isradipine substantially elevates the plasma concentrations of the CYP3A4 substrate triazolam. Triazolam 103-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 10602344-8 1999 High-dose administration of diazepam (10 mg kg-1) or triazolam (1 mg kg-1) reduced mPer1 mRNA level 1 h after treatment in the cerebellum. Triazolam 53-62 period circadian clock 1 Mus musculus 83-88 10230766-2 1999 The in vitro kinetic parameters of CYP3A-mediated metabolism of midazolam (MDZ), triazolam (TRZ), and dexamethasone (DEX) were studied in liver microsomes from three mrdrla(-/-) mice, one mdrla/b(-/-) mouse, and mdrla/b(+/+) controls. Triazolam 81-90 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 35-40 10383917-5 1999 At the substrate concentration of 20 microM, which approximated the apparent KM value, sulfaphenazole (CYP2C9 inhibitor) and triazolam (CYP3A substrate) reduced the N-demethylation activities by 20 to 35% in human liver microsomes, whereas the inhibition induced by mephenytoin (CYP2C19 substrate) or quinidine (CYP2D6 inhibitor) was marginal. Triazolam 125-134 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 103-109 10383917-5 1999 At the substrate concentration of 20 microM, which approximated the apparent KM value, sulfaphenazole (CYP2C9 inhibitor) and triazolam (CYP3A substrate) reduced the N-demethylation activities by 20 to 35% in human liver microsomes, whereas the inhibition induced by mephenytoin (CYP2C19 substrate) or quinidine (CYP2D6 inhibitor) was marginal. Triazolam 125-134 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 279-286 10383917-5 1999 At the substrate concentration of 20 microM, which approximated the apparent KM value, sulfaphenazole (CYP2C9 inhibitor) and triazolam (CYP3A substrate) reduced the N-demethylation activities by 20 to 35% in human liver microsomes, whereas the inhibition induced by mephenytoin (CYP2C19 substrate) or quinidine (CYP2D6 inhibitor) was marginal. Triazolam 125-134 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 312-318 10230766-0 1999 Unchanged cytochrome P450 3A (CYP3A) expression and metabolism of midazolam, triazolam, and dexamethasone in mdr(-/-) mouse liver microsomes. Triazolam 77-86 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 10-28 10230766-0 1999 Unchanged cytochrome P450 3A (CYP3A) expression and metabolism of midazolam, triazolam, and dexamethasone in mdr(-/-) mouse liver microsomes. Triazolam 77-86 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 30-35 10383920-8 1999 However, rokitamycin, LMA7, erythromycin, and clarithromycin inhibited the CYP3A4-catalyzed triazolam alpha-hydroxylation with IC50 (Ki) values of 5.8 (2.0), 40, 33 (20), and 56 (43) microM, respectively. Triazolam 92-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 10230766-2 1999 The in vitro kinetic parameters of CYP3A-mediated metabolism of midazolam (MDZ), triazolam (TRZ), and dexamethasone (DEX) were studied in liver microsomes from three mrdrla(-/-) mice, one mdrla/b(-/-) mouse, and mdrla/b(+/+) controls. Triazolam 92-95 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 35-40 10459684-0 1999 Effects of a small dose of triazolam on P300. Triazolam 27-36 E1A binding protein p300 Homo sapiens 40-44 9698298-4 1998 The BN N-dealkylation activities in 10 human liver microsomal preparations were strongly correlated with microsomal CYP3A-specific metabolic reactions, i.e. triazolam 1"-hydroxylation (r = 0.954), midazolam 1"-hydroxylation (r = 0.928), and testosterone 6beta-hydroxylation (r = 0.897). Triazolam 157-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-121 9783333-1 1998 The effects of short-term use of a small dose of dexamethasone on the pharmacokinetics and pharmacodynamics of the CYP3A4 substrate, triazolam, were examined. Triazolam 133-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 9783333-9 1998 Although dexamethasone had only small effects on the pharmacokinetics and pharmacodynamics of triazolam in the present study, higher doses or prolonged use of dexamethasone might cause a more pronounced induction of CYP3A4. Triazolam 94-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 9765359-4 1998 Coincubation with triazolam showed that delavirdine caused a time- and NADPH-dependent loss of CYP3A4 activity in human liver microsomes as measured by triazolam 1"-hydroxylation. Triazolam 18-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 9765359-4 1998 Coincubation with triazolam showed that delavirdine caused a time- and NADPH-dependent loss of CYP3A4 activity in human liver microsomes as measured by triazolam 1"-hydroxylation. Triazolam 152-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 9333111-2 1997 Erythromycin and itraconazole are potent inhibitors of CYP3A4, and they increase plasma concentrations and effects of certain drugs, for example, oral midazolam and triazolam. Triazolam 165-174 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 9676900-9 1998 In addition, the BZD agonist triazolam (0.05-0.25 mg/kg) also produced a flumazenil- and picrotoxin-sensitive hyperphagic effects, thereby suggesting the changes in feeding behavior by neurosteroids represent GABA-A receptor mediated hyperphagic action. Triazolam 29-38 gamma-aminobutyric acid (GABA) A receptor, subunit gamma 1 Mus musculus 209-215 9626922-2 1998 Itraconazole strongly interacts with many substrates of CYP3A4 such as midazolam and triazolam. Triazolam 85-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 8612379-1 1996 BACKGROUND: Triazolam is metabolized by CYP3A4. Triazolam 12-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 9263374-0 1997 Single-dose pharmacokinetics and pharmacodynamics of oral triazolam in relation to cytochrome P4502C19 (CYP2C19) activity. Triazolam 58-67 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 83-102 9263374-0 1997 Single-dose pharmacokinetics and pharmacodynamics of oral triazolam in relation to cytochrome P4502C19 (CYP2C19) activity. Triazolam 58-67 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 104-111 9263374-1 1997 Previous studies have suggested that triazolam is at least partly metabolized by cytochrome P4503A4 (CYP3A4). Triazolam 37-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-99 9263374-1 1997 Previous studies have suggested that triazolam is at least partly metabolized by cytochrome P4503A4 (CYP3A4). Triazolam 37-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 9263374-2 1997 However, no study has examined the relationship between the metabolism of triazolam and CYP2C19, which is involved in the metabolism of diazepam. Triazolam 74-83 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 88-95 9146848-1 1997 AIMS: Triazolam, a triazolobenzodiazepine hypnotic agent, is metabolized by CYP3A4. Triazolam 6-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 9024169-1 1997 BACKGROUND: Triazolam is metabolized predominantly by cytochrome P450 3A4 (CYP3A4). Triazolam 12-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-73 9024169-1 1997 BACKGROUND: Triazolam is metabolized predominantly by cytochrome P450 3A4 (CYP3A4). Triazolam 12-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 9024169-12 1997 This is most likely due to increased metabolism of triazolam after induction of CYP3A4 in the gut wall and liver by rifampin. Triazolam 51-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 9129558-2 1997 Itraconazole strongly interacts with some of the substrates of CYP3A4 (e.g., terfenadine, triazolam and lovastatin); hence it is important to uncover the possible interaction of itraconazole with felodipine. Triazolam 90-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 8730978-17 1996 Triazolam and probably other drugs metabolized by CYP3A4 can be used in normal doses with terbinafine. Triazolam 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 8612379-11 1996 Prescription of triazolam should be avoided if a patient is using diltiazem or other potent inhibitors of CYP3A. Triazolam 16-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-111 8610817-8 1996 Cytochrome P450 3A4 metabolizes terfenadine, astemizole, carbamazepine, alprazolam, triazolam, and other benzodiazepines. Triazolam 84-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 8830062-3 1995 The metabolism of triazolam is dependent on cytochrome P450 3A4, and because nefazodone has been shown in vitro to be an inhibitor of this isoenzyme, this study was conducted to assess the potential for an interaction between the two drugs. Triazolam 18-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-63 8824695-0 1996 Triazolam pharmacokinetics and pharmacodynamics in Caucasians and Southern Asians: ethnicity and CYP3A activity. Triazolam 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 8830062-13 1995 The increase in triazolam concentrations in plasma appears to be attributable to the inhibition of cytochrome P450 3A4 metabolism by nefazodone. Triazolam 16-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-118 7995001-1 1994 BACKGROUND: Triazolam is metabolized by CYP3A4 isozyme. Triazolam 12-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 7852841-10 1995 In cells from both control and endotoxemic rats, the effects of PAF on intracellular pH were inhibited by the specific PAF antagonist triazolam. Triazolam 134-143 PCNA clamp associated factor Rattus norvegicus 64-67 7852841-10 1995 In cells from both control and endotoxemic rats, the effects of PAF on intracellular pH were inhibited by the specific PAF antagonist triazolam. Triazolam 134-143 PCNA clamp associated factor Rattus norvegicus 119-122 7995001-2 1994 Ketoconazole and itraconazole may seriously interact with some of the substrates of CYP3A4 (e.g., terfenadine); hence their possible interaction with triazolam in humans is important to uncover. Triazolam 150-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 7995001-11 1994 Inhibition of CYP3A4 during the absorption and elimination phases of triazolam seems to explain the interaction observed. Triazolam 69-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 1329159-0 1992 [Changes in plasma cortisol and ACTH caused by diazepam, bromazepam, triazolam, and alprazolam in oral premedication]. Triazolam 69-78 proopiomelanocortin Homo sapiens 32-36 7871096-0 1994 Discriminating the effects of triazolam on stimulus and response processing by means of reaction time and P300 latency. Triazolam 30-39 E1A binding protein p300 Homo sapiens 106-110 7901754-2 1993 We found in this study that even the beta 2 gamma 2 subtype displays gamma-aminobutyric acid-induced Cl- currents that are potentiated by triazolam (a triazolobenzodiazepine). Triazolam 138-147 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 37-43 8396125-5 1993 The calcium response to PAF, which was largely due to mobilization of calcium from intracellular stores, was found to be dose-dependent in the nanomolar concentration range and inhibitable by the PAF receptor antagonist triazolam. Triazolam 220-229 PCNA clamp associated factor Rattus norvegicus 24-27 8396125-5 1993 The calcium response to PAF, which was largely due to mobilization of calcium from intracellular stores, was found to be dose-dependent in the nanomolar concentration range and inhibitable by the PAF receptor antagonist triazolam. Triazolam 220-229 PCNA clamp associated factor Rattus norvegicus 196-199 8383168-7 1993 In both cell types, triazolam and alprazolam, two PAF antagonists, and the calcium channel blocker verapamil inhibited PAF-induced calcium mobilization. Triazolam 20-29 PCNA clamp associated factor Homo sapiens 50-53 8383168-7 1993 In both cell types, triazolam and alprazolam, two PAF antagonists, and the calcium channel blocker verapamil inhibited PAF-induced calcium mobilization. Triazolam 20-29 PCNA clamp associated factor Homo sapiens 119-122 8448651-4 1993 Tz-induced Fos-labeled nuclei were found in superior colliculi, Edinger-Westphal nuclei (EW) and dorsal tegmental nuclei (DTg), but not in the RN. Triazolam 0-2 proto-oncogene c-Fos Mesocricetus auratus 11-14 1642641-2 1992 The clearance of quinidine, midazolam, triazolam, erythromycin, and lidocaine declines with age; these drugs are metabolized by the isoform, CYP3A. Triazolam 39-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-146 1324692-7 1992 PAF antagonists (WEB 2086, CV 3988, triazolam, and SRI 63,441) blocked the action of the four ether lipids on platelets, while SRI 63,441 blocked the antineoplastic activity of the ether lipids on WEHI-3B and HL-60 cells. Triazolam 36-45 patchy fur Mus musculus 0-3 2230061-4 1990 Triazolam-treated patients presented significantly more day-time-interdose anxiety than zopiclone as assessed by the weekly HARS and Clinical Global Assessment of Anxiety. Triazolam 0-9 histidyl-tRNA synthetase 1 Homo sapiens 124-128 1814557-5 1991 Given that hamsters bearing SCN grafts have limited neural connections between the host brain and transplanted SCN tissue, the results suggest that a site outside the SCN, with afferents to these nuclei, mediates the phase-shifting effect of Tz and of exercise. Triazolam 242-244 sorcin Homo sapiens 28-31 1814557-5 1991 Given that hamsters bearing SCN grafts have limited neural connections between the host brain and transplanted SCN tissue, the results suggest that a site outside the SCN, with afferents to these nuclei, mediates the phase-shifting effect of Tz and of exercise. Triazolam 242-244 sorcin Homo sapiens 111-114 1814557-5 1991 Given that hamsters bearing SCN grafts have limited neural connections between the host brain and transplanted SCN tissue, the results suggest that a site outside the SCN, with afferents to these nuclei, mediates the phase-shifting effect of Tz and of exercise. Triazolam 242-244 sorcin Homo sapiens 111-114 2356395-11 1990 Irrespective of the magnitude of the nocturnal elevation, morning PRL levels were slightly but consistently higher after triazolam treatment than under basal conditions. Triazolam 121-130 prolactin Homo sapiens 66-69 3579913-2 1987 The benzodiazepines alprazolam and triazolam, but not diazepam (1-10 microM), inhibit PAF induced aggregation but have no effect on aggregation induced by other platelet agonists such as ADP, epinephrine and collagen. Triazolam 35-44 PCNA clamp associated factor Homo sapiens 86-89 2519888-6 1989 In decreasing order of potency, the following PAF-acether antagonists inhibited the change in platelet cytosolic free calcium elicited by 10 nM PAF-acether: L-652,731, kadsurenone, triazolam, diltiazem and alprazolam. Triazolam 181-190 PCNA clamp associated factor Homo sapiens 46-49 2519888-6 1989 In decreasing order of potency, the following PAF-acether antagonists inhibited the change in platelet cytosolic free calcium elicited by 10 nM PAF-acether: L-652,731, kadsurenone, triazolam, diltiazem and alprazolam. Triazolam 181-190 PCNA clamp associated factor Homo sapiens 144-147 3251503-6 1988 Nocturnal alertness, as measured by subjective report and objective nap latency test, increased significantly following the use of triazolam, 0.25 and 0.50 mg, for the day sleep period. Triazolam 131-140 catenin beta like 1 Homo sapiens 68-71 3046952-4 1988 BN 52021 and another unrelated PAF antagonist, triazolam, partially reduced the restraint-stress-induced gastric damage in young female, but not male, rats. Triazolam 47-56 PCNA clamp associated factor Rattus norvegicus 31-34 2845442-1 1988 The abilities of 4 triazolobenzodiazepines, adinazolam, alprazolam, estazolam and triazolam, to inhibit thyrotropin-releasing hormone (TRH) receptor binding and to antagonize the narcoleptic effects of TRH were examined. Triazolam 82-91 thyrotropin releasing hormone receptor Homo sapiens 104-148 2845442-1 1988 The abilities of 4 triazolobenzodiazepines, adinazolam, alprazolam, estazolam and triazolam, to inhibit thyrotropin-releasing hormone (TRH) receptor binding and to antagonize the narcoleptic effects of TRH were examined. Triazolam 82-91 thyrotropin releasing hormone Homo sapiens 135-138 3694533-3 1987 The negative inotropic effect of PAF was, however, antagonized by drugs known to inhibit PAF-induced platelet aggregation: the order of relative potency was SRI 63-441 greater than CV-3988 greater than alprazolam greater than or equal to triazolam; i.e., the same order in which these compounds antagonize the effects of PAF on platelets. Triazolam 238-247 PCNA clamp associated factor Homo sapiens 33-36 3694533-3 1987 The negative inotropic effect of PAF was, however, antagonized by drugs known to inhibit PAF-induced platelet aggregation: the order of relative potency was SRI 63-441 greater than CV-3988 greater than alprazolam greater than or equal to triazolam; i.e., the same order in which these compounds antagonize the effects of PAF on platelets. Triazolam 238-247 PCNA clamp associated factor Homo sapiens 89-92 3694533-3 1987 The negative inotropic effect of PAF was, however, antagonized by drugs known to inhibit PAF-induced platelet aggregation: the order of relative potency was SRI 63-441 greater than CV-3988 greater than alprazolam greater than or equal to triazolam; i.e., the same order in which these compounds antagonize the effects of PAF on platelets. Triazolam 238-247 PCNA clamp associated factor Homo sapiens 89-92 35351776-13 2022 The canine CYP2B11 was found to appreciably contribute to hydroxylation of midazolam, alprazolam and triazolam, the well-known probes for human CYP3A. Triazolam 101-110 cytochrome P450 2B11 Canis lupus familiaris 11-18 35351776-13 2022 The canine CYP2B11 was found to appreciably contribute to hydroxylation of midazolam, alprazolam and triazolam, the well-known probes for human CYP3A. Triazolam 101-110 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-149 3579913-3 1987 The IC50 for aggregation by PAF (4 nM) in GFP is 1 microM for both alprazolam and triazolam. Triazolam 82-91 PCNA clamp associated factor Homo sapiens 28-31 3579913-7 1987 Alprazolam and triazolam, but not diazepam, caused competitive displacement of 3H-PAF from specific binding sites of GFP. Triazolam 15-24 PCNA clamp associated factor Homo sapiens 82-85 3579913-10 1987 These results are consistent with the interpretation that the specific inhibition of PAF induced platelet aggregation by alprazolam and triazolam, respectively, is due to competitive inhibition of binding of PAF to its receptor. Triazolam 136-145 PCNA clamp associated factor Homo sapiens 85-88 3579913-10 1987 These results are consistent with the interpretation that the specific inhibition of PAF induced platelet aggregation by alprazolam and triazolam, respectively, is due to competitive inhibition of binding of PAF to its receptor. Triazolam 136-145 PCNA clamp associated factor Homo sapiens 208-211 34013847-3 2021 The plasma concentrations ratios of alpha-hydroxytriazolam and 4-hydroxytriazolam to triazolam in portal blood were significantly decreased by multiple administration of clarithromycin in CYP3A-humanised mice.These results suggest that intestinal CYP3A activity was inhibited by macrolide antibiotics in CYP3A-humanised mice in vitro and in vivo. Triazolam 49-58 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 188-193 2893525-3 1987 We have found that the psychotropic triazolobenzodiazepine drugs, alprazolam and triazolam, potently (IC50 less than 1 microM) inhibit PAF-induced shape change, aggregation and secretion of human platelets. Triazolam 81-90 PCNA clamp associated factor Homo sapiens 135-138 6150550-3 1984 It was found that in washed human platelets the psychotropic triazolobenzodiazepine drugs alprazolam and triazolam potently inhibited PAF-induced changes in shape, aggregation, and secretion. Triazolam 105-114 PCNA clamp associated factor Homo sapiens 134-137 6142705-2 1984 Polarographic determination (DPP and CRP) of triazolam in plasma and serum]. Triazolam 45-54 C-reactive protein Homo sapiens 37-40 3587377-1 1987 The triazolodiazepines brotizolam, triazolam and alprazolam inhibited PAF-induced human platelet aggregation in vitro (IC50 = 0.54, 7.6 and 13.7 microM, respectively) but showed only a weak or no effect against other aggregating agents (ADP, adrenaline, collagen, serotonin, arachidonic acid). Triazolam 35-44 PCNA clamp associated factor Homo sapiens 70-73 3587377-4 1987 Brotizolam and triazolam also inhibited PAF-induced human neutrophil aggregation in vitro, with IC50-values 0.21 and 6.6 microM, respectively. Triazolam 15-24 PCNA clamp associated factor Homo sapiens 40-43 3587377-14 1987 Triazolam inhibited these effects of PAF at doses of 50 to 200 mg/kg p.o. Triazolam 0-9 PCNA clamp associated factor Homo sapiens 37-40 3587377-17 1987 In conclusion, these results show that triazolodiazepines, like brotizolam and triazolam, are potent inhibitors of PAF-induced effects in vitro and in vivo. Triazolam 79-88 PCNA clamp associated factor Homo sapiens 115-118 3081931-2 1986 We investigated, therefore, whether a single dose of triazolam, a short-acting benzodiazepine, and flurazepam, a long-acting one, could influence the response of prolactin (PRL), growth hormone (GH) and cortisol to a mild hypoglycemic stress in young healthy volunteers. Triazolam 53-62 prolactin Homo sapiens 162-171 3081931-2 1986 We investigated, therefore, whether a single dose of triazolam, a short-acting benzodiazepine, and flurazepam, a long-acting one, could influence the response of prolactin (PRL), growth hormone (GH) and cortisol to a mild hypoglycemic stress in young healthy volunteers. Triazolam 53-62 prolactin Homo sapiens 173-176 3081931-2 1986 We investigated, therefore, whether a single dose of triazolam, a short-acting benzodiazepine, and flurazepam, a long-acting one, could influence the response of prolactin (PRL), growth hormone (GH) and cortisol to a mild hypoglycemic stress in young healthy volunteers. Triazolam 53-62 growth hormone 1 Homo sapiens 179-193 2859867-0 1985 Coma caused by trivial triazolam overdose. Triazolam 23-32 COMA Homo sapiens 0-4 34013847-4 2021 The plasma concentrations of triazolam and its metabolites in the portal blood of CYP3A-humanised mice would be useful for direct evaluation of intestinal CYP3A-mediated drug-drug interactions. Triazolam 29-38 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 82-87 34013847-4 2021 The plasma concentrations of triazolam and its metabolites in the portal blood of CYP3A-humanised mice would be useful for direct evaluation of intestinal CYP3A-mediated drug-drug interactions. Triazolam 29-38 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 155-160 33959005-1 2021 In order to develop improved anxiolytic drugs, 8-substituted analogs of triazolam were synthesized in an effort to discover compounds with selectivity for alpha2/alpha3 subunit-containing GABAA subtypes. Triazolam 72-81 UDP glucuronosyltransferase 1 family, polypeptide A7C Rattus norvegicus 155-168 31455676-4 2019 Oral administration of the human PXR activator rifampicin increased hepatic expression of CYP3A4 mRNA and triazolam (TRZ) 1"- and 4-hydroxylation activities, CYP3A probe activities, in the liver and intestine microsomes of hCYP3A-MAC/hPXR mice. Triazolam 106-115 nuclear receptor subfamily 1 group I member 2 Homo sapiens 33-36 33863817-7 2021 In vivo CYP3A activity was monitored by measuring changes in the exposure of the CYP3A probe substrate triazolam. Triazolam 103-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-13 33863817-7 2021 In vivo CYP3A activity was monitored by measuring changes in the exposure of the CYP3A probe substrate triazolam. Triazolam 103-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 31455676-11 2019 Expression of CYP3A4 and metabolism of triazolam, a typical CYP3A substrate, in the liver of CYP3A/PXR-humanized mice were enhanced in response to rifampicin, a typical human PXR activator. Triazolam 39-48 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 60-65 33191904-5 2021 MATERIALS AND METHODS: An in silico DDI study was conducted using a population-based physiological pharmacokinetic simulator to estimate the CR of cytochrome P450 (CYP)3A4 for zolpidem, sildenafil, omeprazole, triazolam, and repaglinide. Triazolam 210-219 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-171 31455676-4 2019 Oral administration of the human PXR activator rifampicin increased hepatic expression of CYP3A4 mRNA and triazolam (TRZ) 1"- and 4-hydroxylation activities, CYP3A probe activities, in the liver and intestine microsomes of hCYP3A-MAC/hPXR mice. Triazolam 117-120 nuclear receptor subfamily 1 group I member 2 Homo sapiens 33-36 31455676-11 2019 Expression of CYP3A4 and metabolism of triazolam, a typical CYP3A substrate, in the liver of CYP3A/PXR-humanized mice were enhanced in response to rifampicin, a typical human PXR activator. Triazolam 39-48 nuclear receptor subfamily 1, group I, member 2 Mus musculus 99-102 31455676-5 2019 The plasma concentration of TRZ after oral dosing was significantly decreased by rifampicin treatment in hCYP3A-MAC/hPXR mice but not in hCYP3A-MAC mice. Triazolam 28-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 31455676-11 2019 Expression of CYP3A4 and metabolism of triazolam, a typical CYP3A substrate, in the liver of CYP3A/PXR-humanized mice were enhanced in response to rifampicin, a typical human PXR activator. Triazolam 39-48 nuclear receptor subfamily 1 group I member 2 Homo sapiens 175-178 31455676-6 2019 In addition, mass spectrometry imaging analysis showed that rifampicin treatment increased the formation of hydroxy TRZ in the intestine of hCYP3A-MAC/hPXR mice after oral dosing of TRZ. Triazolam 116-119 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 31455676-12 2019 Enhancement of triazolam metabolism in the intestine of CYP3A/PXR-humanized mice was firstly shown by combination of mass spectrometry imaging of sliced intestine and liquid chromatography with tandem mass spectrometry analysis of metabolite concentration in portal blood after oral dosing of triazolam. Triazolam 15-24 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 56-61 31455676-6 2019 In addition, mass spectrometry imaging analysis showed that rifampicin treatment increased the formation of hydroxy TRZ in the intestine of hCYP3A-MAC/hPXR mice after oral dosing of TRZ. Triazolam 182-185 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 31455676-12 2019 Enhancement of triazolam metabolism in the intestine of CYP3A/PXR-humanized mice was firstly shown by combination of mass spectrometry imaging of sliced intestine and liquid chromatography with tandem mass spectrometry analysis of metabolite concentration in portal blood after oral dosing of triazolam. Triazolam 15-24 nuclear receptor subfamily 1, group I, member 2 Mus musculus 62-65 31455676-11 2019 Expression of CYP3A4 and metabolism of triazolam, a typical CYP3A substrate, in the liver of CYP3A/PXR-humanized mice were enhanced in response to rifampicin, a typical human PXR activator. Triazolam 39-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 31455676-12 2019 Enhancement of triazolam metabolism in the intestine of CYP3A/PXR-humanized mice was firstly shown by combination of mass spectrometry imaging of sliced intestine and liquid chromatography with tandem mass spectrometry analysis of metabolite concentration in portal blood after oral dosing of triazolam. Triazolam 293-302 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 56-61 31455676-12 2019 Enhancement of triazolam metabolism in the intestine of CYP3A/PXR-humanized mice was firstly shown by combination of mass spectrometry imaging of sliced intestine and liquid chromatography with tandem mass spectrometry analysis of metabolite concentration in portal blood after oral dosing of triazolam. Triazolam 293-302 nuclear receptor subfamily 1, group I, member 2 Mus musculus 62-65 31455676-11 2019 Expression of CYP3A4 and metabolism of triazolam, a typical CYP3A substrate, in the liver of CYP3A/PXR-humanized mice were enhanced in response to rifampicin, a typical human PXR activator. Triazolam 39-48 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 14-19 28238899-3 2017 Montelukast and ketoconazole showed a potent and concentration-dependent inhibition of CYP2C8-mediated paclitaxel 6alpha-hydroxylation and CYP3A4-mediated triazolam alpha-hydroxylation, respectively, without dependence on the buffer condition. Triazolam 155-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 29172026-9 2018 A reduction of the enzymatic activity of the UGT2B7 was recorded in the presence of 9 of the 14 drugs under investigation (ketoconazole, miconazole, itraconazole, diclofenac, ibuprofen, clonazepam, lorazepam, lormetazepam, and triazolam), with a consequent significant reduction of the levels of the glucuronide metabolites. Triazolam 227-236 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 45-51 28393714-6 2017 CYP3A activity was determined as alpha- and 4-hydroxylation activity of triazolam in liver and intestinal microsomes. Triazolam 72-81 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 0-5 28393714-9 2017 RESULTS: The results showed that triazolam hydroxylation activities and protein levels of CYP3A in the liver were significantly higher in female than in male CYP3A-HAC mice, whereas those in the intestine were not significantly different between the genders. Triazolam 33-42 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 158-163 30561249-2 2019 To investigate cytochrome P450 3A (CYP3A)-mediated metabolism in vivo, plasma concentrations of triazolam (TRZ) are often monitored as a CYP3A marker in CYP3A-humanised mice. Triazolam 96-105 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 35-40 27489535-7 2016 In addition, decreased protein expression of GluR1 and GluR4, which are excitatory neurotransmitter receptors, was detected in the hippocampi of mice treated with TZ during the juvenile period. Triazolam 163-165 glutamate receptor, ionotropic, AMPA1 (alpha 1) Mus musculus 45-50 27323294-1 2016 Cytochrome P450 (P450) 3A (CYP3A) is an enzyme responsible for the metabolism of therapeutic drugs such as midazolam, nifedipine, testosterone and triazolam. Triazolam 147-156 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 0-25 27323294-1 2016 Cytochrome P450 (P450) 3A (CYP3A) is an enzyme responsible for the metabolism of therapeutic drugs such as midazolam, nifedipine, testosterone and triazolam. Triazolam 147-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 27489535-7 2016 In addition, decreased protein expression of GluR1 and GluR4, which are excitatory neurotransmitter receptors, was detected in the hippocampi of mice treated with TZ during the juvenile period. Triazolam 163-165 glutamate receptor, ionotropic, AMPA4 (alpha 4) Mus musculus 55-60 26290405-0 2016 Effect of buffer conditions on CYP2C8-mediated paclitaxel 6alpha-hydroxylation and CYP3A4-mediated triazolam alpha- and 4-hydroxylation by human liver microsomes. Triazolam 99-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 22659374-4 2012 Triazolam, which is a substrate of Cyp3a, was intraperitoneally administered to the mice in the HF group. Triazolam 0-9 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 35-40 25533998-9 2015 Ramelteon and triazolam significantly increased the time to complete of Trail-Making Test part A and the environmental area in posturography compared to placebo at 1 and 4 h post-dosing. Triazolam 14-23 TNF superfamily member 10 Homo sapiens 72-77 25657337-6 2015 In vitro triazolam 4-hydroxylation (probe reaction for CYP3A4) was reduced by >50% in hepatic microsomes from CYP3A4-HBN mice compared with controls. Triazolam 9-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 25657337-6 2015 In vitro triazolam 4-hydroxylation (probe reaction for CYP3A4) was reduced by >50% in hepatic microsomes from CYP3A4-HBN mice compared with controls. Triazolam 9-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-119 25657337-8 2015 This effect was confirmed by the concentration-dependent restoration of CYP3A4-mediated triazolam turnover and CYP2D6-mediated bufuralol and debrisoquine turnover on addition of Escherichia coli membranes containing recombinant Cyb5. Triazolam 88-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 25657337-9 2015 In vivo, the peak plasma concentration and area under the concentration time curve from 0 to 8 hours (AUC0-8 h) of triazolam were increased 4- and 5.7-fold, respectively, in CYP3A4-HBN mice. Triazolam 115-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 25359648-7 2014 However, patients taking anticoagulants or cytochrome P450 3A4 substrates (such as clarithromycin, erythromycin, ketoconazole, itraconazole, midazolam and triazolam) in addition to specific vitamin or mineral supplements (vitamins D, E, K, calcium, fluoride, iron, magnesium, selenium or zinc) may face additional challenges. Triazolam 155-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-62 25757928-2 2015 This study evaluated the effects of menthol on the pharmacokinetics of the CYP3A substrate triazolam and the CYP2C substrate phenytoin. Triazolam 91-100 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 75-80 25757928-4 2015 In addition, the CYP3A metabolic activity for triazolam and the CYP3A expression level in the liver were determined. Triazolam 46-55 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 17-22 24367698-7 2013 administration of both triazolam (0.03 mg/kg) and ZP (1.0 mg/kg) decreased BDNF protein levels within the HIP relative to vehicle, without any effect on c-Fos. Triazolam 23-32 brain derived neurotrophic factor Mus musculus 75-79 23282066-0 2013 Evaluation of animal models for intestinal first-pass metabolism of drug candidates to be metabolized by CYP3A enzymes via in vivo and in vitro oxidation of midazolam and triazolam. Triazolam 171-180 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 105-110 22943633-2 2013 METHODS: A 50:50 mixture of lowbush and highbush BBJ was evaluated in vitro as an inhibitor of CYP3A activity (hydroxylation of triazolam and dealkylation of buspirone) and of CYP2C9 activity (flurbiprofen hydroxylation) using human liver microsomes. Triazolam 128-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-100 21561794-4 2011 Results demonstrated that diazepam, triazolam, amitriptyline, mianserin, malathion, fenitrothion, chlorpyrifosmethyl, and probenecid significantly inhibited representative substrates of hOAT1 and para-aminohippuric acid uptake by hOAT1. Triazolam 36-45 solute carrier family 22 member 6 Homo sapiens 186-191 22447115-5 2012 The formation of metabolites from triazolam, diclofenac and SN-38 was strongly inhibited by co-treatment with a CYP3A inhibitor (ketoconazole), CYP2C9 inhibitor (sulfaphenazole) and UGT1A1 inhibitor (ketoconazole), respectively. Triazolam 34-43 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 144-150 22447115-5 2012 The formation of metabolites from triazolam, diclofenac and SN-38 was strongly inhibited by co-treatment with a CYP3A inhibitor (ketoconazole), CYP2C9 inhibitor (sulfaphenazole) and UGT1A1 inhibitor (ketoconazole), respectively. Triazolam 34-43 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 182-188 21561794-4 2011 Results demonstrated that diazepam, triazolam, amitriptyline, mianserin, malathion, fenitrothion, chlorpyrifosmethyl, and probenecid significantly inhibited representative substrates of hOAT1 and para-aminohippuric acid uptake by hOAT1. Triazolam 36-45 solute carrier family 22 member 6 Homo sapiens 230-235 20497744-3 2010 Triazolam is primarily metabolized by CYP3A and its plasma concentration is increased remarkably by itraconazole. Triazolam 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 20080160-9 2010 In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Triazolam 127-136 nuclear receptor subfamily 1 group I member 2 Homo sapiens 206-209 20080160-9 2010 In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Triazolam 127-136 aryl hydrocarbon receptor Homo sapiens 215-218 20080160-9 2010 In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Triazolam 127-136 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 253-259 20080160-9 2010 In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Triazolam 127-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 264-270 19752211-3 2009 Triazolam was used as a probe drug because it is a highly specific CYP3A substrate and not a P-glycoprotein substrate. Triazolam 0-9 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 67-72 19752211-4 2009 Triazolam metabolism was profoundly reduced in Cyp3a(-/-) mice both in vitro and in vivo. Triazolam 0-9 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 47-52 19752211-7 2009 To mimic a drug-drug interaction, we coadministered triazolam with the prototypical CYP3A inhibitor ketoconazole, which increased triazolam exposure in all the CYP3A-proficient mouse strains but not in Cyp3a(-/-) mice. Triazolam 52-61 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 160-165 19752211-7 2009 To mimic a drug-drug interaction, we coadministered triazolam with the prototypical CYP3A inhibitor ketoconazole, which increased triazolam exposure in all the CYP3A-proficient mouse strains but not in Cyp3a(-/-) mice. Triazolam 130-139 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 84-89