PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
24417241-6	2014	KEY RESULTS: Pre-exposure of cells to erythromycin resulted in an approximately 14-22-fold rightward shift in the hERG concentration-response curve for thioridazine and terfenadine respectively.	Terfenadine	169-180	ETS transcription factor ERG	Homo sapiens	114-118
24788058-3	2014	Of these, decursin noncompetitively inhibited CYP2J2-mediated astemizole O-demethylation and terfenadine hydroxylation activities with Ki values of 8.34 and 15.8muM, respectively.	Terfenadine	93-104	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	46-52
24048439-0	2014	Terfenadine induces anti-proliferative and apoptotic activities in human hormone-refractory prostate cancer through histamine receptor-independent Mcl-1 cleavage and Bak up-regulation.	Terfenadine	0-11	MCL1 apoptosis regulator, BCL2 family member	Homo sapiens	147-152
25366487-0	2014	Effect of terfenadine and pentamidine on the HERG channel and its intracellular trafficking: combined analysis with automated voltage clamp and confocal microscopy.	Terfenadine	10-21	potassium voltage-gated channel subfamily H member 2	Homo sapiens	45-49
25366487-1	2014	The effects of terfenadine and pentamidine on the human ether-a-go-go related gene (hERG) channel current and its intracellular trafficking were evaluated.	Terfenadine	15-26	ETS transcription factor ERG	Homo sapiens	84-88
25366487-4	2014	Terfenadine directly blocked the hERG channel current but had no effect on trafficking of hERG channels to the cell membrane after application in culture medium for 2 d. In contrast, pentamidine had no direct effect on the hERG channel current but reduced trafficking of hERG channels.	Terfenadine	0-11	ETS transcription factor ERG	Homo sapiens	33-37
25366487-5	2014	The two drugs inhibited hERG channel function through different mechanisms: terfenadine through direct channel blockade and pentamidine through inhibition of channel trafficking to the cell membrane.	Terfenadine	76-87	ETS transcription factor ERG	Homo sapiens	24-28
24048439-0	2014	Terfenadine induces anti-proliferative and apoptotic activities in human hormone-refractory prostate cancer through histamine receptor-independent Mcl-1 cleavage and Bak up-regulation.	Terfenadine	0-11	BCL2 antagonist/killer 1	Homo sapiens	166-169
24048439-5	2014	Terfenadine induced the cleavage of Mcl-1 cleavage into a pro-apoptotic 28-kDa fragment and up-regulation of Bak, resulting in the loss of mitochondrial membrane potential (DeltaPsim) and the release of cytochrome c and apoptosis-inducing factor into the cytosol.	Terfenadine	0-11	MCL1 apoptosis regulator, BCL2 family member	Homo sapiens	36-41
24048439-5	2014	Terfenadine induced the cleavage of Mcl-1 cleavage into a pro-apoptotic 28-kDa fragment and up-regulation of Bak, resulting in the loss of mitochondrial membrane potential (DeltaPsim) and the release of cytochrome c and apoptosis-inducing factor into the cytosol.	Terfenadine	0-11	BCL2 antagonist/killer 1	Homo sapiens	109-112
24048439-5	2014	Terfenadine induced the cleavage of Mcl-1 cleavage into a pro-apoptotic 28-kDa fragment and up-regulation of Bak, resulting in the loss of mitochondrial membrane potential (DeltaPsim) and the release of cytochrome c and apoptosis-inducing factor into the cytosol.	Terfenadine	0-11	cytochrome c, somatic	Homo sapiens	203-215
24048439-8	2014	Terfenadine also induced an indirect-but not direct-DNA damage response through the cleavage and activation of caspase-2, phosphorylation and activation of Chk1 and Chk2 kinases, phosphorylation of RPA32 and acetylation of Histone H3; these processes were highly correlated to severe mitochondrial dysfunction and the activation of caspase cascades.	Terfenadine	0-11	caspase 2	Homo sapiens	111-120
24048439-8	2014	Terfenadine also induced an indirect-but not direct-DNA damage response through the cleavage and activation of caspase-2, phosphorylation and activation of Chk1 and Chk2 kinases, phosphorylation of RPA32 and acetylation of Histone H3; these processes were highly correlated to severe mitochondrial dysfunction and the activation of caspase cascades.	Terfenadine	0-11	checkpoint kinase 1	Homo sapiens	156-160
24048439-8	2014	Terfenadine also induced an indirect-but not direct-DNA damage response through the cleavage and activation of caspase-2, phosphorylation and activation of Chk1 and Chk2 kinases, phosphorylation of RPA32 and acetylation of Histone H3; these processes were highly correlated to severe mitochondrial dysfunction and the activation of caspase cascades.	Terfenadine	0-11	checkpoint kinase 2	Homo sapiens	165-169
24048439-8	2014	Terfenadine also induced an indirect-but not direct-DNA damage response through the cleavage and activation of caspase-2, phosphorylation and activation of Chk1 and Chk2 kinases, phosphorylation of RPA32 and acetylation of Histone H3; these processes were highly correlated to severe mitochondrial dysfunction and the activation of caspase cascades.	Terfenadine	0-11	replication protein A2	Homo sapiens	198-203
24048439-10	2014	The exposure of cells to terfenadine caused the up-regulation and activation of Bak and the cleavage of Mcl-1, leading to the loss of DeltaPsim and activation of caspase cascades which further resulted in DNA damage response and cell apoptosis.	Terfenadine	25-36	BCL2 antagonist/killer 1	Homo sapiens	80-83
24048439-10	2014	The exposure of cells to terfenadine caused the up-regulation and activation of Bak and the cleavage of Mcl-1, leading to the loss of DeltaPsim and activation of caspase cascades which further resulted in DNA damage response and cell apoptosis.	Terfenadine	25-36	MCL1 apoptosis regulator, BCL2 family member	Homo sapiens	104-109
24120820-5	2013	Terfenadine also showed a limited solubility (measured concentrations ranging from 0.597 muM to 0.833 muM instead of 1 muM) and a loss of substance through the superfusion tubing from -30.2% to -39.2% with dimethylsulfoxide, ethanol or methanol.	Terfenadine	0-11	latexin	Homo sapiens	89-92
24021950-8	2013	Compared with recombinant CYP2J2, terfenadine was hydroxylated in cardiomyocytes at a similar K(m) value of 1.5 muM.	Terfenadine	34-45	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	26-32
24021950-9	2013	The V(max) of terfenadine hydroxylation in recombinant enzyme was found to be 29.4 pmol/pmol P450 per minute and in the cells 6.0 pmol/pmol P450 per minute.	Terfenadine	14-25	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	93-97
24021950-9	2013	The V(max) of terfenadine hydroxylation in recombinant enzyme was found to be 29.4 pmol/pmol P450 per minute and in the cells 6.0 pmol/pmol P450 per minute.	Terfenadine	14-25	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	140-144
24120820-5	2013	Terfenadine also showed a limited solubility (measured concentrations ranging from 0.597 muM to 0.833 muM instead of 1 muM) and a loss of substance through the superfusion tubing from -30.2% to -39.2% with dimethylsulfoxide, ethanol or methanol.	Terfenadine	0-11	latexin	Homo sapiens	102-105
24120820-5	2013	Terfenadine also showed a limited solubility (measured concentrations ranging from 0.597 muM to 0.833 muM instead of 1 muM) and a loss of substance through the superfusion tubing from -30.2% to -39.2% with dimethylsulfoxide, ethanol or methanol.	Terfenadine	0-11	latexin	Homo sapiens	102-105
24120820-6	2013	Terfenadine solubility was improved with 2-hydroxypropyl-beta-cyclodextrin, no adsorption was observed, but its capacity to block the hERG channel was decreased.	Terfenadine	0-11	ETS transcription factor ERG	Homo sapiens	134-138
23221912-6	2013	In this study, we show that block of WT HERG by bepridil and terfenadine, two drugs previously shown to be trapped inside the HERG channel after the channel closes, is insensitive to extracellular potassium over the range of 0 mM to 20 mM.	Terfenadine	61-72	potassium voltage-gated channel subfamily H member 2	Homo sapiens	40-44
23518063-9	2013	Three compounds (dofetilide, sertindole, and terfenadine) showed >10-fold discrepancy between hERG potency and inhibitory concentrations in the hESC-CM and IRH assays.	Terfenadine	45-56	ETS transcription factor ERG	Homo sapiens	97-101
23221912-6	2013	In this study, we show that block of WT HERG by bepridil and terfenadine, two drugs previously shown to be trapped inside the HERG channel after the channel closes, is insensitive to extracellular potassium over the range of 0 mM to 20 mM.	Terfenadine	61-72	potassium voltage-gated channel subfamily H member 2	Homo sapiens	126-130
22300168-5	2012	KEY RESULTS: Terfenadine concentration- and use-dependently inhibited I(Na) in rabbit myocytes and in human atrial myocytes and also inhibited the hERG.	Terfenadine	13-24	ETS transcription factor ERG	Homo sapiens	147-151
22498908-5	2012	The treatment of the cells with hERG channel inhibitors such as nifekalant, E-4031, cisapride, terfenadine, and verapamil, recovered the prolonged AP and dose-dependently facilitated cell death upon ES.	Terfenadine	95-106	ETS transcription factor ERG	Homo sapiens	32-36
24296992-7	2013	Infusion of 1 muM Dofetilide and 10 muM Terfenadine prolonged field potentials 10 fold and 2 fold, respectively.	Terfenadine	40-51	latexin	Homo sapiens	36-39
23688135-8	2013	Additionally, specific inhibitors of CYP2J2, derived from terfenadine, exhibit strong anti-tumor activity in vitro and in vivo.	Terfenadine	58-69	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	37-43
23103595-11	2013	Astemizole, terfenadine and quinidine inhibited hERG currents with IC(50) values of 159nM, 224nM and 2muM, respectively (n=51, 10 and 18).	Terfenadine	12-23	ETS transcription factor ERG	Homo sapiens	48-52
22418875-11	2012	The histamine H1 receptor antagonist terfenadine prevented scratching and alloknesis evoked by histamine, but not 5-HT, a PAR-4 agonist or an MrgprC11 agonist.	Terfenadine	37-48	histamine receptor H1	Mus musculus	4-25
22418875-11	2012	The histamine H1 receptor antagonist terfenadine prevented scratching and alloknesis evoked by histamine, but not 5-HT, a PAR-4 agonist or an MrgprC11 agonist.	Terfenadine	37-48	coagulation factor II (thrombin) receptor-like 3	Mus musculus	122-127
22418875-11	2012	The histamine H1 receptor antagonist terfenadine prevented scratching and alloknesis evoked by histamine, but not 5-HT, a PAR-4 agonist or an MrgprC11 agonist.	Terfenadine	37-48	MAS-related GPR, member X1	Mus musculus	142-150
22616812-2	2012	Further, clinically significant interactions with inhibitors of cytochrome P450 (CYP) have previously been reported for drugs of this therapeutic group, such as terfenadine and astemizole, indicating the possibility of drug-drug interactions involving agents that share the same metabolic pathway.	Terfenadine	161-172	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	64-79
22616812-2	2012	Further, clinically significant interactions with inhibitors of cytochrome P450 (CYP) have previously been reported for drugs of this therapeutic group, such as terfenadine and astemizole, indicating the possibility of drug-drug interactions involving agents that share the same metabolic pathway.	Terfenadine	161-172	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	81-84
20847137-3	2010	In this study, catalytic activities of the two alleles found in East Asians, CYP3A4*16 (T185S) and CYP3A4*18 (L293P), were assessed using the following seven substrates: midazolam, carbamazepine, atorvastatin, paclitaxel, docetaxel, irinotecan, and terfenadine.	Terfenadine	249-260	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	77-83
21477627-9	2011	Importantly, soluble epoxide hydrolase (sEH) inhibitors are anti-hypertensive and anti-inflammatory and, therefore, protect the heart from damage, whereas the terfenadine-related, specific inhibitors of CYP2J2 exhibit strong anti-tumor activity in vitro and in vivo.	Terfenadine	159-170	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	203-209
22328583-6	2012	To identify a specific CYP2J2 inhibitor, 138 drugs were screened using terfenadine and astemizole as probe substrates with recombinant CYP2J2.	Terfenadine	71-82	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	23-29
21861192-3	2011	Serum-deprived conditions enhance the cytotoxic effect of terfenadine and caspase-4 and -2 are activated upstream of caspase-9.	Terfenadine	58-69	caspase 9	Homo sapiens	117-126
21624711-7	2011	Docking and molecular mechanics simulations for both enantiomers of bupivacaine and terfenadine (a non-stereoselective blocker) were performed inside an open-state model of the hERG channel.	Terfenadine	84-95	ETS transcription factor ERG	Homo sapiens	177-181
20847137-3	2010	In this study, catalytic activities of the two alleles found in East Asians, CYP3A4*16 (T185S) and CYP3A4*18 (L293P), were assessed using the following seven substrates: midazolam, carbamazepine, atorvastatin, paclitaxel, docetaxel, irinotecan, and terfenadine.	Terfenadine	249-260	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	99-105
20847137-6	2010	On the other hand, K(m) values for CYP3A4.18 were comparable to those for CYP3A4.1 for all substrates except terfenadine; but V(max) values were lower for midazolam, paclitaxel, docetaxel, and irinotecan, resulting in partially reduced intrinsic clearance values (by 34-52%).	Terfenadine	109-120	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	35-41
20847137-6	2010	On the other hand, K(m) values for CYP3A4.18 were comparable to those for CYP3A4.1 for all substrates except terfenadine; but V(max) values were lower for midazolam, paclitaxel, docetaxel, and irinotecan, resulting in partially reduced intrinsic clearance values (by 34-52%).	Terfenadine	109-120	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	74-80
19923256-1	2010	Several antihistamine drugs including terfenadine, ebastine, and astemizole have been identified as substrates for CYP2J2.	Terfenadine	38-49	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	115-121
20153443-7	2010	RESULTS: AP prolongation was observed upon exposure to hERG channel blockers (terfenadine, quinidine, cisapride, sotalol, E-4031 and verapamil), with significantly shorter latencies than in PF assays.	Terfenadine	78-89	ETS transcription factor ERG	Homo sapiens	55-59
20071423-2	2010	The aim of the present study was to characterize possible interactions between terfenadine, binding to a site located inside the central cavity, and the following substances with various binding sites: dofetilide, fluvoxamine, chlorobutanol, and a hERG-specific toxin isolated from scorpion venom (CnErg1).	Terfenadine	79-90	ETS transcription factor ERG	Homo sapiens	248-252
20071423-5	2010	Slight subadditive inhibitory effects on hERG peak tail currents were observed when terfenadine and CnErg1 were administered in combination.	Terfenadine	84-95	ETS transcription factor ERG	Homo sapiens	41-45
20071423-6	2010	Terfenadine and chlorobutanol synergistically inhibit hERG peak tail currents and enhance each other"s inhibitory effect in a concentration-dependent way.	Terfenadine	0-11	ETS transcription factor ERG	Homo sapiens	54-58
20071423-7	2010	In conclusion, terfenadine interacts with CnErg1 and chlorobutanol, but not with dofetilide or fluvoxamine, at hERG channels.	Terfenadine	15-26	ETS transcription factor ERG	Homo sapiens	111-115
20071423-8	2010	It is shown that interactions between chlorobutanol and a hERG channel blocker binding inside the central cavity (terfenadine) produce synergistic effects on hERG currents.	Terfenadine	114-125	ETS transcription factor ERG	Homo sapiens	58-62
20071423-8	2010	It is shown that interactions between chlorobutanol and a hERG channel blocker binding inside the central cavity (terfenadine) produce synergistic effects on hERG currents.	Terfenadine	114-125	ETS transcription factor ERG	Homo sapiens	158-162
20104563-6	2010	We docked the known hERG inhibitors (+)-cisapride, (S)-terfenadine, and MK-499 into the hERG models and simulation snapshots.	Terfenadine	51-66	ETS transcription factor ERG	Homo sapiens	20-24
20104563-6	2010	We docked the known hERG inhibitors (+)-cisapride, (S)-terfenadine, and MK-499 into the hERG models and simulation snapshots.	Terfenadine	51-66	ETS transcription factor ERG	Homo sapiens	88-92
18701618-3	2008	Four high-affinity drugs (cisapride, dofetilide, terfenadine, and astemizole) demonstrated lower affinity for the inactivation-deficient N588K mutant hERG channel compared with N588E and wild-type hERG.	Terfenadine	49-60	ETS transcription factor ERG	Homo sapiens	150-154
19426697-5	2009	We also evaluated the potency of these analogs on an S6 mutant of hERG (F656A) previously shown to significantly reduce the affinity for MK-499 and other known hERG antagonists (e.g. cisapride, terfenadine).	Terfenadine	194-205	ETS transcription factor ERG	Homo sapiens	66-70
19775279-1	2010	Following reports of death from cardiac arrhythmias with drugs like terfenadine and cisapride, the International Conference for Harmonization formulated a guidance (E14) document.	Terfenadine	68-79	nuclear protein, coactivator of histone transcription	Homo sapiens	165-168
19289568-0	2009	Selective inhibitors of CYP2J2 related to terfenadine exhibit strong activity against human cancers in vitro and in vivo.	Terfenadine	42-53	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	24-30
19289568-3	2009	In the present study, we tested the hypothesis that specific inhibitors of CYP2J2 related to the drug terfenadine are effective antitumor agents.	Terfenadine	102-113	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	75-81
18701618-3	2008	Four high-affinity drugs (cisapride, dofetilide, terfenadine, and astemizole) demonstrated lower affinity for the inactivation-deficient N588K mutant hERG channel compared with N588E and wild-type hERG.	Terfenadine	49-60	ETS transcription factor ERG	Homo sapiens	197-201
18508907-13	2008	Small (but not large) cholangiocytes proliferate in response to HTMT dimaleate and are blocked by terfenadine (HRH1 antagonist), BAPTA/AM, and W7.	Terfenadine	98-109	histamine receptor H1	Mus musculus	111-115
18987434-0	2008	Molecular determinants of hERG channel block by terfenadine and cisapride.	Terfenadine	48-59	ETS transcription factor ERG	Homo sapiens	26-30
18987434-1	2008	Block of cardiac hERG K+ channels by the antihistamine terfenadine and the prokinetic agent cisapride is associated with prolonged ventricular repolarization and an increased risk of ventricular arrhythmia.	Terfenadine	55-66	ETS transcription factor ERG	Homo sapiens	17-21
18987434-2	2008	Here, we used a site-directed mutagenesis approach to determine the molecular determinants of hERG block by terfenadine and cisapride.	Terfenadine	108-119	ETS transcription factor ERG	Homo sapiens	94-98
18560330-0	2008	Identification of terfenadine as an inhibitor of human CD81-receptor HCV-E2 interaction: synthesis and structure optimization.	Terfenadine	18-29	CD81 molecule	Homo sapiens	55-59
18560330-1	2008	Terfenadine (4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-(4-tert-butylphenyl)-butan-1-ol) was identified in a biological screening to be a moderate inhibitor (27% inhibition) of the CD81-LEL-HCV-E2 interaction.	Terfenadine	0-11	CD81 molecule	Homo sapiens	182-186
18974610-3	2008	Ketoconazole strongly inhibited CYP3A4-mediated terfenadine metabolism in vitro, and the method predicted 6- to 37-fold increase of terfenadine AUC by the concomitant dosing of ketoconazole, which reasonably well agreed with the observed 13- to 59-fold increase of AUC in clinical studies.	Terfenadine	48-59	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	32-38
18174239-5	2008	In addition, we have observed that knocking down the H1 histamine receptor (HRH1) by small interference RNA approach protects melanoma cells only slightly from TEF-induced apoptosis.	Terfenadine	160-163	histamine receptor H1	Homo sapiens	76-80
18974610-3	2008	Ketoconazole strongly inhibited CYP3A4-mediated terfenadine metabolism in vitro, and the method predicted 6- to 37-fold increase of terfenadine AUC by the concomitant dosing of ketoconazole, which reasonably well agreed with the observed 13- to 59-fold increase of AUC in clinical studies.	Terfenadine	132-143	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	32-38
17767395-1	2007	Fexofenadine, an active metabolite of the second-generation histamine H1 receptor antagonist (antihistamine) terfenadine, does not have the disadvantage of QT prolongation.	Terfenadine	109-120	histamine receptor H1	Homo sapiens	60-81
17470359-1	2007	Twenty five derivatives of the drugs terfenadine and ebastine have been designed, synthesized and evaluated as inhibitors of recombinant human CYP2J2.	Terfenadine	37-48	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	143-149
17355118-2	2007	G1 PAMAM dendrimer-based prodrugs of the water-insoluble P-gp substrate terfenadine (Ter) were synthesized using succinic acid (suc) or succinyl-diethylene glycol (suc-deg) as a linker/spacer (to yield G1-suc-Ter and G1-suc-deg-Ter, respectively).	Terfenadine	72-83	ATP binding cassette subfamily B member 1	Homo sapiens	57-61
17355118-2	2007	G1 PAMAM dendrimer-based prodrugs of the water-insoluble P-gp substrate terfenadine (Ter) were synthesized using succinic acid (suc) or succinyl-diethylene glycol (suc-deg) as a linker/spacer (to yield G1-suc-Ter and G1-suc-deg-Ter, respectively).	Terfenadine	85-88	ATP binding cassette subfamily B member 1	Homo sapiens	57-61
17180728-8	2007	The second generation antihistamines terfenadine and loratadine, achieved substantial brain penetration, which was further enhanced by Pgp inhibition by cyclosporin A (CSA).	Terfenadine	37-48	PGP	Canis lupus familiaris	135-138
15684493-3	2005	This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for the degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased.	Terfenadine	145-156	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	69-88
17078945-8	2006	At a concentration of 1 muM, terfenadine significantly increased the spontaneous Na-Ca exchange current (I(NCX)) frequency from 0.48+/-0.25 to 1.93+/-0.67 s(-1).	Terfenadine	29-40	T cell leukemia homeobox 2	Homo sapiens	107-110
16569656-6	2006	Treatment of melanoma cells with terfenadine induced DNA damage and caspases 2, 3, 6, 8 and 9 activation.	Terfenadine	33-44	caspase 2	Homo sapiens	68-93
16569656-7	2006	Furthermore, the general caspase inhibitor (z-VAD-FMK) and a selective inhibitor of caspase-2 (z-VDVAD-FMK) protected melanoma cells from terfenadine-induced apoptosis.	Terfenadine	138-149	caspase 2	Homo sapiens	84-93
16495056-2	2006	This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with K(i) values as low as 160nM, that should be useful tools to determine the biological roles of CYP2J2.	Terfenadine	100-111	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	62-68
16495056-2	2006	This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with K(i) values as low as 160nM, that should be useful tools to determine the biological roles of CYP2J2.	Terfenadine	100-111	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	212-218
15684493-3	2005	This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for the degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased.	Terfenadine	145-156	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	90-96
15762770-11	2005	For example, when aforementioned CYP3A4 inhibitors are coadministered with terfenadine, cisapride or astemizole (all CYP3A4 substrates), torsades de pointes (a life-threatening ventricular arrhythmia associated with QT prolongation) may occur.However, predicting drug-drug interactions involving CYP3A4 inactivation is difficult, since the clinical outcomes depend on a number of factors that are associated with drugs and patients.	Terfenadine	75-86	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	33-39
15133245-3	2004	This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased.	Terfenadine	141-152	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	69-88
15304429-6	2004	This small magnitude in change is in contrast to drugs primarily cleared by cytochrome P450 enzymes, where exposures have been reported to increase as much as 35-fold on coadministration with an inhibitor (e.g., ketoconazole inhibition of CYP3A4-catalyzed terfenadine metabolism).	Terfenadine	256-267	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	239-245
15331914-7	2004	Finally, terfenadine had a brain-to-plasma ratio of 2.21 +/- 1.00 even though it underwent Pgp-mediated efflux (in vitro ratio = 2.88).	Terfenadine	9-20	ATP-binding cassette, subfamily B (MDR/TAP), member 1B	Rattus norvegicus	91-94
15331914-8	2004	Terfenadine"s high passive permeability (285 nm/s) overcame the Pgp-mediated efflux to yield brain-to-plasma ratio >1.	Terfenadine	0-11	ATP-binding cassette, subfamily B (MDR/TAP), member 1B	Rattus norvegicus	64-67
15272206-5	2004	Binding affinities for 32 reference compounds (including dofetilide, cisapride, and terfenadine) with diverse structures demonstrated a similar potency rank order for HERG inhibition to that reported in the literature.	Terfenadine	84-95	potassium voltage-gated channel subfamily H member 2	Homo sapiens	167-171
16050267-7	2005	Our findings suggest that the position of Tyr652 and Phe656 in hERG is optimal for interaction with multiple drugs, Tyr652 is an important determinant of voltage-dependent block, and the hydrophobic surface area of residue 656 and aromaticity of residue 652 are the physicochemical features required for high-affinity block by MK-499, cisapride and terfenadine.	Terfenadine	349-360	ETS transcription factor ERG	Homo sapiens	63-67
15288570-4	2004	Terfenadine stimulated caspase-8, -9 and -3-like activities in an incubation time-dependent manner in thymocytes.	Terfenadine	0-11	caspase 8	Rattus norvegicus	23-43
15288570-5	2004	The active forms of caspase-3 and -9 were detected in the extract from terfenadine-treated cells by immunoblotting analysis using specific antibodies to caspases, but active caspase-8 was not found in this fraction.	Terfenadine	71-82	caspase 3	Rattus norvegicus	20-36
15288570-5	2004	The active forms of caspase-3 and -9 were detected in the extract from terfenadine-treated cells by immunoblotting analysis using specific antibodies to caspases, but active caspase-8 was not found in this fraction.	Terfenadine	71-82	caspase 8	Rattus norvegicus	153-161
15133245-3	2004	This might be because concomitant drugs such as itraconazole inhibit cytochrome P450 3A4 (CYP3A4), the enzyme responsible for degradation of terfenadine and astemizole, and thus the blood concentrations of the drugs are abnormally increased.	Terfenadine	141-152	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	90-96
12925206-0	2003	Terfenadine antagonism against interleukin-4-modulated gene expression of T cell cytokines.	Terfenadine	0-11	interleukin 4	Homo sapiens	31-44
14709917-5	2004	Terfenadine 1 microM completely inhibited the human ether a go-go-related gene (HERG) channel current expressed in HEK293 cells in the same experimental solution as in microelectrode experiments.	Terfenadine	0-11	potassium voltage-gated channel subfamily H member 2	Homo sapiens	80-84
14570767-8	2003	Mechanism-based inhibition of CYP1A2 may explain why zileuton decreases the oral clearance of antipyrine, propranolol, (R)-warfarin, and theophylline, at doses that have a minimal effect on the pharmacokinetics of (S)-warfarin, phenytoin, and terfenadine.	Terfenadine	243-254	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	30-36
12925206-6	2003	Electrophoretic mobility shift assays using [32P]-labeled synthetic oligonucleotides encoding the consensus binding motif of activator protein-1 demonstrated that interleukin-4-induced binding of activator protein-1 composed of JunB was interfered by terfenadine.	Terfenadine	251-262	JunB proto-oncogene, AP-1 transcription factor subunit	Homo sapiens	125-144
12925206-6	2003	Electrophoretic mobility shift assays using [32P]-labeled synthetic oligonucleotides encoding the consensus binding motif of activator protein-1 demonstrated that interleukin-4-induced binding of activator protein-1 composed of JunB was interfered by terfenadine.	Terfenadine	251-262	interleukin 4	Homo sapiens	163-176
12925206-6	2003	Electrophoretic mobility shift assays using [32P]-labeled synthetic oligonucleotides encoding the consensus binding motif of activator protein-1 demonstrated that interleukin-4-induced binding of activator protein-1 composed of JunB was interfered by terfenadine.	Terfenadine	251-262	JunB proto-oncogene, AP-1 transcription factor subunit	Homo sapiens	196-215
12925206-1	2003	Here, we investigated whether an anti-allergy drug, terfenadine, affects interleukin-4-modulated cytokine expression in peripheral T cells.	Terfenadine	52-63	interleukin 4	Homo sapiens	73-86
12925206-6	2003	Electrophoretic mobility shift assays using [32P]-labeled synthetic oligonucleotides encoding the consensus binding motif of activator protein-1 demonstrated that interleukin-4-induced binding of activator protein-1 composed of JunB was interfered by terfenadine.	Terfenadine	251-262	JunB proto-oncogene, AP-1 transcription factor subunit	Homo sapiens	228-232
12925206-7	2003	This study indicates that terfenadine, at least partially, interferes with interleukin-4-activated signaling, leading to terfenadine antagonism against the modulatory impact of interleukin-4 on T cell cytokines.	Terfenadine	26-37	interleukin 4	Homo sapiens	75-88
12925206-4	2003	Interestingly, the interleukin-4-induced expression of all T helper 2 cytokines examined was markedly downregulated by terfenadine.	Terfenadine	119-130	interleukin 4	Homo sapiens	19-32
12925206-7	2003	This study indicates that terfenadine, at least partially, interferes with interleukin-4-activated signaling, leading to terfenadine antagonism against the modulatory impact of interleukin-4 on T cell cytokines.	Terfenadine	26-37	interleukin 4	Homo sapiens	177-190
12925206-7	2003	This study indicates that terfenadine, at least partially, interferes with interleukin-4-activated signaling, leading to terfenadine antagonism against the modulatory impact of interleukin-4 on T cell cytokines.	Terfenadine	121-132	interleukin 4	Homo sapiens	75-88
12860441-0	2003	H1-receptor blocker antihistamine, terfenadine durably influences the glucocorticoid receptor, and lymphocyte histamine content of weanling rats.	Terfenadine	35-46	nuclear receptor subfamily 3, group C, member 1	Rattus norvegicus	70-93
12948015-9	2003	The rank order in P-gp inhibitory potency for terfenadine, verapamil, ritonavir.	Terfenadine	46-57	ATP binding cassette subfamily B member 1	Homo sapiens	18-22
15618727-0	2003	Substrate dependent inhibition profiles of fourteen drugs on CYP3A4 activity measured by a high throughput LCMS/MS method with four probe drugs, midazolam, testosterone, nifedipine and terfenadine.	Terfenadine	185-196	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	61-67
12720299-1	2003	Terfenadine (TF), a highly potent histamine H1 receptor antagonist, has been shown to exert no significant central nervous system side effects in clinically effective doses.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	34-55
12720299-1	2003	Terfenadine (TF), a highly potent histamine H1 receptor antagonist, has been shown to exert no significant central nervous system side effects in clinically effective doses.	Terfenadine	13-15	histamine receptor H1	Homo sapiens	34-55
12388285-5	2003	Astemizole, terfenadine, cisapride, and MK-499 inhibited cERG and human ERG (hERG) currents with IC(50) values of 1.3, 13, 19, and 15 nM and 1.2, 9, 14, and 21 nM, respectively, and competitively displaced [(35)S]MK-499 binding from cERG and hERG with IC(50) values of 0.4, 12, 35, and 0.6 nM and 0.8, 5, 47, and 0.7 nM, respectively.	Terfenadine	12-23	potassium voltage-gated channel subfamily H member 2	Canis lupus familiaris	57-61
12388285-5	2003	Astemizole, terfenadine, cisapride, and MK-499 inhibited cERG and human ERG (hERG) currents with IC(50) values of 1.3, 13, 19, and 15 nM and 1.2, 9, 14, and 21 nM, respectively, and competitively displaced [(35)S]MK-499 binding from cERG and hERG with IC(50) values of 0.4, 12, 35, and 0.6 nM and 0.8, 5, 47, and 0.7 nM, respectively.	Terfenadine	12-23	ETS transcription factor ERG	Homo sapiens	58-61
12388285-5	2003	Astemizole, terfenadine, cisapride, and MK-499 inhibited cERG and human ERG (hERG) currents with IC(50) values of 1.3, 13, 19, and 15 nM and 1.2, 9, 14, and 21 nM, respectively, and competitively displaced [(35)S]MK-499 binding from cERG and hERG with IC(50) values of 0.4, 12, 35, and 0.6 nM and 0.8, 5, 47, and 0.7 nM, respectively.	Terfenadine	12-23	ETS transcription factor ERG	Homo sapiens	77-81
12388285-5	2003	Astemizole, terfenadine, cisapride, and MK-499 inhibited cERG and human ERG (hERG) currents with IC(50) values of 1.3, 13, 19, and 15 nM and 1.2, 9, 14, and 21 nM, respectively, and competitively displaced [(35)S]MK-499 binding from cERG and hERG with IC(50) values of 0.4, 12, 35, and 0.6 nM and 0.8, 5, 47, and 0.7 nM, respectively.	Terfenadine	12-23	potassium voltage-gated channel subfamily H member 2	Canis lupus familiaris	233-237
12388285-5	2003	Astemizole, terfenadine, cisapride, and MK-499 inhibited cERG and human ERG (hERG) currents with IC(50) values of 1.3, 13, 19, and 15 nM and 1.2, 9, 14, and 21 nM, respectively, and competitively displaced [(35)S]MK-499 binding from cERG and hERG with IC(50) values of 0.4, 12, 35, and 0.6 nM and 0.8, 5, 47, and 0.7 nM, respectively.	Terfenadine	12-23	ETS transcription factor ERG	Homo sapiens	242-246
11878205-6	2002	Azelastine and terfenadine inhibited TNF alpha release with IC50 values of 6.2 mumol/l and 4.3 mumol/l, respectively.	Terfenadine	15-26	tumor necrosis factor	Homo sapiens	37-46
12365197-0	2002	Effects of terfenadine and diphenhydramine on the CYP2D6 activity in healthy volunteers.	Terfenadine	11-22	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	50-56
12365197-1	2002	The aim of this study was to investigate the effects of two antihistaminic drugs, terfenadine and diphenhydramine on CYP2D6 activity by using debrisoquine as a model substrate.	Terfenadine	82-93	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	117-123
15618707-2	2002	The effect of addition of rat liver cytosol to an in vitro system using human liver microsomes was examined by measuring the catalytic activities of CYP2C9 (tolbutamide and diclofenac) and CYP3A4 (terfenadine).	Terfenadine	197-208	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	189-195
15618707-4	2002	After addition of rat liver cytosol, the unbound Km value (Km,u) for terfenadine metabolism by CYP3A4, and the unbound Ki value of miconazole (Ki,u) for CYP2C9 were smaller than for the controls.	Terfenadine	69-80	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	95-101
15618707-5	2002	Addition of HSA resulted in smaller Km,u values for diclofenac and terfenadine metabolism by CYP2C9 and CYP3A4, respectively, and the Ki,u value for ketoconazole inhibition of CYP3A4 was also reduced.	Terfenadine	67-78	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	93-99
15618695-7	2002	In contrast, the inhibitory effects of phenacetin, diclofenac, S-mephenytoin, dextromethorphan, bufuralol and terfenadine, typical substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, respectively, on each recombinant CYP activity decreased after preincubation.	Terfenadine	110-121	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	146-152
15618707-5	2002	Addition of HSA resulted in smaller Km,u values for diclofenac and terfenadine metabolism by CYP2C9 and CYP3A4, respectively, and the Ki,u value for ketoconazole inhibition of CYP3A4 was also reduced.	Terfenadine	67-78	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	104-110
15618695-7	2002	In contrast, the inhibitory effects of phenacetin, diclofenac, S-mephenytoin, dextromethorphan, bufuralol and terfenadine, typical substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, respectively, on each recombinant CYP activity decreased after preincubation.	Terfenadine	110-121	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	154-160
12244568-0	2002	Ketoconazole potentiates terfenadine-induced apoptosis in human Hep G2 cells through inhibition of cytochrome p450 3A4 activity.	Terfenadine	25-36	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	99-118
12244568-1	2002	Terfenadine (TF) is a highly potent histamine H1 receptor antagonist that in clinically effective doses is free of significant central nervous system side effects.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	36-57
12244568-1	2002	Terfenadine (TF) is a highly potent histamine H1 receptor antagonist that in clinically effective doses is free of significant central nervous system side effects.	Terfenadine	13-15	histamine receptor H1	Homo sapiens	36-57
10730552-1	2000	UNLABELLED: Fexofenadine, the active metabolite of terfenadine, is a selective histamine H1 receptor antagonist that does not cross the blood brain barrier and appears to display some anti-inflammatory properties.	Terfenadine	51-62	histamine receptor H1	Homo sapiens	79-100
11240972-1	2001	BACKGROUND AND OBJECTIVE: Nefazodone inhibits CYP3A; therefore coadministration with CYP3A substrates such as terfenadine or loratadine may result in increased exposure to these drugs.	Terfenadine	110-121	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	46-51
11240972-1	2001	BACKGROUND AND OBJECTIVE: Nefazodone inhibits CYP3A; therefore coadministration with CYP3A substrates such as terfenadine or loratadine may result in increased exposure to these drugs.	Terfenadine	110-121	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	85-90
11259984-9	2001	These differences in P450 isozymes involved in the metabolism of astemizole and terfenadine may associate with distinct pharmacokinetic influences observed with coadministration of drugs metabolized by CYP3A4.	Terfenadine	80-91	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	202-208
18034580-3	2000	The 2 initial second generation less sedating antihistamines, astemizole and terfenadine, were found to prolong the cardiac QT(c) interval, especially when administered with other medications metabolised by the same cytochrome (CYP) P450 isoenzyme, CYP3A4.	Terfenadine	77-88	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	249-255
11032986-1	2000	We previously reported that the histamine H1 receptor antagonist terfenadine enhances the excitotoxic response to N-methyl-D-aspartate (NMDA) receptor agonists in cerebellar neurons.	Terfenadine	65-76	histamine receptor H1	Homo sapiens	32-53
10752642-3	2000	During clinical investigations of drug-drug interactions with therapeutics (terfenadine and cyclosporine) known to be metabolized by CYP3A4, pharmacokinetic interactions were noted upon troglitazone multiple-dose treatments.	Terfenadine	76-87	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	133-139
11290874-3	2001	Terfenadine, an antihistamine, has been shown to be a P-gp inhibitor.	Terfenadine	0-11	ATP-binding cassette, subfamily B (MDR/TAP), member 1B	Rattus norvegicus	54-58
11575008-9	2001	On the other hand terfenadine and astemizole effectively blocked HERG K+ channels with nanomolar affinities (330 and 480 nmol/L, respectively), whereas loratadine was about 300-fold less potent.	Terfenadine	18-29	potassium voltage-gated channel subfamily H member 2	Homo sapiens	65-69
10828461-3	2000	We demonstrate that HERGS631C in its reduced state is fully blocked by 1 microM astemizole, terfenadine and dofetilide, similar to wild-type HERG channels.	Terfenadine	92-103	potassium voltage-gated channel subfamily H member 2	Homo sapiens	20-24
10872584-10	2000	The reproducibility and sensitivity of the assay, combined with the selectivity of mass spectrometric detection, should allow an accurate kinetic characterization of terfenadine oxidation mediated by the high affinity CYP3A enzymes in human liver and intestinal microsomes.	Terfenadine	166-177	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	218-223
10772630-5	2000	Known Pgp inhibitors, such as cyclosporin A, nicardipine, verapamil, quinidine, terfenadine, tamoxifen, and vinblastine were demonstrated to inhibit the Pgp-mediated efflux of daunorubicin.	Terfenadine	80-91	ATP binding cassette subfamily B member 1	Homo sapiens	6-9
10772630-5	2000	Known Pgp inhibitors, such as cyclosporin A, nicardipine, verapamil, quinidine, terfenadine, tamoxifen, and vinblastine were demonstrated to inhibit the Pgp-mediated efflux of daunorubicin.	Terfenadine	80-91	ATP binding cassette subfamily B member 1	Homo sapiens	153-156
10556670-1	1999	Terfenadine, a histamine H(1) receptor antagonist, has been associated with clinical ventricular arrhythmias and in vitro excitation-conduction blocks, whereas anti-ischemic and antiarrhythmic effects have been shown with cicletanine, a prostacyclin generation stimulator.	Terfenadine	0-11	histamine H1 receptor	Cavia porcellus	15-38
10597902-1	1999	Cetirizine, terfenadine, loratadine, astemizole and mizolastine were compared for their ability to inhibit marker activities for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and for some glucuronidation isoenzymes in human liver microsomes.	Terfenadine	12-23	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	129-135
10597902-1	1999	Cetirizine, terfenadine, loratadine, astemizole and mizolastine were compared for their ability to inhibit marker activities for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and for some glucuronidation isoenzymes in human liver microsomes.	Terfenadine	12-23	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	137-143
10597902-2	1999	The most pronounced effects were observed with terfenadine, astemizole and loratadine which inhibited CYP3A4-mediated testosterone 6beta-hydroxylation (IC50 of 23, 21 and 32 microM, respectively) and CYP2D6-mediated dextromethorphan O-demethylation (IC50 of 18, 36 and 15 microM, respectively).	Terfenadine	47-58	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	102-108
10604956-10	2000	However, both drugs potently blocked HERG current amplitude, with a mean IC(50) of 173 nM for loratadine and 204 nM for terfenadine (pacing rate, 0.1 Hz).	Terfenadine	120-131	potassium voltage-gated channel subfamily H member 2	Homo sapiens	37-41
10469039-6	1999	RESULTS: Terfenadine inhibited T-cell proliferation and IL-4 and IL-5 production under each costimulatory condition tested, whereas it had no effect on IL-2 and IFN-gamma production.	Terfenadine	9-20	interleukin 4	Homo sapiens	56-60
10469039-6	1999	RESULTS: Terfenadine inhibited T-cell proliferation and IL-4 and IL-5 production under each costimulatory condition tested, whereas it had no effect on IL-2 and IFN-gamma production.	Terfenadine	9-20	interleukin 5	Homo sapiens	65-69
10422790-1	1999	Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG).	Terfenadine	0-11	potassium voltage-gated channel subfamily H member 2	Homo sapiens	171-175
10496299-12	1999	Troglitazone may enhance the activities of cytochrome P450 (CYP) 3A and/or transporter(s) thereby reducing the plasma concentrations of terfenadine, cyclosporin, atorvastatin and fexofenadine.	Terfenadine	136-147	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	43-67
10444235-4	1999	In fact, both terfenadine and astemizole have been shown to block HERG K+ channels in a concentration range similar to that found in the plasma of subjects with cardiotoxic manifestations.	Terfenadine	14-25	potassium voltage-gated channel subfamily H member 2	Homo sapiens	66-70
10422790-4	1999	Terfenadine and astemizole suppressed the HERG current with IC50 of 431 nM and 69 nM, respectively.	Terfenadine	0-11	potassium voltage-gated channel subfamily H member 2	Homo sapiens	42-46
10213372-5	1999	RESULTS: Some (terfenadine, erythromycin and lovastatin) but not all (nifedipine and midazolam) CYP3A substrates were found to be P-gp substrates.	Terfenadine	15-26	phosphoglycolate phosphatase	Homo sapiens	130-134
10350002-8	1999	The relative affinity of CYP3A for terfenadine metabolism in the two cell lines was comparable, but the maximum reaction rate in the TC7 cells was 8-fold higher.	Terfenadine	35-46	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	25-30
10350002-11	1999	Ketoconazole increased the AP-BL transport terfenadine dramatically by inhibiting both terfenadine metabolism and Pgp efflux.	Terfenadine	43-54	ATP binding cassette subfamily B member 1	Homo sapiens	114-117
10371095-8	1999	RESULTS: Only children treated with terfenadine achieved significant control of symptoms (P<0.05 in 8 out of 12 months) and allergic inflammation, as shown by inflammatory cell infiltrate and ICAM-1 expression at nasal level (P<0.001), and had significantly fewer extra visits and school absences than the placebo group (P<0.03).	Terfenadine	36-47	intercellular adhesion molecule 1	Homo sapiens	195-201
10371095-10	1999	CONCLUSIONS: The present study demonstrates that continuous terfenadine treatment (1 mg/kg body weight per day) could decrease respiratory symptoms and allergic inflammation, and it had an additional antiallergic effect in reducing ICAM-1 expression on nasal epithelial cells.	Terfenadine	60-71	intercellular adhesion molecule 1	Homo sapiens	232-238
10371099-4	1999	Moreover, the bronchoconstriction induced by IL-8 was significantly inhibited by the antihistamines diphenhydramine and terfenadine, suggesting the involvement of histamine release in the IL-8-induced bronchoconstriction.	Terfenadine	120-131	interleukin-8	Cavia porcellus	45-49
10371099-4	1999	Moreover, the bronchoconstriction induced by IL-8 was significantly inhibited by the antihistamines diphenhydramine and terfenadine, suggesting the involvement of histamine release in the IL-8-induced bronchoconstriction.	Terfenadine	120-131	interleukin-8	Cavia porcellus	188-192
9867310-3	1998	The main probe drugs include caffeine and theophylline, whose metabolism is catalysed by CYP1A2, tolbutamide, phenytoin and ibuprofen, catalysed by CYP2C9, amitriptyline and nortriptyline, catalysed by CYP2C19, acetaminophen, catalysed by CYP2E1 and lidocaine, midazolam and terfenadine, catalysed by 3A3/4.	Terfenadine	275-286	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	89-95
10078334-1	1999	Exposure of cultured cerebellar neurons to the histamine H1 receptor antagonist terfenadine resulted in neuronal degeneration and death.	Terfenadine	80-91	histamine receptor H1	Homo sapiens	47-68
9733666-0	1998	Interaction of terfenadine and its primary metabolites with cytochrome P450 2D6.	Terfenadine	15-26	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	60-79
9733666-1	1998	The substrate structure-activity relationships described for the major human drug-metabolizing cytochrome P450 (P450 or CYP) enzymes suggest that the H1 receptor antagonist terfenadine could interact with CYP2D6 either as a substrate or as an inhibitor, in addition to its known ability to act as a substrate for CYP3A4.	Terfenadine	173-184	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	106-110
9733666-1	1998	The substrate structure-activity relationships described for the major human drug-metabolizing cytochrome P450 (P450 or CYP) enzymes suggest that the H1 receptor antagonist terfenadine could interact with CYP2D6 either as a substrate or as an inhibitor, in addition to its known ability to act as a substrate for CYP3A4.	Terfenadine	173-184	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	112-123
9733666-1	1998	The substrate structure-activity relationships described for the major human drug-metabolizing cytochrome P450 (P450 or CYP) enzymes suggest that the H1 receptor antagonist terfenadine could interact with CYP2D6 either as a substrate or as an inhibitor, in addition to its known ability to act as a substrate for CYP3A4.	Terfenadine	173-184	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	205-211
9733666-1	1998	The substrate structure-activity relationships described for the major human drug-metabolizing cytochrome P450 (P450 or CYP) enzymes suggest that the H1 receptor antagonist terfenadine could interact with CYP2D6 either as a substrate or as an inhibitor, in addition to its known ability to act as a substrate for CYP3A4.	Terfenadine	173-184	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	313-319
9733666-2	1998	Based on this substrate structure-activity relationship, computer modeling studies were undertaken to explore the likely interactions of terfenadine with CYP2D6.	Terfenadine	137-148	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	154-160
9733666-3	1998	An overlay of terfenadine and dextromethorphan, a known substrate of CYP2D6, showed that it was possible to superimpose the site of hydroxylation (t-butyl group) and the nitrogen atom of terfenadine with similar regions in dextromethorphan.	Terfenadine	14-25	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	69-75
9733666-3	1998	An overlay of terfenadine and dextromethorphan, a known substrate of CYP2D6, showed that it was possible to superimpose the site of hydroxylation (t-butyl group) and the nitrogen atom of terfenadine with similar regions in dextromethorphan.	Terfenadine	187-198	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	69-75
9733666-4	1998	These observations were substantiated by the ease of docking of terfenadine into a protein model of CYP2D6.	Terfenadine	64-75	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	100-106
9733666-5	1998	Experimentally, terfenadine inhibited CYP2D6 activity in human liver microsomes with an IC50 of 14-27 microM, depending on the CYP2D6 substrate used.	Terfenadine	16-27	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	38-44
9733666-5	1998	Experimentally, terfenadine inhibited CYP2D6 activity in human liver microsomes with an IC50 of 14-27 microM, depending on the CYP2D6 substrate used.	Terfenadine	16-27	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	127-133
9733666-6	1998	The inhibition of CYP2D6 was further defined by determining the Ki for terfenadine against bufuralol 1"-hydroxylase activity in four human livers.	Terfenadine	71-82	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	18-24
9733666-11	1998	These data indicate that, as predicted from modeling studies, terfenadine has the structural features necessary for interaction with CYP2D6.	Terfenadine	62-73	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	133-139
10597864-1	1999	The use of terfenadine and astemizole, two long-acting nonsedating histamine H1 receptor antagonists, has been associated with prolongation of the QT interval, development of ventricular arrhythmias, particularly torsade de pointes, and sudden cardiac death.	Terfenadine	11-22	histamine receptor H1	Homo sapiens	67-88
10597865-4	1999	Acquired LQTS can be induced by a variety of drugs, including some nonsedative histamine H1 receptor antagonists (astemizole, terfenadine).	Terfenadine	126-137	histamine receptor H1	Homo sapiens	79-100
10597866-1	1999	Since 1990 it has repeatedly been reported that some histamine H1 receptor antagonists (e.g. terfenadine and astemizole) are able to produce ventricular arrhythmias (e.g. torsade de pointes) when they are given at dosages above the therapeutic range and/or administered together with cytochrome P-450 3A4 inhibitors, such as ketoconazole or erythromycin.	Terfenadine	93-104	histamine H1 receptor	Cavia porcellus	53-74
9892033-0	1998	Terfenadine and fexofenadine reduce in vitro ICAM-1 expression on human continuous cell lines.	Terfenadine	0-11	intercellular adhesion molecule 1	Homo sapiens	45-51
9892033-3	1998	OBJECTIVE: The aim of the study was to evaluate the effect exerted by terfenadine and fexofenadine on adhesion molecules expression (CD54/ICAM-1 and CD29) of a human continuously cultured conjunctival epithelial cell line (WK) and a fibroblast cell line (HEL).	Terfenadine	70-81	intercellular adhesion molecule 1	Homo sapiens	133-137
9892033-3	1998	OBJECTIVE: The aim of the study was to evaluate the effect exerted by terfenadine and fexofenadine on adhesion molecules expression (CD54/ICAM-1 and CD29) of a human continuously cultured conjunctival epithelial cell line (WK) and a fibroblast cell line (HEL).	Terfenadine	70-81	intercellular adhesion molecule 1	Homo sapiens	138-144
9892033-6	1998	RESULTS: Terfenadine and fexofenadine significantly reduced ICAM-1 basal expression on WK cells at the concentration of 1 microg/mL and 50 microg/mL, respectively.	Terfenadine	9-20	intercellular adhesion molecule 1	Homo sapiens	60-66
9892033-7	1998	In addition, both terfenadine and fexofenadine were able to decrease soluble ICAM-1 levels in IFN gamma-stimulated WK cells.	Terfenadine	18-29	intercellular adhesion molecule 1	Homo sapiens	77-83
9892033-7	1998	In addition, both terfenadine and fexofenadine were able to decrease soluble ICAM-1 levels in IFN gamma-stimulated WK cells.	Terfenadine	18-29	interferon gamma	Homo sapiens	94-103
9892033-10	1998	CONCLUSION: This study shows that terfenadine and fexofenadine exert a biologic effect directly on epithelial cells and fibroblasts reducing ICAM-1 expression and partially reducing soluble ICAM-1 release.	Terfenadine	34-45	intercellular adhesion molecule 1	Homo sapiens	141-147
9892033-10	1998	CONCLUSION: This study shows that terfenadine and fexofenadine exert a biologic effect directly on epithelial cells and fibroblasts reducing ICAM-1 expression and partially reducing soluble ICAM-1 release.	Terfenadine	34-45	intercellular adhesion molecule 1	Homo sapiens	190-196
9694927-12	1998	These potential dual actions on HERG currents suggest that precautions should be taken in long-term ketoconazole treatment, particularly for patients who have decreased liver function or are on a drug regimen requiring simultaneous medications that use cytochrome-P450 for breakdown, such as terfenadine or erythromycin, or Class III antiarrhythmic drugs.	Terfenadine	292-303	potassium voltage-gated channel subfamily H member 2	Homo sapiens	32-36
9694927-2	1998	Both compounds use the same cytochrome-P450 metabolic pathway, resulting in an increase in plasma concentration of terfenadine.	Terfenadine	115-126	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	28-43
9694927-3	1998	We previously showed that terfenadine blocked HERG (Human Ether-a-Gogo Related Gene), an important component of the repolarizing cardiac delayed rectifier IK with concentration needed to obtain 50% of the block (IC50) in the therapeutic range (300 nM).	Terfenadine	26-37	potassium voltage-gated channel subfamily H member 2	Homo sapiens	46-50
9694927-11	1998	We conclude that ketoconazole may potentiate the effects of terfenadine first by an indirect pharmacokinetic action to elevate plasma levels and second by a direct pharmacodynamic action on HERG currents.	Terfenadine	60-71	potassium voltage-gated channel subfamily H member 2	Homo sapiens	190-194
9694927-12	1998	These potential dual actions on HERG currents suggest that precautions should be taken in long-term ketoconazole treatment, particularly for patients who have decreased liver function or are on a drug regimen requiring simultaneous medications that use cytochrome-P450 for breakdown, such as terfenadine or erythromycin, or Class III antiarrhythmic drugs.	Terfenadine	292-303	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	253-268
9867310-3	1998	The main probe drugs include caffeine and theophylline, whose metabolism is catalysed by CYP1A2, tolbutamide, phenytoin and ibuprofen, catalysed by CYP2C9, amitriptyline and nortriptyline, catalysed by CYP2C19, acetaminophen, catalysed by CYP2E1 and lidocaine, midazolam and terfenadine, catalysed by 3A3/4.	Terfenadine	275-286	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	148-154
9618706-8	1998	Some antihistamines (i.e., levocabastine, terfenadine, loratadine, azelastine and oxatomide) can reduce ICAM-1 expression.	Terfenadine	42-53	intercellular adhesion molecule 1	Homo sapiens	104-110
9691225-15	1998	The PPD antihistamines, namely terfenadine and astemizole, inhibited cough (MED 30 and 10 mg/kg p.o.)	Terfenadine	31-42	mediator of RNA polymerase II transcription subunit 30	Cavia porcellus	76-82
9658196-1	1998	In the current study, the potential blocking ability of K+ channels encoded by the human ether-a-go-go related gene (HERG) by the piperazine H1 receptor antagonist cetirizine has been examined and compared with that of other second-generation antihistamines (astemizole, terfenadine, and loratadine).	Terfenadine	271-282	potassium voltage-gated channel subfamily H member 2	Homo sapiens	117-121
9658196-3	1998	On the other hand, terfenadine and astemizole effectively blocked HERG K+ channels with nanomolar affinities (the estimated IC50 values were 330 and 480 nM, respectively), whereas loratadine was approximately 300-fold less potent (IC50 approximately 100 microM).	Terfenadine	19-30	potassium voltage-gated channel subfamily H member 2	Homo sapiens	66-70
9714291-5	1998	In fact, interference with HERG K+ channels seems to be the main mechanism explaining both the therapeutic actions of the class III antiarrhythmics and the potential cardiotoxicity of second-generation H1 receptor antagonists such as terfenadine and astemizole, as well as of psychotropic drugs such as some antidepressants and neuroleptics.	Terfenadine	234-245	potassium voltage-gated channel subfamily H member 2	Homo sapiens	27-31
9626585-6	1998	The potentiating effect of smoking on ethanol-induced gastric mucosal lesion and MPO activity was abolished by pretreatment with allopurinol, terfenadine or ranitidine.	Terfenadine	142-153	myeloperoxidase	Rattus norvegicus	81-84
9650812-5	1998	The beta-2 agonist salmeterol, the H1-receptor antagonist terfenadine and the phosphodiesterase inhibitor theophylline inhibited the release of IL-4 and IL-13 by more than 50% following 4 h of basophil stimulation with anti-IgE.	Terfenadine	58-69	interleukin 4	Homo sapiens	144-148
9650812-5	1998	The beta-2 agonist salmeterol, the H1-receptor antagonist terfenadine and the phosphodiesterase inhibitor theophylline inhibited the release of IL-4 and IL-13 by more than 50% following 4 h of basophil stimulation with anti-IgE.	Terfenadine	58-69	interleukin 13	Homo sapiens	153-158
9660842-7	1998	In a one-sequence crossover study in 12 healthy volunteers, nelfinavir inhibited the elimination of the CYP3A substrate terfenadine and the carboxylate metabolite of terfenadine.	Terfenadine	120-131	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	104-109
9649346-3	1998	Ketoconazole, terfenadine, and astemizole were observed to inhibit amprenavir depletion, consistent with their known specificity for CYP3A4.	Terfenadine	14-25	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	133-139
9562230-6	1998	Although terfenadine is a substrate for CYP3A (cytochrome P-450 3A), while sertindole is a substrate for both CYP2D6 and CYP3A4, the results in this study suggest that sertindole, at a clinical dose, is not an inhibitor of the metabolism of terfenadine.	Terfenadine	9-20	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	40-45
10022752-0	1998	Human cytochrome P450 3A (CYP3A) mediated midazolam metabolism: the effect of assay conditions and regioselective stimulation by alpha-naphthoflavone, terfenadine and testosterone.	Terfenadine	151-162	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	6-24
10022752-0	1998	Human cytochrome P450 3A (CYP3A) mediated midazolam metabolism: the effect of assay conditions and regioselective stimulation by alpha-naphthoflavone, terfenadine and testosterone.	Terfenadine	151-162	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	26-31
10022752-1	1998	The effect of ionic strength, assay constituents, alpha-naphthoflavone (aNF), terfenadine and testosterone on human CYP3A mediated midazolam (MDZ) 1"-hydroxylation (MDZ 1"-OH) and 4-hydroxylation (MDZ 4-OH) in vitro was examined.	Terfenadine	78-89	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	116-121
10022752-9	1998	Surprisingly, with expressed CYP3A4, terfenadine (20 microM) inhibited MDZ 1"-OH formation.	Terfenadine	37-48	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	29-35
9342502-18	1997	The potential for a clinically significant interaction between nefazodone and other drugs cleared by CYP3A4 (e.g. terfenadine) should be considered before the coadministration of these compounds.	Terfenadine	114-125	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	101-107
9506246-1	1998	The nonsedating histamine H1 receptor antagonist fexofenadine is the active metabolite of terfenadine.	Terfenadine	90-101	histamine receptor H1	Homo sapiens	16-37
9408807-1	1997	Potent CYP3A4 inhibitors such as ketoconazole can cause dangerous increases in plasma concentrations of the H-1 antagonist terfenadine.	Terfenadine	123-134	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	7-13
9541729-8	1998	In contrast, at anti-histamine, doses, the histamine H1-receptor antagonists terfenadine (1 to 30 mg/kg p.o.	Terfenadine	77-88	histamine receptor H 1	Rattus norvegicus	43-64
9485522-8	1997	CYP3A4 (testosterone 6 beta-hydroxylation) activity was strongly inhibited by terfenadine with a Ki value of 25 microM, whereas epinastine had no effect at up to 100 microM.	Terfenadine	78-89	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-6
9270401-2	1997	TDP has been associated with terfenadine use in cases of liver disease, electrolyte abnormalities, concomitant administration of drugs that inhibit cytochrome P-450, or deliberate overdose.	Terfenadine	29-40	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	148-164
9291293-0	1997	Effect of terfenadine on TNF alpha release from peripheral blood mononuclear cells during cow"s milk allergy.	Terfenadine	10-21	tumor necrosis factor	Bos taurus	25-34
9349334-9	1997	The mean +/- SEM percentage reduction in flare area for 200 pmol/site of substance P in non-atopics and atopics was 53 +/- 10% and 73 +/- 4% with terfenadine, and 74 +/- 7% and 75 +/- 4% with topical doxepin, respectively.	Terfenadine	146-157	tachykinin precursor 1	Homo sapiens	73-84
9349334-11	1997	The inhibitory effects of doxepin were as great as those of terfenadine, and doxepin had a significantly greater effect than terfenadine in inhibiting the weal response to histamine and flare response to substance P in normal volunteers (P < 0.05).	Terfenadine	125-136	tachykinin precursor 1	Homo sapiens	204-215
9291293-3	1997	OBJECTIVES: To test the potential ability of terfenadine to inhibit TNF alpha secretion by mononuclear cells from infants with cow"s milk allergy.	Terfenadine	45-56	tumor necrosis factor	Homo sapiens	68-77
9291293-7	1997	There was a dose-dependent decrease in TNF alpha secretion in the presence of terfenadine, with a maximal inhibition of 62% of this secretion at 1 microM.	Terfenadine	78-89	tumor necrosis factor	Bos taurus	39-48
9291293-9	1997	CONCLUSION: These results indicate that in infants with intestinal dysfunction due to cow"s milk allergy, terfenadine is a potent inhibitor of the TNF alpha secretion induced by sensitizing milk protein antigens.	Terfenadine	106-117	tumor necrosis factor	Bos taurus	147-156
9196279-0	1997	Comparative effects of nonsedating histamine H1 receptor antagonists, ebastine and terfenadine, on human Kv1.5 channels.	Terfenadine	83-94	potassium voltage-gated channel subfamily A member 5	Homo sapiens	105-110
9279883-1	1997	PURPOSE: To compare the activity of the CYP3A enzyme expressed by TC7, a cell culture model of the intestinal epithelial cell, to the activity of human intestinal CYP3A4, using terfenadine as a substrate.	Terfenadine	177-188	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	40-45
9279883-1	1997	PURPOSE: To compare the activity of the CYP3A enzyme expressed by TC7, a cell culture model of the intestinal epithelial cell, to the activity of human intestinal CYP3A4, using terfenadine as a substrate.	Terfenadine	177-188	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	163-169
9279883-3	1997	The effect of two CYP3A inhibitors, ketoconazole and troleandomycin (TAO), on the metabolism of terfenadine was also examined.	Terfenadine	96-107	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	18-23
9196279-2	1997	Upon depolarization to +60 mV, terfenadine, 1 microM and 3 microM, inhibited the hKv1.5 current by 42.4 +/- 6.4% and 69.3 +/- 4.2% (P < 0.01).	Terfenadine	31-42	potassium voltage-gated channel subfamily A member 5	Homo sapiens	81-87
8886862-4	1996	Pre-treatment of the subjects with the H1 histamine receptor antgonist cetirizine (10 mg, orally) or terfenadine (60 mg, orally) 3 h before bradykinin administration caused significant reduction of the bradykinin-induced increase in nasal airway resistance in the upper range of bradykinin doses (300-1000 micrograms) but not in the lower range (10-100 micrograms).	Terfenadine	101-112	kininogen 1	Homo sapiens	140-150
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.	Terfenadine	77-88	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	63-69
9232548-5	1997	Terfenadine prolonged the QT interval in an infusion-rate-dependent manner, its EC50 value was 792-1039 ng mL-1.	Terfenadine	0-11	L1 cell adhesion molecule	Mus musculus	107-111
9232548-6	1997	An obvious QT prolongation was, moreover, observed even at a plasma terfenadine concentration of 100-200 ng mL-1, which is clinically quite high, but might be achieved under a definite condition such as a restrained terfenadine metabolism.	Terfenadine	68-79	L1 cell adhesion molecule	Mus musculus	108-112
9232548-6	1997	An obvious QT prolongation was, moreover, observed even at a plasma terfenadine concentration of 100-200 ng mL-1, which is clinically quite high, but might be achieved under a definite condition such as a restrained terfenadine metabolism.	Terfenadine	216-227	L1 cell adhesion molecule	Mus musculus	108-112
9165365-6	1997	HSR-609 was found to display selective displacement of the [3H]mepyramine binding to H1-receptors for lung vs cerebral cortex as found with terfenadine in guinea pigs ex vivo.	Terfenadine	140-151	component of Sp100-rs	Mus musculus	0-3
9186817-3	1997	In 6 of the 7 women the effect of terfenadine (TRF, 120 mg os at -60 min), another H1-receptor antagonist, on the GH response to GHRH or HEX was also studied.	Terfenadine	34-45	growth hormone releasing hormone	Homo sapiens	129-133
9186817-3	1997	In 6 of the 7 women the effect of terfenadine (TRF, 120 mg os at -60 min), another H1-receptor antagonist, on the GH response to GHRH or HEX was also studied.	Terfenadine	47-50	growth hormone releasing hormone	Homo sapiens	129-133
9013373-1	1996	Terfenadine is metabolized by the cytochrome P-450 3A subfamily of enzymes (CYP3A).	Terfenadine	0-11	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	76-81
9013373-3	1996	The authors compared the abilities of dirithromycin (a new macrolide antibiotic agent), its major metabolite erythromycylamine, and the known CYP3A substrate terfenadine to inhibit CYP3A in vitro.	Terfenadine	158-169	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	142-147
9013373-3	1996	The authors compared the abilities of dirithromycin (a new macrolide antibiotic agent), its major metabolite erythromycylamine, and the known CYP3A substrate terfenadine to inhibit CYP3A in vitro.	Terfenadine	158-169	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	181-186
8886862-4	1996	Pre-treatment of the subjects with the H1 histamine receptor antgonist cetirizine (10 mg, orally) or terfenadine (60 mg, orally) 3 h before bradykinin administration caused significant reduction of the bradykinin-induced increase in nasal airway resistance in the upper range of bradykinin doses (300-1000 micrograms) but not in the lower range (10-100 micrograms).	Terfenadine	101-112	kininogen 1	Homo sapiens	202-212
8886862-4	1996	Pre-treatment of the subjects with the H1 histamine receptor antgonist cetirizine (10 mg, orally) or terfenadine (60 mg, orally) 3 h before bradykinin administration caused significant reduction of the bradykinin-induced increase in nasal airway resistance in the upper range of bradykinin doses (300-1000 micrograms) but not in the lower range (10-100 micrograms).	Terfenadine	101-112	kininogen 1	Homo sapiens	202-212
8887714-1	1996	A sensitive LC-MS-MS method capable of quantifying terfenadine at levels down to 100 pg ml-1 in human plasma is reported.	Terfenadine	51-62	interleukin 17F	Homo sapiens	88-92
8610817-8	1996	Cytochrome P450 3A4 metabolizes terfenadine, astemizole, carbamazepine, alprazolam, triazolam, and other benzodiazepines.	Terfenadine	32-43	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	0-19
8772706-5	1996	We found that HERG was 10 times more sensitive than Kv1.5 to terfenadine block.	Terfenadine	61-72	potassium voltage-gated channel subfamily H member 2	Homo sapiens	14-18
8772706-5	1996	We found that HERG was 10 times more sensitive than Kv1.5 to terfenadine block.	Terfenadine	61-72	potassium voltage-gated channel subfamily A member 5	Homo sapiens	52-57
8772706-8	1996	The Kd value for HERG block is relevant to the toxicity of the antihistamine, since the clinical terfenadine concentrations in human plasma may reach the 100 nmol/L range.	Terfenadine	97-108	potassium voltage-gated channel subfamily H member 2	Homo sapiens	17-21
8772706-10	1996	We propose that the blocking of HERG by terfenadine explains the acquired long QT syndrome.	Terfenadine	40-51	potassium voltage-gated channel subfamily H member 2	Homo sapiens	32-36
8735853-6	1996	Oral terfenadine and cetirizine and intranasal levocabastine and azelastine have also demonstrated a lowering of ICAM-1 expression on epithelial cells.	Terfenadine	5-16	intercellular adhesion molecule 1	Homo sapiens	113-119
8641472-0	1996	Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole.	Terfenadine	93-104	potassium voltage-gated channel subfamily H member 2	Homo sapiens	12-16
8641472-2	1996	Here, terfenadine and astemizole both inhibited the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion.	Terfenadine	6-17	potassium voltage-gated channel subfamily H member 2	Homo sapiens	86-90
8641472-4	1996	These results suggest that blockade of HERG channels by terfenadine and astemizole might contribute to the cardiac side effects of these compounds.	Terfenadine	56-67	potassium voltage-gated channel subfamily H member 2	Homo sapiens	39-43
8880073-1	1996	The effects of chronic treatment with the non-sedative histamine H1 receptor antagonist terfenadine (5 mg/kg, i.p.)	Terfenadine	88-99	histamine receptor H 1	Rattus norvegicus	55-76
8880073-7	1996	These results suggest that the histamine H1 receptor antagonist terfenadine may have antidepressant properties and that terfenadine is effective in reversing some of behavioural and immune changes in the olfactory bulbectomized rat model of depression.	Terfenadine	64-75	histamine receptor H 1	Rattus norvegicus	31-52
8613951-5	1996	Ritonavir was found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation, IC50) = 0.07 microM; 17alpha-ethynylestradiol 2-hydroxylation, IC50 = 2 microM; terfenadine hydroxylation, IC50 = 0.14 microM).	Terfenadine	185-196	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	48-53
8689766-2	1996	The aim of this study was to compare the effects of terfenadine (an H1-antagonist) and cimetidine (an H2-antagonist) on weal and flare responses to PAF and BK in healthy non-atopic human volunteers.	Terfenadine	52-63	PCNA clamp associated factor	Homo sapiens	148-151
8689766-2	1996	The aim of this study was to compare the effects of terfenadine (an H1-antagonist) and cimetidine (an H2-antagonist) on weal and flare responses to PAF and BK in healthy non-atopic human volunteers.	Terfenadine	52-63	kininogen 1	Homo sapiens	156-158
8689766-19	1996	The aim of this study was to compare the effects of terfenadine (an H1-antagonist) and cimetidine (an H2-antagonist) on PAF- and BK-induced weal and flare responses in healthy, non-atopic human volunteers.	Terfenadine	52-63	PCNA clamp associated factor	Homo sapiens	120-123
8689766-4	1996	Terfenadine significantly reduced weal and flare responses to PAF (mean reduction 53 and 73%, respectively) and flare responses to BK (mean reduction 78%) but had no effect on weal responses to BK.	Terfenadine	0-11	PCNA clamp associated factor	Homo sapiens	62-65
8689766-19	1996	The aim of this study was to compare the effects of terfenadine (an H1-antagonist) and cimetidine (an H2-antagonist) on PAF- and BK-induced weal and flare responses in healthy, non-atopic human volunteers.	Terfenadine	52-63	kininogen 1	Homo sapiens	129-131
8689766-4	1996	Terfenadine significantly reduced weal and flare responses to PAF (mean reduction 53 and 73%, respectively) and flare responses to BK (mean reduction 78%) but had no effect on weal responses to BK.	Terfenadine	0-11	kininogen 1	Homo sapiens	131-133
8788208-6	1995	In rat liver, only the N-dealkylation pathway appears to be mediated by CYP3A since anti-rat CYP3A antibody inhibited azacyclonol but not alcohol metabolite formation in incubations of terfenadine with liver microsomes.	Terfenadine	185-196	cytochrome P450, family 3, subfamily a, polypeptide 62	Rattus norvegicus	72-77
8626361-10	1996	On the basis of the inhibition of cytochrome P450 3A4 isoenzyme by nefazodone in vitro, coadministration of terfenadine or astemizole with nefazodone is contraindicated because nefazodone can increase the plasma levels of these two drugs.	Terfenadine	108-119	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	34-53
8748566-11	1995	Nefazodone, an inhibitor of the hepatic P-450 isoenzyme CYP3A4, may increase concentrations of drugs metabolized by this isoenzyme, such as terfenadine, astemizole, triazolam, alprazolam, and midazolam.	Terfenadine	140-151	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	56-62
8788208-6	1995	In rat liver, only the N-dealkylation pathway appears to be mediated by CYP3A since anti-rat CYP3A antibody inhibited azacyclonol but not alcohol metabolite formation in incubations of terfenadine with liver microsomes.	Terfenadine	185-196	cytochrome P450, family 3, subfamily a, polypeptide 62	Rattus norvegicus	93-98
8584574-1	1995	Chronic administration of a low dose of the histamine H1 receptor antagonist terfenadine (2 mg/kg/day) induced an increase in gamma-glutamyltransferase serum activity in rats, 360 h after partial hepatectomy while the enzymatic activity appeared not to be affected during liver regeneration following treatment with the histamine H2 receptor antagonist cimetidine (20 mg/kg/day).	Terfenadine	77-88	histamine receptor H 1	Rattus norvegicus	44-65
8564726-0	1995	Terfenadine exerts antiallergic activity reducing ICAM-1 expression on nasal epithelial cells in patients with pollen allergy.	Terfenadine	0-11	intercellular adhesion molecule 1	Homo sapiens	50-56
8564726-7	1995	RESULTS: As opposed to the placebo group, patients treated with Terfenadine showed a significant improvement of both symptoms (P < 0.022) and signs P < 0.001), a significant reduction of inflammatory cells infiltrate (P < 0.005), of ECP levels (P < 0.002) and ICAM-1 expression on nasal epithelial cells (P < 0.005).	Terfenadine	64-75	ribonuclease A family member 3	Homo sapiens	242-245
8564726-7	1995	RESULTS: As opposed to the placebo group, patients treated with Terfenadine showed a significant improvement of both symptoms (P < 0.022) and signs P < 0.001), a significant reduction of inflammatory cells infiltrate (P < 0.005), of ECP levels (P < 0.002) and ICAM-1 expression on nasal epithelial cells (P < 0.005).	Terfenadine	64-75	intercellular adhesion molecule 1	Homo sapiens	272-278
8564726-8	1995	CONCLUSIONS: In conclusion, these data demonstrate that Terfenadine exerts antiallergic activity since it is able to reduce inflammatory cell infiltrate and downregulates ICAM-1 expression.	Terfenadine	56-67	intercellular adhesion molecule 1	Homo sapiens	171-177
8584574-1	1995	Chronic administration of a low dose of the histamine H1 receptor antagonist terfenadine (2 mg/kg/day) induced an increase in gamma-glutamyltransferase serum activity in rats, 360 h after partial hepatectomy while the enzymatic activity appeared not to be affected during liver regeneration following treatment with the histamine H2 receptor antagonist cimetidine (20 mg/kg/day).	Terfenadine	77-88	gamma-glutamyltransferase 1	Rattus norvegicus	126-151
8584574-1	1995	Chronic administration of a low dose of the histamine H1 receptor antagonist terfenadine (2 mg/kg/day) induced an increase in gamma-glutamyltransferase serum activity in rats, 360 h after partial hepatectomy while the enzymatic activity appeared not to be affected during liver regeneration following treatment with the histamine H2 receptor antagonist cimetidine (20 mg/kg/day).	Terfenadine	77-88	histamine receptor H 2	Rattus norvegicus	320-341
7654486-9	1995	Mean (95% CI) measurements for terfenadine vs placebo treatment periods were 1.5 vs 1.5 (-0.3, 0.3) l for FEV1, 259 vs 260 (-42, 40) l min-1 for morning PEF and 0.8 vs 0.8 (-0.3, 0.3) for global symptom scores.	Terfenadine	31-42	CD59 molecule (CD59 blood group)	Homo sapiens	135-140
7587966-0	1995	In vitro metabolism of terfenadine by a purified recombinant fusion protein containing cytochrome P4503A4 and NADPH-P450 reductase.	Terfenadine	23-34	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	87-105
7587966-2	1995	The metabolism of terfenadine was studied with a cDNA-expressed/purified recombinant fusion protein containing human liver microsomal cytochrome P4503A4 (CYP3A4) linked to rat NADPH-P450 reductase (rF450[mHum3A4/mRatOR]L1) and was compared with that observed in the presence of human liver microsomes and precision-cut human liver tissue slices.	Terfenadine	18-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	134-152
7587966-2	1995	The metabolism of terfenadine was studied with a cDNA-expressed/purified recombinant fusion protein containing human liver microsomal cytochrome P4503A4 (CYP3A4) linked to rat NADPH-P450 reductase (rF450[mHum3A4/mRatOR]L1) and was compared with that observed in the presence of human liver microsomes and precision-cut human liver tissue slices.	Terfenadine	18-29	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	154-160
7587966-7	1995	Ketoconazole, a well-documented CYP3A inhibitor, effectively inhibited terfenadine metabolism in all three models.	Terfenadine	71-82	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	32-37
7587966-9	1995	It is concluded that cDNA-expressed CYP3A4, in the form of a NADPH-P450 reductase-linked fusion protein, may also serve as a model for studying the metabolism of terfenadine in vitro and many other drugs.	Terfenadine	162-173	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	36-42
8001268-0	1995	Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine.	Terfenadine	93-104	histamine H1 receptor	Cavia porcellus	44-65
7670728-8	1995	Upon depolarization, racemic terfenadine and its enantiomers induced a fast decline of hKv1.5 current towards a reduced steady state current level.	Terfenadine	29-40	potassium voltage-gated channel subfamily A member 5	Homo sapiens	87-93
7670728-14	1995	The EC50 for hKv1.5 block by racemic terfenadine was 0.88 microM, while the values for R- and S-terfenadine were 1.19 microM and 1.16 microM, respectively.	Terfenadine	37-48	potassium voltage-gated channel subfamily A member 5	Homo sapiens	13-19
7697852-6	1995	Both astemizole and terfenadine suppressed the IK1 channel by 17% to 50% in a voltage-dependent manner in rat and guinea pig myocytes.	Terfenadine	20-31	potassium calcium-activated channel subfamily N member 4	Rattus norvegicus	47-50
7587944-0	1995	Metabolism of terfenadine associated with CYP3A(4) activity in human hepatic microsomes.	Terfenadine	14-25	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	42-50
7587944-3	1995	Although testosterone 6 beta-hydroxylation [CYP3A(4)] has been shown to be the principal enzyme involved in the first step in terfenadine"s biotransformation (formation of azacyclonol and terfenadine alcohol), the enzymes catalyzing the subsequent metabolic steps in the conversion of terfenadine alcohol to azacyclonol and terfenadine acid have not been identified.	Terfenadine	126-137	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	44-52
7587944-7	1995	The formation of azacyclonol and terfenadine alcohol from terfenadine is confirmed to be catalyzed predominantly by CYP3A(4) isozyme, and the ratio of the rate of terfenadine alcohol formation to that of azacyclonol is 3:1.	Terfenadine	33-44	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	116-124
7587944-8	1995	Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4).	Terfenadine	31-42	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	19-27
7587944-8	1995	Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4).	Terfenadine	31-42	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	212-220
7587944-8	1995	Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4).	Terfenadine	31-42	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	212-220
7573821-4	1995	Terfenadine caused significant inhibition of both PGD2 and LTC4/D4 (49 +/- 9 and 29 +/- 19%, respectively) from human lung cells but had a less marked effect on PGD2 release from human colon cells (21 +/- 9% for PGD2 and 18 +/- 9% for LTC4/D4).	Terfenadine	0-11	prostaglandin D2 synthase	Homo sapiens	212-223
8067599-3	1994	Since eosinophil degranulation is also associated with tissue inflammation, we further examined the effect of terfenadine on the PAF-induced release of eosinophil cationic protein.	Terfenadine	110-121	ribonuclease A family member 3	Homo sapiens	152-179
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.	Terfenadine	98-109	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	84-90
7895601-7	1994	Other CYP3A substrates (cyclosporin A, naringenin, and midazolam) also demonstrated potent inhibition of terfenadine biotransformation in human liver microsomes (IC50 = 17-24 microM).	Terfenadine	105-116	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	6-11
7895601-8	1994	Substrates of other P450 families [sparteine (CYP2D6), caffeine (CYP1A), and diclofenac (CYP2C)] only very weakly inhibited terfenadine metabolism.	Terfenadine	124-135	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	46-52
8067599-8	1994	Terfenadine, at concentrations of 500 and 1000 ng/mL, significantly inhibited PAF-induced and FMLP-induced eosinophil chemotaxis, whereas 1000 ng/mL of terfenadine was necessary to suppress neutrophil chemotaxis.	Terfenadine	0-11	formyl peptide receptor 1	Homo sapiens	94-98
8067599-8	1994	Terfenadine, at concentrations of 500 and 1000 ng/mL, significantly inhibited PAF-induced and FMLP-induced eosinophil chemotaxis, whereas 1000 ng/mL of terfenadine was necessary to suppress neutrophil chemotaxis.	Terfenadine	152-163	formyl peptide receptor 1	Homo sapiens	94-98
8119047-4	1993	Macrolides inhibit cytochrome P450IIIA4 (CYP3A4), which appears to be the most common metabolic enzyme in the human liver and is involved in the metabolism of many drugs, including cyclosporin, warfarin and terfenadine.	Terfenadine	207-218	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	41-47
7515418-2	1994	During terfenadine treatment, the mean substance P concentrations in nasal secretions from patients allergic to house dust or pollen were significantly decreased to 62 and 39% of the initial values, respectively.	Terfenadine	7-18	tachykinin precursor 1	Homo sapiens	39-50
8112815-1	1993	Terfenadine is a selective histamine H1 receptor antagonist which binds preferentially to peripheral receptors in vivo and is devoid of central nervous system depressant activity and thus has an improved adverse effect profile (1).	Terfenadine	0-11	histamine receptor H1	Homo sapiens	27-48
8257954-1	1993	Terfenadine was the first non-sedating histamine H1 receptor antagonist and one of the most frequently prescribed H1 antihistamines.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	39-60
8257958-4	1993	The increased risk of both H1-antihistamines was associated with exposure to supratherapeutic doses; for terfenadine the risk was also associated with concomitant exposure to the cytochrome P-450 inhibitors ketoconazole, erythromycin and cimetidine.	Terfenadine	105-116	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	179-195
8112439-0	1993	Effect of oral terfenadine on bronchoconstrictor response to inhaled neurokinin A and histamine in asthmatic subjects.	Terfenadine	15-26	tachykinin precursor 1	Homo sapiens	69-81
7693504-2	1993	Our aim was to determine the relationship between the contributions of vagal stimulation (determined by the use of the muscarinic receptor antagonist, ipratropium bromide) and histamine release (determined by the use of the histamine H1-receptor antagonist terfenadine) in EIA.	Terfenadine	257-268	histamine receptor H1	Homo sapiens	224-245
8388006-0	1993	The effect of oral terfenadine on neurokinin-A-induced bronchoconstriction.	Terfenadine	19-30	tachykinin precursor 1	Homo sapiens	34-46
1587633-0	1992	Effect of terfenadine on neutrophil and eosinophil chemotactic activities after inhalation of platelet-activating factor in vivo and on neutrophil chemotaxis in vitro.	Terfenadine	10-21	PCNA clamp associated factor	Homo sapiens	94-120
8466096-3	1993	The results of the study showed that both cetirizine, 10 mg, QD and terfenadine, 60 mg, BID used for 1 week are safe and effective in the management of allergic rhinitis.	Terfenadine	68-79	BH3 interacting domain death agonist	Homo sapiens	88-91
7681268-11	1993	An inhibition of eicosanoids was observed at both 1 and 10 mumol terfenadine (median percentage of inhibition of PGD2: 38.00 +/- 15.65 and 56.00 +/- 13.12; median percentage of inhibition of LTC4/D4: 37.5 +/- 19.80 and 52.5 +/- 26.8).	Terfenadine	65-76	prostaglandin D2 synthase	Homo sapiens	113-117
8094615-1	1993	In our efforts to identify clinically effective drugs for reversing multidrug resistance (MDR) mediated by P-glycoprotein, we tested terfenadine for anti-MDR activity because it appeared to sensitize a patient to doxorubicin and because it met structural requirements defined for this activity.	Terfenadine	133-144	ATP binding cassette subfamily B member 1	Homo sapiens	107-121
8094615-6	1993	The mechanism of action of terfenadine appeared to be due to inhibition of the function of P-glycoprotein since it augmented the accumulation of doxorubicin and inhibited the efflux of rhodamine 123 from MDR lines but had no effect on drug accumulation or efflux in sensitive cells.	Terfenadine	27-38	ATP binding cassette subfamily B member 1	Homo sapiens	91-105
8094615-7	1993	Terfenadine displaced azidopine from P-glycoprotein, but at concentrations higher than expected based on its overall potency.	Terfenadine	0-11	ATP binding cassette subfamily B member 1	Homo sapiens	37-51
1280680-0	1992	Effect of terfenadine on the plasma concentrations of substance P and vasoactive intestinal polypeptide in volunteers.	Terfenadine	10-21	tachykinin precursor 1	Homo sapiens	54-65
1280680-0	1992	Effect of terfenadine on the plasma concentrations of substance P and vasoactive intestinal polypeptide in volunteers.	Terfenadine	10-21	vasoactive intestinal peptide	Homo sapiens	70-103
1280680-1	1992	The effect of terfenadine on the plasma concentrations of substance P and vasoactive intestinal polypeptide (VIP) was studied in 7 healthy subjects and 8 subjects with the common cold.	Terfenadine	14-25	tachykinin precursor 1	Homo sapiens	58-69
1280680-1	1992	The effect of terfenadine on the plasma concentrations of substance P and vasoactive intestinal polypeptide (VIP) was studied in 7 healthy subjects and 8 subjects with the common cold.	Terfenadine	14-25	vasoactive intestinal peptide	Homo sapiens	74-107
1280680-1	1992	The effect of terfenadine on the plasma concentrations of substance P and vasoactive intestinal polypeptide (VIP) was studied in 7 healthy subjects and 8 subjects with the common cold.	Terfenadine	14-25	vasoactive intestinal peptide	Homo sapiens	109-112
1280680-2	1992	Before terfenadine administration, the mean plasma substance P concentration of the subjects with the common cold was significantly higher than that of the healthy subjects.	Terfenadine	7-18	tachykinin precursor 1	Homo sapiens	51-62
1280680-3	1992	The increased mean plasma substance P concentration of the subjects with the common cold was decreased after terfenadine administration.	Terfenadine	109-120	tachykinin precursor 1	Homo sapiens	26-37
1280680-5	1992	The mean plasma VIP concentration of the subjects with common cold was slightly higher than that of the healthy subjects before and after terfenadine administration, with no significant difference.	Terfenadine	138-149	vasoactive intestinal peptide	Homo sapiens	16-19
1418048-1	1992	In a double-blind placebo-controlled randomized two-phase cross-over study comprising 10 (5/5) male subjects the effect of oral therapeutic doses of terfenadine (Teldane, CAS 50679-08-8) on rated performance, systolic and diastolic blood pressure, heart rate and the electroencephalogram of the subjects in an instrument flight (IF) procedure trainer was investigated.	Terfenadine	149-160	BCAR1 scaffold protein, Cas family member	Homo sapiens	171-174
8100726-2	1993	Oral terfenadine reduces the release of prostaglandin D2 (PGD2) and, to a lesser extent, the release of histamine in patients after nasal challenge with allergen.	Terfenadine	5-16	prostaglandin D2 synthase	Homo sapiens	40-56
1387041-5	1992	Bradykinin challenge induced mean maximal increases of 57%, 59%, 77% and 72% in NAR on the placebo, terfenadine, ipratropium bromide and terfenadine plus ipratropium bromide pretreatment days respectively.	Terfenadine	100-111	kininogen 1	Homo sapiens	0-10
1387041-5	1992	Bradykinin challenge induced mean maximal increases of 57%, 59%, 77% and 72% in NAR on the placebo, terfenadine, ipratropium bromide and terfenadine plus ipratropium bromide pretreatment days respectively.	Terfenadine	137-148	kininogen 1	Homo sapiens	0-10
1387041-8	1992	Bradykinin nasal challenge caused a mean maximal increase in albumin levels in recovered nasal lavages of 11.5, 13.0, 12.2 and 12.3 times of baseline levels on the placebo, terfenadine, ipratropium bromide and terfenadine plus ipratroprium bromide pretreatment days respectively.	Terfenadine	173-184	kininogen 1	Homo sapiens	0-10
1387041-8	1992	Bradykinin nasal challenge caused a mean maximal increase in albumin levels in recovered nasal lavages of 11.5, 13.0, 12.2 and 12.3 times of baseline levels on the placebo, terfenadine, ipratropium bromide and terfenadine plus ipratroprium bromide pretreatment days respectively.	Terfenadine	210-221	kininogen 1	Homo sapiens	0-10
1587633-1	1992	In this double-blind crossover study we evaluated the effect of terfenadine on the rise in neutrophil chemotactic activity (NCA) and eosinophil chemotactic activity (ECA) in serum induced by platelet-activating factor (PAF) inhalation in 8 asthmatics.	Terfenadine	64-75	PCNA clamp associated factor	Homo sapiens	191-217
1587633-4	1992	An initial elevation of NCA after PAF inhalation was inhibited by terfenadine, but the effect was diminished after subsequent PAF inhalations.	Terfenadine	66-77	PCNA clamp associated factor	Homo sapiens	34-37
1587633-6	1992	In vitro PAF- and fMLP-induced neutrophil chemotaxis were significantly inhibited by terfenadine.	Terfenadine	85-96	PCNA clamp associated factor	Homo sapiens	9-12
1587633-6	1992	In vitro PAF- and fMLP-induced neutrophil chemotaxis were significantly inhibited by terfenadine.	Terfenadine	85-96	formyl peptide receptor 1	Homo sapiens	18-22
1970226-4	1990	In nine atopic asthmatic subjects, terfenadine 180 mg, when compared to placebo, increased the geometric mean provocation concentration of inhaled agonist required to reduce FEV1 by 20% of baseline (PC20) from 0.7 to greater than 22.9 mg/ml for histamine (P less than 0.01) and 0.3 to 0.5 mg/ml for bradykinin (P less than 0.01).	Terfenadine	35-46	kininogen 1	Homo sapiens	299-309
1914619-7	1991	Terfenadine significantly inhibited the wheal and flare response to histamine and the flare response to injected PAF.	Terfenadine	0-11	PCNA clamp associated factor	Homo sapiens	113-116
1677829-4	1991	Terfenadine, a non-sedating histamine H1-receptor antagonist, caused bronchodilatation in a single dose.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	28-49
1707048-6	1991	The H1 antagonist terfenadine (120 mg po) significantly reduced the flare area associated with endothelin 1: flare 5 min after intradermal endothelin (10 pmol, placebo treated), 668 +/- 405 mm2; terfenadine treated, 201 +/- 257 mm2 (P less than 0.05).	Terfenadine	18-29	endothelin 1	Homo sapiens	95-107
1976343-2	1990	We have assessed the effect of a specific histamine H1-receptor antagonist, terfenadine, in the treatment of atopic asthmatics during the grass pollen season.	Terfenadine	76-87	histamine receptor H1	Homo sapiens	42-63
1777375-5	1991	Terfenadine improved 04.00 h baseline mean PEFR from 242 to 278 l min-1 (P less than 0.05) but a 38 l min-1 diurnal variation in mean PEFR persisted (P less than 0.05).	Terfenadine	0-11	CD59 molecule (CD59 blood group)	Homo sapiens	66-71
1976665-1	1990	We used a nonsedating, selective histamine H1-receptor antagonist, terfenadine, to investigate the effects of antihistamines on the microcirculatory changes and vascular permeability induced by topical histamine provocation challenge.	Terfenadine	67-78	histamine receptor H1	Homo sapiens	33-54
1976343-0	1990	Terfenadine, a potent histamine H1-receptor antagonist in the treatment of grass pollen sensitive asthma.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	22-43
1970226-7	1990	Pharmacological intervention with terfenadine and flurbiprofen led to a significant protection of the airways against the constrictor effect of bradykinin but the effect in each case was small.	Terfenadine	34-45	kininogen 1	Homo sapiens	144-154
1972050-2	1990	Terfenadine is a selective histamine H1-receptor antagonist which, in pharmacodynamic studies, is devoid of central nervous system depressant activity.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	27-48
1972050-4	1990	Terfenadine is superior to placebo, has a more rapid onset of action than astemizole and is as effective as most other histamine H1-receptor antagonists, in relieving rhinitis symptoms.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	119-140
33151169-0	2021	Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels.	Terfenadine	21-32	potassium inwardly rectifying channel subfamily J member 2	Homo sapiens	36-42
34680411-9	2021	Tg(myl7:GA) larvae treated with terfenadine showed bradycardia, 2:1 atrioventricular block, decreased time-averaged ventricular calcium levels but increased calcium transient amplitude, and reduced cardiac output.	Terfenadine	32-43	myosin, light chain 7, regulatory	Danio rerio	3-7
18585198-4	2008	Beer"s law is obeyed over the concentration ranges of 3-72, 3-96, 12-168 and 24-240 microg mL(-1) terfenadine using TCNQ, TCNE, DDQ and p-CLA, respectively, with correlation coefficients 0.9999, 0.9974, 0.9997 and 0.9979 and detection limits 0.3, 0.4, 2.6 and 12.3 microg mL(-1), for the reagents in the same order.	Terfenadine	98-109	selectin P ligand	Homo sapiens	138-141
18585198-5	2008	DDQ and p-CLA react spontaneously with terfenadine to give colored complexes that can be applied for the flow injection analysis of terfenadine in the concentration ranges 2.4-120 and 24-240 microg with correlation coefficients 0.9990 and 0.9985 and detection limits 0.8 and 2.7 microg for DDQ and p-CLA, respectively, in addition to the high sampling through output of 40 sample h(-1).	Terfenadine	39-50	selectin P ligand	Homo sapiens	10-13
18585198-5	2008	DDQ and p-CLA react spontaneously with terfenadine to give colored complexes that can be applied for the flow injection analysis of terfenadine in the concentration ranges 2.4-120 and 24-240 microg with correlation coefficients 0.9990 and 0.9985 and detection limits 0.8 and 2.7 microg for DDQ and p-CLA, respectively, in addition to the high sampling through output of 40 sample h(-1).	Terfenadine	39-50	selectin P ligand	Homo sapiens	300-303
18585198-5	2008	DDQ and p-CLA react spontaneously with terfenadine to give colored complexes that can be applied for the flow injection analysis of terfenadine in the concentration ranges 2.4-120 and 24-240 microg with correlation coefficients 0.9990 and 0.9985 and detection limits 0.8 and 2.7 microg for DDQ and p-CLA, respectively, in addition to the high sampling through output of 40 sample h(-1).	Terfenadine	132-143	selectin P ligand	Homo sapiens	10-13
18585198-5	2008	DDQ and p-CLA react spontaneously with terfenadine to give colored complexes that can be applied for the flow injection analysis of terfenadine in the concentration ranges 2.4-120 and 24-240 microg with correlation coefficients 0.9990 and 0.9985 and detection limits 0.8 and 2.7 microg for DDQ and p-CLA, respectively, in addition to the high sampling through output of 40 sample h(-1).	Terfenadine	132-143	selectin P ligand	Homo sapiens	300-303
33151169-0	2021	Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels.	Terfenadine	21-32	potassium inwardly rectifying channel subfamily J member 4	Homo sapiens	47-53
33151169-4	2021	Terfenadine inhibited Kir2.3 channels with a strikingly greater potency (IC50 = 1.06 +- 0.11 mumol L-1) compared to Kir2.1 channels (IC50 = 27.8 +- 4.8 mumol L-1).	Terfenadine	0-11	potassium inwardly rectifying channel subfamily J member 4	Homo sapiens	22-28
33151169-5	2021	The Kir2.3(I213L) mutant, possessing a larger affinity for phosphatidylinositol 4,5-bisphosphate (PIP2) than the wild-type Kir2.3, was less sensitive to terfenadine inhibition (IC50 = 13.0 +- 2.9 mumol L-1).	Terfenadine	153-164	potassium inwardly rectifying channel subfamily J member 4	Homo sapiens	4-10
33151169-5	2021	The Kir2.3(I213L) mutant, possessing a larger affinity for phosphatidylinositol 4,5-bisphosphate (PIP2) than the wild-type Kir2.3, was less sensitive to terfenadine inhibition (IC50 = 13.0 +- 2.9 mumol L-1).	Terfenadine	153-164	potassium inwardly rectifying channel subfamily J member 4	Homo sapiens	123-129
33151169-6	2021	Additionally, the PIP2 intracellular application had largely reduced the inhibition of Kir2.1 channels by terfenadine.	Terfenadine	106-117	potassium inwardly rectifying channel subfamily J member 2	Homo sapiens	87-93
2892555-9	1987	5 The H1-histamine antagonist terfenadine (60 mg orally) significantly inhibited the wheal and distant flare response to histamine (5 nmol) and NKA, but not that caused by NKB.	Terfenadine	30-41	tachykinin precursor 1	Homo sapiens	144-147
2568881-1	1989	We have attempted to use a potent and selective histamine H1-receptor antagonist terfenadine to allow a larger dose of allergen to be administered to previous single early responders to investigate if an increased dose of allergen could induce a late asthmatic response.	Terfenadine	81-92	histamine receptor H1	Homo sapiens	48-69
2562852-3	1989	In particular 1-[4-[3-[4-[bis(4-fluorophenyl)hydroxymethyl]-1-piperidinyl] propoxy]-3-methoxyphenyl]ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.	Terfenadine	158-169	aryl hydrocarbon receptor	Homo sapiens	113-116
3147222-7	1988	Two of these non-sedating antihistamines, terfenadine and astemizole, have novel binding characteristics with the histamine H1 receptor, exhibiting irreversible binding at higher concentrations.	Terfenadine	42-53	histamine receptor H1	Homo sapiens	114-135
2903817-2	1988	In patients with chronic idiopathic urticaria, terfenadine was found to be as effective as the traditional antihistamine clemastine in reducing the number of wheals and the severity of itch, without causing drowsiness.	Terfenadine	47-58	itchy E3 ubiquitin protein ligase	Homo sapiens	185-189
2574555-1	1989	Results of a double-blind, randomized, placebo-controlled, parallel study in 37 patients indicate that terfenadine, 60 mg bid, is significantly more effective than placebo and as effective as hydroxyzine, 25 mg qid, in the treatment of chronic idiopathic urticaria without causing the somnolence that was associated with the use of hydroxyzine.	Terfenadine	103-114	BH3 interacting domain death agonist	Homo sapiens	122-125
2568212-1	1989	The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed.	Terfenadine	148-159	histamine receptor H1	Homo sapiens	114-135
3125852-2	1987	Terfenadine, a histamine H1-receptor antagonist, was studied in 52 patients with stable mild perennial asthma with an allergic basis.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	15-36
2879489-0	1987	Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways.	Terfenadine	0-11	histamine receptor H1	Homo sapiens	48-69
2885357-1	1987	For some patients, terfenadine, in the currently recommended dose of 60 mg twice daily (bid), may be only modestly effective in the treatment of allergic rhinitis.	Terfenadine	19-30	BH3 interacting domain death agonist	Homo sapiens	88-91
2885357-4	1987	The 300 mg bid terfenadine regimen produced significantly greater skin test suppression (p less than 0.05) than the currently recommended 60 mg bid dose.	Terfenadine	15-26	BH3 interacting domain death agonist	Homo sapiens	11-14
2879489-0	1987	Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways.	Terfenadine	13-20	histamine receptor H1	Homo sapiens	48-69
6129861-5	1982	The result of this exercise is terfenadine, a preferred antihistamine, potent and selective in antagonizing histamine H1-receptor-mediated responses but lacking the usual side effect profile of known histamine H1-receptor antagonists.	Terfenadine	31-42	histamine receptor H1	Homo sapiens	108-129
2857636-8	1985	Thus, terfenadine offers a worthwhile improvement in side effect profile over "traditional" antihistamines, and could well become an "agent of choice" (along with other non-sedating antihistamines) in many patients in whom a histamine H1-receptor antagonist is indicated.	Terfenadine	6-17	histamine receptor H1	Homo sapiens	225-246
2875234-7	1986	Terfenadine, a purportedly selective histamine H1-receptor antagonist, blocked both histamine and acetylcholine-induced bronchoconstriction at doses similar to SK&F 93944.	Terfenadine	0-11	histamine receptor H1	Canis lupus familiaris	37-58
6129861-5	1982	The result of this exercise is terfenadine, a preferred antihistamine, potent and selective in antagonizing histamine H1-receptor-mediated responses but lacking the usual side effect profile of known histamine H1-receptor antagonists.	Terfenadine	31-42	histamine receptor H1	Homo sapiens	200-221
6129862-5	1982	The unsurmountable antagonism of histamine by terfenadine may result from a slow dissociation of terfenadine from the histamine H1-receptor.	Terfenadine	46-57	histamine H1 receptor	Cavia porcellus	118-139
6129862-7	1982	It is concluded that terfenadine is a potent, selective histamine H1-receptor antagonist; the kinetics of association/dissociation of terfenadine with histamine H1-receptors may account for the long-lasting antihistaminic effect in various animal models.	Terfenadine	21-32	histamine H1 receptor	Cavia porcellus	56-77
6129874-1	1982	alpha-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1- piperidinebutanol (terfenadine, RMI 9918, Triludan, Teldane, resp.) is a new histamine H1-receptor antagonist.	Terfenadine	0-82	histamine receptor H1	Homo sapiens	142-163
30561737-7	2019	Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37 C with an IC50 of 7 nM, 18 nM, 343 muM, 165 nM, and 214 nM, respectively.	Terfenadine	32-43	ETS transcription factor ERG	Homo sapiens	67-71
31730936-13	2020	Recalculating the TdP metric and margin values for terfenadine, risperidone and astemizole using the unbound concentration normally associated with treatment and a clinical worst case changes the qNet metric to higher risk values and illustrates the potential benefit to the algorithm of consistently using a clinical high exposure scenario accounting for all "hERG-active species".	Terfenadine	51-62	ETS transcription factor ERG	Homo sapiens	361-365
6109770-2	1980	The keto analog of terfenadine was converted to its O-carboxymethyloxime derivative, which was conjugated to bovine thyroglobulin by a mixed anhydride technique.	Terfenadine	19-30	thyroglobulin	Bos taurus	116-129
33335233-7	2020	Molecular docking of a series of compounds including amiodarone, astemizole, danazol, ebastine, ketoconazole, terfenadine, terfenadone, and arachidonic acid to CYP2J2 confirmed the role of those residues in determining substrate binding and specificity of CYP2J2.	Terfenadine	110-121	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	160-166
33335233-7	2020	Molecular docking of a series of compounds including amiodarone, astemizole, danazol, ebastine, ketoconazole, terfenadine, terfenadone, and arachidonic acid to CYP2J2 confirmed the role of those residues in determining substrate binding and specificity of CYP2J2.	Terfenadine	110-121	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	256-262
32164398-6	2020	Treatment with terfenadine was associated with 10-fold higher expression of atrial natriuretic peptide (p < 0.001 vs. vehicle), increased p53 mRNA expression, and chromatin fragmentation in the TUNEL assay, all of which were significantly reduced by fimasartan treatment.	Terfenadine	15-26	tumor protein p53	Danio rerio	138-141
32249832-8	2020	In addition, hiPSC-IECs oxidatively metabolized terfenadine (CYP3A and CYP2J2 substrate) and midazolam (CYP3A substrate).	Terfenadine	48-59	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	61-66
32249832-8	2020	In addition, hiPSC-IECs oxidatively metabolized terfenadine (CYP3A and CYP2J2 substrate) and midazolam (CYP3A substrate).	Terfenadine	48-59	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	71-77
31664867-5	2019	Our functional data from isolated zkcnh6a channels show that these channels respond to hERG1a channel blockers (dofetilide and terfenadine), and type 1 (RPR260243) and type 2 (NS1643, PD-118057) hERG1a activator compounds, in a similar manner to hKCNH2a channels, with minor differences largely accounted for by subtly different biophysical properties in the two channels.	Terfenadine	127-138	potassium voltage-gated channel subfamily H member 2	Homo sapiens	87-92
31183371-8	2019	Conclusions: Our study revealed for the first time that second-generation antihistamines, including cetirizine, fexofenadine, azelastine, and terfenadine, exert suppressive effects on lymphocyte Kv1.3-channels.	Terfenadine	142-153	potassium voltage-gated channel, shaker-related subfamily, member 3	Mus musculus	195-200
30483130-5	2018	In vivo arrhythmia model in Cmlc2-GFP transgenic zebrafish was induced by terfenadine, which exhibited obvious reduction of heart rate and occurrence of atrioventricular block.	Terfenadine	74-85	myosin, light chain 7, regulatory	Danio rerio	28-33
30206647-7	2018	In current clamp, ERG channel blockers, terfenadine (10 microM) and E-4031 (10 microM), were applied in both cell types.	Terfenadine	40-51	ETS transcription factor	Mus musculus	18-21
28436281-2	2018	Roles of human cytochrome P450 (P450) 3A4 in oxidation of an antihistaminic drug terfenadine have been previously investigated in association with terfenadine-ketoconazole interaction.	Terfenadine	81-92	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	15-41
29759885-2	2018	In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine.	Terfenadine	237-248	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	136-142
29759885-2	2018	In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine.	Terfenadine	237-248	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	136-142
29759885-4	2018	Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs).	Terfenadine	139-150	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	15-21
29759885-4	2018	Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs).	Terfenadine	139-150	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	80-86
29759885-4	2018	Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs).	Terfenadine	139-150	latexin	Homo sapiens	192-195
29548821-5	2018	Using terfenadine, a selective chemical inhibitor of HRH1, we showed that the inhibition of HRH1 activity in basal BC cells leads to sub-G0 cell accumulation, suppresses proliferation, promotes cell motility and triggers the activation of extracellular signal-regulated kinase (ERK) signaling, initiating the mitochondrial apoptotic pathway.	Terfenadine	6-17	histamine receptor H1	Homo sapiens	53-57
29548821-5	2018	Using terfenadine, a selective chemical inhibitor of HRH1, we showed that the inhibition of HRH1 activity in basal BC cells leads to sub-G0 cell accumulation, suppresses proliferation, promotes cell motility and triggers the activation of extracellular signal-regulated kinase (ERK) signaling, initiating the mitochondrial apoptotic pathway.	Terfenadine	6-17	histamine receptor H1	Homo sapiens	92-96
29548821-5	2018	Using terfenadine, a selective chemical inhibitor of HRH1, we showed that the inhibition of HRH1 activity in basal BC cells leads to sub-G0 cell accumulation, suppresses proliferation, promotes cell motility and triggers the activation of extracellular signal-regulated kinase (ERK) signaling, initiating the mitochondrial apoptotic pathway.	Terfenadine	6-17	mitogen-activated protein kinase 1	Homo sapiens	239-276
29548821-5	2018	Using terfenadine, a selective chemical inhibitor of HRH1, we showed that the inhibition of HRH1 activity in basal BC cells leads to sub-G0 cell accumulation, suppresses proliferation, promotes cell motility and triggers the activation of extracellular signal-regulated kinase (ERK) signaling, initiating the mitochondrial apoptotic pathway.	Terfenadine	6-17	mitogen-activated protein kinase 1	Homo sapiens	278-281
29548821-6	2018	Furthermore, HER2-targeted therapy-resistant cells express higher levels of HRH1 and are more sensitive to terfenadine treatment.	Terfenadine	107-118	erb-b2 receptor tyrosine kinase 2	Homo sapiens	13-17
28436281-2	2018	Roles of human cytochrome P450 (P450) 3A4 in oxidation of an antihistaminic drug terfenadine have been previously investigated in association with terfenadine-ketoconazole interaction.	Terfenadine	147-158	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	15-41
29563525-7	2018	Here, we have directly assessed the role of inactivation in cisparide and terfenadine drug binding in mutant (I663P) hERG channels where the activation gate is trapped-open.	Terfenadine	74-85	ETS transcription factor ERG	Homo sapiens	117-121
29223463-0	2018	Terfenadine metabolism of human cytochrome P450 2J2 containing genetic variations (G312R, P351L and P115L).	Terfenadine	0-11	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	32-51
29035434-11	2017	A significant increase of natriuretic peptide B (NPPB) mRNA was found in terfenadine-treated zebrafish.	Terfenadine	73-84	natriuretic peptide B	Danio rerio	26-47
29175952-4	2018	Three chemically diverse ERG channel blockers (terfenadine, ErgToxin-1, and E-4031) abolished persistent firing and the underlying increase in input resistance in deep pyramidal cells in temporal and prefrontal association neocortex.	Terfenadine	47-58	ETS transcription factor ERG	Rattus norvegicus	25-28
29035434-11	2017	A significant increase of natriuretic peptide B (NPPB) mRNA was found in terfenadine-treated zebrafish.	Terfenadine	73-84	natriuretic peptide B	Danio rerio	49-53
26899760-0	2016	Marmoset cytochrome P450 2J2 mainly expressed in small intestines and livers effectively metabolizes human P450 2J2 probe substrates, astemizole and terfenadine.	Terfenadine	149-160	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	9-28
27553911-7	2017	Compared to PSS, the IC50 values, conducted at room temperature, of the classic hERG blocking drugs cisapride, moxifloxacin, and terfenadine were shifted to the right by an extent predicted by their known plasma protein binding, but we did not detect any differences in IC50 s between male and female serum.	Terfenadine	129-140	ETS transcription factor ERG	Homo sapiens	80-84
28237650-4	2017	Additionally, CYP2J2 metabolizes a number of xenobiotics such as astemizole and terfenadine and is potently inhibited by danazol and telmisartan.	Terfenadine	80-91	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	14-20
29911373-3	2017	Additionally, CYP2J2 plays an indispensable role in the intestinal metabolism of various drugs, such as astemizole, terfenadine and ebastine.	Terfenadine	116-127	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	14-20
27681411-6	2016	Using qRT-PCR analysis, we demonstrated that, among those genes, p21 (Cdc42/Rac)-activated kinase 1 (pak1) mRNA was downregulated by treatment with terfenadine and astemizole.	Terfenadine	148-159	KRAS proto-oncogene, GTPase	Rattus norvegicus	65-68
27681411-6	2016	Using qRT-PCR analysis, we demonstrated that, among those genes, p21 (Cdc42/Rac)-activated kinase 1 (pak1) mRNA was downregulated by treatment with terfenadine and astemizole.	Terfenadine	148-159	cell division cycle 42	Rattus norvegicus	70-99
27681411-6	2016	Using qRT-PCR analysis, we demonstrated that, among those genes, p21 (Cdc42/Rac)-activated kinase 1 (pak1) mRNA was downregulated by treatment with terfenadine and astemizole.	Terfenadine	148-159	p21 (RAC1) activated kinase 1	Rattus norvegicus	101-105
27035465-7	2016	RESULTS: A 48 hours exposure of human erythrocytes to Terfenadine (&gt;= 5 microM) significantly increased the percentage of annexin-V-binding cells and triggered hemolysis without significantly modifying the average forward scatter.	Terfenadine	54-65	annexin A5	Homo sapiens	125-134
27035465-9	2016	The effect of Terfenadine on annexin-V-binding was significantly blunted but not abolished by removal of extracellular Ca2+.	Terfenadine	14-25	annexin A5	Homo sapiens	29-38
27035465-10	2016	Exposure of human erythrocytes to Ca2+ ionophore ionomycin (1 microM, 15 min) triggered annexin-V-binding, an effect augmented by Terfenadine pretreatment (10 microM, 48 hours).	Terfenadine	130-141	annexin A5	Homo sapiens	88-97
26358220-6	2015	The alpha-MSH-induced scratching was inhibited by the mu-opioid receptor antagonist naltrexone and the H1 histamine receptor antagonist terfenadine.	Terfenadine	136-147	pro-opiomelanocortin-alpha	Mus musculus	4-13
26358220-7	2015	In mast cell-deficient mice, alpha-MSH also elicited scratching, which was inhibited by terfenadine.	Terfenadine	88-99	pro-opiomelanocortin-alpha	Mus musculus	29-38
26048912-4	2015	Of these four CYP2J2 inhibitors, danazol strongly inhibited CYP2J2-mediated albendazole, astemizole, ebastine, and terfenadine metabolism in a substrate-independent manner, with IC50 values of 0.05, 0.07, 0.18, and 0.34 muM, respectively.	Terfenadine	115-126	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	60-66
26376488-11	2015	Furthermore, the equine KV11.1 channel was susceptible to pharmacological block with terfenadine.	Terfenadine	85-96	potassium voltage-gated channel subfamily H member 2	Homo sapiens	24-30
26048912-1	2015	Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine.	Terfenadine	202-213	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	0-19
26048912-1	2015	Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine.	Terfenadine	202-213	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	21-27
26048912-6	2015	Terfenadone strongly inhibited CYP2J2-mediated albendazole, astemizole, and terfenadine metabolism (IC50 &lt; 0.21 muM), whereas it showed weak inhibition against CYP2J2-catalyzed ebastine hydroxylase activity (IC50 = 6.04 muM).	Terfenadine	76-87	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	31-37
25238555-5	2014	This scaffold suffers from hERG liabilities which were not remedied through this round of optimization; however, given the overall improvement in activity of the set, terfenadine-based analogues provide a novel structural class of antimicrobial compounds with potential for further characterization as part of the continuing process to meet the current need for new antibiotics.	Terfenadine	167-178	ETS transcription factor ERG	Homo sapiens	27-31
25857771-6	2015	RESULTS: We show that drug-related compounds, debrisoquine and terfenadine derivatives, subtrates of CYP2D6 and CYP2J2, are hydroxylated by recombinant CYP2U1 with regioselectivities different from those reported for CYP2D6 and 2J2.	Terfenadine	63-74	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	101-107
25857771-6	2015	RESULTS: We show that drug-related compounds, debrisoquine and terfenadine derivatives, subtrates of CYP2D6 and CYP2J2, are hydroxylated by recombinant CYP2U1 with regioselectivities different from those reported for CYP2D6 and 2J2.	Terfenadine	63-74	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	112-118
25857771-6	2015	RESULTS: We show that drug-related compounds, debrisoquine and terfenadine derivatives, subtrates of CYP2D6 and CYP2J2, are hydroxylated by recombinant CYP2U1 with regioselectivities different from those reported for CYP2D6 and 2J2.	Terfenadine	63-74	cytochrome P450 family 2 subfamily U member 1	Homo sapiens	152-158
25857771-6	2015	RESULTS: We show that drug-related compounds, debrisoquine and terfenadine derivatives, subtrates of CYP2D6 and CYP2J2, are hydroxylated by recombinant CYP2U1 with regioselectivities different from those reported for CYP2D6 and 2J2.	Terfenadine	63-74	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	217-223
24997310-0	2014	A note on CYP2J2-mediated terfenadine hydroxylation in human liver microsomes.	Terfenadine	26-37	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	10-16
24998194-0	2014	Response to comment: "A note on CYP2J2-mediated terfenadine hydroxylation in human liver microsomes".	Terfenadine	48-59	cytochrome P450 family 2 subfamily J member 2	Homo sapiens	32-38