PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32583097-10 2020 In addition, we have identified novel FXR antagonistic effects of well-studied hepatotoxic drugs, including bosentan, tolcapone and ritonavir. Bosentan 108-116 nuclear receptor subfamily 1 group H member 4 Homo sapiens 38-41 33856498-2 2021 Bosentan (BST) is the first approved oral targeted drug of endothelin-1 (ET-1) receptor antagonists for the treatment of PAH. Bosentan 0-8 endothelin 1 Homo sapiens 73-77 33856498-2 2021 Bosentan (BST) is the first approved oral targeted drug of endothelin-1 (ET-1) receptor antagonists for the treatment of PAH. Bosentan 10-13 endothelin 1 Homo sapiens 59-71 33856498-2 2021 Bosentan (BST) is the first approved oral targeted drug of endothelin-1 (ET-1) receptor antagonists for the treatment of PAH. Bosentan 10-13 endothelin 1 Homo sapiens 73-77 32918210-1 2021 OBJECTIVE: This systematic review and meta-analysis was conducted to identify if long-term bosentan is an effective and safe treatment for pulmonary arterial hypertension (PAH) regardless of type, including idiopathic PAH (IPAH), and PAH associated with congenital heart disease (APAH-CHD), connective tissue disease (APAH-CTD), and human immunodeficiency virus (APAH-HIV). Bosentan 91-99 CTD Homo sapiens 323-326 32918210-8 2021 Furthermore, among the hemodynamic parameters, long-term bosentan led to a significant decrease in mean pulmonary artery pressure (SMD - 0.86, p < 0.0001) in APAH-CTD, and a decrease in pulmonary vascular resistance (SMD - 0.65, p < 0.0001) and elevated oxygen saturation (SMD 0.30, p = 0.006) in APAH-CHD. Bosentan 57-65 CTD Homo sapiens 163-166 32918210-12 2021 In addition, we conclude that long-term oral bosentan should be considered for patients with CTD to achieve a satisfactory exercise capacity, and for those with APAH-HIV to improve survivals, where more attention on adverse events is required. Bosentan 45-53 CTD Homo sapiens 93-96 33039464-11 2021 LoT positively predicts genomic predisposition (CYP2C9*2) for Bosentan-induced cholestasis. Bosentan 62-70 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 48-54 32535962-7 2021 RESULTS: Topical application of bosentan significantly attenuated the development of mite-induced AD-like skin inflammation, dermatitis scores, ear thickness, scratching bouts, and serum level of thymus and activation-regulated chemokine in NC/Nga mice. Bosentan 32-40 reticulon 4 Mus musculus 244-247 32535962-8 2021 Bosentan application also significantly reduced the gene expression of Il13, Il17, and Ifng in the treated lesions. Bosentan 0-8 interleukin 13 Mus musculus 71-75 32535962-8 2021 Bosentan application also significantly reduced the gene expression of Il13, Il17, and Ifng in the treated lesions. Bosentan 0-8 interleukin 17A Mus musculus 77-81 32535962-8 2021 Bosentan application also significantly reduced the gene expression of Il13, Il17, and Ifng in the treated lesions. Bosentan 0-8 interferon gamma Mus musculus 87-91 32535962-9 2021 Histologically, the number of infiltrated dermal cells, the epidermal EDN1 expression, and the number of intraepidermal nerve fibers were significantly inhibited upon bosentan application. Bosentan 167-175 endothelin 1 Mus musculus 70-74 33209081-3 2020 Results: Whether ET-1 is present or not in the tumor area, bosentan exerts anti-proliferative effect on breast cancer. Bosentan 59-67 endothelin 1 Homo sapiens 17-21 33209081-4 2020 However, ET-1 and bosentan group showed important inhibitory effect on tumor migration compared to bosentan alone, which can be attributed to increased activity of ET-1 axis in the presence of ET-1. Bosentan 18-26 endothelin 1 Homo sapiens 164-168 33209081-4 2020 However, ET-1 and bosentan group showed important inhibitory effect on tumor migration compared to bosentan alone, which can be attributed to increased activity of ET-1 axis in the presence of ET-1. Bosentan 18-26 endothelin 1 Homo sapiens 164-168 33209081-4 2020 However, ET-1 and bosentan group showed important inhibitory effect on tumor migration compared to bosentan alone, which can be attributed to increased activity of ET-1 axis in the presence of ET-1. Bosentan 99-107 endothelin 1 Homo sapiens 9-13 33209081-4 2020 However, ET-1 and bosentan group showed important inhibitory effect on tumor migration compared to bosentan alone, which can be attributed to increased activity of ET-1 axis in the presence of ET-1. Bosentan 99-107 endothelin 1 Homo sapiens 164-168 33209081-4 2020 However, ET-1 and bosentan group showed important inhibitory effect on tumor migration compared to bosentan alone, which can be attributed to increased activity of ET-1 axis in the presence of ET-1. Bosentan 99-107 endothelin 1 Homo sapiens 164-168 33209081-5 2020 The imbalance among the NF-kB, caspases, and VEGF, which are predictive factors of carcinogenesis significantly improved after bosentan administration. Bosentan 127-135 vascular endothelial growth factor A Homo sapiens 45-49 33209081-7 2020 The second major finding was that bosentan inhibited ET-1-mediated effects on tumor proliferation and migration. Bosentan 34-42 endothelin 1 Homo sapiens 53-57 32561219-8 2020 FPI-induced expression levels of ET-1 and ETB receptors were reduced by bosentan, but not by ambrisentan. Bosentan 72-80 endothelin 1 Mus musculus 33-37 32561219-8 2020 FPI-induced expression levels of ET-1 and ETB receptors were reduced by bosentan, but not by ambrisentan. Bosentan 72-80 endothelin receptor type B Homo sapiens 42-45 32561219-9 2020 In cultured mouse astrocytes and brain microvessel endothelial cells, ET-1 (100 nM) increased prepro--ET-1 mRNA, which was inhibited by bosentan, but not by ambrisentan. Bosentan 136-144 endothelin 1 Mus musculus 70-74 32561219-9 2020 In cultured mouse astrocytes and brain microvessel endothelial cells, ET-1 (100 nM) increased prepro--ET-1 mRNA, which was inhibited by bosentan, but not by ambrisentan. Bosentan 136-144 endothelin 1 Mus musculus 102-106 32561219-10 2020 FPI-induced alterations of the expression levels of matrix metalloproteinase-9, vascular endothelial growth factor-A, and angiopoietin-1 in the mouse cerebrum were reduced by delayed administration of bosentan, while ambrisentan had no significant effects. Bosentan 201-209 matrix metallopeptidase 9 Mus musculus 52-78 32561219-10 2020 FPI-induced alterations of the expression levels of matrix metalloproteinase-9, vascular endothelial growth factor-A, and angiopoietin-1 in the mouse cerebrum were reduced by delayed administration of bosentan, while ambrisentan had no significant effects. Bosentan 201-209 vascular endothelial growth factor A Mus musculus 80-116 32561219-10 2020 FPI-induced alterations of the expression levels of matrix metalloproteinase-9, vascular endothelial growth factor-A, and angiopoietin-1 in the mouse cerebrum were reduced by delayed administration of bosentan, while ambrisentan had no significant effects. Bosentan 201-209 angiopoietin 1 Mus musculus 122-136 34023918-3 2021 Here, we use functional investigation of CFTR to show that a nearby arginine (R134) plays a functionally analogous role. Bosentan 78-82 CF transmembrane conductance regulator Homo sapiens 41-45 33856498-0 2021 The Influence of Bosentan on MicroRNA-27a/PPARgamma/ET-1 Signaling Pathway in Pulmonary Artery Hypertension. Bosentan 17-25 microRNA 27a Homo sapiens 29-41 33856498-0 2021 The Influence of Bosentan on MicroRNA-27a/PPARgamma/ET-1 Signaling Pathway in Pulmonary Artery Hypertension. Bosentan 17-25 peroxisome proliferator activated receptor gamma Homo sapiens 42-51 33856498-0 2021 The Influence of Bosentan on MicroRNA-27a/PPARgamma/ET-1 Signaling Pathway in Pulmonary Artery Hypertension. Bosentan 17-25 endothelin 1 Homo sapiens 52-56 33856498-2 2021 Bosentan (BST) is the first approved oral targeted drug of endothelin-1 (ET-1) receptor antagonists for the treatment of PAH. Bosentan 0-8 endothelin 1 Homo sapiens 59-71 33026618-11 2021 Notably, treatment with bosentan attenuated arsenic-induced renal damage and resisted arsenic-led reduction in renal eNOS expression. Bosentan 24-32 nitric oxide synthase 3 Rattus norvegicus 117-121 33026618-12 2021 In addition, sodium arsenite-induced alteration in hepatic parameters (serum aspartate aminotransferase, alanine transferase, alkaline phosphatase, bilirubin), oxidative stress and histological changes were abrogated by bosentan treatment in rats. Bosentan 220-228 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 77-103 33026618-13 2021 Hence, we conclude that bosentan treatment attenuated sodium arsenite-induced oxidative stress, fibrosis and reduction in renal eNOS expression in rat kidneys. Bosentan 24-32 nitric oxide synthase 3 Rattus norvegicus 128-132 33359621-7 2021 Bosentan (1E-7 M) and macitentan (1E-8 M, 3E-8 M, 1E-7 M) inhibited ET-1 induced contractions, whereas vardenafil (1E-6 M, 3E-6 M, 1E-5 M) inhibited only the NE induced part of the contractions. Bosentan 0-8 endothelin 1 Homo sapiens 68-72 32489640-9 2020 Quantitative real-time PCR analysis revealed that interleukin 6, stromal cell-derived factor-1, and monocyte chemoattractant protein-1 were upregulated by hypoxia, in which interleukin 6 and monocyte chemoattractant protein-1 were downregulated and stromal cell-derived factor-1 was upregulated by bosentan. Bosentan 298-306 interleukin 6 Mus musculus 50-63 32765401-4 2020 A preliminary study in patients with MS showed that CBF could be restored to normal values after a single dose of 62.5 mg of the ET-1 antagonist bosentan. Bosentan 145-153 endothelin 1 Homo sapiens 129-133 32765401-15 2020 Future studies with bosentan in MS should focus on patients with elevated ET-1 levels in cerebrospinal fluid or blood. Bosentan 20-28 endothelin 1 Homo sapiens 74-78 32433892-3 2020 Previously, we demonstrated, using drug metabolism enzymes and transporters (DMET) analysis, that the carbohydrate sulfotransferase 3 (CHST3) and CHST13 alleles are significantly more frequent in patients with elevated amino-transferases during therapy with bosentan than they are in patients without liver toxicity. Bosentan 258-266 carbohydrate sulfotransferase 3 Homo sapiens 102-133 32433892-3 2020 Previously, we demonstrated, using drug metabolism enzymes and transporters (DMET) analysis, that the carbohydrate sulfotransferase 3 (CHST3) and CHST13 alleles are significantly more frequent in patients with elevated amino-transferases during therapy with bosentan than they are in patients without liver toxicity. Bosentan 258-266 carbohydrate sulfotransferase 3 Homo sapiens 135-140 32433892-3 2020 Previously, we demonstrated, using drug metabolism enzymes and transporters (DMET) analysis, that the carbohydrate sulfotransferase 3 (CHST3) and CHST13 alleles are significantly more frequent in patients with elevated amino-transferases during therapy with bosentan than they are in patients without liver toxicity. Bosentan 258-266 carbohydrate sulfotransferase 13 Homo sapiens 146-152 32423820-8 2020 Furthermore, our results revealed that bosentan, an ETAR antagonist, enhanced the growth-inhibiting and proapoptotic effects of gemcitabine on pancreatic cancer cells. Bosentan 39-47 endothelin receptor type A Homo sapiens 52-56 32259555-7 2020 Among them, kaempferol decreased the concentration most significantly, by 54.17 %, which indicated that flavonoids may alleviate bosentan-induced liver injury by inhibiting OATP1B1-mediated bosentan uptake. Bosentan 129-137 solute carrier organic anion transporter family member 1B1 Homo sapiens 173-180 32259555-7 2020 Among them, kaempferol decreased the concentration most significantly, by 54.17 %, which indicated that flavonoids may alleviate bosentan-induced liver injury by inhibiting OATP1B1-mediated bosentan uptake. Bosentan 190-198 solute carrier organic anion transporter family member 1B1 Homo sapiens 173-180 32259555-9 2020 Taken together, our findings would provide helpful information for predicting the potential risks of flavonoid-containing food/herb-drug interactions in humans and alleviating bosentan -induced liver injury by OATP1B1 regulation. Bosentan 176-184 solute carrier organic anion transporter family member 1B1 Homo sapiens 210-217 32489640-9 2020 Quantitative real-time PCR analysis revealed that interleukin 6, stromal cell-derived factor-1, and monocyte chemoattractant protein-1 were upregulated by hypoxia, in which interleukin 6 and monocyte chemoattractant protein-1 were downregulated and stromal cell-derived factor-1 was upregulated by bosentan. Bosentan 298-306 chemokine (C-X-C motif) ligand 12 Mus musculus 65-94 32489640-9 2020 Quantitative real-time PCR analysis revealed that interleukin 6, stromal cell-derived factor-1, and monocyte chemoattractant protein-1 were upregulated by hypoxia, in which interleukin 6 and monocyte chemoattractant protein-1 were downregulated and stromal cell-derived factor-1 was upregulated by bosentan. Bosentan 298-306 chemokine (C-C motif) ligand 2 Mus musculus 100-134 32489640-10 2020 Protein level of endothelial nitric oxide synthase (eNOS) in the whole lung was significantly upregulated by hypoxia, which was further upregulated by bosentan. Bosentan 151-159 nitric oxide synthase 3, endothelial cell Mus musculus 17-50 32343134-1 2020 We have previously reported the crystal structures of endothelin-1 (ET-1)-bound, ligand-free, and antagonist bosentan-bound forms of the thermostabilized ET type B receptor (ETB). Bosentan 109-117 endothelin receptor type B Homo sapiens 154-172 32489640-10 2020 Protein level of endothelial nitric oxide synthase (eNOS) in the whole lung was significantly upregulated by hypoxia, which was further upregulated by bosentan. Bosentan 151-159 nitric oxide synthase 3, endothelial cell Mus musculus 52-56 32343134-1 2020 We have previously reported the crystal structures of endothelin-1 (ET-1)-bound, ligand-free, and antagonist bosentan-bound forms of the thermostabilized ET type B receptor (ETB). Bosentan 109-117 endothelin receptor type B Homo sapiens 174-177 31886257-0 2019 The Protective Effect of Bosentan against Atherosclerosis in Apolipoprotein E-Deficient Mice Is Mediated by miRNA-21. Bosentan 25-33 apolipoprotein E Mus musculus 61-77 31600800-1 2020 INTRODUCTION: Bosentan is an endothelin-1 receptor antagonist with anti-inflammatory, antioxidant, and antiproliferative effects. Bosentan 15-23 endothelin receptor type A Rattus norvegicus 30-51 32728000-7 2020 P < 0.01), heart rate, brain natriuretic peptide, arterial oxygen saturation, and mixed venous oxygen saturation than the 1st generation ERA bosentan.We conclude that all ERAs could successfully improve the hemodynamics of PAH patients and that the newer generation ERAs, ambrisentan and macitentan, seemed to be preferable to bosentan. Bosentan 327-335 ES cell expressed Ras Homo sapiens 171-175 31886257-3 2019 We hypothesized that atherosclerosis would be associated with endothelial dysfunction and that bosentan (Tracleer ), a dual endothelin-receptor antagonist, would preserve endothelial cell function in an apolipoprotein E-deficient (ApoE-/-) mouse model of atherosclerosis. Bosentan 95-103 apolipoprotein E Mus musculus 231-235 31886257-6 2019 Notably, bosentan treatment was associated with decreased concentrations of these proteins and of blood lipids in ApoE-/- mice. Bosentan 9-17 apolipoprotein E Mus musculus 114-118 31886257-7 2019 Consistent with these findings, we observed increased concentrations of miRNA-21 and PDCD4 mRNA expression in the aortic arch endothelium after bosentan treatment. Bosentan 144-152 programmed cell death 4 Mus musculus 85-90 31886257-8 2019 We conclude that bosentan can prevent endothelial cell death and protect against atherosclerosis in ApoE-deficient mice by upregulating miRNA-21. Bosentan 17-25 apolipoprotein E Mus musculus 100-104 31063771-6 2019 Bosentan (10, 20 & 30 mg/kg) pretreatment caused dose-dependent inhibition of the MAP increase as well as PVC and HVC decreases to endothelin-1. Bosentan 0-8 endothelin 1 Rattus norvegicus 131-143 31386893-10 2019 The NaHS-induced ANP secretion during hypoxia was also blocked by the pretreatment with HIF-1alpha inhibitor (2-methoxy- estradiol), PPAR-gamma inhibitor (GW9662) but not by NOS inhibitor (L-NAME) and endothelin receptor inhibitor (bosentan). Bosentan 232-240 natriuretic peptide A Rattus norvegicus 17-20 30986528-11 2019 The effects of ET-1 were blocked by co-injection of ET receptor antagonists, bosentan or BQ-123. Bosentan 77-85 endothelin 1 Rattus norvegicus 15-19 30660098-8 2019 In ECs, endothelin-1 (ET-1) induced KLF4 S-nitrosation, which was inhibited by an endothelin receptor antagonist Bosentan. Bosentan 113-121 endothelin 1 Rattus norvegicus 8-20 31025223-6 2019 Pretreatment with bosentan (dual blocker of ETA and ETB receptors), amino-oxyacetic acid (CBS synthase inhibitor), and DL-propargylglycine (CLS inhibitor) significantly attenuated RIPC-mediated beneficial effects and biochemical alterations. Bosentan 18-26 endothelin receptor type A Mus musculus 44-47 30739341-10 2019 Importantly, endothelin-1 stimulation suppressed galectin-7 expression in normal human keratinocytes, and bosentan, a dual endothelin receptor antagonist, reversed circulating galectin-7 levels and epidermal galectin-7 expression in SSc patients. Bosentan 106-114 galectin 7 Homo sapiens 176-186 30739341-10 2019 Importantly, endothelin-1 stimulation suppressed galectin-7 expression in normal human keratinocytes, and bosentan, a dual endothelin receptor antagonist, reversed circulating galectin-7 levels and epidermal galectin-7 expression in SSc patients. Bosentan 106-114 galectin 7 Homo sapiens 176-186 30563869-8 2019 Endothelin-1 (ET-1) and hypoxia-inducible factor-1alpha (HIF-1alpha) were key mediators of REDD1-driven NETs as demonstrated by their inhibition with bosentan and L-ascorbic acid, respectively. Bosentan 150-158 endothelin 1 Homo sapiens 0-12 30563869-8 2019 Endothelin-1 (ET-1) and hypoxia-inducible factor-1alpha (HIF-1alpha) were key mediators of REDD1-driven NETs as demonstrated by their inhibition with bosentan and L-ascorbic acid, respectively. Bosentan 150-158 hypoxia inducible factor 1 subunit alpha Homo sapiens 24-55 30563869-8 2019 Endothelin-1 (ET-1) and hypoxia-inducible factor-1alpha (HIF-1alpha) were key mediators of REDD1-driven NETs as demonstrated by their inhibition with bosentan and L-ascorbic acid, respectively. Bosentan 150-158 hypoxia inducible factor 1 subunit alpha Homo sapiens 57-67 30563869-8 2019 Endothelin-1 (ET-1) and hypoxia-inducible factor-1alpha (HIF-1alpha) were key mediators of REDD1-driven NETs as demonstrated by their inhibition with bosentan and L-ascorbic acid, respectively. Bosentan 150-158 DNA damage inducible transcript 4 Homo sapiens 91-96 31237545-3 2019 Here, we describe the case of a 3-year-old boy with a failed Fontan operation who was treated with bosentan, an endothelin-1 receptor blocker. Bosentan 99-107 endothelin receptor type A Homo sapiens 112-133 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. Bosentan 27-35 solute carrier organic anion transporter family member 1B1 Homo sapiens 151-158 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. Bosentan 27-35 solute carrier organic anion transporter family member 1B3 Homo sapiens 160-167 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. Bosentan 27-35 solute carrier organic anion transporter family member 2B1 Homo sapiens 172-179 30660098-8 2019 In ECs, endothelin-1 (ET-1) induced KLF4 S-nitrosation, which was inhibited by an endothelin receptor antagonist Bosentan. Bosentan 113-121 Kruppel like factor 4 Rattus norvegicus 36-40 30261985-6 2018 Here, based on our clinical experience, we provide our recommendations for dose titration schemes for PAH medications that require individualized dosing in adult patients, including agents acting on the endothelin-1 pathway (bosentan and ambrisentan), the prostacyclin pathway (epoprostenol, treprostinil, and selexipag), and the nitric oxide pathway (tadalafil and the soluble guanylate cyclase stimulator riociguat). Bosentan 225-233 endothelin 1 Homo sapiens 203-215 30185506-5 2018 Rapamycin, an mTORC1 inhibitor, and bosentan, an EDN1 antagonist, eliminated the difference in renal function between TSC1fl/fl and Fibro-TSC1-/- mice after LPS injection. Bosentan 36-44 endothelin 1 Mus musculus 49-53 30185506-5 2018 Rapamycin, an mTORC1 inhibitor, and bosentan, an EDN1 antagonist, eliminated the difference in renal function between TSC1fl/fl and Fibro-TSC1-/- mice after LPS injection. Bosentan 36-44 TSC complex subunit 1 Mus musculus 118-122 30185506-5 2018 Rapamycin, an mTORC1 inhibitor, and bosentan, an EDN1 antagonist, eliminated the difference in renal function between TSC1fl/fl and Fibro-TSC1-/- mice after LPS injection. Bosentan 36-44 TSC complex subunit 1 Mus musculus 138-142 29206487-1 2018 The treatment of human pulmonary artery smooth muscle cells with ET-1 stimulates the activity of PLD and NADPH oxidase, but this stimulation is inhibited by pretreatment with bosentan (ET-1 receptor antagonist), FIPI (PLD inhibitor), apocynin (NADPH oxidase inhibitor), and EGCG and ECG (catechins having a galloyl group), but not EGC and EC (catechins devoid of a galloyl group). Bosentan 175-183 glycosylphosphatidylinositol specific phospholipase D1 Homo sapiens 97-100 30058129-11 2018 CONCLUSIONS: Bosentan, initiated early post-transplant, was associated with a significant decrease in PVR. Bosentan 13-21 PVR cell adhesion molecule Homo sapiens 102-105 30118797-0 2018 CHST3 and CHST13 polymorphisms as predictors of bosentan-induced liver toxicity in Japanese patients with pulmonary arterial hypertension. Bosentan 48-56 carbohydrate sulfotransferase 3 Homo sapiens 0-5 30118797-0 2018 CHST3 and CHST13 polymorphisms as predictors of bosentan-induced liver toxicity in Japanese patients with pulmonary arterial hypertension. Bosentan 48-56 carbohydrate sulfotransferase 13 Homo sapiens 10-16 30118797-7 2018 We extracted 16 SNPs (P < 0.05) using the Jonckheere-Terpstra trend test and multiplex logistic analysis; we identified two SNPs in two genes, CHST3 and CHST13, which are responsible for proteoglycan sulfation and were significantly associated with bosentan-induced liver injury. Bosentan 253-261 carbohydrate sulfotransferase 3 Homo sapiens 147-152 30118797-7 2018 We extracted 16 SNPs (P < 0.05) using the Jonckheere-Terpstra trend test and multiplex logistic analysis; we identified two SNPs in two genes, CHST3 and CHST13, which are responsible for proteoglycan sulfation and were significantly associated with bosentan-induced liver injury. Bosentan 253-261 carbohydrate sulfotransferase 13 Homo sapiens 157-163 29206487-1 2018 The treatment of human pulmonary artery smooth muscle cells with ET-1 stimulates the activity of PLD and NADPH oxidase, but this stimulation is inhibited by pretreatment with bosentan (ET-1 receptor antagonist), FIPI (PLD inhibitor), apocynin (NADPH oxidase inhibitor), and EGCG and ECG (catechins having a galloyl group), but not EGC and EC (catechins devoid of a galloyl group). Bosentan 175-183 glycosylphosphatidylinositol specific phospholipase D1 Homo sapiens 218-221 29947542-10 2018 Even though ET-1 levels were low (less than 10 nM levels used under normal growth conditions), blocking of ET receptors with bosentan inhibited the necroptosis pathway and improved the cell migration ability of BMVECs, suggesting that under inflammatory conditions, ET-1 activates PCD pathways in BMVECs even at physiological levels. Bosentan 125-133 endothelin 1 Homo sapiens 266-270 29099661-6 2018 Given the demonstrated vasoreactivity, the boy was started on the calcium channel blocker amlodipine, in combination with the endothelin-1 receptor antagonist bosentan. Bosentan 159-167 endothelin receptor type A Homo sapiens 126-147 29475833-1 2018 Bosentan is a substrate of hepatic uptake transporter organic anion-transporting polypeptides (OATPs), and undergoes extensive hepatic metabolism by cytochrome P450 (P450), namely, CYP3A4 and CYP2C9. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 192-198 29475833-2 2018 Several clinical investigations have reported a nonlinear relationship between bosentan doses and its systemic exposure, which likely involves the saturation of OATP-mediated uptake, P450-mediated metabolism, or both in the liver. Bosentan 79-87 solute carrier organic anion transporter family member 1A2 Homo sapiens 161-165 29344607-0 2018 Bosentan for Cutaneous Ulcers in Anti-MDA5 Dermatomyositis. Bosentan 0-8 interferon induced with helicase C domain 1 Homo sapiens 38-42 28735030-3 2018 Bosentan, an oral endothelin-1 receptor antagonist, reduces pulmonary vascular resistance and hence may play a role in the treatment of PPHN. Bosentan 0-8 endothelin receptor type A Homo sapiens 18-39 28401480-1 2017 BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. Bosentan 27-35 endothelin receptor type B Homo sapiens 67-94 28401480-1 2017 BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. Bosentan 27-35 endothelin receptor type A Homo sapiens 96-99 28401480-1 2017 BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. Bosentan 27-35 endothelin receptor type B Homo sapiens 104-107 28401480-1 2017 BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. Bosentan 27-35 endothelin 1 Homo sapiens 152-164 28401480-1 2017 BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. Bosentan 27-35 endothelin 1 Homo sapiens 166-170 28401480-10 2017 ET-1 plasma and urine profiles were successfully integrated into the bosentan two-compartment, TMDD model encompassing competition for the same receptor. Bosentan 69-77 endothelin 1 Homo sapiens 0-4 29226623-4 2017 In rat small mesenteric arteries, bosentan displaced endothelin-1 CRC competitively indicative of ETA receptor antagonism. Bosentan 34-42 endothelin 1 Rattus norvegicus 53-65 29226623-4 2017 In rat small mesenteric arteries, bosentan displaced endothelin-1 CRC competitively indicative of ETA receptor antagonism. Bosentan 34-42 endothelin receptor type A Rattus norvegicus 98-101 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin 1 Rattus norvegicus 268-280 29226623-5 2017 In rat small pulmonary arteries, bosentan 10 mumol L-1 left-shifted the endothelin-1 CRC, demonstrating potentiation consistent with antagonism of an ETB receptor-mediated endothelin-1 clearance mechanism. Bosentan 33-41 endothelin 1 Rattus norvegicus 72-84 29226623-5 2017 In rat small pulmonary arteries, bosentan 10 mumol L-1 left-shifted the endothelin-1 CRC, demonstrating potentiation consistent with antagonism of an ETB receptor-mediated endothelin-1 clearance mechanism. Bosentan 33-41 endothelin receptor type B Rattus norvegicus 150-153 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin receptor type B Rattus norvegicus 296-299 29226623-5 2017 In rat small pulmonary arteries, bosentan 10 mumol L-1 left-shifted the endothelin-1 CRC, demonstrating potentiation consistent with antagonism of an ETB receptor-mediated endothelin-1 clearance mechanism. Bosentan 33-41 endothelin 1 Rattus norvegicus 172-184 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin 1 Rattus norvegicus 268-280 29226623-7 2017 In the presence of BQ788 and L-NAME, bosentan displayed ETA receptor antagonism. Bosentan 37-45 endothelin receptor type A Rattus norvegicus 56-59 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin receptor type A Rattus norvegicus 376-379 29226623-8 2017 In rat trachea (ETB ), bosentan was a competitive ETB antagonist against endothelin-1 or sarafotoxin S6c. Bosentan 23-31 endothelin receptor type B Rattus norvegicus 16-19 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin receptor type B Rattus norvegicus 296-299 29226623-8 2017 In rat trachea (ETB ), bosentan was a competitive ETB antagonist against endothelin-1 or sarafotoxin S6c. Bosentan 23-31 endothelin receptor type B Rattus norvegicus 50-53 29226623-8 2017 In rat trachea (ETB ), bosentan was a competitive ETB antagonist against endothelin-1 or sarafotoxin S6c. Bosentan 23-31 endothelin 1 Rattus norvegicus 73-85 29226623-10 2017 In conclusion, the rat pulmonary artery is an example of a special vascular bed where the resistance to antagonism of endothelin-1 constriction by ET dual antagonists, such as bosentan or the ETB antagonist BQ788, is possibly due to the competition of potentiation of endothelin-1 by blockade of ETB -mediated endothelin-1 clearance located on smooth muscle and antagonism of ETA - and ETB -mediated contraction. Bosentan 176-184 endothelin 1 Rattus norvegicus 118-130 28597546-8 2017 Pharmacological blockade with the dual EDN1 receptor antagonist bosentan decreased cell viability and MAPK activation of U266 and RPMI-8226 cells. Bosentan 64-72 endothelin 1 Homo sapiens 39-43 28819231-7 2017 Compared with metabolic biomarker-based hPSC assay by Stemina, the microP-hPST could successfully identify misclassified drugs Bosentan, Diphenylhydantoin and Lovastatin, and show a higher accuracy and sensitivity. Bosentan 127-135 sulfotransferase family 1A member 1 Homo sapiens 74-78 28500979-5 2017 The assay was successfully applied to assess the time course of plasma ET-1 concentrations in two human volunteers after co-administration of bosentan and clarithromycin. Bosentan 142-150 endothelin 1 Homo sapiens 71-75 28484975-9 2017 The plasma AUC of bosentan (with relatively large beta and small Rdif) was dominated by OATP-mediated uptake. Bosentan 18-26 solute carrier organic anion transporter family member 1A2 Homo sapiens 88-92 28871941-9 2017 Airway inflammation was attenuated and the staining intensity of ET-2 in the lung tissue was reduced in the dexamethasone treated group, bosentan treated group, and dexamethasone-bosentan treated group, which were more obvious in the dexamethasone-bosentan treated group. Bosentan 137-145 endothelin 2 Rattus norvegicus 65-69 28871941-9 2017 Airway inflammation was attenuated and the staining intensity of ET-2 in the lung tissue was reduced in the dexamethasone treated group, bosentan treated group, and dexamethasone-bosentan treated group, which were more obvious in the dexamethasone-bosentan treated group. Bosentan 179-187 endothelin 2 Rattus norvegicus 65-69 27145076-9 2017 BOS regulates significantly eNOS, iNOS and TNF-alpha expressions in a dose-dependent manner. Bosentan 0-3 nitric oxide synthase 2 Rattus norvegicus 34-38 28274813-11 2017 Treatment of bosentan attenuated Abeta+l-Methionine induced impairment of learning and memory, enhanced Abeta level, mitochondrial and endothelial dysfunction. Bosentan 13-21 amyloid beta precursor protein Rattus norvegicus 33-38 28274813-11 2017 Treatment of bosentan attenuated Abeta+l-Methionine induced impairment of learning and memory, enhanced Abeta level, mitochondrial and endothelial dysfunction. Bosentan 13-21 amyloid beta precursor protein Rattus norvegicus 104-109 28315689-6 2017 The compounds resulting in the smallest root-mean square deviation hit by pharmacophore search were the well-known PXR inducers such as Bosentan. Bosentan 136-144 nuclear receptor subfamily 1 group I member 2 Homo sapiens 115-118 28640077-1 2017 RATIONALE: Sildenafil, a phosphodiesterase-5-inhibitor and Bosentan, an endothelin-1-receptor antagonist combined therapy could have beneficial effect in systemic sclerosis (SSc) patients with peripheral artery disease. Bosentan 59-67 endothelin receptor type A Homo sapiens 72-93 28393009-0 2017 A case of anti-aminoacyl tRNA synthetase (ARS) antibody-positive polymyositis (PM)/dermatomyositis (DM)-associated interstitial pneumonia (IP) successfully controlled with bosentan therapy. Bosentan 172-180 secreted LY6/PLAUR domain containing 1 Homo sapiens 10-40 28393009-0 2017 A case of anti-aminoacyl tRNA synthetase (ARS) antibody-positive polymyositis (PM)/dermatomyositis (DM)-associated interstitial pneumonia (IP) successfully controlled with bosentan therapy. Bosentan 172-180 secreted LY6/PLAUR domain containing 1 Homo sapiens 42-45 28393009-6 2017 In addition, she was confirmed to be anti-ARS antibody-positive after 5 years of bosentan therapy, when anti-aminoacyl tRNA synthetase (anti-ARS) antibody testing became available. Bosentan 81-89 secreted LY6/PLAUR domain containing 1 Homo sapiens 42-45 28871941-9 2017 Airway inflammation was attenuated and the staining intensity of ET-2 in the lung tissue was reduced in the dexamethasone treated group, bosentan treated group, and dexamethasone-bosentan treated group, which were more obvious in the dexamethasone-bosentan treated group. Bosentan 179-187 endothelin 2 Rattus norvegicus 65-69 28300593-0 2017 Functional estimation of endothelin-1 receptor antagonism by bosentan, macitentan and ambrisentan in human pulmonary and radial arteries in vitro. Bosentan 61-69 endothelin receptor type A Homo sapiens 25-46 28173639-0 2017 Bosentan and Rifampin Interactions Modulate Influx Transporter and Cytochrome P450 Expression and Activities in Primary Human Hepatocytes. Bosentan 0-8 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 67-82 28173639-3 2017 In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. Bosentan 30-38 solute carrier organic anion transporter family member 1A2 Homo sapiens 88-122 28173639-3 2017 In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. Bosentan 30-38 solute carrier organic anion transporter family member 1A2 Homo sapiens 124-128 28173639-3 2017 In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. Bosentan 30-38 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 134-149 28173639-3 2017 In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. Bosentan 30-38 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 151-157 28173639-3 2017 In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. Bosentan 30-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 167-173 28173639-4 2017 HEK293 cells and primary human hepatocytes overexpressing the target genes were treated with bosentan and various concentrations of rifampin, which decreased the uptake activities of OATP transporters in a dose-dependent manner. Bosentan 93-101 solute carrier organic anion transporter family member 1A2 Homo sapiens 183-187 28173639-5 2017 In primary human hepatocytes, CYP2C9 and CYP3A4 gene expression and activities decreased upon treatment with 20 muM bosentan+200 muM rifampin. Bosentan 116-124 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 30-36 28173639-5 2017 In primary human hepatocytes, CYP2C9 and CYP3A4 gene expression and activities decreased upon treatment with 20 muM bosentan+200 muM rifampin. Bosentan 116-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 28173639-7 2017 These results confirm rifampin- and bosentan-induced interactions between OATP transporters and CYP450. Bosentan 36-44 solute carrier organic anion transporter family member 1A2 Homo sapiens 74-78 28173639-7 2017 These results confirm rifampin- and bosentan-induced interactions between OATP transporters and CYP450. Bosentan 36-44 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 96-102 27145076-9 2017 BOS regulates significantly eNOS, iNOS and TNF-alpha expressions in a dose-dependent manner. Bosentan 0-3 tumor necrosis factor Rattus norvegicus 43-52 28357073-0 2017 Effect of bosentan is correlated with MMP-9/TIMP-1 ratio in bleomycin-induced pulmonary fibrosis. Bosentan 10-18 matrix metallopeptidase 9 Rattus norvegicus 38-43 28357073-0 2017 Effect of bosentan is correlated with MMP-9/TIMP-1 ratio in bleomycin-induced pulmonary fibrosis. Bosentan 10-18 TIMP metallopeptidase inhibitor 1 Rattus norvegicus 44-50 28357073-10 2017 In addition, the concentrations of MMP-9 and TIMP-1 appeared to be altered following bosentan treatment, improving the bleomycin-induced PF. Bosentan 85-93 matrix metallopeptidase 9 Rattus norvegicus 35-40 28357073-10 2017 In addition, the concentrations of MMP-9 and TIMP-1 appeared to be altered following bosentan treatment, improving the bleomycin-induced PF. Bosentan 85-93 TIMP metallopeptidase inhibitor 1 Rattus norvegicus 45-51 28338297-7 2016 In our case, bosentan reduced both mean pulmonary artery pressure (mPAP) value and right heart chambers pressures. Bosentan 13-21 phospholipid phosphatase 1 Mus musculus 67-71 27906839-7 2017 Bosentan suppressed completely the increase in SBP during a 5-min hypoxic challenge (143 +- 5 mmHg during hypoxia vs. 133 +- 5 mmHg during normoxia with placebo and 127 +- 3 mmHg during hypoxia vs. 125 +- 3 mmHg during normoxia under bosentan, P = 0.023). Bosentan 0-8 selenium binding protein 1 Homo sapiens 47-50 27906839-7 2017 Bosentan suppressed completely the increase in SBP during a 5-min hypoxic challenge (143 +- 5 mmHg during hypoxia vs. 133 +- 5 mmHg during normoxia with placebo and 127 +- 3 mmHg during hypoxia vs. 125 +- 3 mmHg during normoxia under bosentan, P = 0.023). Bosentan 234-242 selenium binding protein 1 Homo sapiens 47-50 27905105-8 2017 In the presence of bosentan, a mixed ETA and ETB receptor antagonist ET-1-mediated pSmad2C levels were inhibited. Bosentan 19-27 endothelin receptor type A Bos taurus 37-40 27905105-8 2017 In the presence of bosentan, a mixed ETA and ETB receptor antagonist ET-1-mediated pSmad2C levels were inhibited. Bosentan 19-27 endothelin 1 Bos taurus 69-73 27716320-3 2016 In the present study, we evaluated the ability of endothelin-1 (ET-1) dual receptor antagonists bosentan (BOS) and macitentan (MAC) to antagonize EndoMT in vitro. Bosentan 96-104 endothelin 1 Homo sapiens 50-62 26883974-8 2016 HT22 cells synthesize high levels of ET-1 in normal conditions, which was reduced with palmitate and bosentan as well as low and high glucose conditions. Bosentan 101-109 endothelin 1 Mus musculus 37-41 27534881-4 2016 The goal of improved safety was based on the discovery of the role of ETB receptors in vascular permeability and vasopressin release and on the elucidation of the mechanism by which bosentan (the first approved oral dual ETA/ETB ERA) caused liver enzyme changes. Bosentan 182-190 endothelin receptor type A Homo sapiens 221-224 27534881-4 2016 The goal of improved safety was based on the discovery of the role of ETB receptors in vascular permeability and vasopressin release and on the elucidation of the mechanism by which bosentan (the first approved oral dual ETA/ETB ERA) caused liver enzyme changes. Bosentan 182-190 endothelin receptor type B Homo sapiens 225-228 26631506-1 2016 AIMS: We have shown that glycemic control with metformin or endothelin-1 (ET-1) inhibition with bosentan prevents and restores diabetes-mediated cerebral pathological remodeling and neovascularization. Bosentan 96-104 endothelin 1 Rattus norvegicus 60-72 27188586-0 2016 Bosentan reverses the hypoxia-induced downregulation of the bone morphogenetic protein signaling in pulmonary artery smooth muscle cells. Bosentan 0-8 bone morphogenetic protein 1 Homo sapiens 60-86 27188586-8 2016 Bosentan pretreatment restored expressions of BMPR-2 and ID1, as well as the activation (by phosphorylation) of Smad1/5/8 signaling induced by BMP2. Bosentan 0-8 bone morphogenetic protein receptor type 2 Homo sapiens 46-52 27188586-8 2016 Bosentan pretreatment restored expressions of BMPR-2 and ID1, as well as the activation (by phosphorylation) of Smad1/5/8 signaling induced by BMP2. Bosentan 0-8 inhibitor of DNA binding 1, HLH protein Homo sapiens 57-60 27188586-8 2016 Bosentan pretreatment restored expressions of BMPR-2 and ID1, as well as the activation (by phosphorylation) of Smad1/5/8 signaling induced by BMP2. Bosentan 0-8 SMAD family member 1 Homo sapiens 112-119 26631506-1 2016 AIMS: We have shown that glycemic control with metformin or endothelin-1 (ET-1) inhibition with bosentan prevents and restores diabetes-mediated cerebral pathological remodeling and neovascularization. Bosentan 96-104 endothelin 1 Rattus norvegicus 74-78 27313275-1 2016 Bosentan, an endothelin-1 (ET) receptor antagonist is an important drug for the effective management of patients with pulmonary arterial hypertension. Bosentan 0-8 endothelin receptor type A Homo sapiens 13-39 27188586-8 2016 Bosentan pretreatment restored expressions of BMPR-2 and ID1, as well as the activation (by phosphorylation) of Smad1/5/8 signaling induced by BMP2. Bosentan 0-8 bone morphogenetic protein 2 Homo sapiens 143-147 27444511-8 2016 Irbesartan and the mixed ET-1 receptor antagonist bosentan prevented these changes in a blood pressure-independent fashion (P < 0.001 for both versus controls). Bosentan 50-58 endothelin 1 Rattus norvegicus 25-29 27045668-1 2016 Bosentan, an endothelin-1 (ET) receptor antagonist is an important drug for the effective management of patients with pulmonary arterial hypertension. Bosentan 0-8 endothelin receptor type A Homo sapiens 13-39 27313275-3 2016 Bosentan is mainly metabolized by cytochrome P450 (CYP) 3A4 and 2C9 enzymes with the involvement of multiple transporters that control its hepatic uptake and biliary excretion. Bosentan 0-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-67 27045668-3 2016 Bosentan is mainly metabolized by cytochrome P450 (CYP) 3A4 and 2C9 enzymes with the involvement of multiple transporters that control its hepatic uptake and biliary excretion. Bosentan 0-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-67 27045668-5 2016 While bosentan exhibits high protein binding restricting the drug from extensive distribution and significant urinary excretion, bosentan induces its own metabolism by an increased expression of CYP3A4 on repeated dosing. Bosentan 129-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 195-201 27313275-5 2016 While bosentan exhibits high protein binding restricting the drug from extensive distribution and significant urinary excretion, bosentan induces its own metabolism by an increased expression of CYP3A4 on repeated dosing. Bosentan 129-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 195-201 26861196-6 2016 Treatment on day 21 after surgery with the ETAR selective antagonist BQ-123 (40 and 90 pmol, intrathecally) or the dual ETAR/ETBR antagonist bosentan (30 and 100mg/kg, orally) transiently reduced SCI-induced mechanical allodynia, but the ETBR antagonist BQ-788 was ineffective. Bosentan 141-149 endothelin receptor type B Homo sapiens 238-242 27169750-6 2016 The remaining compounds (1-naphthyl isothiocyanate, deoxycholic acid and bosentan) caused BC dilation without modulating ROCK activity, although they were associated with a steady decrease in MLC2 phosphorylation via MLCK. Bosentan 73-81 myosin light chain 2 Homo sapiens 192-196 27169750-6 2016 The remaining compounds (1-naphthyl isothiocyanate, deoxycholic acid and bosentan) caused BC dilation without modulating ROCK activity, although they were associated with a steady decrease in MLC2 phosphorylation via MLCK. Bosentan 73-81 myosin light chain kinase 3 Homo sapiens 217-221 26399195-10 2016 Importantly, bosentan significantly reversed circulating EPCR and PIC levels in patients with SSc, and the expression of Fli1 and EPCR in dermal small vessels was elevated in patients treated with bosentan compared with untreated patients. Bosentan 13-21 protein C receptor Homo sapiens 57-61 26663321-7 2016 Moreover, IH induced a 2-fold increase in ET-1 transcription and ETA-R expression in adipose tissue that was reversed by bosentan. Bosentan 121-129 endothelin 1 Rattus norvegicus 42-46 26663321-7 2016 Moreover, IH induced a 2-fold increase in ET-1 transcription and ETA-R expression in adipose tissue that was reversed by bosentan. Bosentan 121-129 endothelin receptor type A Rattus norvegicus 65-70 26663321-8 2016 In 3T3-L1 adipocytes, ET-1 upregulated its own and its ETA-R transcription and this effect was abolished by bosentan. Bosentan 108-116 endothelin 1 Rattus norvegicus 22-26 26663321-8 2016 In 3T3-L1 adipocytes, ET-1 upregulated its own and its ETA-R transcription and this effect was abolished by bosentan. Bosentan 108-116 endothelin receptor type A Rattus norvegicus 55-60 26663321-11 2016 Bosentan also reversed the ET-1-induced phosphorylation of hormone-sensitive lipase (HSL) on Ser(660) . Bosentan 0-8 endothelin 1 Rattus norvegicus 27-31 26399195-10 2016 Importantly, bosentan significantly reversed circulating EPCR and PIC levels in patients with SSc, and the expression of Fli1 and EPCR in dermal small vessels was elevated in patients treated with bosentan compared with untreated patients. Bosentan 197-205 Fli-1 proto-oncogene, ETS transcription factor Homo sapiens 121-125 26399195-10 2016 Importantly, bosentan significantly reversed circulating EPCR and PIC levels in patients with SSc, and the expression of Fli1 and EPCR in dermal small vessels was elevated in patients treated with bosentan compared with untreated patients. Bosentan 197-205 protein C receptor Homo sapiens 130-134 26055516-6 2015 Importantly, bosentan, a dual endothelin receptor antagonist with a potential disease-modifying effect on SSc vasculopathy, reverses the expression of Fli1 protein by increasing its protein stability. Bosentan 13-21 Fli-1 proto-oncogene, ETS transcription factor Homo sapiens 151-155 27189349-3 2016 OBJECTIVE: The present study has been structured to explore the effects of bosentan, an ET-1 antagonist on two-kidneyone- clip: 2K1C method induced hypertension provoked vascular dementia (VaD). Bosentan 75-83 endothelin 1 Homo sapiens 88-92 27189349-11 2016 Treatment with bosentan has also restored 2K1C induced a rise in brain TBARS, AChE, MPO activity, reduction in brain GSH, SOD and CAT as well as brain damage. Bosentan 15-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 27189349-11 2016 Treatment with bosentan has also restored 2K1C induced a rise in brain TBARS, AChE, MPO activity, reduction in brain GSH, SOD and CAT as well as brain damage. Bosentan 15-23 myeloperoxidase Homo sapiens 84-87 27189349-11 2016 Treatment with bosentan has also restored 2K1C induced a rise in brain TBARS, AChE, MPO activity, reduction in brain GSH, SOD and CAT as well as brain damage. Bosentan 15-23 superoxide dismutase 1 Homo sapiens 122-125 27189349-11 2016 Treatment with bosentan has also restored 2K1C induced a rise in brain TBARS, AChE, MPO activity, reduction in brain GSH, SOD and CAT as well as brain damage. Bosentan 15-23 catalase Homo sapiens 130-133 26502773-9 2016 These results suggest that Ro 64-1056 is directly involved in bosentan-induced liver injury partly because CYP2C9 specifically mediates hydroxylation of the t-butyl group of Ro 47-8634. Bosentan 62-70 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 107-113 27415782-6 2016 Bosentan treatment elevated plasma renin activity, renal renin, and AT1R expression in UUO mice. Bosentan 0-8 angiotensin II, type I receptor-associated protein Mus musculus 68-72 27415782-10 2016 Co-treatment with valsartan and bosentan reduced TGF-beta, alpha-SMA, and collagen IV expression, and the Masson"s trichrome stained area in their kidneys. Bosentan 32-40 actin alpha 2, smooth muscle, aorta Mus musculus 59-68 27129065-8 2016 Phosphodiesterase inhibitors (e.g., sildenafil) can also improve RP symptoms and ulcer healing whereas endothelin-1 receptor antagonists (e.g., bosentan) are mainly considered treatment options in secondary prevention for patients with digital skin ulcers related to systemic sclerosis. Bosentan 144-152 endothelin receptor type A Homo sapiens 103-124 26526351-4 2015 This is blocked by endothelin receptor antagonists (ERAs), like bosentan, which targets both receptors, ETAR-selective ambrisentan and ETBR-specific BQ788. Bosentan 64-72 endothelin receptor type A Homo sapiens 104-108 26526351-4 2015 This is blocked by endothelin receptor antagonists (ERAs), like bosentan, which targets both receptors, ETAR-selective ambrisentan and ETBR-specific BQ788. Bosentan 64-72 endothelin receptor type B Homo sapiens 135-139 26246053-6 2015 Bosentan (100 mg/kg) inhibited superoxide anion-induced mechanical and thermal hyperalgesia, overt pain-like behavior (abdominal writhings, paw flinching, and licking), paw edema, myeloperoxidase activity (neutrophil marker) in the paw skin, and leukocyte recruitment in the peritoneal cavity. Bosentan 0-8 myeloperoxidase Mus musculus 180-195 26246053-7 2015 Bosentan also inhibited superoxide anion-induced interleukin-1 beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) production, while it enhanced IL-10 production in the paw skin and spinal cord. Bosentan 0-8 interleukin 1 beta Mus musculus 49-67 26246053-7 2015 Bosentan also inhibited superoxide anion-induced interleukin-1 beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) production, while it enhanced IL-10 production in the paw skin and spinal cord. Bosentan 0-8 interleukin 1 beta Mus musculus 69-77 26246053-7 2015 Bosentan also inhibited superoxide anion-induced interleukin-1 beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) production, while it enhanced IL-10 production in the paw skin and spinal cord. Bosentan 0-8 tumor necrosis factor Mus musculus 83-110 26246053-7 2015 Bosentan also inhibited superoxide anion-induced interleukin-1 beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) production, while it enhanced IL-10 production in the paw skin and spinal cord. Bosentan 0-8 tumor necrosis factor Mus musculus 112-121 26246053-7 2015 Bosentan also inhibited superoxide anion-induced interleukin-1 beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) production, while it enhanced IL-10 production in the paw skin and spinal cord. Bosentan 0-8 interleukin 10 Mus musculus 153-158 25298328-8 2015 Bosentan treatment also decreased tissue endothelin 1 expression relative to that in the fracture control group. Bosentan 0-8 endothelin 1 Rattus norvegicus 41-53 25847324-2 2015 We tested the hypothesis that dual ET-1 receptor antagonism via bosentan can reverse diabetes-induced lung injury. Bosentan 64-72 endothelin 1 Rattus norvegicus 35-39 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 0-8 endothelin 1 Rattus norvegicus 90-94 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 0-8 endothelin receptor type A Rattus norvegicus 96-100 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 0-8 endothelin receptor type B Rattus norvegicus 106-110 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 22-30 endothelin 1 Rattus norvegicus 90-94 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 22-30 endothelin receptor type A Rattus norvegicus 96-100 25847324-7 2015 Bosentan 50 mg/kg and bosentan 100 mg/kg showed a significantly down-regulatory effect on ET-1, ET-A, and ET-B mRNA expression. Bosentan 22-30 endothelin receptor type B Rattus norvegicus 106-110 25707716-7 2015 RESULTS: In human dermal microvascular endothelial cells, endothelin 1 induced phosphorylation of Fli-1 at Thr(312) through the sequential activation of c-Abl and protein kinase Cdelta, leading to a decrease in Fli-1 protein levels as well as a decrease in binding of Fli-1 to the target gene promoters, whereas bosentan treatment reversed those effects. Bosentan 312-320 endothelin 1 Homo sapiens 58-70 26015909-0 2015 Role of endothelin-1 antagonist; bosentan, against cisplatin-induced nephrotoxicity in male and female rats. Bosentan 33-41 endothelin 1 Rattus norvegicus 8-20 26015909-3 2015 Bosentan (BOS) is a nonselective ET-1 receptor antagonist, having vasodilatory and anti-hypertension effects. Bosentan 0-8 endothelin 1 Rattus norvegicus 33-37 26015909-3 2015 Bosentan (BOS) is a nonselective ET-1 receptor antagonist, having vasodilatory and anti-hypertension effects. Bosentan 10-13 endothelin 1 Rattus norvegicus 33-37 26015909-11 2015 CONCLUSION: Renoprotective effect of BOS, as ET-1 blocker, was not observed against CP-induced nephrotoxicity neither in male nor in female rats. Bosentan 37-40 endothelin 1 Rattus norvegicus 45-49 24918345-1 2015 BACKGROUND: This study was designed to investigate the protective effects of bosentan an orally active non-peptide mixed ETA/ETB receptor antagonist, on liver injury in streptozotocin-induced diabetic rats. Bosentan 77-85 endothelin receptor type A Rattus norvegicus 121-124 24918345-1 2015 BACKGROUND: This study was designed to investigate the protective effects of bosentan an orally active non-peptide mixed ETA/ETB receptor antagonist, on liver injury in streptozotocin-induced diabetic rats. Bosentan 77-85 endothelin receptor type B Rattus norvegicus 125-128 24918345-7 2015 Bosentan treatment showed a significant up-regulatory effect on ET-1, TNF-alpha and TGF-beta mRNA expression. Bosentan 0-8 endothelin 1 Rattus norvegicus 64-68 24918345-7 2015 Bosentan treatment showed a significant up-regulatory effect on ET-1, TNF-alpha and TGF-beta mRNA expression. Bosentan 0-8 tumor necrosis factor Rattus norvegicus 70-79 24918345-7 2015 Bosentan treatment showed a significant up-regulatory effect on ET-1, TNF-alpha and TGF-beta mRNA expression. Bosentan 0-8 transforming growth factor, beta 1 Rattus norvegicus 84-92 26111581-2 2015 Remarkably, among the ten PPP-enlisted drugs are three endothelin-1 (ET-1) receptor antagonists (ERA"s: ambrisentan, bosentan and macitentan), which are approved for the treatment of Pulmonary Arterial Hypertension (PAH). Bosentan 117-125 endothelin 1 Homo sapiens 55-67 25855530-6 2015 In concentration-response experiments, bosentan led to a significantly greater reduction of GM-CSF and MMP12 protein release than ambrisentan, whereas there was no significant difference in their effect on GM-CSF and MMP12 mRNA. Bosentan 39-47 colony stimulating factor 2 Homo sapiens 92-98 25855530-6 2015 In concentration-response experiments, bosentan led to a significantly greater reduction of GM-CSF and MMP12 protein release than ambrisentan, whereas there was no significant difference in their effect on GM-CSF and MMP12 mRNA. Bosentan 39-47 matrix metallopeptidase 12 Homo sapiens 103-108 25855530-9 2015 In the presence of the transcription inhibitor actinomycin D, bosentan, but not ambrisentan, reduced GM-CSF but not MMP12 or CXCL3 mRNA. Bosentan 62-70 colony stimulating factor 2 Homo sapiens 101-107 25707716-7 2015 RESULTS: In human dermal microvascular endothelial cells, endothelin 1 induced phosphorylation of Fli-1 at Thr(312) through the sequential activation of c-Abl and protein kinase Cdelta, leading to a decrease in Fli-1 protein levels as well as a decrease in binding of Fli-1 to the target gene promoters, whereas bosentan treatment reversed those effects. Bosentan 312-320 Fli-1 proto-oncogene, ETS transcription factor Homo sapiens 98-103 25707716-8 2015 In Fli-1 ECKO mice, 4 weeks of treatment with bosentan increased endothelial Fli-1 expression, resulting in vascular stabilization and the restoration of impaired leaky vessels. Bosentan 46-54 Friend leukemia integration 1 Mus musculus 3-8 25844688-8 2015 Bosentan but not imatinib ameliorated superoxide dismutase and catalase activities, which were lowered following bleomycin instillation. Bosentan 0-8 catalase Mus musculus 63-71 25707716-8 2015 In Fli-1 ECKO mice, 4 weeks of treatment with bosentan increased endothelial Fli-1 expression, resulting in vascular stabilization and the restoration of impaired leaky vessels. Bosentan 46-54 Friend leukemia integration 1 Mus musculus 77-82 25707716-9 2015 CONCLUSION: The vascular fragility of Fli-1 ECKO mice was improved by bosentan through the normalization of Fli-1 protein levels and activity in endothelial cells, which may explain, in part, the mechanism underlying the beneficial effects of endothelin receptor blockade on SSc vasculopathy. Bosentan 70-78 Friend leukemia integration 1 Mus musculus 38-43 25707716-9 2015 CONCLUSION: The vascular fragility of Fli-1 ECKO mice was improved by bosentan through the normalization of Fli-1 protein levels and activity in endothelial cells, which may explain, in part, the mechanism underlying the beneficial effects of endothelin receptor blockade on SSc vasculopathy. Bosentan 70-78 Friend leukemia integration 1 Mus musculus 108-113 25467130-9 2015 Bosentan exhibited a positive exposure-adjusted signal in one assay (BSEP inhibition) and a moderate CVB body burden. Bosentan 0-8 ATP binding cassette subfamily B member 11 Homo sapiens 69-73 25966344-9 2015 Nonpeptide antagonists, bosentan, macitentan, and ambrisentan, that are either mixed ET(A)/ET(B) antagonists or display ET(A) selectivity, have been approved for clinical use but to date are limited to pulmonary hypertension. Bosentan 24-32 endothelin receptor type B Homo sapiens 91-96 25660617-2 2015 In a murine doxorubicin cardiotoxicity model, increased endothelin-1 (ET-1) expression and cardioprotective effects of the dual ET-1 blocker bosentan were demonstrated. Bosentan 141-149 endothelin 1 Mus musculus 128-132 25200216-4 2015 The aim of this study was to examine the roles of the endothelin (ET)-1 in brain damage formed in a streptozocin (STZ)-induced diabetes model, and the effect of bosentan, which is the non-specific ET1 receptor blocker in the prevention of the diabetes-induced brain damage. Bosentan 161-169 endothelin 1 Rattus norvegicus 197-200 25593238-9 2015 Macitentan or ACT-132577 antagonized the ability of ET-1 to further induce alpha-SMA expression (p = 0.03), COL-1, and FN synthesis (p = 0.03, p = 0.005); bosentan showed similar effects. Bosentan 155-163 endothelin 1 Homo sapiens 52-56 25787798-6 2015 His BNP level subsequently increased, so the bosentan dose was increased to 125 mg. Bosentan 45-53 natriuretic peptide B Homo sapiens 4-7 25535031-1 2015 The endothelin-1 receptor antagonists bosentan and ambrisentan used for the treatment of pulmonary arterial hypertension remarkably differ in their potential to act as perpetrators in pharmacokinetic drug-drug interactions. Bosentan 38-46 endothelin receptor type A Homo sapiens 4-25 25535031-4 2015 The hydroxylated metabolites of ambrisentan and bosentan neither induced any of the genes investigated at the mRNA level, nor inhibited P-glycoprotein (P-gp) measured by calcein assay in L-MDR1 cells, and only weakly inhibited organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 measured by 8-fluorescein-cAMP uptake in HEK-OATP1B1 and HEK-OATP1B3 cells. Bosentan 48-56 phosphoglycolate phosphatase Mus musculus 136-150 25535031-4 2015 The hydroxylated metabolites of ambrisentan and bosentan neither induced any of the genes investigated at the mRNA level, nor inhibited P-glycoprotein (P-gp) measured by calcein assay in L-MDR1 cells, and only weakly inhibited organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 measured by 8-fluorescein-cAMP uptake in HEK-OATP1B1 and HEK-OATP1B3 cells. Bosentan 48-56 phosphoglycolate phosphatase Mus musculus 152-156 25424997-4 2015 We also found that readily detectable cholestatic liver injury develops in TK-NOG mice with humanized livers after 1 week of treatment with bosentan (160, 32, or 6 mg/kg per day by mouth), whereas liver toxicity did not develop in control mice after 1 month of treatment. Bosentan 140-148 noggin Mus musculus 78-81 25179655-0 2015 Bosentan protects the spinal cord from ischemia reperfusion injury in rats through vascular endothelial growth factor receptors. Bosentan 0-8 vascular endothelial growth factor A Rattus norvegicus 83-117 26090478-3 2015 Endothelin receptors antagonists such as bosentan have beneficial effects on vasoconstriction and fibrosis, but less is known about their potential anti-inflammatory effects. Bosentan 41-49 endothelin 1 Homo sapiens 0-10 25332267-2 2014 Bosentan is metabolized by the cytochrome CYP2C9 and inhibits the bile salt export pump, which is encoded by ABCB11. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 42-48 25426072-3 2014 In this paper, we use DILIsym to simulate the DILI response of the hepatotoxic BSEP inhibitors bosentan and CP-724,714 and the non-hepatotoxic BSEP inhibitor telmisartan in humans in order to explore whether we can predict that hepatotoxic BSEP inhibitors can cause bile acid accumulation to reach toxic levels. Bosentan 96-104 ATP binding cassette subfamily B member 11 Homo sapiens 80-84 24632478-7 2014 The patient fully recovered after intensive treatment and administration of the endothelin receptor antagonist bosentan. Bosentan 111-119 endothelin 1 Homo sapiens 80-90 24690389-11 2014 SIGNIFICANCE: Long-term advanced therapy with bosentan significantly improves symptoms, pulmonary vascular resistance, plasma BNP concentration, and time to clinical worsening in Japanese patients with inoperable CTEPH. Bosentan 46-54 natriuretic peptide B Homo sapiens 126-129 25332267-2 2014 Bosentan is metabolized by the cytochrome CYP2C9 and inhibits the bile salt export pump, which is encoded by ABCB11. Bosentan 0-8 ATP binding cassette subfamily B member 11 Homo sapiens 109-115 25332267-3 2014 This suggests that genetic variants of CYP2C9 and/or ABCB11 may predispose patients to bosentan-induced liver injury. Bosentan 87-95 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 39-45 25332267-3 2014 This suggests that genetic variants of CYP2C9 and/or ABCB11 may predispose patients to bosentan-induced liver injury. Bosentan 87-95 ATP binding cassette subfamily B member 11 Homo sapiens 53-59 25332267-4 2014 MATERIAL AND METHODS: PH patients with (n = 23) or without (n = 25) an increase of alanine aminotransferase (ALT) or aspartate-aminotransferase (AST) during bosentan therapy were included in our analysis. Bosentan 157-165 solute carrier family 17 member 5 Homo sapiens 145-148 25332267-9 2014 CONCLUSION: Our data indicate hepatotoxicity of bosentan from decreased hepatic metabolism due to common variants of CYP2C9. Bosentan 48-56 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 117-123 25048859-9 2014 ET-1/ETR signalling inhibitor, bosentan, inhibited Gd-induced proliferation and calcification of hMSC. Bosentan 31-39 endothelin 1 Homo sapiens 0-4 25142737-0 2014 Effects of cytochrome P450 2C9 polymorphism on bosentan metabolism. Bosentan 47-55 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 11-30 25142737-3 2014 The aim of this study was to assess the catalytic activities of 38 human CYP2C9 alleles, including 24 novel alleles (*36-*60) found in the Han Chinese population, toward bosentan (BOS) in vitro. Bosentan 170-178 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 73-79 25142737-3 2014 The aim of this study was to assess the catalytic activities of 38 human CYP2C9 alleles, including 24 novel alleles (*36-*60) found in the Han Chinese population, toward bosentan (BOS) in vitro. Bosentan 180-183 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 73-79 25142737-8 2014 These findings suggest that more attention should be directed to subjects carrying these infrequent CYP2C9 alleles when administering BOS in the clinic. Bosentan 134-137 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 100-106 25048859-10 2014 In addition, bosentan inhibited Gd-induced phosphorylation of ERK and Akt in hMSC. Bosentan 13-21 mitogen-activated protein kinase 1 Homo sapiens 62-65 25048859-10 2014 In addition, bosentan inhibited Gd-induced phosphorylation of ERK and Akt in hMSC. Bosentan 13-21 AKT serine/threonine kinase 1 Homo sapiens 70-73 24836182-0 2014 Efficacy of bosentan, a dual ETA and ETB endothelin receptor antagonist, in experimental diabetes induced vascular endothelial dysfunction and associated dementia in rats. Bosentan 12-20 endothelin receptor type A Rattus norvegicus 29-60 24836182-1 2014 The study was designed to investigate the efficacy of bosentan a dual endothelin (ETA and ETB) receptor antagonist in experimental diabetes induced vascular endothelial dysfunction and associated dementia. Bosentan 54-62 endothelin receptor type A Rattus norvegicus 82-85 24836182-1 2014 The study was designed to investigate the efficacy of bosentan a dual endothelin (ETA and ETB) receptor antagonist in experimental diabetes induced vascular endothelial dysfunction and associated dementia. Bosentan 54-62 endothelin receptor type B Rattus norvegicus 90-93 24604341-2 2014 The present study aimed to compare the Endothelin1 (ET1) inhibitor bosentan which is regarded as standard therapy with different dose regimens of palosuran which is urotensin-II (UII) inhibitor and explore the discrepancy for mean pulmonary arterial pressure (mPAP), UII, ET1 levels, and pulmonary vascular pathology. Bosentan 67-75 endothelin 1 Rattus norvegicus 39-50 24604341-2 2014 The present study aimed to compare the Endothelin1 (ET1) inhibitor bosentan which is regarded as standard therapy with different dose regimens of palosuran which is urotensin-II (UII) inhibitor and explore the discrepancy for mean pulmonary arterial pressure (mPAP), UII, ET1 levels, and pulmonary vascular pathology. Bosentan 67-75 endothelin 1 Rattus norvegicus 52-55 24604341-10 2014 UII inhibitor is at least as effective as standard therapy bosentan. Bosentan 59-67 urotensin 2 Rattus norvegicus 0-3 24769543-2 2014 Mechanistically, bosentan inhibits the bile salt export pump (BSEP) leading to an intrahepatic accumulation of cytotoxic bile salts, which eventually results in hepatocellular damage. Bosentan 17-25 ATP binding cassette subfamily B member 11 Homo sapiens 39-60 25015229-6 2014 Both patients had initially received bosentan monotherapy, which caused liver toxicity as indicated by increased levels of alanine aminotransferase, alkaline phosphatase, and gamma-glutamyltransferase. Bosentan 37-45 glutamic--pyruvic transaminase Homo sapiens 123-147 24937643-2 2014 OBJECTIVES: To evaluate the safety and clinical efficacy of the dual endothelin-1 receptor antagonist bosentan in this patient group. Bosentan 102-110 endothelin receptor type A Homo sapiens 69-90 24851934-3 2014 Prior to October 2013, ambrisentan, a selective ETA receptor antagonist and bosentan, a dual ETA/ETB antagonist, were the only currently available agents for PAH targeting the endothelin pathway. Bosentan 76-84 endothelin receptor type A Homo sapiens 93-96 24851934-3 2014 Prior to October 2013, ambrisentan, a selective ETA receptor antagonist and bosentan, a dual ETA/ETB antagonist, were the only currently available agents for PAH targeting the endothelin pathway. Bosentan 76-84 endothelin receptor type B Homo sapiens 97-100 24769543-2 2014 Mechanistically, bosentan inhibits the bile salt export pump (BSEP) leading to an intrahepatic accumulation of cytotoxic bile salts, which eventually results in hepatocellular damage. Bosentan 17-25 ATP binding cassette subfamily B member 11 Homo sapiens 62-66 24769543-3 2014 BSEP inhibition by bosentan is amplified by its accumulation in the liver as bosentan is a substrate of organic anion-transporting polypeptide (OATP) transport proteins. Bosentan 19-27 ATP binding cassette subfamily B member 11 Homo sapiens 0-4 24769543-3 2014 BSEP inhibition by bosentan is amplified by its accumulation in the liver as bosentan is a substrate of organic anion-transporting polypeptide (OATP) transport proteins. Bosentan 19-27 solute carrier organic anion transporter family member 1A2 Homo sapiens 144-148 24769543-3 2014 BSEP inhibition by bosentan is amplified by its accumulation in the liver as bosentan is a substrate of organic anion-transporting polypeptide (OATP) transport proteins. Bosentan 77-85 ATP binding cassette subfamily B member 11 Homo sapiens 0-4 24769543-3 2014 BSEP inhibition by bosentan is amplified by its accumulation in the liver as bosentan is a substrate of organic anion-transporting polypeptide (OATP) transport proteins. Bosentan 77-85 solute carrier organic anion transporter family member 1A2 Homo sapiens 144-148 24177203-9 2014 For those treated with bosentan, repeat hemodynamic studies at 16 weeks demonstrated a significant mean+-SD fall in PA mean pressure (-4+-6.6 mm Hg, P=.0105) and PVR (-1.7+-2.75 Wood units, P=.0104). Bosentan 23-31 PVR cell adhesion molecule Homo sapiens 162-165 24833743-9 2014 Bosentan treatment at doses of 50 and 100 mg/kg significantly decreased iNOS expression compared to LPS-injected animals (P < 0.001). Bosentan 0-8 nitric oxide synthase 2 Rattus norvegicus 72-76 24833743-10 2014 The ET-1 expression was suppressed significantly by bosentan and dexamethasone at 3 and 24 hours after LPS administration (P < 0.001). Bosentan 52-60 endothelin 1 Rattus norvegicus 4-8 24833743-11 2014 The EDNRA expression in the bosentan treatment groups was statistically significantly lower than that in the LPS-induced uveitis control group at 3 and 24 hours after LPS administration (P < 0.05). Bosentan 28-36 endothelin receptor type A Rattus norvegicus 4-9 24708674-0 2014 Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Bosentan 0-8 Friend leukemia integration 1 Mus musculus 145-149 24708674-9 2014 On the other hand, bosentan reduced the expression of c-Abl and PKC-delta, the nuclear localization of PKC-delta, and Fli1 phosphorylation, resulting in the increased DNA binding of Fli1 and the suppression of type I collagen expression in SSc fibroblasts. Bosentan 19-27 c-abl oncogene 1, non-receptor tyrosine kinase Mus musculus 54-59 24708674-9 2014 On the other hand, bosentan reduced the expression of c-Abl and PKC-delta, the nuclear localization of PKC-delta, and Fli1 phosphorylation, resulting in the increased DNA binding of Fli1 and the suppression of type I collagen expression in SSc fibroblasts. Bosentan 19-27 protein kinase C, delta Mus musculus 64-73 24708674-9 2014 On the other hand, bosentan reduced the expression of c-Abl and PKC-delta, the nuclear localization of PKC-delta, and Fli1 phosphorylation, resulting in the increased DNA binding of Fli1 and the suppression of type I collagen expression in SSc fibroblasts. Bosentan 19-27 protein kinase C, delta Mus musculus 103-112 24708674-9 2014 On the other hand, bosentan reduced the expression of c-Abl and PKC-delta, the nuclear localization of PKC-delta, and Fli1 phosphorylation, resulting in the increased DNA binding of Fli1 and the suppression of type I collagen expression in SSc fibroblasts. Bosentan 19-27 Friend leukemia integration 1 Mus musculus 118-122 24708674-9 2014 On the other hand, bosentan reduced the expression of c-Abl and PKC-delta, the nuclear localization of PKC-delta, and Fli1 phosphorylation, resulting in the increased DNA binding of Fli1 and the suppression of type I collagen expression in SSc fibroblasts. Bosentan 19-27 Friend leukemia integration 1 Mus musculus 182-186 24708674-10 2014 In bleomycin-treated mice, bosentan prevented dermal fibrosis and increased Fli1 expression in lesional dermal fibroblasts. Bosentan 27-35 Friend leukemia integration 1 Mus musculus 76-80 24842639-0 2014 CYP2C9, SLCO1B1, SLCO1B3, and ABCB11 polymorphisms in patients with bosentan-induced liver toxicity. Bosentan 68-76 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 0-6 24842639-0 2014 CYP2C9, SLCO1B1, SLCO1B3, and ABCB11 polymorphisms in patients with bosentan-induced liver toxicity. Bosentan 68-76 solute carrier organic anion transporter family member 1B3 Homo sapiens 17-24 24842639-0 2014 CYP2C9, SLCO1B1, SLCO1B3, and ABCB11 polymorphisms in patients with bosentan-induced liver toxicity. Bosentan 68-76 ATP binding cassette subfamily B member 11 Homo sapiens 30-36 24842639-4 2014 We conducted a nested case-control study to further explore the relationship between functional polymorphisms of gene products involved in bosentan pharmacokinetics (OATP1B1, OATP1B3, and CYP2C9) or hepatobiliary transporters affected by bosentan (ABCB11) and bosentan-induced liver toxicity. Bosentan 139-147 solute carrier organic anion transporter family member 1B1 Homo sapiens 166-173 24842639-4 2014 We conducted a nested case-control study to further explore the relationship between functional polymorphisms of gene products involved in bosentan pharmacokinetics (OATP1B1, OATP1B3, and CYP2C9) or hepatobiliary transporters affected by bosentan (ABCB11) and bosentan-induced liver toxicity. Bosentan 139-147 solute carrier organic anion transporter family member 1B3 Homo sapiens 175-182 24842639-4 2014 We conducted a nested case-control study to further explore the relationship between functional polymorphisms of gene products involved in bosentan pharmacokinetics (OATP1B1, OATP1B3, and CYP2C9) or hepatobiliary transporters affected by bosentan (ABCB11) and bosentan-induced liver toxicity. Bosentan 139-147 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 188-194 24842639-4 2014 We conducted a nested case-control study to further explore the relationship between functional polymorphisms of gene products involved in bosentan pharmacokinetics (OATP1B1, OATP1B3, and CYP2C9) or hepatobiliary transporters affected by bosentan (ABCB11) and bosentan-induced liver toxicity. Bosentan 139-147 ATP binding cassette subfamily B member 11 Homo sapiens 248-254 24276417-11 2014 The protein expressions of Bcl-2, Bax, Caspase-8, Caspase-9 and Caspase-3 were significantly increased in response to Bosentan treatment after IR. Bosentan 118-126 BCL2 associated X, apoptosis regulator Rattus norvegicus 34-37 24276417-11 2014 The protein expressions of Bcl-2, Bax, Caspase-8, Caspase-9 and Caspase-3 were significantly increased in response to Bosentan treatment after IR. Bosentan 118-126 caspase 8 Rattus norvegicus 39-48 24276417-11 2014 The protein expressions of Bcl-2, Bax, Caspase-8, Caspase-9 and Caspase-3 were significantly increased in response to Bosentan treatment after IR. Bosentan 118-126 BCL2, apoptosis regulator Rattus norvegicus 27-32 24276417-11 2014 The protein expressions of Bcl-2, Bax, Caspase-8, Caspase-9 and Caspase-3 were significantly increased in response to Bosentan treatment after IR. Bosentan 118-126 caspase 9 Rattus norvegicus 50-59 24276417-11 2014 The protein expressions of Bcl-2, Bax, Caspase-8, Caspase-9 and Caspase-3 were significantly increased in response to Bosentan treatment after IR. Bosentan 118-126 caspase 3 Rattus norvegicus 64-73 24276417-12 2014 CONCLUSION: These results suggest Bosentan decreases apoptosis rate after IR injury in the spinal cord, possibly through the ET-1-ETRB signaling pathway. Bosentan 34-42 endothelin 1 Rattus norvegicus 125-129 24276417-12 2014 CONCLUSION: These results suggest Bosentan decreases apoptosis rate after IR injury in the spinal cord, possibly through the ET-1-ETRB signaling pathway. Bosentan 34-42 endothelin receptor type B Rattus norvegicus 130-134 24361136-6 2014 The results show that bosentan treatment induced a bell shaped dose-dependent antidepressant-like effect with increase in circulating IL-6 levels in animals exposed to FST. Bosentan 22-30 interleukin 6 Mus musculus 134-138 24337925-11 2014 ET-1 decreased PPARgamma protein and activity, which was prevented by bosentan. Bosentan 70-78 EDN1 Ovis aries 0-4 24337925-11 2014 ET-1 decreased PPARgamma protein and activity, which was prevented by bosentan. Bosentan 70-78 peroxisome proliferator-activated receptor gamma Ovis aries 15-24 24361136-5 2014 Moreover, the influence of bosentan treatment on circulating IL-6 levels was also addressed after FST. Bosentan 27-35 interleukin 6 Mus musculus 61-65 24361136-10 2014 Therefore, this is the first study to demonstrate the antidepressant-like activity of bosentan in mice, unveiling a previous unrecognized role of endothelin in depression and its possible relation with increased circulating IL-6 levels. Bosentan 86-94 interleukin 6 Mus musculus 224-228 24583865-0 2014 Endothelin-1 receptors in rat tissues: characterization by bosentan, ambrisentan and CI-1020. Bosentan 59-67 endothelin 1 Rattus norvegicus 0-12 24193244-10 2014 Bosentan (1E-7 M) significantly attenuated combined ET-1/NE dose-response curves in PA (93.1 +- 47.4 vs. 125.3 +- 41.0%; n = 12; p < 0.001) whereas the effect of sildenafil (1E-5 M) was less pronounced (103.6 +- 20.2%; p < 0.05). Bosentan 0-8 endothelin 1 Homo sapiens 52-59 24071933-0 2014 Improvement of plasma endothelin-1 and nitric oxide in patients with systemic sclerosis by bosentan therapy. Bosentan 91-99 endothelin 1 Homo sapiens 22-34 24071933-1 2014 The aim of this study was to evaluate the effects of bosentan on plasma endothelin-1 (ET-1) and nitric oxide (NO) as pulmonary hypertension (PH)-associated biochemical markers in patients with systemic sclerosis (SSc). Bosentan 53-61 endothelin 1 Homo sapiens 72-84 24071933-1 2014 The aim of this study was to evaluate the effects of bosentan on plasma endothelin-1 (ET-1) and nitric oxide (NO) as pulmonary hypertension (PH)-associated biochemical markers in patients with systemic sclerosis (SSc). Bosentan 53-61 endothelin 1 Homo sapiens 86-90 24071933-6 2014 Plasma ET-1 levels were significantly decreased after 24 weeks of bosentan therapy (p < 0.0001), and ET-1 levels of SSc patients with PH decreased to a level comparable to that in patients without PH. Bosentan 66-74 endothelin 1 Homo sapiens 7-11 24071933-10 2014 Additionally, changes in plasma ET-1 levels may indicate the response to bosentan therapy in SSc patients with PH. Bosentan 73-81 endothelin 1 Homo sapiens 32-36 24498134-8 2014 Macitentan and bosentan also inhibited NTCP with IC50 values of 10 and 36 microM, respectively. Bosentan 15-23 solute carrier family 10 member 1 Homo sapiens 39-43 24498134-9 2014 Similar to previously reported findings with sitaxsentan, BSEP inhibition was observed for bosentan and macitentan with IC50 values of 42 and 12 microM, respectively. Bosentan 91-99 ATP binding cassette subfamily B member 11 Homo sapiens 58-62 24583865-3 2014 ET-1, bosentan, ambrisentan, and CI-1020 inhibited specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. Bosentan 6-14 endothelin 1 Rattus norvegicus 68-72 24583865-6 2014 Oral administration of bosentan caused a dose-dependent decrease in specific [(125)I]ET-1 binding in the rat lung, kidney and bladder, suggesting significant binding of the tissue ET-1 receptors in vivo. Bosentan 23-31 endothelin 1 Rattus norvegicus 85-89 24583865-6 2014 Oral administration of bosentan caused a dose-dependent decrease in specific [(125)I]ET-1 binding in the rat lung, kidney and bladder, suggesting significant binding of the tissue ET-1 receptors in vivo. Bosentan 23-31 endothelin 1 Rattus norvegicus 180-184 24583865-7 2014 In conclusion, it has been shown that a significant amount of pharmacologically relevant ET-1 receptors may exist in rat tissues and that ET-1 receptor antagonists such as bosentan at pharmacological doses may exert some pharmacological effects by binding these ET-1 receptors. Bosentan 172-180 endothelin 1 Rattus norvegicus 89-93 24583865-7 2014 In conclusion, it has been shown that a significant amount of pharmacologically relevant ET-1 receptors may exist in rat tissues and that ET-1 receptor antagonists such as bosentan at pharmacological doses may exert some pharmacological effects by binding these ET-1 receptors. Bosentan 172-180 endothelin 1 Rattus norvegicus 138-142 24583865-7 2014 In conclusion, it has been shown that a significant amount of pharmacologically relevant ET-1 receptors may exist in rat tissues and that ET-1 receptor antagonists such as bosentan at pharmacological doses may exert some pharmacological effects by binding these ET-1 receptors. Bosentan 172-180 endothelin 1 Rattus norvegicus 138-142 23738582-1 2014 AIMS: The aim of this study was to assess the effect of the cytochrome P450 (CYP) 3A4 and organic anion-transporting polypeptide (OATP) 1B1 inhibitor clarithromycin on the pharmacokinetics of bosentan. Bosentan 192-200 solute carrier organic anion transporter family member 1B1 Homo sapiens 90-139 23738582-3 2014 METHODS: We assessed the effect of the OATP and CYP3A inhibitor clarithromycin on bosentan pharmacokinetics at steady state and concurrently quantified changes of CYP3A activity using midazolam as a probe drug. Bosentan 82-90 solute carrier organic anion transporter family member 1A2 Homo sapiens 39-43 23738582-3 2014 METHODS: We assessed the effect of the OATP and CYP3A inhibitor clarithromycin on bosentan pharmacokinetics at steady state and concurrently quantified changes of CYP3A activity using midazolam as a probe drug. Bosentan 82-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-53 24389822-0 2014 Bladder endothelin-1 receptor binding of bosentan and ambrisentan. Bosentan 41-49 endothelin receptor type A Rattus norvegicus 8-29 24389822-4 2014 ET-1, bosentan, ambrisentan, and CI-1020 inhibited specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Bosentan 6-14 endothelin 1 Rattus norvegicus 68-72 24389822-6 2014 Bosentan and ambrisentan significantly increased the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). Bosentan 0-8 endothelin 1 Rattus norvegicus 95-99 24389822-7 2014 Thus, bosentan and ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. Bosentan 6-14 endothelin 1 Rattus norvegicus 55-59 24389822-8 2014 Oral administration of bosentan caused a dose-dependent decrease in Bmax for bladder [(125)I]ET-1 binding, suggesting significant binding of bladder ET-1 receptors in vivo. Bosentan 23-31 endothelin 1 Rattus norvegicus 93-97 24389822-8 2014 Oral administration of bosentan caused a dose-dependent decrease in Bmax for bladder [(125)I]ET-1 binding, suggesting significant binding of bladder ET-1 receptors in vivo. Bosentan 23-31 endothelin 1 Rattus norvegicus 149-153 23987157-10 2013 RESULTS: Cavernous tissue endothelin 1, adenosine deaminase, heme oxygenase 1 enzymatic activity levels, and apoptosis index were significantly decreased in bosentan, theophylline, and ZnPP-treated rats compared with the controls. Bosentan 157-165 endothelin 1 Rattus norvegicus 26-38 25748132-7 2014 Given that potential disease modifying drugs, bosentan and imatinib, reverse the expression and transcriptional activity of Fli1, the studies on the pathological process of double heterozygous mice and the impact of these transcription factors on various cell types may provide a new clue to further understand the pathogenesis of SSc leading to the development of new therapies. Bosentan 46-54 Friend leukemia integration 1 Mus musculus 124-128 23863877-0 2013 Association of CYP2C9*2 with bosentan-induced liver injury. Bosentan 29-37 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 15-21 23863877-6 2013 Bosentan metabolism by CYP2C9*2 in vitro was significantly reduced compared with CYP2C9*1 and was comparable to that by CYP2C9*3. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 23-29 23863877-6 2013 Bosentan metabolism by CYP2C9*2 in vitro was significantly reduced compared with CYP2C9*1 and was comparable to that by CYP2C9*3. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 81-87 23863877-6 2013 Bosentan metabolism by CYP2C9*2 in vitro was significantly reduced compared with CYP2C9*1 and was comparable to that by CYP2C9*3. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 81-87 23863877-7 2013 These results suggest that CYP2C9*2 is a potential genetic marker for prediction of bosentan-induced liver injury and warrants investigation for the optimization of bosentan treatment. Bosentan 84-92 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 27-33 23863877-7 2013 These results suggest that CYP2C9*2 is a potential genetic marker for prediction of bosentan-induced liver injury and warrants investigation for the optimization of bosentan treatment. Bosentan 165-173 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 27-33 24524605-3 2013 Bosentan was applied within 7 days after Fontan surgery as follows: at the first month, 7.8125 mg Bid for patients with body weight <= 10 kg; 15.625 mg Bid for patients with body weight between 10-20 kg; 31.25 mg Bid for patients with body weight 20-30 kg and 62.5 mg Bid for patients with body weight > 30 kg. Bosentan 0-8 BH3 interacting domain death agonist Homo sapiens 98-101 24524605-3 2013 Bosentan was applied within 7 days after Fontan surgery as follows: at the first month, 7.8125 mg Bid for patients with body weight <= 10 kg; 15.625 mg Bid for patients with body weight between 10-20 kg; 31.25 mg Bid for patients with body weight 20-30 kg and 62.5 mg Bid for patients with body weight > 30 kg. Bosentan 0-8 BH3 interacting domain death agonist Homo sapiens 155-158 24524605-3 2013 Bosentan was applied within 7 days after Fontan surgery as follows: at the first month, 7.8125 mg Bid for patients with body weight <= 10 kg; 15.625 mg Bid for patients with body weight between 10-20 kg; 31.25 mg Bid for patients with body weight 20-30 kg and 62.5 mg Bid for patients with body weight > 30 kg. Bosentan 0-8 BH3 interacting domain death agonist Homo sapiens 155-158 24524605-3 2013 Bosentan was applied within 7 days after Fontan surgery as follows: at the first month, 7.8125 mg Bid for patients with body weight <= 10 kg; 15.625 mg Bid for patients with body weight between 10-20 kg; 31.25 mg Bid for patients with body weight 20-30 kg and 62.5 mg Bid for patients with body weight > 30 kg. Bosentan 0-8 BH3 interacting domain death agonist Homo sapiens 155-158 23696678-8 2013 In the BIRD-1 cohort, serum ET-1 was elevated in all cases at SRC (median healthy controls 0.50 pg/ml; SRC 1.48 pg/ml; P < 0.0005), and increased further with bosentan therapy (1.46 vs. 3.05 pg/ml; t-test P < 0.05). Bosentan 162-170 endothelin 1 Homo sapiens 28-32 23987157-10 2013 RESULTS: Cavernous tissue endothelin 1, adenosine deaminase, heme oxygenase 1 enzymatic activity levels, and apoptosis index were significantly decreased in bosentan, theophylline, and ZnPP-treated rats compared with the controls. Bosentan 157-165 adenosine deaminase Rattus norvegicus 40-59 23987157-10 2013 RESULTS: Cavernous tissue endothelin 1, adenosine deaminase, heme oxygenase 1 enzymatic activity levels, and apoptosis index were significantly decreased in bosentan, theophylline, and ZnPP-treated rats compared with the controls. Bosentan 157-165 heme oxygenase 1 Rattus norvegicus 61-77 24015303-5 2013 ET-1 was inhibited by Bosentan, ERK1/2 mitogen activated protein kinase (MAPK) was inhibited by U0126 and p38 MAPK was inhibited by SB203580. Bosentan 22-30 endothelin 1 Homo sapiens 0-4 24015303-7 2013 This effect involved the mitogen activated protein kinases (MAPK) ERK1/2 MAPK and was abrogated by Bosentan which caused a G1- arrest through activation of p27((Kip)). Bosentan 99-107 interferon alpha inducible protein 27 Homo sapiens 156-159 24015303-10 2013 Bosentan dose-dependently reduced the stimulatory effect of ET-1 on collagen type-I and fibronectin, but had no effect on TGF-beta1. Bosentan 0-8 fibronectin 1 Homo sapiens 60-99 23720457-8 2013 Bosentan and BQ788 inhibited M-LPS-induced release of all cytokines and soluble CD14 (sCD14) but not TLR4 expression. Bosentan 0-8 CD14 molecule Homo sapiens 80-84 23988169-1 2013 We examined the effect of bosentan, an ETA and ETB receptor antagonist, on EEG, an indicator of neuronal activity, in rats with experimentally induced cerebral ischemia-reperfusion. Bosentan 26-34 endothelin receptor type A Rattus norvegicus 39-42 23359533-9 2013 Bosentan treatment was more effective than TGFbeta blockade in reversing the actions of IFN-gamma, including downregulation of alpha-SMA and TGFbeta2, suggesting that activation of the ET-1 pathway plays a main role in the IFN-gamma responses in HDMECs. Bosentan 0-8 interferon gamma Homo sapiens 88-97 23359533-9 2013 Bosentan treatment was more effective than TGFbeta blockade in reversing the actions of IFN-gamma, including downregulation of alpha-SMA and TGFbeta2, suggesting that activation of the ET-1 pathway plays a main role in the IFN-gamma responses in HDMECs. Bosentan 0-8 transforming growth factor beta 2 Homo sapiens 141-149 23359533-9 2013 Bosentan treatment was more effective than TGFbeta blockade in reversing the actions of IFN-gamma, including downregulation of alpha-SMA and TGFbeta2, suggesting that activation of the ET-1 pathway plays a main role in the IFN-gamma responses in HDMECs. Bosentan 0-8 endothelin 1 Homo sapiens 185-189 23359533-9 2013 Bosentan treatment was more effective than TGFbeta blockade in reversing the actions of IFN-gamma, including downregulation of alpha-SMA and TGFbeta2, suggesting that activation of the ET-1 pathway plays a main role in the IFN-gamma responses in HDMECs. Bosentan 0-8 interferon gamma Homo sapiens 223-232 23720457-10 2013 IL-8 release induced by S-LPS, which requires CD14 to activate TLR4, was blocked by bosentan and BQ788. Bosentan 84-92 C-X-C motif chemokine ligand 8 Homo sapiens 0-4 23720457-10 2013 IL-8 release induced by S-LPS, which requires CD14 to activate TLR4, was blocked by bosentan and BQ788. Bosentan 84-92 CD14 molecule Homo sapiens 46-50 21763017-6 2013 Clinical characteristics, six minute walking distances (6 MWD), laboratory tests and images were obtained from medical records and the responses to Bosentan, an endothelin-1 receptor antagonist, were assessed. Bosentan 148-156 endothelin receptor type A Homo sapiens 161-182 23720457-10 2013 IL-8 release induced by S-LPS, which requires CD14 to activate TLR4, was blocked by bosentan and BQ788. Bosentan 84-92 toll like receptor 4 Homo sapiens 63-67 23984086-6 2013 The reduction of ET-1 levels in DUs patients in therapy with bosentan confirms the efficacy of this molecule both for treatment and prevention of digital ulcers. Bosentan 61-69 endothelin 1 Homo sapiens 17-21 22265324-0 2013 Relationship between baseline ET-1 plasma levels and outcome in patients with idiopathic pulmonary hypertension treated with bosentan. Bosentan 125-133 endothelin 1 Homo sapiens 30-34 22265324-1 2013 OBJECTIVES: To address if baseline endothelin-1 (ET-1) plasma levels might predict clinical worsening (CW) in patients with idiopathic pulmonary hypertension (IPAH) treated with bosentan. Bosentan 178-186 endothelin 1 Homo sapiens 35-47 23590298-3 2013 We hypothesized that human airway smooth muscle cells (HASMCs) participate in linking inflammation with remodeling and that associated genes become differentially suppressed by ambrisentan (A-receptor selective ETRA) and bosentan (nonselective/dual ETRA). Bosentan 221-229 endothelin receptor type A Homo sapiens 249-253 23590298-10 2013 Chemokine (C-C motif) ligands 2 and 5, granulocyte macrophage colony-stimulating factor, and MMP13 had increased sensitivity to bosentan or bosentan/dexamethasone combination versus dexamethasone alone. Bosentan 128-136 matrix metallopeptidase 13 Homo sapiens 93-98 23590298-10 2013 Chemokine (C-C motif) ligands 2 and 5, granulocyte macrophage colony-stimulating factor, and MMP13 had increased sensitivity to bosentan or bosentan/dexamethasone combination versus dexamethasone alone. Bosentan 140-148 matrix metallopeptidase 13 Homo sapiens 93-98 23387445-0 2013 Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line. Bosentan 54-62 ATP binding cassette subfamily C member 2 Homo sapiens 30-34 23387445-0 2013 Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line. Bosentan 54-62 solute carrier organic anion transporter family member 1B1 Homo sapiens 75-82 23387445-0 2013 Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line. Bosentan 54-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 23387445-0 2013 Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line. Bosentan 54-62 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 90-96 23387445-0 2013 Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line. Bosentan 54-62 ATP binding cassette subfamily C member 2 Homo sapiens 97-101 23387445-3 2013 EXPERIMENTAL APPROACH: A newly established quadruple-transfected MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 cell line was used to investigate metabolism and transcellular transport of the endothelin receptor antagonist bosentan. Bosentan 210-218 solute carrier organic anion transporter family member 1B1 Homo sapiens 72-79 23387445-4 2013 KEY RESULTS: Intracellular accumulation of bosentan equivalents (i.e. parent compound and metabolites) was significantly lower in all cell lines expressing MRP2 compared to cell lines lacking this transporter (P < 0.001). Bosentan 43-51 ATP binding cassette subfamily C member 2 Homo sapiens 156-160 23387445-5 2013 Accordingly, considerably higher amounts of bosentan equivalents were detectable in the apical compartments of cell lines with MRP2 expression (P < 0.001). Bosentan 44-52 ATP binding cassette subfamily C member 2 Homo sapiens 127-131 23387445-8 2013 Additionally, a direct glucuronide of bosentan could be identified intracellularly in cell lines expressing UGT1A1 and in the apical compartments of cell lines expressing UGT1A1 and MRP2. Bosentan 38-46 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 108-114 23387445-8 2013 Additionally, a direct glucuronide of bosentan could be identified intracellularly in cell lines expressing UGT1A1 and in the apical compartments of cell lines expressing UGT1A1 and MRP2. Bosentan 38-46 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 171-177 23387445-8 2013 Additionally, a direct glucuronide of bosentan could be identified intracellularly in cell lines expressing UGT1A1 and in the apical compartments of cell lines expressing UGT1A1 and MRP2. Bosentan 38-46 ATP binding cassette subfamily C member 2 Homo sapiens 182-186 23387445-9 2013 CONCLUSIONS AND IMPLICATIONS: These in vitro data indicate that bosentan is a substrate of UGT1A1. Bosentan 64-72 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 91-97 23387445-10 2013 Moreover, the efflux transporter MRP2 mediates export of bosentan and most likely also of bosentan glucuronide in the cell system. Bosentan 57-65 ATP binding cassette subfamily C member 2 Homo sapiens 33-37 23363065-0 2013 The effect of the endothelin-1 receptor antagonist, bosentan, on patients with poorly controlled asthma: a 17-week, double-blind, placebo-controlled crossover pilot study. Bosentan 52-60 endothelin receptor type A Homo sapiens 18-39 23509249-6 2013 We then used arterial spin-labeling MRI to noninvasively measure CBF and assess the effect of the administration of the ET-1 antagonist bosentan. Bosentan 136-144 endothelin 1 Homo sapiens 120-124 23200808-8 2013 Treatment with the combined ET receptor antagonist bosentan (250 mg/kg/day; day 10 to 21) prevented further increase in RVPSP and RV hypertrophy, decreased ETA/ETB protein levels, reduced oxidative stress and protein nitration, and resulted in marked attenuation of pulmonary vascular cell proliferation. Bosentan 51-59 endothelin receptor type A Homo sapiens 156-159 23200808-8 2013 Treatment with the combined ET receptor antagonist bosentan (250 mg/kg/day; day 10 to 21) prevented further increase in RVPSP and RV hypertrophy, decreased ETA/ETB protein levels, reduced oxidative stress and protein nitration, and resulted in marked attenuation of pulmonary vascular cell proliferation. Bosentan 51-59 endothelin receptor type B Homo sapiens 160-163 23219525-1 2013 The combinations of the endothelin-1 receptor antagonists bosentan or ambrisentan with the phosphodiesterase 5 inhibitors sildenafil or tadalafil are current standard therapies of advanced pulmonary arterial hypertension. Bosentan 58-66 endothelin receptor type A Homo sapiens 24-45 23202724-7 2013 ET-1-ROCK interactions were assessed by measuring ROCK activity after ET-1, ET-1 siRNA, and bosentan treatments, and tube formation with ET-1 and Y-27632 (ROCK inhibitor). Bosentan 92-100 EDN1 Ovis aries 0-4 23233754-8 2013 In modified Langendorff perfusions, ERAs (BQ-123 and bosentan 10(-7,-6,-5) mol/L) decreased contractility in the hypertrophied, but not normal RV, in a dose-dependent manner (P<0.01). Bosentan 53-61 ES cell expressed Ras Homo sapiens 36-40 24826287-4 2013 Oral bosentan and intravenous epoprostenol then led to a ~50% decrease of mPAP (TPG between 16 and 22 mmHg). Bosentan 5-13 phospholipid phosphatase 1 Mus musculus 74-78 22861120-5 2013 RESULTS: After four months, PVR decreased by 38% in patients receiving bosentan (n = 22), while it increased by 25% in the control group (p = 0.001). Bosentan 71-79 PVR cell adhesion molecule Homo sapiens 28-31 22861120-6 2013 Those patients who received bosentan for 12 months (n = 9), experienced a 60% reduction in PVR compared to baseline (p = 0.003). Bosentan 28-36 PVR cell adhesion molecule Homo sapiens 91-94 22861120-9 2013 Patients with high PVR who received bosentan showed a trend toward better one-yr survival after transplantation than patients with PVR <= 2.5 Wood units transplanted in the same period of time (93% vs. 83%). Bosentan 36-44 PVR cell adhesion molecule Homo sapiens 19-22 22861120-10 2013 CONCLUSIONS: In patients considered high-risk candidates for heart transplantation because of high PVR, therapy with bosentan is associated with a significant reduction in PVR and a good outcome after transplantation. Bosentan 117-125 PVR cell adhesion molecule Homo sapiens 99-102 22861120-10 2013 CONCLUSIONS: In patients considered high-risk candidates for heart transplantation because of high PVR, therapy with bosentan is associated with a significant reduction in PVR and a good outcome after transplantation. Bosentan 117-125 PVR cell adhesion molecule Homo sapiens 172-175 22899584-9 2013 These drugs lowered hepatic ischemia and inflammation, whereas pretreatment of rats with the dual endothelin-1 receptor blocker, bosentan, improved cell engraftment independently of hepatic ischemia or inflammation, without improving liver repopulation. Bosentan 129-137 endothelin receptor type A Rattus norvegicus 98-119 23292819-3 2013 Key developments are the increased use of phosphodiesterase type V inhibitors in severe RP, and of bosentan (an endothelin-1 receptor antagonist) for prevention of recurrent SSc-related digital ulcers. Bosentan 99-107 endothelin receptor type A Homo sapiens 112-133 23720841-6 2013 RESULTS: Bosentan treatment resulted in a reduction in pulmonary artery systolic pressure and mPAP (at 12 months: 76.8 +/- 11.5 and 58.8 +/- 11.4 mm Hg, respectively; p < 0.01) and an increase in CO (at 12 months: 4.2 +/- 1.2 l/min; p = 0.002). Bosentan 9-17 phospholipid phosphatase 1 Mus musculus 94-98 24296902-1 2013 OBJECTIVES: The dual endothelin receptor antagonist bosentan improves pulmonary vascular resistance (PVR) in patients with primary pulmonary hypertension (PH). Bosentan 52-60 PVR cell adhesion molecule Homo sapiens 101-104 22205719-2 2012 Bosentan, an endothelin (ET) receptor-type ET(A) and ET(B) antagonist, is metabolized to active metabolites by and an inducer of cytochrome P450 (CYP)2C9 and CYP3A. Bosentan 0-8 endothelin receptor type B Homo sapiens 53-58 23053682-1 2012 Bosentan, a dual endothelin receptor antagonist, may reduce blood pressure by blocking the vasoconstrictor effect of endothelin-1. Bosentan 0-8 endothelin 1 Homo sapiens 117-129 22205719-2 2012 Bosentan, an endothelin (ET) receptor-type ET(A) and ET(B) antagonist, is metabolized to active metabolites by and an inducer of cytochrome P450 (CYP)2C9 and CYP3A. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 129-153 22205719-2 2012 Bosentan, an endothelin (ET) receptor-type ET(A) and ET(B) antagonist, is metabolized to active metabolites by and an inducer of cytochrome P450 (CYP)2C9 and CYP3A. Bosentan 0-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 158-163 22561246-6 2012 An antagonist of ET(A), bosentan, prevented the interaction between p9-ET(A) and ET-1 in a concentration-dependent manner. Bosentan 24-32 endothelin receptor type A Homo sapiens 17-22 22407503-7 2012 In primary chondrocyte cultures, Bosentan did not block TGFalpha responses of the anabolic genes Sox9, Agc1, and Col2a1, but reduced the induction of Mmp13 and Ednra transcripts by TGFalpha. Bosentan 33-41 matrix metallopeptidase 13 Rattus norvegicus 150-155 22407503-7 2012 In primary chondrocyte cultures, Bosentan did not block TGFalpha responses of the anabolic genes Sox9, Agc1, and Col2a1, but reduced the induction of Mmp13 and Ednra transcripts by TGFalpha. Bosentan 33-41 endothelin receptor type A Rattus norvegicus 160-165 22407503-7 2012 In primary chondrocyte cultures, Bosentan did not block TGFalpha responses of the anabolic genes Sox9, Agc1, and Col2a1, but reduced the induction of Mmp13 and Ednra transcripts by TGFalpha. Bosentan 33-41 transforming growth factor alpha Rattus norvegicus 181-189 22480514-9 2012 Bosentan was significantly more effective an inhibitor of beta-arrestin recruitment mediated by ET(A) compared to the ET(B) receptor. Bosentan 0-8 endothelin receptor type A Homo sapiens 96-101 22480514-11 2012 SIGNIFICANCE: These data suggest that the pharmacology of ET(A) and ET(B) receptors linked to G-protein- and beta-arrestin mediated responses was different and bosentan appeared to show bias, preferentially blocking ET(A) mediated beta-arrestin recruitment. Bosentan 160-168 endothelin receptor type A Homo sapiens 58-63 22480514-11 2012 SIGNIFICANCE: These data suggest that the pharmacology of ET(A) and ET(B) receptors linked to G-protein- and beta-arrestin mediated responses was different and bosentan appeared to show bias, preferentially blocking ET(A) mediated beta-arrestin recruitment. Bosentan 160-168 endothelin receptor type A Homo sapiens 216-221 22483689-4 2012 The stimulatory effect of ET-1 on beta(2)-adrenoceptor mRNA was prevented by the non-selective ET-A/ET-B receptor antagonist bosentan, indicating that it was mediated via specific ET receptors. Bosentan 125-133 endothelin 1 Homo sapiens 26-30 22483689-4 2012 The stimulatory effect of ET-1 on beta(2)-adrenoceptor mRNA was prevented by the non-selective ET-A/ET-B receptor antagonist bosentan, indicating that it was mediated via specific ET receptors. Bosentan 125-133 adrenoceptor beta 2 Homo sapiens 34-54 22483689-4 2012 The stimulatory effect of ET-1 on beta(2)-adrenoceptor mRNA was prevented by the non-selective ET-A/ET-B receptor antagonist bosentan, indicating that it was mediated via specific ET receptors. Bosentan 125-133 endothelin receptor type A Homo sapiens 95-99 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 endothelin receptor type A Rattus norvegicus 89-93 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 interleukin 1 beta Rattus norvegicus 233-250 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 interleukin 1 beta Rattus norvegicus 252-260 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 interleukin 6 Rattus norvegicus 263-276 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 interleukin 6 Rattus norvegicus 278-282 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 tumor necrosis factor Rattus norvegicus 285-312 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 tumor necrosis factor Rattus norvegicus 314-322 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 C-C motif chemokine ligand 2 Rattus norvegicus 329-363 22994521-5 2012 Immnofluorescence and quantitative PCR studies showed that concurrent treatment with the ET-A/B receptor antagonist, bosentan (200 mg/kg/day), blocked CH-induced ED-1+ macrophage invasion and the upregulation of cytokines, including interleukin-1beta (IL-1beta), interleukin-6 (IL-6), tumor necrosis factor alpha (TNFalpha), and monocyte chemoattractant protein-1 (MCP-1). Bosentan 117-125 C-C motif chemokine ligand 2 Rattus norvegicus 365-370 21920972-8 2012 Importantly, the ET-1 receptor A/B (ET(A/B)) antagonist bosentan normalized endothelial function in SHR-T (P < 0.05). Bosentan 56-64 endothelin 1 Rattus norvegicus 17-21 21920972-8 2012 Importantly, the ET-1 receptor A/B (ET(A/B)) antagonist bosentan normalized endothelial function in SHR-T (P < 0.05). Bosentan 56-64 endothelin receptor type A Rattus norvegicus 36-43 22561246-6 2012 An antagonist of ET(A), bosentan, prevented the interaction between p9-ET(A) and ET-1 in a concentration-dependent manner. Bosentan 24-32 endothelin receptor type A Homo sapiens 71-76 22561246-6 2012 An antagonist of ET(A), bosentan, prevented the interaction between p9-ET(A) and ET-1 in a concentration-dependent manner. Bosentan 24-32 endothelin 1 Homo sapiens 81-85 22249931-0 2012 Bosentan, an endothelin receptor antagonist, ameliorates collagen-induced arthritis: the role of TNF-alpha in the induction of endothelin system genes. Bosentan 0-8 tumor necrosis factor Mus musculus 97-106 22260985-7 2012 Bosentan pretreatment (n=8, P<0.05) suggested endothelin-1 as the inferred contractile neurogenic endothelial-dependent factor. Bosentan 0-8 endothelin-1 Sus scrofa 49-61 21828025-3 2012 CS extract (CSE) increased ET(A) and ET(B) expression in HPASMCs and small intrapulmonary arteries, which was attenuated by bosentan, the ET(A) antagonist BQ123 and the ET(B) antagonist BQ788, and by blocking ET-1 with a monoclonal antibody against ET-1, suggesting a feed-forward mechanism mediated by ET-1 release. Bosentan 124-132 endothelin receptor type A Homo sapiens 27-32 21828025-3 2012 CS extract (CSE) increased ET(A) and ET(B) expression in HPASMCs and small intrapulmonary arteries, which was attenuated by bosentan, the ET(A) antagonist BQ123 and the ET(B) antagonist BQ788, and by blocking ET-1 with a monoclonal antibody against ET-1, suggesting a feed-forward mechanism mediated by ET-1 release. Bosentan 124-132 endothelin receptor type B Homo sapiens 37-42 21828025-3 2012 CS extract (CSE) increased ET(A) and ET(B) expression in HPASMCs and small intrapulmonary arteries, which was attenuated by bosentan, the ET(A) antagonist BQ123 and the ET(B) antagonist BQ788, and by blocking ET-1 with a monoclonal antibody against ET-1, suggesting a feed-forward mechanism mediated by ET-1 release. Bosentan 124-132 endothelin 1 Homo sapiens 209-213 21828025-3 2012 CS extract (CSE) increased ET(A) and ET(B) expression in HPASMCs and small intrapulmonary arteries, which was attenuated by bosentan, the ET(A) antagonist BQ123 and the ET(B) antagonist BQ788, and by blocking ET-1 with a monoclonal antibody against ET-1, suggesting a feed-forward mechanism mediated by ET-1 release. Bosentan 124-132 endothelin 1 Homo sapiens 249-253 21828025-3 2012 CS extract (CSE) increased ET(A) and ET(B) expression in HPASMCs and small intrapulmonary arteries, which was attenuated by bosentan, the ET(A) antagonist BQ123 and the ET(B) antagonist BQ788, and by blocking ET-1 with a monoclonal antibody against ET-1, suggesting a feed-forward mechanism mediated by ET-1 release. Bosentan 124-132 endothelin 1 Homo sapiens 249-253 21828025-5 2012 Furthermore, CSE exposure increased the acute ET-1-induced small intrapulmonary artery contraction, which was attenuated by bosentan, BQ123 and BQ788. Bosentan 124-132 endothelin 1 Homo sapiens 46-50 22365914-1 2012 The aim was to analyze the effect of tacrolimus on the aortic expression of proteins associated with the energetic metabolism and cytoskeleton and if it could be reverted by ET-1-receptor antagonist bosentan. Bosentan 199-207 endothelin 1 Rattus norvegicus 174-178 22365914-7 2012 Bosentan co-administration with tacrolimus prevented also changes in ET-1 content and the expression of proteins associated with energetic metabolism. Bosentan 0-8 endothelin 1 Rattus norvegicus 69-73 22365914-8 2012 Bosentan did not affect the increased expression of gp91-phox related to tacrolimus although significantly enhanced aortic MnSOD expression. Bosentan 0-8 superoxide dismutase 2 Rattus norvegicus 123-128 22249931-11 2012 Bosentan treatment also reduced joint damage, leukocyte infiltration and pro-inflammatory cytokine levels (IL-1beta, TNFalpha and IL-17) in the joint tissues. Bosentan 0-8 interleukin 1 beta Mus musculus 107-115 22249931-11 2012 Bosentan treatment also reduced joint damage, leukocyte infiltration and pro-inflammatory cytokine levels (IL-1beta, TNFalpha and IL-17) in the joint tissues. Bosentan 0-8 tumor necrosis factor Mus musculus 117-125 22249931-11 2012 Bosentan treatment also reduced joint damage, leukocyte infiltration and pro-inflammatory cytokine levels (IL-1beta, TNFalpha and IL-17) in the joint tissues. Bosentan 0-8 interleukin 17A Mus musculus 130-135 21432755-2 2012 We assessed whether low dose treatment with the dual endothelin-1 receptor antagonist bosentan is associated with improved hemodynamics and clinical outcome in these patients. Bosentan 86-94 endothelin receptor type A Homo sapiens 53-74 22320712-7 2012 Treatment with the non-selective ET(A)/ET(B) receptor antagonist bosentan, and selective ET(A) or ET(B) receptor antagonists BQ-123 or BQ-788, respectively, inhibited ET-1- and ovalbumin-induced neutrophil migration to the peritoneal cavity. Bosentan 65-73 endothelin receptor type A Mus musculus 33-38 22320712-7 2012 Treatment with the non-selective ET(A)/ET(B) receptor antagonist bosentan, and selective ET(A) or ET(B) receptor antagonists BQ-123 or BQ-788, respectively, inhibited ET-1- and ovalbumin-induced neutrophil migration to the peritoneal cavity. Bosentan 65-73 endothelin 1 Mus musculus 167-172 22320712-7 2012 Treatment with the non-selective ET(A)/ET(B) receptor antagonist bosentan, and selective ET(A) or ET(B) receptor antagonists BQ-123 or BQ-788, respectively, inhibited ET-1- and ovalbumin-induced neutrophil migration to the peritoneal cavity. Bosentan 65-73 serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene Mus musculus 177-186 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 endothelin 1 Mus musculus 4-8 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene Mus musculus 14-23 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 tumor necrosis factor receptor superfamily, member 1b Mus musculus 71-76 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 chemokine (C-X-C motif) ligand 1 Mus musculus 121-126 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 chemokine (C-X-C motif) receptor 2 Mus musculus 156-161 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 endothelin 1 Mus musculus 226-230 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 tumor necrosis factor Mus musculus 266-274 22320712-9 2012 The ET-1- and ovalbumin-induced neutrophil recruitment were reduced in TNFR1 deficient mice, and by treatments targeting CXCL1 or CXC chemokine receptor 2 (CXCR2); further, treatment with bosentan, BQ-123, or BQ-788 inhibited ET-1- and antigen-induced production of TNFalpha and CXCL1. Bosentan 188-196 chemokine (C-X-C motif) ligand 1 Mus musculus 279-284 21432755-11 2012 CONCLUSION: Treatment with the endothelin-1 antagonist bosentan is associated with improvements in hemodynamics and clinical outcome in end-stage heart failure patients with PH. Bosentan 55-63 endothelin 1 Homo sapiens 31-43 22359440-3 2012 Bosentan is intended to affect vasoconstriction, hypertrophic and fibrotic effects by blocking the actions of receptors ET(A) and ET(B). Bosentan 0-8 endothelin receptor type A Homo sapiens 120-125 22359440-3 2012 Bosentan is intended to affect vasoconstriction, hypertrophic and fibrotic effects by blocking the actions of receptors ET(A) and ET(B). Bosentan 0-8 endothelin receptor type B Homo sapiens 130-135 22359440-4 2012 In this study we identified the action of Bosentan on endothelin B receptor using docking studies with homology modeled endothelin B receptor. Bosentan 42-50 endothelin receptor type B Homo sapiens 54-75 22359440-4 2012 In this study we identified the action of Bosentan on endothelin B receptor using docking studies with homology modeled endothelin B receptor. Bosentan 42-50 endothelin receptor type B Homo sapiens 120-141 22359440-6 2012 The results indicated that amino acid ARG82, ARG84 and HIS197 present in endothelin B receptor are core important for binding activities and these residues are having strong hydrogen bond interactions with Bosentan. Bosentan 206-214 endothelin receptor type B Homo sapiens 73-94 22359440-8 2012 Among the docked compounds, one of the Bosentan derivatives BD(6) shows better interaction than Bosentan with endothelin B receptor. Bosentan 39-47 endothelin receptor type B Homo sapiens 110-131 22359440-8 2012 Among the docked compounds, one of the Bosentan derivatives BD(6) shows better interaction than Bosentan with endothelin B receptor. Bosentan 96-104 endothelin receptor type B Homo sapiens 110-131 22468718-0 2012 Relation of bosentan, iloprost, and sildenafil with growth factor levels in monocrotaline-induced pulmonary hypertension. Bosentan 12-20 myotrophin Rattus norvegicus 52-65 22029879-9 2011 We selected this particular combination upon finding that VIP down-regulates endothelin receptor expression which is further suppressed by bosentan. Bosentan 139-147 vasoactive intestinal peptide Rattus norvegicus 58-61 22558517-9 2012 Plasma ET-1 in hypoxia during the bosentan period was 2.8 times higher than during for both CS and HS. Bosentan 34-42 endothelin 1 Homo sapiens 7-11 21834070-10 2011 Moreover, inhibition of ET-1 signaling by bosentan abolished the TF-mediated fibrotic capacity of HCMFs. Bosentan 42-50 endothelin 1 Homo sapiens 24-28 21547665-6 2011 In the experiment to assess prevention of endothelin-1-induced sudden death in mice, compound 5b showed comparable activity to bosentan, and 30 was more potent than bosentan. Bosentan 165-173 endothelin 1 Mus musculus 42-54 21914519-1 2011 OBJECTIVES: Bosentan, a dual endothelin receptor antagonist (ERA), was the first oral drug approved for the treatment of pulmonary arterial hypertension (PAH), a rare disease with poor prognosis. Bosentan 12-20 estrogen receptor 1 Homo sapiens 29-59 21501604-0 2011 Differential modulation of the expression of important drug metabolising enzymes and transporters by endothelin-1 receptor antagonists ambrisentan and bosentan in vitro. Bosentan 151-159 endothelin receptor type A Homo sapiens 101-122 21501604-3 2011 We therefore investigated the impact of the endothelin-1 receptor antagonists bosentan and ambrisentan on the expression of relevant human efflux and uptake transporters and on phase 1 and phase 2 enzymes. Bosentan 78-86 endothelin receptor type A Homo sapiens 44-65 21777087-6 2011 Bosentan (10(-5) mol/L), an inhibitor of endothelin-1 (ET-1) receptors, corrected the attenuated vasodilatation observed with r-HuEPO and inhibited the vasoconstriction induced by flow in the presence of r-HuEPO and L-NAME. Bosentan 0-8 endothelin 1 Homo sapiens 41-53 21777087-6 2011 Bosentan (10(-5) mol/L), an inhibitor of endothelin-1 (ET-1) receptors, corrected the attenuated vasodilatation observed with r-HuEPO and inhibited the vasoconstriction induced by flow in the presence of r-HuEPO and L-NAME. Bosentan 0-8 endothelin 1 Homo sapiens 55-59 21205912-5 2011 Diabetes increased vascular smooth muscle (VSM) ET(A) and ET(B) receptors; the increase was prevented by chronic bosentan treatment. Bosentan 113-121 endothelin receptor type A Rattus norvegicus 48-53 21205912-9 2011 Attenuation of changes in ET receptor profile with bosentan treatment suggests that ET-1 has a positive feedback on the expression of its receptors in the cerebrovasculature. Bosentan 51-59 endothelin 1 Rattus norvegicus 84-88 21839301-0 2011 Combination therapy with an endothelin-1 receptor antagonist (bosentan) and a phosphodiesterase V inhibitor (sildenafil) for the management of severe digital ulcerations in systemic sclerosis. Bosentan 62-70 endothelin receptor type A Homo sapiens 28-49 21527360-6 2011 In patients with pulmonary arterial hypertension (PAH), therapy with bosentan, an endothelin-1 receptor antagonist, has demonstrated to improve exercise capacity and to reduce the elevated PVR. Bosentan 69-77 endothelin receptor type A Homo sapiens 82-103 21527360-6 2011 In patients with pulmonary arterial hypertension (PAH), therapy with bosentan, an endothelin-1 receptor antagonist, has demonstrated to improve exercise capacity and to reduce the elevated PVR. Bosentan 69-77 PVR cell adhesion molecule Homo sapiens 189-192 21527360-8 2011 However, the long term effect of reducing the PVR by bosentan treatment on exercise capacity in Fontan patients is still unknown. Bosentan 53-61 PVR cell adhesion molecule Homo sapiens 46-49 21527360-11 2011 CONCLUSION: We hypothesize that treatment with bosentan, an endothelin-1 receptor antagonist, improves maximum exercise capacity and functional capacity in adult Fontan patients. Bosentan 47-55 endothelin receptor type A Homo sapiens 60-81 21501604-8 2011 50 muM bosentan up-regulated e.g. CYP3A4 8.5-fold, ABCB1 5.1-fold, and ABCB11 1.9-fold at the mRNA level in LS180 cells. Bosentan 7-15 latexin Homo sapiens 3-6 21501604-8 2011 50 muM bosentan up-regulated e.g. CYP3A4 8.5-fold, ABCB1 5.1-fold, and ABCB11 1.9-fold at the mRNA level in LS180 cells. Bosentan 7-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 21501604-8 2011 50 muM bosentan up-regulated e.g. CYP3A4 8.5-fold, ABCB1 5.1-fold, and ABCB11 1.9-fold at the mRNA level in LS180 cells. Bosentan 7-15 ATP binding cassette subfamily B member 1 Homo sapiens 51-56 21501604-8 2011 50 muM bosentan up-regulated e.g. CYP3A4 8.5-fold, ABCB1 5.1-fold, and ABCB11 1.9-fold at the mRNA level in LS180 cells. Bosentan 7-15 ATP binding cassette subfamily B member 11 Homo sapiens 71-77 21501604-9 2011 In HuH-7 cells induction was much less pronounced (e.g. CYP3A4 1.9-fold for bosentan). Bosentan 76-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 21084678-10 2011 Administration of mixed ET(A/B) receptor antagonist bosentan attenuated the stretch-induced activation of GATA-4 in isolated atria, whereas ANG II receptor type-1 antagonist CV-11974 had no effect. Bosentan 52-60 GATA binding protein 4 Rattus norvegicus 106-112 21132305-5 2011 An oral dual endothelin receptor (ET(A)/ET(B)) antagonist, bosentan, was prescribed, and her symptoms, exercise capacity and laboratory findings improved greatly after treatment. Bosentan 59-67 endothelin receptor type A Homo sapiens 34-39 21132305-5 2011 An oral dual endothelin receptor (ET(A)/ET(B)) antagonist, bosentan, was prescribed, and her symptoms, exercise capacity and laboratory findings improved greatly after treatment. Bosentan 59-67 endothelin receptor type B Homo sapiens 40-45 21430993-0 2011 Gene expressions of nitric oxide synthase and matrix metalloproteinase-2 in monocrotaline-induced pulmonary hypertension in rats after bosentan treatment. Bosentan 135-143 matrix metallopeptidase 2 Rattus norvegicus 46-72 21430993-3 2011 The purpose of this study was to determine the gene expression of eNOS and MMP-2 in the lungs of a rat model of pulmonary hypertension after bosentan treatment. Bosentan 141-149 nitric oxide synthase 3 Rattus norvegicus 66-70 21430993-3 2011 The purpose of this study was to determine the gene expression of eNOS and MMP-2 in the lungs of a rat model of pulmonary hypertension after bosentan treatment. Bosentan 141-149 matrix metallopeptidase 2 Rattus norvegicus 75-80 21430993-9 2011 Following bosentan treatment to reduce pulmonary hypertension, the expression levels of MMP-2 gene were significantly decreased on day 7 and 28. Bosentan 10-18 matrix metallopeptidase 2 Rattus norvegicus 88-93 21430993-10 2011 eNOS and tissue inhibitor of MMPs genes were also significantly decreased on day 28 after bosentan treatment. Bosentan 90-98 nitric oxide synthase 3 Rattus norvegicus 0-4 21430993-10 2011 eNOS and tissue inhibitor of MMPs genes were also significantly decreased on day 28 after bosentan treatment. Bosentan 90-98 matrix metallopeptidase 2 Rattus norvegicus 29-33 20851640-2 2011 Bosentan (BOS), an ET-1 antagonist, and tetrahydrobiopterin (BH4), an eNOS cofactor, may reduce endothelial dysfunction by improving ET-1/NO homeostasis. Bosentan 0-8 endothelin 1 Rattus norvegicus 133-137 21496413-5 2011 In animal models and in vitro models, after treatment with Bosentan, a significant reduction of cytokine (TNF alpha, IFN gamma,IL-8, IL-4) levels was observed. Bosentan 59-67 tumor necrosis factor Homo sapiens 106-115 21496413-5 2011 In animal models and in vitro models, after treatment with Bosentan, a significant reduction of cytokine (TNF alpha, IFN gamma,IL-8, IL-4) levels was observed. Bosentan 59-67 interferon gamma Homo sapiens 117-126 21496413-5 2011 In animal models and in vitro models, after treatment with Bosentan, a significant reduction of cytokine (TNF alpha, IFN gamma,IL-8, IL-4) levels was observed. Bosentan 59-67 C-X-C motif chemokine ligand 8 Homo sapiens 127-131 21496413-5 2011 In animal models and in vitro models, after treatment with Bosentan, a significant reduction of cytokine (TNF alpha, IFN gamma,IL-8, IL-4) levels was observed. Bosentan 59-67 interleukin 4 Homo sapiens 133-137 21496413-11 2011 Bosentan significantly reduced IL-2, IL-6, IL-8 and IFN- gamma levels in SSc patients, probably slowing progression to fibrosis and vascular damage. Bosentan 0-8 interleukin 2 Homo sapiens 31-35 21496413-11 2011 Bosentan significantly reduced IL-2, IL-6, IL-8 and IFN- gamma levels in SSc patients, probably slowing progression to fibrosis and vascular damage. Bosentan 0-8 interleukin 6 Homo sapiens 37-41 21496413-11 2011 Bosentan significantly reduced IL-2, IL-6, IL-8 and IFN- gamma levels in SSc patients, probably slowing progression to fibrosis and vascular damage. Bosentan 0-8 C-X-C motif chemokine ligand 8 Homo sapiens 43-47 21496413-11 2011 Bosentan significantly reduced IL-2, IL-6, IL-8 and IFN- gamma levels in SSc patients, probably slowing progression to fibrosis and vascular damage. Bosentan 0-8 interferon gamma Homo sapiens 52-62 20851640-2 2011 Bosentan (BOS), an ET-1 antagonist, and tetrahydrobiopterin (BH4), an eNOS cofactor, may reduce endothelial dysfunction by improving ET-1/NO homeostasis. Bosentan 10-13 endothelin 1 Rattus norvegicus 133-137 19171388-1 2010 Sitaxentan, a highly-selective endothelin receptor antagonist (ETRA) and bosentan a non-selective ETRA are both approved for the treatment of idiopathic pulmonary arterial hypertension (iPAH). Bosentan 73-81 endothelin receptor type A Homo sapiens 98-102 21283970-7 2011 Bosentan, an oral endothelin receptor antagonists (ETRA), was shown to prevent new DU, but failed to heal existing DU, while the oral phopshodiesterase inhibitor (PDI) Sildenafil reduces the occurrence of RP and might be effective in ulcer healing. Bosentan 0-8 endothelin receptor type A Homo sapiens 51-55 20698855-6 2010 CSE-induced ET(B) expression was attenuated by bosentan, the ET(B) receptor antagonist BQ788, the Rho kinase antagonist Y27632 and the antioxidant N-acetylcysteine. Bosentan 47-55 endothelin receptor type B Homo sapiens 12-17 20690805-1 2010 We investigated the effects of the endothelin-1 (ET-1) receptor dual antagonist (Bosentan ) on the inflammatory cytokines and the chemoattractant molecules associated with breast cancer growth and the development of tumor infiltration in bone explants. Bosentan 81-89 endothelin 1 Mus musculus 35-47 20690805-1 2010 We investigated the effects of the endothelin-1 (ET-1) receptor dual antagonist (Bosentan ) on the inflammatory cytokines and the chemoattractant molecules associated with breast cancer growth and the development of tumor infiltration in bone explants. Bosentan 81-89 endothelin 1 Mus musculus 49-53 20690805-4 2010 The Bosentan treatment in vivo was associated with a local increase of the anti-inflammatory IL-1alpha cytokine concentration and decrease of the pro-inflammatory TNF-alpha and IL-17 cytokine concentrations (p < .05). Bosentan 4-12 interleukin 1 alpha Mus musculus 94-103 20690805-4 2010 The Bosentan treatment in vivo was associated with a local increase of the anti-inflammatory IL-1alpha cytokine concentration and decrease of the pro-inflammatory TNF-alpha and IL-17 cytokine concentrations (p < .05). Bosentan 4-12 tumor necrosis factor Mus musculus 164-173 20690805-4 2010 The Bosentan treatment in vivo was associated with a local increase of the anti-inflammatory IL-1alpha cytokine concentration and decrease of the pro-inflammatory TNF-alpha and IL-17 cytokine concentrations (p < .05). Bosentan 4-12 interleukin 17A Mus musculus 178-183 20967148-0 2010 Gene expression of endothelin-1 and endothelin receptor a on monocrotaline-induced pulmonary hypertension in rats after bosentan treatment. Bosentan 120-128 endothelin 1 Rattus norvegicus 19-31 21244767-2 2010 Bosentan, an Endothelin-1 receptor antagonist used for the treatment of pulmonary arterial hypertension, retards the beginning of new sclerodermic digital ulcers (DU). Bosentan 0-8 endothelin receptor type A Homo sapiens 13-34 20625315-4 2010 Endothelin-1 treatment led to a time- and concentration-dependent increase in cytosolic phosphoSmad2C, which was inhibited by the mixed endothelin receptor antagonist bosentan and the T[beta]RI antagonist SB431542. Bosentan 167-175 endothelin 1 Homo sapiens 0-12 20625315-6 2010 Endothelin-1-stimulated proteoglycan synthesis was partially inhibited (40%) by SB431542 and completely blocked by bosentan. Bosentan 115-123 endothelin 1 Homo sapiens 0-12 20965396-5 2010 The endothelin-1 receptor antagonist bosentan, the phosphodiesterase-5 inhibitor sildenafil, and prostanoids have been shown to improve symptoms, exercise capacity and haemodynamics. Bosentan 37-45 endothelin receptor type A Homo sapiens 4-25 20967148-2 2010 Bosentan, a dual ET receptor (ET(A)/ET(B)) antagonist, is efficacious in treatment of pulmonary hypertension. Bosentan 0-8 endothelin receptor type B Rattus norvegicus 36-41 20967148-8 2010 The levels of ET-1 and ERA gene expression were significantly increased in the MCT group compared with control group on day 5, and bosentan decreased the expression of ET-1 on day 5. Bosentan 131-139 endothelin 1 Rattus norvegicus 168-172 20967148-10 2010 Administration of bosentan reduced ET-1 gene expression in MCT-induced pulmonary hypertension in rats. Bosentan 18-26 endothelin 1 Rattus norvegicus 35-39 19967386-4 2010 The discovery of two receptor subtypes in 1990, ET(A) and ET(B), permitted optimization of the first dual ET-1 receptor antagonist in 1993 by Dr. Clozel"s team, who entered clinical development with bosentan, which was offered to patients with pulmonary arterial hypertension in 2001. Bosentan 199-207 endothelin 1 Homo sapiens 106-110 20466804-8 2010 Bosentan enhanced connexin43 amount in infarcted rats and did not have additional beneficial effects on pravastatin-treated rats. Bosentan 0-8 gap junction protein, alpha 1 Rattus norvegicus 18-28 20392896-5 2010 Our results indicate, for the first time, a dose-dependent CAR mRNA and protein downregulation upon Valsartan and Bosentan treatment. Bosentan 114-122 CXADR Ig-like cell adhesion molecule Homo sapiens 59-62 20133511-3 2010 It is expected that oral treprostinil will be administered with bosentan, approved for the treatment of PAH and known to induce CYP2C9 and 3A4. Bosentan 64-72 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 128-134 20628426-5 2010 Bosentan completely prevented the increase in M/L ratio and MMP-2 activity in diabetes but paradoxically increased M/L ratio and MMP activation in control animals. Bosentan 0-8 matrix metallopeptidase 2 Rattus norvegicus 60-65 20628426-5 2010 Bosentan completely prevented the increase in M/L ratio and MMP-2 activity in diabetes but paradoxically increased M/L ratio and MMP activation in control animals. Bosentan 0-8 matrix metallopeptidase 2 Rattus norvegicus 60-63 20186146-6 2010 The effects of ET1 and aldosterone were blocked by bosentan, an ET type-A/B receptor (ETA/BR) antagonist, and eplerenone, a selective mineralocorticoid receptor (MR) blocker, respectively. Bosentan 51-59 endothelin 1 Homo sapiens 15-18 20628435-8 2010 Only sitaxsentan decreased OATP transport (52%), and only bosentan reduced BSEP transport (78%). Bosentan 58-66 ATP binding cassette subfamily B member 11 Homo sapiens 75-79 20628435-13 2010 Only bosentan and darusentan were shown as substrates for both BSEP and P-glycoprotein efflux. Bosentan 5-13 ATP binding cassette subfamily B member 11 Homo sapiens 63-67 20628435-13 2010 Only bosentan and darusentan were shown as substrates for both BSEP and P-glycoprotein efflux. Bosentan 5-13 ATP binding cassette subfamily B member 1 Homo sapiens 72-86 20093323-1 2010 OBJECTIVE: To compare the level of expression of the renin-angiotensin-aldosterone system (RAAS) in mice with or without the endothelin-1 receptor antagonist bosentan and to examine the potential value in blood pressure regulation. Bosentan 158-166 endothelin receptor type A Mus musculus 125-146 19660388-5 2010 The primary objective of this study was to determine whether the dual endothelin-1 antagonist bosentan improves pulmonary hemodynamics and functional capacity in patients with proximal chronic thromboembolic pulmonary hypertension waiting for pulmonary endarterectomy. Bosentan 94-102 endothelin 1 Homo sapiens 70-82 19958325-8 2010 The MAPK/ERK pathway was activated by cyclosporine administration and was inhibited by cotreatment with bosentan. Bosentan 104-112 mitogen-activated protein kinase 1 Mus musculus 4-8 19958325-8 2010 The MAPK/ERK pathway was activated by cyclosporine administration and was inhibited by cotreatment with bosentan. Bosentan 104-112 mitogen-activated protein kinase 1 Mus musculus 9-12 19969421-10 2010 Treatment with doxycycline (non-specific MMPs inhibitor), bosentan (ET(A)/ET(B) antagonist), indomethacin (COX inhibitor) or guanethidine (sympathetic blocker) inhibited IL-17-induced hypernociception. Bosentan 58-66 interleukin 17A Mus musculus 170-175 21081213-4 2010 The discovery of two receptor subtypes in 1990, ET(A) and ET(B), permitted optimization of bosentan, which entered clinical development in 1993, and was offered to patients with pulmonary arterial hypertension in 2001. Bosentan 91-99 endothelin receptor type A Homo sapiens 48-53 21081213-4 2010 The discovery of two receptor subtypes in 1990, ET(A) and ET(B), permitted optimization of bosentan, which entered clinical development in 1993, and was offered to patients with pulmonary arterial hypertension in 2001. Bosentan 91-99 endothelin receptor type B Homo sapiens 58-63 20171411-1 2010 BACKGROUND: Bosentan is an endothelin-receptor antagonist that reportedly induces both cytochrome P450 (CYP) 3A4 and CYP2C9 enzymes, which are also involved in warfarin metabolism. Bosentan 12-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-112 20171411-1 2010 BACKGROUND: Bosentan is an endothelin-receptor antagonist that reportedly induces both cytochrome P450 (CYP) 3A4 and CYP2C9 enzymes, which are also involved in warfarin metabolism. Bosentan 12-20 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 117-123 20171411-5 2010 Three weeks after starting bosentan 62.5 mg BID, a therapeutic INR concentration was reached with a weekly warfarin dose 14% higher (an increase of 7.5 mg/wk) than her weekly warfarin dose before initiation of bosentan. Bosentan 27-35 BH3 interacting domain death agonist Homo sapiens 44-47 20171411-7 2010 CONCLUSIONS: Bosentan has CYP3A4- and CYP2C9-inducing properties and is therefore likely to cause decreased concentrations of warfarin. Bosentan 13-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 20171411-7 2010 CONCLUSIONS: Bosentan has CYP3A4- and CYP2C9-inducing properties and is therefore likely to cause decreased concentrations of warfarin. Bosentan 13-21 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 38-44 20646409-14 2010 Comparing with the control group, expression of caspase-3 was prominently enhanced in CSE groups, but both BQ123 and bosentan treatments markedly inhabited the increases of the cleaved caspase-3 protein levels in rats injected with CSE. Bosentan 117-125 caspase 3 Rattus norvegicus 185-194 20646409-17 2010 BQ123 and bosentan significantly prevented the increases of the levels of TNFalpha and IL-1ss in lungs of rats with injection of CSE. Bosentan 10-18 tumor necrosis factor Rattus norvegicus 74-82 19897563-7 2010 Both BQ-123 and bosentan prevented the development of CSE-induced emphysema, blocked the expression of ET(A) receptor, inhibited pulmonary apoptosis, inactivated MMP-2 and MMP-9 activities in the lung tissues, reduced the concentrations of inflammatory cytokines TNF-alpha and IL-1beta, and improved the biological antioxidant activity in the serum. Bosentan 16-24 endothelin receptor type A Rattus norvegicus 103-108 19897563-7 2010 Both BQ-123 and bosentan prevented the development of CSE-induced emphysema, blocked the expression of ET(A) receptor, inhibited pulmonary apoptosis, inactivated MMP-2 and MMP-9 activities in the lung tissues, reduced the concentrations of inflammatory cytokines TNF-alpha and IL-1beta, and improved the biological antioxidant activity in the serum. Bosentan 16-24 matrix metallopeptidase 2 Rattus norvegicus 162-167 19897563-7 2010 Both BQ-123 and bosentan prevented the development of CSE-induced emphysema, blocked the expression of ET(A) receptor, inhibited pulmonary apoptosis, inactivated MMP-2 and MMP-9 activities in the lung tissues, reduced the concentrations of inflammatory cytokines TNF-alpha and IL-1beta, and improved the biological antioxidant activity in the serum. Bosentan 16-24 matrix metallopeptidase 9 Rattus norvegicus 172-177 19897563-7 2010 Both BQ-123 and bosentan prevented the development of CSE-induced emphysema, blocked the expression of ET(A) receptor, inhibited pulmonary apoptosis, inactivated MMP-2 and MMP-9 activities in the lung tissues, reduced the concentrations of inflammatory cytokines TNF-alpha and IL-1beta, and improved the biological antioxidant activity in the serum. Bosentan 16-24 tumor necrosis factor Rattus norvegicus 263-272 19897563-7 2010 Both BQ-123 and bosentan prevented the development of CSE-induced emphysema, blocked the expression of ET(A) receptor, inhibited pulmonary apoptosis, inactivated MMP-2 and MMP-9 activities in the lung tissues, reduced the concentrations of inflammatory cytokines TNF-alpha and IL-1beta, and improved the biological antioxidant activity in the serum. Bosentan 16-24 interleukin 1 beta Rattus norvegicus 277-285 20131241-8 2010 Treatment with bosentan prevented the effects of TGFbeta1. Bosentan 15-23 transforming growth factor beta 1 Homo sapiens 49-57 20131241-11 2010 ET-1 receptor antagonists, such as bosentan, may represent a useful therapeutic tool in the treatment of excessive scarring and fibrosis-related diseases. Bosentan 35-43 endothelin 1 Homo sapiens 0-4 20034342-1 2010 Bosentan is a dual endothelin-1 (ET-1) receptor antagonist that has affinity for ET-1 receptors A and B. Bosentan 0-8 endothelin 1 Homo sapiens 19-31 19829016-7 2010 Treatment with bosentan in SHRs significantly reduced the expression of ET-1 (p < 0.05), and both the ET(A) (p < 0.0001) and ET(B) (p < 0.05) receptor subtypes. Bosentan 15-23 endothelin 1 Rattus norvegicus 72-76 19829016-7 2010 Treatment with bosentan in SHRs significantly reduced the expression of ET-1 (p < 0.05), and both the ET(A) (p < 0.0001) and ET(B) (p < 0.05) receptor subtypes. Bosentan 15-23 endothelin receptor type A Rattus norvegicus 105-110 19829016-7 2010 Treatment with bosentan in SHRs significantly reduced the expression of ET-1 (p < 0.05), and both the ET(A) (p < 0.0001) and ET(B) (p < 0.05) receptor subtypes. Bosentan 15-23 endothelin receptor type B Rattus norvegicus 131-136 19737554-8 2009 However, the non-specific endothelin-1 (ET-1) receptor antagonist Bosentan [10(-5)M] increased dilatation in LPS exposed arteries at 1 and 2h, reaching significance at 4h [14.0+/-3.4%, P<0.05]. Bosentan 66-74 endothelin 1 Rattus norvegicus 26-38 19850966-9 2009 ET-1- and TNFalpha-induced GM-CSF expression were both reduced by bosentan as well as by specific inhibition of either ET(A)R, ET(B)R, p38(MAPK) or ERK-1/-2. Bosentan 66-74 tumor necrosis factor Homo sapiens 10-18 19684201-9 2009 In HV rats, ET receptor antagonism with bosentan resulted in reduced EphA2 mRNA and protein expression (P<0.01). Bosentan 40-48 Eph receptor A2 Rattus norvegicus 69-74 19850966-4 2009 To elucidate the anti-inflammatory properties of the dual endothelin receptor antagonist bosentan that targets both endothelin receptor subtypes A (ET(A)R) and B (ET(B)R), its effect on the TNFalpha/ET-1/GM-CSF network was investigated. Bosentan 89-97 endothelin receptor type A Homo sapiens 148-161 19850966-4 2009 To elucidate the anti-inflammatory properties of the dual endothelin receptor antagonist bosentan that targets both endothelin receptor subtypes A (ET(A)R) and B (ET(B)R), its effect on the TNFalpha/ET-1/GM-CSF network was investigated. Bosentan 89-97 endothelin receptor type B Homo sapiens 163-169 19850966-4 2009 To elucidate the anti-inflammatory properties of the dual endothelin receptor antagonist bosentan that targets both endothelin receptor subtypes A (ET(A)R) and B (ET(B)R), its effect on the TNFalpha/ET-1/GM-CSF network was investigated. Bosentan 89-97 tumor necrosis factor Homo sapiens 190-198 19850966-4 2009 To elucidate the anti-inflammatory properties of the dual endothelin receptor antagonist bosentan that targets both endothelin receptor subtypes A (ET(A)R) and B (ET(B)R), its effect on the TNFalpha/ET-1/GM-CSF network was investigated. Bosentan 89-97 endothelin 1 Homo sapiens 199-203 19850966-4 2009 To elucidate the anti-inflammatory properties of the dual endothelin receptor antagonist bosentan that targets both endothelin receptor subtypes A (ET(A)R) and B (ET(B)R), its effect on the TNFalpha/ET-1/GM-CSF network was investigated. Bosentan 89-97 colony stimulating factor 2 Homo sapiens 204-210 19850966-9 2009 ET-1- and TNFalpha-induced GM-CSF expression were both reduced by bosentan as well as by specific inhibition of either ET(A)R, ET(B)R, p38(MAPK) or ERK-1/-2. Bosentan 66-74 endothelin 1 Homo sapiens 0-4 19850966-9 2009 ET-1- and TNFalpha-induced GM-CSF expression were both reduced by bosentan as well as by specific inhibition of either ET(A)R, ET(B)R, p38(MAPK) or ERK-1/-2. Bosentan 66-74 colony stimulating factor 2 Homo sapiens 27-33 19850966-11 2009 Since bosentan impairs ET-1 autoregulation and TNFalpha-induced ET-1 release, as well as TNFalpha- and ET-1-induced GM-CSF release, the present data suggest therapeutic utility for bosentan in treating particularly the early stages of chronic inflammatory airway diseases. Bosentan 6-14 endothelin 1 Homo sapiens 23-27 19850966-11 2009 Since bosentan impairs ET-1 autoregulation and TNFalpha-induced ET-1 release, as well as TNFalpha- and ET-1-induced GM-CSF release, the present data suggest therapeutic utility for bosentan in treating particularly the early stages of chronic inflammatory airway diseases. Bosentan 6-14 tumor necrosis factor Homo sapiens 47-55 19850966-11 2009 Since bosentan impairs ET-1 autoregulation and TNFalpha-induced ET-1 release, as well as TNFalpha- and ET-1-induced GM-CSF release, the present data suggest therapeutic utility for bosentan in treating particularly the early stages of chronic inflammatory airway diseases. Bosentan 6-14 endothelin 1 Homo sapiens 64-68 19850966-11 2009 Since bosentan impairs ET-1 autoregulation and TNFalpha-induced ET-1 release, as well as TNFalpha- and ET-1-induced GM-CSF release, the present data suggest therapeutic utility for bosentan in treating particularly the early stages of chronic inflammatory airway diseases. Bosentan 6-14 endothelin 1 Homo sapiens 64-68 19737554-8 2009 However, the non-specific endothelin-1 (ET-1) receptor antagonist Bosentan [10(-5)M] increased dilatation in LPS exposed arteries at 1 and 2h, reaching significance at 4h [14.0+/-3.4%, P<0.05]. Bosentan 66-74 endothelin 1 Rattus norvegicus 40-44 19523174-2 2009 Alternative (less expensive) treatments are being sought and bosentan, an oral dual endothelin-1 receptor antagonist, may be an option for the treatment of PPHN. Bosentan 61-69 endothelin receptor type A Homo sapiens 84-105 19106820-9 2009 Endothelin receptors were blocked with bosentan. Bosentan 39-47 endothelin 1 Rattus norvegicus 0-10 19217622-7 2009 Endothelin-1 stimulated an increase in the 6:4 position sulfation ratio on the disaccharides of the GAG chains, an effect that was blocked by bosentan. Bosentan 142-150 endothelin 1 Homo sapiens 0-12 19747014-1 2009 Bosentan (Tracleer) is an orally administered dual endothelin-1 (ET-1) receptor antagonist approved in the EU for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease. Bosentan 0-8 endothelin 1 Homo sapiens 51-63 19302565-0 2009 Low-dose combination therapy of severe digital ulcers in diffuse progressive systemic sclerosis with the endothelin-1 receptor antagonist bosentan and the phosphodiesterase V inhibitor sildenafil. Bosentan 138-146 endothelin receptor type A Homo sapiens 105-126 19575782-11 2009 Increase in bosentan concentration up to 10 microM further inhibited ET-1-induced activation of ERK1/2 and had a stronger inhibitory effect than BQ123 or the combined use of BQ123 and BQ788. Bosentan 12-20 mitogen-activated protein kinase 3 Homo sapiens 96-102 19335744-6 2009 MATERIALS AND METHODS: The Sitaxsentan To Relieve ImpaireD Exercise-2 (STRIDE-2) study followed by STRIDE-2X exposed patients with pulmonary arterial hypertension to the highly selective ET(A) antagonist sitaxsentan (n = 145), or to bosentan (n = 84), a nonselective ET(A) and ET(B) antagonist. Bosentan 233-241 endothelin receptor type A Homo sapiens 187-192 19391127-8 2009 Leptin receptor antagonist (leptin quadruple mutant) and dual endothelin A endothelin B (ETA/ETB) receptor blocker bosentan normalized such abnormalities. Bosentan 115-123 endothelin receptor type A Rattus norvegicus 89-106 19417139-9 2009 Inhibition of the ET-1 receptor ETR-A with bosentan restored the antiproliferative effects of PEP005 in Colo205-R cells and decreased the invasive properties of this cell line. Bosentan 43-51 endothelin 1 Homo sapiens 18-22 19477379-11 2009 In addition, plasma BNP levels significantly decreased from baseline in the higher group compared with those in the lower group after 12-week bosentan administration (-44+/-11% vs. 7+/-20%, p<0.05). Bosentan 142-150 natriuretic peptide B Homo sapiens 20-23 19417139-9 2009 Inhibition of the ET-1 receptor ETR-A with bosentan restored the antiproliferative effects of PEP005 in Colo205-R cells and decreased the invasive properties of this cell line. Bosentan 43-51 endothelin receptor type A Homo sapiens 32-37 19139972-8 2009 Bosentan treatment significantly reduced plasma Ang II levels, while L-158,809 treatment significantly increased vascular ET-1-immunoreactivity in fructose-fed rats. Bosentan 0-8 angiotensinogen Rattus norvegicus 48-54 19081217-5 2009 Unlike bosentan, which is non-selective, inhibiting both ETA and ETB receptors, sodium sitaxentan is highly selective for ETA receptors; this could favor pulmonary vasodilation. Bosentan 7-15 endothelin receptor type A Homo sapiens 57-60 19688101-2 2009 Bosentan is an oral endothelin-1 receptor antagonist (ERA) that has been shown in a large randomized placebo-controlled trial (BREATHE-1) to be effective at improving exercise tolerance in patients with PAH in functional class III and IV. Bosentan 0-8 endothelin receptor type A Homo sapiens 20-41 19791841-1 2009 Bosentan (Tracleer) is an orally administered dual endothelin-1 (ET-1) receptor antagonist approved for use in patients with WHO class II (mildly symptomatic) pulmonary arterial hypertension (PAH). Bosentan 0-8 endothelin 1 Homo sapiens 51-63 19198237-7 2009 After four months of therapy with bosentan, her 6-minute walk distance, estimated pulmonary arterial pressure and brain natriuretic peptide (BNP) improved. Bosentan 34-42 natriuretic peptide B Homo sapiens 114-139 19198237-7 2009 After four months of therapy with bosentan, her 6-minute walk distance, estimated pulmonary arterial pressure and brain natriuretic peptide (BNP) improved. Bosentan 34-42 natriuretic peptide B Homo sapiens 141-144 19049669-8 2008 The NO-independent relaxation was partially restored in bosentan-treated TSK1(+), and this was abolished by a cyclo-oxygenase inhibitor. Bosentan 56-64 testis-specific serine kinase 1 Mus musculus 73-77 19095129-8 2008 A statistically significant treatment effect (TE) of bosentan over placebo on PVR was demonstrated: -24.1% of baseline (95% confidence interval [CI]: -31.5% to -16.0%; p < 0.0001). Bosentan 53-61 PVR cell adhesion molecule Homo sapiens 78-81 18515326-7 2008 Histological analysis showed that ET(A) or ET(B) receptor blockade suppressed zymosan-induced neutrophil accumulation in articular tissue at 6 h. Likewise, dual blockade of ET(A)/ET(B) with bosentan (10 mg/kg, i.v.) Bosentan 190-198 endothelin receptor type A Homo sapiens 34-39 18796317-1 2008 OBJECTIVE: Bosentan, an endothelin (ET) ETA-ETB receptors antagonist, is an effective therapy for idiopathic pulmonary arterial hypertension (PAH) and for PAH related to connective tissue disease (CTD). Bosentan 11-19 CTD Homo sapiens 197-200 18796317-15 2008 Bosentan therapy seems to elicit different patterns in ET-1 and BNP plasma levels, with decrease of the peptides only in patients with higher activation of the systemic endothelin system. Bosentan 0-8 natriuretic peptide B Homo sapiens 64-67 18951296-2 2008 Endothelin-1 may underlie the pathogenesis of lung fibrosis, therefore it was hypothesized that the oral dual endothelin receptor antagonist bosentan may have efficacy for the treatment of IPF. Bosentan 141-149 endothelin 1 Homo sapiens 0-12 18855258-8 2008 Endothelial NOS (eNOS) expression increased in the Lean with bosentan. Bosentan 61-69 nitric oxide synthase 3 Rattus norvegicus 0-15 18694375-3 2008 OBJECTIVE: To evaluate the role of the endothelin-1 (ET-1) pathway in IPF pathogenesis and the effects of therapeutic targeting with bosentan, an ET-1 antagonist. Bosentan 133-141 endothelin 1 Homo sapiens 146-150 18515326-7 2008 Histological analysis showed that ET(A) or ET(B) receptor blockade suppressed zymosan-induced neutrophil accumulation in articular tissue at 6 h. Likewise, dual blockade of ET(A)/ET(B) with bosentan (10 mg/kg, i.v.) Bosentan 190-198 endothelin receptor type A Homo sapiens 173-178 18029384-9 2008 CD3-L-selectin T cells were significantly lower in SSc-PAH at baseline than in HD or SSc and rose to normal levels after bosentan therapy. Bosentan 121-129 selectin L Homo sapiens 4-14 18788437-10 2008 Epoprostenol administration along with bosentan resulted in decrease of BNP and right ventricular function improvement. Bosentan 39-47 natriuretic peptide B Homo sapiens 72-75 18178727-1 2008 The objective of this study was to investigate the effect a nonselective endothelin-1 (ET-1) receptor antagonist (bosentan) had on the acute myocardial remodeling process including left ventricular (LV) mast cells and matrix metalloproteinase (MMP) activity secondary to volume overload. Bosentan 114-122 endothelin 1 Rattus norvegicus 73-85 18470553-2 2008 Endothelin (ET)-1 is elevated in SCD and appears to play a key role in many of the pathologic processes in this disease, including PH, suggesting that endothelin receptor antagonists such as bosentan may be effective in treating patients with SCD, particularly those with PH. Bosentan 191-199 endothelin 1 Homo sapiens 0-17 18243424-7 2008 Two ET-1 receptor antagonists, orally active, can be used: bosentan (ET(A)/ET(B)=20) is nonselective and sitaxentan (ET(A)/ET(B)=6500) is highly selective. Bosentan 59-67 endothelin 1 Homo sapiens 4-8 18305126-3 2008 Tadalafil is mainly metabolized by cytochrome P450 (CYP) 3A4, and as bosentan induces CYP2C9 and CYP3A4, a pharmacokinetic interaction is possible between these agents. Bosentan 69-77 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 86-92 18305126-3 2008 Tadalafil is mainly metabolized by cytochrome P450 (CYP) 3A4, and as bosentan induces CYP2C9 and CYP3A4, a pharmacokinetic interaction is possible between these agents. Bosentan 69-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 18536629-5 2008 The endothelin-1 receptor antagonist bosentan, the phosphodiesterase-5 inhibitor sildenafil, and prostanoids have been shown to improve symptoms, exercise capacity and haemodynamics. Bosentan 37-45 endothelin receptor type A Homo sapiens 4-25 18322086-5 2008 Infusion of the pan-ET-receptor (ET-R) antagonist Bosentan or the selective ET(B)-R antagonist BQ788 into the corpus callosum prevented postlesion astrocyte proliferation and JNK phosphorylation. Bosentan 50-58 mitogen-activated protein kinase 8 Homo sapiens 175-178 18178727-1 2008 The objective of this study was to investigate the effect a nonselective endothelin-1 (ET-1) receptor antagonist (bosentan) had on the acute myocardial remodeling process including left ventricular (LV) mast cells and matrix metalloproteinase (MMP) activity secondary to volume overload. Bosentan 114-122 endothelin 1 Rattus norvegicus 87-91 18178727-5 2008 Additionally, the substantial increase in MMP-2 activation in the untreated fistula at 1 day was prevented following bosentan treatment (1.6 +/- 0.3 vs. 0.9 +/- 0.1 arbitrary activity units, Fist vs. Fist + Bos, P <or= 0.01). Bosentan 117-125 matrix metallopeptidase 2 Rattus norvegicus 42-47 18783297-9 2008 Using this equation, the ICCYP3A4 was calculated for seven inducers (bosentan, carbamazepine, efavirenz, phenytoin, pioglitazone, rifampicin [rifampin], and St John"s wort [hypericum]) on the basis of the reduction in the AUC of a coadministered standard substrate of CYP3A4, such as simvastatin, in ten DDI studies. Bosentan 69-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 17604287-7 2008 Elevation of CCL2 serum levels in the lcSSc subset was not associated with pulmonary arterial hypertension, although there was a trend for reduction following treatment with prostacyclin analogues or bosentan. Bosentan 200-208 C-C motif chemokine ligand 2 Homo sapiens 13-17 17919123-4 2008 Perfusate ET-1 (endothelin-1) increased transiently during EPO infusion, and the ET(A/)ET(B) antagonist bosentan abolished the inotropic response to EPO. Bosentan 104-112 erythropoietin Rattus norvegicus 149-152 17919123-5 2008 BNP (B-type natriuretic peptide) secretion (28+/-8%; P<0.05) and nuclear transcription factor GATA-4 DNA-binding activity (51%; P<0.05) were both significantly increased by EPO and blocked by bosentan. Bosentan 198-206 natriuretic peptide B Rattus norvegicus 0-3 17919123-5 2008 BNP (B-type natriuretic peptide) secretion (28+/-8%; P<0.05) and nuclear transcription factor GATA-4 DNA-binding activity (51%; P<0.05) were both significantly increased by EPO and blocked by bosentan. Bosentan 198-206 GATA binding protein 4 Rattus norvegicus 97-103 18390125-7 2008 Bosentan, an oral non-specific endothelin-receptor antagonist with dual activity on both ETA and ETB receptors, has been shown to improve the patient"s quality of life on the overall. Bosentan 0-8 endothelin receptor type A Homo sapiens 89-92 18295521-8 2008 Inhibition of ETB receptors in LPS-stimulated monocytes by bosentan was responded with suppression of PGE2 and increased production of leukotrienes indicating strong effects in the cyclooxygenase pathway that is known to control cellular ET transcription. Bosentan 59-67 endothelin receptor type B Homo sapiens 14-17 17496208-0 2007 Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Bosentan 0-8 solute carrier organic anion transporter family member 1B1 Homo sapiens 33-40 18295521-3 2008 The objective of this study was to further elucidate the pro-inflammatory effects of ET-1 on ETB receptors in cultured human monocytes (10(5)/20 h) compared with non-specific stimulation with LPS in vitro and to define the antagonizing effects of bosentan, a dual ETA/ETB-receptor antagonist, on inflammatory mediator production. Bosentan 247-255 endothelin 1 Homo sapiens 85-89 18295521-7 2008 ETB-receptor antagonism attenuated ET- and LPS-responses in monocytes, in particular of TNF-alpha and PGE2 to a similar extend (40%) that were only demonstrable following LPS at therapeutic plasma concentrations of bosentan and had no effect on IL-1 beta. Bosentan 215-223 endothelin receptor type B Homo sapiens 0-3 18612919-6 2008 Treatment with Bosentan resulted in a significantly lower expression of PGIS mRNA compared to Ambrisentan and MCT only (7 % versus 18 %, p = 0.003 and 7 % versus 17 %, p = 0.004). Bosentan 15-23 prostaglandin I2 synthase Rattus norvegicus 72-76 18612919-9 2008 CONCLUSIONS: Treatment with Bosentan leads to lower PGIS expression in pulmonary arteries compared to Ambrisentan, although the greater PGIS expression by Ambrisentan treatment had no benefical effect on pulmonary haemodynamics. Bosentan 28-36 prostaglandin I2 synthase Rattus norvegicus 52-56 17663518-3 2007 Bosentan, a dual ET (A/B)-receptor antagonist, was used to inhibit the binding of endothelin-1 and its receptors and cut down its biological role. Bosentan 0-8 endothelin 1 Homo sapiens 82-94 17974986-12 2007 Moreover, bosentan pretreatment resulted in reduced tumor necrosis factor-alpha content, lipid peroxidation, and Bax expression, as well as increased GATA-4 expression. Bosentan 10-18 tumor necrosis factor Mus musculus 52-79 17974986-12 2007 Moreover, bosentan pretreatment resulted in reduced tumor necrosis factor-alpha content, lipid peroxidation, and Bax expression, as well as increased GATA-4 expression. Bosentan 10-18 BCL2-associated X protein Mus musculus 113-116 17974986-12 2007 Moreover, bosentan pretreatment resulted in reduced tumor necrosis factor-alpha content, lipid peroxidation, and Bax expression, as well as increased GATA-4 expression. Bosentan 10-18 GATA binding protein 4 Mus musculus 150-156 17911460-6 2007 Bosentan, the first oral endothelin receptor antagonist (with affinity for endothelin A and B receptors) improves exercise function and survival in PAH, both primary and secondary to autoimmune rheumatic diseases. Bosentan 0-8 endothelin receptor type B Homo sapiens 75-103 17496208-0 2007 Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Bosentan 0-8 solute carrier organic anion transporter family member 1B3 Homo sapiens 45-52 17496208-1 2007 The elimination process of the endothelin receptor antagonist bosentan (Tracleer) in humans is entirely dependent on metabolism mediated by two cytochrome P450 (P450) enzymes, i.e., CYP3A4 and CYP2C9. Bosentan 62-70 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 193-199 17496208-5 2007 Bosentan uptake into Chinese hamster ovary cells expressing these OATP transporters was efficiently inhibited by cyclosporin A and rifampicin with IC(50) values significantly below their effective plasma concentrations in humans. Bosentan 0-8 solute carrier organic anion transporter family member 1A2 Homo sapiens 66-70 17334537-10 2007 In vitro, pre-incubation with ET-1 (0.1 microM) 4 h before infection enhanced the uptake of the parasites by peritoneal macrophages, and this effect was abrogated when macrophages were pre-treated with bosentan (1 microM) 15 min before incubation with ET-1. Bosentan 202-210 endothelin 1 Mus musculus 30-34 17341678-10 2007 Treatment of mice with bosentan (endothelin-1 receptor antagonist) normalized the coronary perfusion pressure, demonstrating that the elevated endothelin-1 release was sufficient to account for the increased coronary perfusion pressure. Bosentan 23-31 endothelin receptor type A Mus musculus 33-54 17374746-0 2007 Differential inhibition of rat and human Na+-dependent taurocholate cotransporting polypeptide (NTCP/SLC10A1)by bosentan: a mechanism for species differences in hepatotoxicity. Bosentan 112-120 solute carrier family 10 member 1 Homo sapiens 96-100 17374746-0 2007 Differential inhibition of rat and human Na+-dependent taurocholate cotransporting polypeptide (NTCP/SLC10A1)by bosentan: a mechanism for species differences in hepatotoxicity. Bosentan 112-120 solute carrier family 10 member 1 Homo sapiens 101-108 17374746-1 2007 Bile acid accumulation in hepatocytes due to inhibition of the canalicular bile salt export pump (BSEP/ABCB11) has been proposed as a mechanism for bosentan-induced hepatotoxicity. Bosentan 148-156 ATP binding cassette subfamily B member 11 Rattus norvegicus 98-102 17374746-1 2007 Bile acid accumulation in hepatocytes due to inhibition of the canalicular bile salt export pump (BSEP/ABCB11) has been proposed as a mechanism for bosentan-induced hepatotoxicity. Bosentan 148-156 ATP binding cassette subfamily B member 11 Rattus norvegicus 103-109 17374746-2 2007 The observation that bosentan does not induce hepatotoxicity in rats, although bosentan has been reported to inhibit rat Bsep and cause elevated serum bile acids, challenges this mechanism. Bosentan 79-87 ATP binding cassette subfamily B member 11 Rattus norvegicus 121-125 17374746-5 2007 In addition, bosentan was a more potent inhibitor of taurocholate uptake by rat Na(+)-dependent taurocholate co-transporting polypeptide (Ntcp/Slc10a1) (IC(50) 0.71 microM) than human NTCP (SLC10A1) (IC(50) 24 microM) expressed in HEK293 cells. Bosentan 13-21 solute carrier family 10 member 1 Rattus norvegicus 138-142 17374746-5 2007 In addition, bosentan was a more potent inhibitor of taurocholate uptake by rat Na(+)-dependent taurocholate co-transporting polypeptide (Ntcp/Slc10a1) (IC(50) 0.71 microM) than human NTCP (SLC10A1) (IC(50) 24 microM) expressed in HEK293 cells. Bosentan 13-21 solute carrier family 10 member 1 Rattus norvegicus 143-150 17374746-5 2007 In addition, bosentan was a more potent inhibitor of taurocholate uptake by rat Na(+)-dependent taurocholate co-transporting polypeptide (Ntcp/Slc10a1) (IC(50) 0.71 microM) than human NTCP (SLC10A1) (IC(50) 24 microM) expressed in HEK293 cells. Bosentan 13-21 solute carrier family 10 member 1 Homo sapiens 184-188 17374746-5 2007 In addition, bosentan was a more potent inhibitor of taurocholate uptake by rat Na(+)-dependent taurocholate co-transporting polypeptide (Ntcp/Slc10a1) (IC(50) 0.71 microM) than human NTCP (SLC10A1) (IC(50) 24 microM) expressed in HEK293 cells. Bosentan 13-21 solute carrier family 10 member 1 Homo sapiens 190-197 17374746-6 2007 Thus, bosentan is a more potent inhibitor of Ntcp than NTCP, and this should result in less intrahepatocyte accumulation of bile acids in rats during bosentan treatment. Bosentan 6-14 solute carrier family 10 member 1 Rattus norvegicus 45-49 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Rattus norvegicus 55-59 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Rattus norvegicus 81-85 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Homo sapiens 107-111 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Rattus norvegicus 119-123 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Rattus norvegicus 119-123 17374746-8 2007 The mode of bosentan inhibition was noncompetitive for Ntcp, and competitive for NTCP (K(i) 18 microM) and NTCP(1-140)/Ntcp(141-362) (K(i) 1.7 microM); bosentan affected both the K(m) and V(max) of Ntcp(1-140)/NTCP(141-349) (K(i) 7.0 microM). Bosentan 12-20 solute carrier family 10 member 1 Rattus norvegicus 107-111 17374746-10 2007 In conclusion, differential inhibition of Ntcp and NTCP may represent a novel mechanism for species differences in bosentan-induced hepatotoxicity. Bosentan 115-123 solute carrier family 10 member 1 Rattus norvegicus 42-46 17374746-10 2007 In conclusion, differential inhibition of Ntcp and NTCP may represent a novel mechanism for species differences in bosentan-induced hepatotoxicity. Bosentan 115-123 solute carrier family 10 member 1 Rattus norvegicus 51-55 17603693-0 2007 [Treatment of digital ulcers in systemtic sclerosis with endothelin-1 receptor antagonist (bosentan)]. Bosentan 91-99 endothelin receptor type A Homo sapiens 57-78 17612651-3 2007 We have previously shown that chronic treatment with either the dual endothelin receptor blocker, bosentan, or the thromboxane synthase inhibitor, dazmegrel, prevented fructose-induced increases in blood pressure, suggesting that both ET-1 and TXA2 play important roles in the development of hyperinsulinemia/insulin resistance-associated hypertension. Bosentan 98-106 endothelin 1 Rattus norvegicus 235-239 17612651-9 2007 Protein expression of cyclooxygenase 2 (COX2) was elevated significantly in FHR aortas and treatment with bosentan and dazmegrel corrected these changes. Bosentan 106-114 prostaglandin-endoperoxide synthase 2 Rattus norvegicus 22-38 17612651-9 2007 Protein expression of cyclooxygenase 2 (COX2) was elevated significantly in FHR aortas and treatment with bosentan and dazmegrel corrected these changes. Bosentan 106-114 prostaglandin-endoperoxide synthase 2 Rattus norvegicus 40-44 17612651-11 2007 Bosentan may prevent the development of hypertension in fructose-fed rats through inhibition of COX2 induction and subsequently the reduction in plasma TXA2. Bosentan 0-8 prostaglandin-endoperoxide synthase 2 Rattus norvegicus 96-100 17322637-0 2007 Effect of bosentan on plasma endothelin-1 concentration in patients with pulmonary arterial hypertension. Bosentan 10-18 endothelin 1 Homo sapiens 29-41 17194566-3 2007 In naive mice, the intraplantar injection of IL-18 induced dose- and time-dependent mechanical hypernociception, which was inhibited in IFN-gamma deficient (-/-) mice, and by the pre-treatment with bosentan (dual endothelin [ET] receptor antagonist), BQ123 (ET(A) receptor antagonist) or indomethacin (cyclooxygenase inhibitor). Bosentan 198-206 interleukin 18 Mus musculus 45-50 17024690-6 2007 Treatment of cells with ET antagonist bosentan and NHE-1 inhibitor cariporide prevented glucose-induced cardiomyocyte hypertrophy and expression of ANP, Agt, and iNOS. Bosentan 38-46 angiotensinogen Rattus norvegicus 153-156 17024690-6 2007 Treatment of cells with ET antagonist bosentan and NHE-1 inhibitor cariporide prevented glucose-induced cardiomyocyte hypertrophy and expression of ANP, Agt, and iNOS. Bosentan 38-46 nitric oxide synthase 2 Rattus norvegicus 162-166 17341678-10 2007 Treatment of mice with bosentan (endothelin-1 receptor antagonist) normalized the coronary perfusion pressure, demonstrating that the elevated endothelin-1 release was sufficient to account for the increased coronary perfusion pressure. Bosentan 23-31 endothelin 1 Mus musculus 33-45 17563825-1 2007 We present a case of the successful use of bosentan for increased pulmonary vascular resistance (PVR) in a 10-year-old male who underwent late single ventricle surgical palliation for double-inlet left ventricle with pulmonary artery banding and a bidirectional Glenn shunt. Bosentan 43-51 PVR cell adhesion molecule Homo sapiens 97-100 17563825-4 2007 Bosentan is a relatively new oral therapy option for increased PVR in patients with single ventricle physiology and bidirectional Glenn shunts. Bosentan 0-8 PVR cell adhesion molecule Homo sapiens 63-66 17494952-8 2007 The incidence of PCNA expression was significantly (P < 0.05) reduced in bosentan-treated animals. Bosentan 76-84 proliferating cell nuclear antigen Rattus norvegicus 17-21 17457488-14 2007 Cyclooxygenase-2 inhibitors caused ulcer in the presence of bosentan. Bosentan 60-68 prostaglandin-endoperoxide synthase 2 Rattus norvegicus 0-16 17188849-5 2007 A mixed ET(A/B) receptor antagonist bosentan attenuated the BNP gene expression response to load by 58% (P<0.005). Bosentan 36-44 endothelin receptor type B Mus musculus 8-14 17188849-5 2007 A mixed ET(A/B) receptor antagonist bosentan attenuated the BNP gene expression response to load by 58% (P<0.005). Bosentan 36-44 natriuretic peptide type B Mus musculus 60-63 17334537-10 2007 In vitro, pre-incubation with ET-1 (0.1 microM) 4 h before infection enhanced the uptake of the parasites by peritoneal macrophages, and this effect was abrogated when macrophages were pre-treated with bosentan (1 microM) 15 min before incubation with ET-1. Bosentan 202-210 endothelin 1 Mus musculus 252-256 17767746-4 2007 Although a relationship between raised levels of ET-1 and clinical phenotype is yet to be identified, early evidence from studies of ET-1 blockade with drugs such as bosentan is encouraging. Bosentan 166-174 endothelin 1 Homo sapiens 133-137 17251982-4 2007 In vitro experiments were performed to investigate the effect of rifampin on the uptake of bosentan into Chinese hamster ovary cells expressing the human organic anion-transporting polypeptide (OATP)1B1, -1B3, and -2B1. Bosentan 91-99 solute carrier organic anion transporter family member 1B1 Homo sapiens 154-218 17251982-7 2007 Rifampin potently inhibited the uptake of bosentan into cells expressing human OATP1B1 and -1B3. Bosentan 42-50 solute carrier organic anion transporter family member 1B1 Homo sapiens 79-95 17234519-1 2007 BACKGROUND: Bosentan, an oral ET(A)/ET(B) receptor antagonist, is approved for the treatment of pulmonary arterial hypertension (PAH). Bosentan 12-20 endothelin receptor type A Homo sapiens 30-35 17061295-4 2007 The adenosine 5"-triphosphate (ATP)-dependent uptake of (3)H-taurocholic acid into membrane vesicles for BSEP/Bsep was inhibited by bosentan, and its IC(50) values were 76.8 and 101 microM for BSEP and Bsep, respectively. Bosentan 132-140 ATP binding cassette subfamily B member 11 Rattus norvegicus 105-109 17061295-4 2007 The adenosine 5"-triphosphate (ATP)-dependent uptake of (3)H-taurocholic acid into membrane vesicles for BSEP/Bsep was inhibited by bosentan, and its IC(50) values were 76.8 and 101 microM for BSEP and Bsep, respectively. Bosentan 132-140 ATP binding cassette subfamily B member 11 Rattus norvegicus 110-114 17061295-4 2007 The adenosine 5"-triphosphate (ATP)-dependent uptake of (3)H-taurocholic acid into membrane vesicles for BSEP/Bsep was inhibited by bosentan, and its IC(50) values were 76.8 and 101 microM for BSEP and Bsep, respectively. Bosentan 132-140 ATP binding cassette subfamily B member 11 Rattus norvegicus 193-197 17061295-4 2007 The adenosine 5"-triphosphate (ATP)-dependent uptake of (3)H-taurocholic acid into membrane vesicles for BSEP/Bsep was inhibited by bosentan, and its IC(50) values were 76.8 and 101 microM for BSEP and Bsep, respectively. Bosentan 132-140 ATP binding cassette subfamily B member 11 Rattus norvegicus 202-206 17061295-5 2007 In contrast, bosentan stimulated the MRP2/Mrp2-mediated ATP-dependent vesicular transport of (3)H-estradiol 17beta-glucuronide by shifting the sigmoidal dependence of transport rate on substrate concentration to a more hyperbolic one. Bosentan 13-21 ATP binding cassette subfamily C member 2 Rattus norvegicus 37-41 17061295-5 2007 In contrast, bosentan stimulated the MRP2/Mrp2-mediated ATP-dependent vesicular transport of (3)H-estradiol 17beta-glucuronide by shifting the sigmoidal dependence of transport rate on substrate concentration to a more hyperbolic one. Bosentan 13-21 ATP binding cassette subfamily C member 2 Rattus norvegicus 42-46 17061295-6 2007 Collectively, these results suggest that bosentan inhibits BSEP in humans with a similar potency to rats, and that increased bile salt-independent flow in rats by bosentan is at least partly attributable to the activation of Mrp2. Bosentan 163-171 ATP binding cassette subfamily C member 2 Rattus norvegicus 225-229 17061295-0 2007 Effects of bosentan, an endothelin receptor antagonist, on bile salt export pump and multidrug resistance-associated protein 2. Bosentan 11-19 ATP binding cassette subfamily B member 11 Rattus norvegicus 59-80 17061295-0 2007 Effects of bosentan, an endothelin receptor antagonist, on bile salt export pump and multidrug resistance-associated protein 2. Bosentan 11-19 ATP binding cassette subfamily C member 2 Rattus norvegicus 85-126 17061295-2 2007 It has been reported that bosentan, an endothelin receptor antagonist, inhibits Bsep, which may lead to cholestatic liver injury due to the intracellular accumulation of bile salts, while increasing bile salt-independent bile flow. Bosentan 26-34 ATP binding cassette subfamily B member 11 Rattus norvegicus 80-84 17439935-2 2007 This study aimed to examine the long-term effects of bosentan, a dual endothelin-1 receptor antagonist, on symptomatology, haemodynamics and quality of life measures in SLE patients with symptomatic PAH. Bosentan 53-61 endothelin receptor type A Homo sapiens 70-91 17053380-12 2006 Agents such as the endothelin-1 receptor antagonist bosentan, the phosphodiesterase-5 inhibitor sildenafil, and the prostanoids have been shown to improve symptoms, exercise capacity, and, in most instances, delay clinical worsening. Bosentan 52-60 endothelin receptor type A Homo sapiens 19-40 17901934-9 2007 Two patients had ALT/AST elevations >3x normal limit, requiring bosentan-dose reduction or discontinuation (one case each). Bosentan 67-75 solute carrier family 17 member 5 Homo sapiens 21-24 16807127-1 2006 Male heterozygous Ren-2 transgenic rats and Hannover Sprague-Dawley rats fed a normal or high-salt diet were either untreated or treated with the nonselective receptor ET(A)/ET(B) receptor blocker bosentan or the selective ET(A) receptor blocker, ABT-627, known as atrasentan. Bosentan 197-205 endothelin receptor type A Rattus norvegicus 168-173 17097496-9 2006 The beneficial effects of bosentan and ramipril, alone or in combination, were associated with reduced mRNA levels of transforming growth factor (TGF)-beta1 and platelet-derived growth factor (PDGF)-A in the tracheal allografts. Bosentan 26-34 transforming growth factor, beta 1 Rattus norvegicus 118-156 16919005-4 2006 The oral dual endothelin (ET(A)/ET(B)) antagonist bosentan has been shown to improve exercise capacity, time to clinical worsening, haemodynamics and quality of life in short-term studies. Bosentan 50-58 endothelin receptor type A Homo sapiens 26-31 16919005-4 2006 The oral dual endothelin (ET(A)/ET(B)) antagonist bosentan has been shown to improve exercise capacity, time to clinical worsening, haemodynamics and quality of life in short-term studies. Bosentan 50-58 endothelin receptor type B Homo sapiens 32-37 16919016-6 2006 In the eight bosentan-treated patients, TIMP-1 and TIMP-2 levels did not change during 1 year of treatment, while bosentan increased the 6-min walking distance by 136 meters after 1 year, as well as clinical outcomes. Bosentan 13-21 TIMP metallopeptidase inhibitor 1 Homo sapiens 40-46 16919016-6 2006 In the eight bosentan-treated patients, TIMP-1 and TIMP-2 levels did not change during 1 year of treatment, while bosentan increased the 6-min walking distance by 136 meters after 1 year, as well as clinical outcomes. Bosentan 13-21 TIMP metallopeptidase inhibitor 2 Homo sapiens 51-57 16757538-9 2006 In perfused kidneys of rats exposed to gentamicin (100 mg/kg) for seven consecutive days, an increase in Mrp2 function and expression was found, which was prevented by addition of a dual endothelin-receptor antagonist, bosentan. Bosentan 219-227 ATP binding cassette subfamily C member 2 Rattus norvegicus 105-109 16793845-3 2006 OBJECTIVE: To present a subgroup analysis that summarises experiences from the pivotal studies and their open-label extensions with the oral dual endothelin-1 receptor antagonist bosentan in patients with PAH and CTD, mostly SSc and lupus erythematosus. Bosentan 179-187 endothelin receptor type A Homo sapiens 146-167 16793845-3 2006 OBJECTIVE: To present a subgroup analysis that summarises experiences from the pivotal studies and their open-label extensions with the oral dual endothelin-1 receptor antagonist bosentan in patients with PAH and CTD, mostly SSc and lupus erythematosus. Bosentan 179-187 CTD Homo sapiens 213-216 16793845-7 2006 RESULTS: 44 patients with PAH secondary to CTD who were treated with bosentan were stable in 6-min walk distance at the end of the study (+19.5 m, 95% confidence interval (CI) -3.2 to 42.2), whereas patients treated with placebo deteriorated (-2.6 m, 95% CI -54.0 to 48.7). Bosentan 69-77 CTD Homo sapiens 43-46 16793845-12 2006 CONCLUSION: Short-term bosentan treatment in a subgroup of patients with PAH secondary to CTD seems to have a favourable effect compared with placebo. Bosentan 23-31 CTD Homo sapiens 90-93 17111027-8 2006 Immunohistochemical analyses in diabetic SMA revealed an increase in ETA receptor level that was normalized by chronic bosentan treatment. Bosentan 119-127 endothelin receptor type A Rattus norvegicus 69-72 16906041-13 2006 Treatment of allograft recipient rats with bosentan prevented upregulation of ED-B FN and TGF-beta1. Bosentan 43-51 transforming growth factor, beta 1 Rattus norvegicus 90-99 17111027-1 2006 Increased vasoconstrictor response to norepinephrine (NE) and endothelin (ET)-1 in arteries from diabetic animals is ameliorated by chronic endothelin receptor blockade with bosentan and was absent in endothelium-denuded arteries, suggesting the involvement of ET-1 and an endothelium-derived contracting factor such as thromboxane A2 (TxA2). Bosentan 174-182 endothelin 1 Rattus norvegicus 62-79 16820593-15 2006 ET-1 antagonism with bosentan stimulates translocation of PKClambda and leads to increased PKC activity and NO production. Bosentan 21-29 endothelin 1 Homo sapiens 0-4 17111027-1 2006 Increased vasoconstrictor response to norepinephrine (NE) and endothelin (ET)-1 in arteries from diabetic animals is ameliorated by chronic endothelin receptor blockade with bosentan and was absent in endothelium-denuded arteries, suggesting the involvement of ET-1 and an endothelium-derived contracting factor such as thromboxane A2 (TxA2). Bosentan 174-182 endothelin 1 Rattus norvegicus 62-72 16877428-2 2006 METHODS: In benchtop experiments, ET-1 was acutely injected into the vitreous of control and 5- to 7-day bosentan-treated nondiabetic rats. Bosentan 105-113 endothelin 1 Rattus norvegicus 34-38 16877428-6 2006 RESULTS: ET-1 produced a significant (P < 0.05) reduction in retinal arterial diameter that was suppressed (P > 0.05) in rats fed bosentan chow admix. Bosentan 136-144 endothelin 1 Rattus norvegicus 9-13 16820593-15 2006 ET-1 antagonism with bosentan stimulates translocation of PKClambda and leads to increased PKC activity and NO production. Bosentan 21-29 proline rich transmembrane protein 2 Homo sapiens 58-61 16809784-7 2006 Fibrotic lung fibroblasts display constitutive JNK activation, which was reduced by the dual ETA/ETB receptor inhibitor, bosentan, providing evidence of an autocrine endothelin loop. Bosentan 121-129 mitogen-activated protein kinase 8 Homo sapiens 47-50 16866076-1 2006 Therapy with the endothelin-1 receptor antagonist bosentan]. Bosentan 50-58 endothelin receptor type A Homo sapiens 17-38 16866076-3 2006 The endothelin-1 receptor antagonist bosentan inhibits the action of endothelin-1 at both receptor subtypes (ET(A) and ET(B) receptors) and has been approved for PAH therapy since 2001. Bosentan 37-45 endothelin receptor type A Homo sapiens 4-25 16866076-3 2006 The endothelin-1 receptor antagonist bosentan inhibits the action of endothelin-1 at both receptor subtypes (ET(A) and ET(B) receptors) and has been approved for PAH therapy since 2001. Bosentan 37-45 endothelin 1 Homo sapiens 4-16 16809784-7 2006 Fibrotic lung fibroblasts display constitutive JNK activation, which was reduced by the dual ETA/ETB receptor inhibitor, bosentan, providing evidence of an autocrine endothelin loop. Bosentan 121-129 endothelin receptor type A Homo sapiens 93-96 16563629-8 2006 Bosentan (dual ET(A)/ET(B) receptor antagonist, 10 mg/kg, i.v.) Bosentan 0-8 endothelin receptor type A Rattus norvegicus 15-20 16563629-8 2006 Bosentan (dual ET(A)/ET(B) receptor antagonist, 10 mg/kg, i.v.) Bosentan 0-8 endothelin receptor type B Rattus norvegicus 21-26 16741059-7 2006 Bosentan potentiated Fas ligand-induced apoptosis only in one melanoma cell line. Bosentan 0-8 Fas ligand Homo sapiens 21-31 16766656-5 2006 IL-15-induced hypernociception was inhibited by treatment with a dual endothelin receptor type A (ET(A))/endothelin receptor type B (ET(B)) antagonist (bosentan), ET(A) receptor antagonist (BQ123), or cyclooxygenase inhibitor (indomethacin). Bosentan 152-160 interleukin 15 Mus musculus 0-5 16766656-5 2006 IL-15-induced hypernociception was inhibited by treatment with a dual endothelin receptor type A (ET(A))/endothelin receptor type B (ET(B)) antagonist (bosentan), ET(A) receptor antagonist (BQ123), or cyclooxygenase inhibitor (indomethacin). Bosentan 152-160 endothelin receptor type B Mus musculus 133-138 16741032-9 2006 Bosentan, but not sildenafil, decreased norepinephrine and BNP plasma concentrations, reduced kidney weight, and normalized systemic hemodynamics. Bosentan 0-8 natriuretic peptide B Rattus norvegicus 59-62 16741042-8 2006 Diabetes increased FN and ED-B FN in all three organs, which was prevented by ET antagonist bosentan. Bosentan 92-100 fibronectin 1 Homo sapiens 26-30 16802735-2 2006 Bosentan, an inhibitor of endothelin A and B receptors, is a new molecule previously validated in the treatment of primary pulmonary hypertension. Bosentan 0-8 endothelin receptor type B Homo sapiens 26-54 16219361-4 2006 The first dual ETA/ETB receptor blocker, bosentan, has already been approved by the Food and Drug Administration for the treatment of pulmonary arterial hypertension (PAH). Bosentan 41-49 endothelin receptor type A Homo sapiens 15-18 16219361-4 2006 The first dual ETA/ETB receptor blocker, bosentan, has already been approved by the Food and Drug Administration for the treatment of pulmonary arterial hypertension (PAH). Bosentan 41-49 endothelin receptor type B Homo sapiens 19-22 16775506-6 2006 Bosentan, a dual ETA/B receptor antagonist, and BQ788 (ETB receptor antagonist) treatment resulted in a 1.6-fold and 1.3-fold increase, respectively in luciferase activity as compared with the untreated control. Bosentan 0-8 endothelin receptor type A Bos taurus 17-20 16775506-8 2006 Transgenic mice that express the luciferase gene under the control of PPE-1 promoter were treated with Bosentan. Bosentan 103-111 endothelin 1 Bos taurus 70-75 16775506-9 2006 Luciferase activity, PPE-1 mRNA levels, and plasma immunoreactive ET-1 levels were increased by 1.6-fold to 2.0-fold in the Bosentan-treated group compared with the untreated, control group. Bosentan 124-132 endothelin 1 Bos taurus 21-26 16516557-7 2006 The implication of ET-1 receptors on both endothelial and smooth muscle cells is confirmed by the significant reduced sensitivity to ET-1 in the four groups when bosentan is present in organ bath. Bosentan 162-170 endothelin 1 Rattus norvegicus 19-23 16516557-7 2006 The implication of ET-1 receptors on both endothelial and smooth muscle cells is confirmed by the significant reduced sensitivity to ET-1 in the four groups when bosentan is present in organ bath. Bosentan 162-170 endothelin 1 Rattus norvegicus 133-137 16431896-2 2006 Recently, it was shown that blocking the signal from the endothelin-1 (ET-1) receptor (ET(A)R/ET(B)R) by a non-selective receptor antagonist, bosentan, reduced parathyroid cell proliferation, parathyroid gland hyperplasia and parathyroid hormone (PTH) levels in normal rats on a calcium deficient diet. Bosentan 142-150 endothelin 1 Rattus norvegicus 57-69 16431896-2 2006 Recently, it was shown that blocking the signal from the endothelin-1 (ET-1) receptor (ET(A)R/ET(B)R) by a non-selective receptor antagonist, bosentan, reduced parathyroid cell proliferation, parathyroid gland hyperplasia and parathyroid hormone (PTH) levels in normal rats on a calcium deficient diet. Bosentan 142-150 endothelin 1 Rattus norvegicus 71-75 16431896-2 2006 Recently, it was shown that blocking the signal from the endothelin-1 (ET-1) receptor (ET(A)R/ET(B)R) by a non-selective receptor antagonist, bosentan, reduced parathyroid cell proliferation, parathyroid gland hyperplasia and parathyroid hormone (PTH) levels in normal rats on a calcium deficient diet. Bosentan 142-150 endothelin receptor type B Rattus norvegicus 94-100 16431896-2 2006 Recently, it was shown that blocking the signal from the endothelin-1 (ET-1) receptor (ET(A)R/ET(B)R) by a non-selective receptor antagonist, bosentan, reduced parathyroid cell proliferation, parathyroid gland hyperplasia and parathyroid hormone (PTH) levels in normal rats on a calcium deficient diet. Bosentan 142-150 parathyroid hormone Rattus norvegicus 247-250 16431896-3 2006 Our goal was to determine whether in 5/6 nephrectomized (NPX) rats with developing or established hyperparathyroidism, the endothelin receptor blocker, bosentan, reduced the increase in parathyroid cell proliferation, parathyroid gland hyperplasia and PTH values. Bosentan 152-160 parathyroid hormone Rattus norvegicus 252-255 16431896-13 2006 RESULTS: In the study of developing hyperparathyroidism, bosentan reduced ET-1 expression in the parathyroid glands of rats on the NPD and HPD (P<0.05). Bosentan 57-65 endothelin 1 Rattus norvegicus 74-78 16431896-15 2006 In the study of established hyperparathyroidism, in which 5/6 NPX rats were given a HPD for 15 days, bosentan started on day 15 reduced (P<0.05) ET-1 expression in rats maintained for 15 additional days on the HPD or the VLPD. Bosentan 101-109 endothelin 1 Rattus norvegicus 148-152 16431896-18 2006 PTH values were lowest in the VLPD group, intermediate in the NPD group, and highest in the HPD group, but in none of the three groups did bosentan decrease PTH values. Bosentan 139-147 parathyroid hormone Rattus norvegicus 157-160 16676248-14 2006 Myeloperoxidase activity in adhesion tissue was significantly higher in bosentan group. Bosentan 72-80 myeloperoxidase Rattus norvegicus 0-15 16614599-1 2006 OBJECTIVES: To describe the effect of bosentan and its dual inhibition of endothelin-1 ETA and ETB receptors on digital ulcers in patients with systemic sclerosis (SSc). Bosentan 38-46 endothelin 1 Homo sapiens 74-86 16550733-1 2006 OBJECTIVE: Bosentan has been shown in vitro and in vivo to induce the cytochrome P450 enzymes CYP2C9 and CYP3A4. Bosentan 11-19 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 94-100 16550733-1 2006 OBJECTIVE: Bosentan has been shown in vitro and in vivo to induce the cytochrome P450 enzymes CYP2C9 and CYP3A4. Bosentan 11-19 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 16932638-2 2005 Bosentan, an antagonist with dual specificity for the endothelin-receptor subtypes A and B, has been shown to be efficacious and well tolerated in placebo-controlled clinical trials and is now approved in many countries, including the US, Canada, and Europe, for treatment of pulmonary arterial hypertension (PAH), including PAH associated with rheumatic diseases. Bosentan 0-8 endothelin receptor type A Homo sapiens 54-90 16040626-9 2005 ET receptor blockade with bosentan prevented this increase in lung VEGF content, suggesting that ET promotes VEGF accumulation in the lung in this setting. Bosentan 26-34 vascular endothelial growth factor A Rattus norvegicus 67-71 16040626-9 2005 ET receptor blockade with bosentan prevented this increase in lung VEGF content, suggesting that ET promotes VEGF accumulation in the lung in this setting. Bosentan 26-34 vascular endothelial growth factor A Rattus norvegicus 109-113 16601312-8 2006 ET(A/)ET(B) receptor inhibition with bosentan during NO synthase inhibition in the renal denervated rats did not produce changes in urine flow rate or electrolyte excretion. Bosentan 37-45 endothelin receptor type A Rattus norvegicus 0-20 16552365-0 2006 Inhibition of endothelin-1-mediated up-regulation of iNOS by bosentan ameliorates endotoxin-induced liver injury in cirrhosis. Bosentan 61-69 endothelin 1 Rattus norvegicus 14-26 16552365-0 2006 Inhibition of endothelin-1-mediated up-regulation of iNOS by bosentan ameliorates endotoxin-induced liver injury in cirrhosis. Bosentan 61-69 nitric oxide synthase 2 Rattus norvegicus 53-57 16552365-11 2006 Bosentan significantly inhibited the up-regulations of ET-1, iNOS, and COX-2 mRNA. Bosentan 0-8 endothelin 1 Rattus norvegicus 55-59 16552365-11 2006 Bosentan significantly inhibited the up-regulations of ET-1, iNOS, and COX-2 mRNA. Bosentan 0-8 nitric oxide synthase 2 Rattus norvegicus 61-65 16552365-11 2006 Bosentan significantly inhibited the up-regulations of ET-1, iNOS, and COX-2 mRNA. Bosentan 0-8 cytochrome c oxidase II, mitochondrial Rattus norvegicus 71-76 16311906-7 2005 The goal of the present study was to determine whether chronic treatment of diabetic rats with bosentan influences the activation of specific PKC isoforms in SMA from diabetic rats. Bosentan 95-103 protein kinase C, gamma Rattus norvegicus 142-145 16236895-5 2005 RESULTS: After 3 months of treatment with bosentan, PVR decreased from 914 +/- 329 to 611 +/- 220 dyne.s.cm(-5) (p < 0.001). Bosentan 42-50 PVR cell adhesion molecule Homo sapiens 52-55 16236930-1 2005 BACKGROUND: Bosentan, an oral endothelin (ET)-A/ET-B receptor antagonist, is effective in the treatment of pulmonary arterial hypertension. Bosentan 12-20 endothelin receptor type A Homo sapiens 30-47 16248783-5 2005 However, to date the only prescribed ET-1 antagonist is bosentan for pulmonary arterial hypertension. Bosentan 56-64 endothelin 1 Homo sapiens 37-41 16248783-6 2005 Bosentan is a "dual" ET-1 antagonist (i.e. it acts on both ET(A) and ET(B) receptors). Bosentan 0-8 endothelin 1 Homo sapiens 21-25 15870840-0 2005 Endothelin A and B receptor antagonist bosentan reduces postischemic myocardial injury in the rat: critical timing of administration. Bosentan 39-47 endothelin receptor type A Rattus norvegicus 0-27 16100158-8 2005 INTERVENTIONS: Combination therapy with bosentan (final dosage, 125 mg bid) was initiated following an interval of 3-months minimum of unchanged prostanoid therapy. Bosentan 40-48 BH3 interacting domain death agonist Homo sapiens 71-74 16013984-3 2005 Bosentan (Tracleer, Actelion Pharmaceuticals), an oral ETA/ETB receptor antagonist, has been shown to improve exercise capacity, quality of life, haemodynamics and time to clinical worsening of patients with PAH in short-term placebo-controlled trials. Bosentan 0-8 endothelin receptor type A Homo sapiens 55-58 16093917-9 2005 Bosentan decreased MMP-2 (78.9 +/- 3.8 versus 117.4 +/- 12.2 AU; P = 0.014) and proMMP-2 activity (P < 0.006) in the senescent SHR group. Bosentan 0-8 matrix metallopeptidase 2 Rattus norvegicus 19-24 16093917-13 2005 However, bosentan decreased pro and active MMP-2 activity in senescent SHR rats, indicating that ET modulates late events in vascular remodelling in hypertension. Bosentan 9-17 matrix metallopeptidase 2 Rattus norvegicus 43-48 15640287-7 2005 Exposing type II pneumocytes to endothelin-1 receptor antagonists PD-156707 or bosentan before exposure to SNAP partially prevented the decrease in surfactant protein gene expression. Bosentan 79-87 endothelin receptor type A Homo sapiens 32-53 15610070-0 2005 The endothelin-1 receptor antagonist bosentan protects against ischaemia/reperfusion-induced endothelial dysfunction in humans. Bosentan 37-45 endothelin receptor type A Homo sapiens 4-25 15610070-11 2005 The vaso-constrictor response induced by intra-arterial infusion of ET-1 was attenuated significantly by bosentan (P<0.001). Bosentan 105-113 endothelin 1 Homo sapiens 68-72 16231952-4 2005 These measures were taken for the oral dual endothelin ET(A)/ET(B) antagonist bosentan (Tracleer). Bosentan 78-86 endothelin receptor type B Homo sapiens 61-66 15811199-0 2005 The effect of bosentan on matrix metalloproteinase-9 levels in patients with systemic sclerosis-induced pulmonary hypertension. Bosentan 14-22 matrix metallopeptidase 9 Homo sapiens 26-52 15811199-6 2005 Recently, a dual inhibitor of endothelin-1, bosentan, has been successfully evaluated in clinical trials in PAH patients. Bosentan 44-52 endothelin 1 Homo sapiens 30-42 15811199-7 2005 RESEARCH DESIGN AND METHOD: The aim of this study is to investigate the expression of MMP-2 and MMP-9 in the serum of different subsets of SSc patients, and in patients treated with bosentan. Bosentan 182-190 matrix metallopeptidase 2 Homo sapiens 86-91 15811199-7 2005 RESEARCH DESIGN AND METHOD: The aim of this study is to investigate the expression of MMP-2 and MMP-9 in the serum of different subsets of SSc patients, and in patients treated with bosentan. Bosentan 182-190 matrix metallopeptidase 9 Homo sapiens 96-101 15811199-14 2005 Moreover, in bosentan-treated patients, after 12 months of therapy MMP-9 significantly (p < 0.05) increased and correlated with an improved clinical outcome, as measured by the "6-minutes walking" test. Bosentan 13-21 matrix metallopeptidase 9 Homo sapiens 67-72 15811199-15 2005 CONCLUSIONS: This is the first time that MMP-9 serum levels are reported to be down-regulated in PAH patients and up-regulated following bosentan treatment. Bosentan 137-145 matrix metallopeptidase 9 Homo sapiens 41-46 15353403-7 2005 Bosentan, a dual-ET receptor antagonist, blocked the increase in THAL eNOS expression caused by high salt (2.66 +/- 0.44 absorbance units with bosentan vs. 5.15 +/- 0.67 for vehicle; P < 0.05). Bosentan 0-8 nitric oxide synthase 2 Homo sapiens 65-74 15353403-7 2005 Bosentan, a dual-ET receptor antagonist, blocked the increase in THAL eNOS expression caused by high salt (2.66 +/- 0.44 absorbance units with bosentan vs. 5.15 +/- 0.67 for vehicle; P < 0.05). Bosentan 143-151 nitric oxide synthase 2 Homo sapiens 65-74 15902842-3 2005 Bosentan is an orally active, dual endothelin receptor antagonist, which competitively antagonizes the binding of endothelin to both endothelin receptors ETA and ETB. Bosentan 0-8 endothelin receptor type A Homo sapiens 154-157 15902842-3 2005 Bosentan is an orally active, dual endothelin receptor antagonist, which competitively antagonizes the binding of endothelin to both endothelin receptors ETA and ETB. Bosentan 0-8 endothelin receptor type B Homo sapiens 162-165 15902842-6 2005 The anti-fibrotic effects of bosentan extend to fibrosis induced by mediators other than endothelin such as transforming growth factor-beta, angiotensin II and aldosterone, indicating a central role of endothelin and endothelin receptors in fibrotic processes. Bosentan 29-37 angiotensinogen Homo sapiens 141-155 15633133-2 2005 Endothelin-1, a potent vasoconstrictor, is likely to play a role in the pathogenesis of primary pulmonary hypertension, and, in 2 recent trials, the dual endothelin receptor antagonist bosentan has shown beneficial effects in this disease. Bosentan 185-193 endothelin 1 Homo sapiens 0-12 15591146-3 2005 Pretreatments with Bosentan, a dual ET(A)/ET(B) receptor antagonist, or cyclooxygenase (COX) inhibitor blocked the luteolytic action of ET-1 but not that induced by prostaglandin F2alpha (PGF2alpha). Bosentan 19-27 endothelin-1 Oryctolagus cuniculus 136-140 15583218-7 2005 Acute HGF infusion into rats caused a decline in blood pressure that was enhanced by pretreatment with bosentan (an endothelin A and B receptor antagonist). Bosentan 103-111 hepatocyte growth factor Rattus norvegicus 6-9 15583218-8 2005 HGF infusion also resulted in a decline in glomerular filtration rate (GFR) that could be entirely prevented by bosentan, suggesting that HGF acutely increases production and/or release of ET-1, which then mediates the observed decline in GFR. Bosentan 112-120 hepatocyte growth factor Rattus norvegicus 0-3 15583218-8 2005 HGF infusion also resulted in a decline in glomerular filtration rate (GFR) that could be entirely prevented by bosentan, suggesting that HGF acutely increases production and/or release of ET-1, which then mediates the observed decline in GFR. Bosentan 112-120 hepatocyte growth factor Rattus norvegicus 138-141 15583218-8 2005 HGF infusion also resulted in a decline in glomerular filtration rate (GFR) that could be entirely prevented by bosentan, suggesting that HGF acutely increases production and/or release of ET-1, which then mediates the observed decline in GFR. Bosentan 112-120 endothelin 1 Rattus norvegicus 189-193 15317671-5 2004 In PASMCs, endothelin-1 (1 microM) and PDGF (10 ng/ml) both upregulated protein expression of TRPC6, whereas bosentan markedly downregulated TRPC6 protein levels. Bosentan 109-117 transient receptor potential cation channel subfamily C member 6 Homo sapiens 141-146 15497138-6 2004 The gene expression pattern of IRX1b is altered in silent heart genetic mutant embryos and in embryos treated with the endothelin receptor antagonist bosentan. Bosentan 150-158 iroquois homeobox 1b Danio rerio 31-36 15465654-1 2004 Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile. Bosentan 14-22 ATP binding cassette subfamily B member 11 Rattus norvegicus 53-74 15465654-1 2004 Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile. Bosentan 14-22 ATP binding cassette subfamily B member 11 Rattus norvegicus 76-80 15317671-4 2004 Bosentan (20-50 microM) significantly inhibited endothelin-1- or platelet-derived growth factor (PDGF)-mediated PASMC growth and [3H]thymidine uptake. Bosentan 0-8 endothelin 1 Homo sapiens 48-60 15317671-7 2004 These observations demonstrate that the antiproliferative effect of bosentan on PASMCs involves the downregulation of TRPC6 channels via a mechanism possibly independent of endothelin receptor blockade. Bosentan 68-76 transient receptor potential cation channel subfamily C member 6 Homo sapiens 118-123 15317671-8 2004 The greater effect of bosentan on IPAH-PASMCs than on normal PASMCs suggests that increased TRPC6 expression and function may be involved in the overgrowth of PASMCs in patients with IPAH. Bosentan 22-30 transient receptor potential cation channel subfamily C member 6 Homo sapiens 92-97 15246919-1 2004 Bosentan, an endothelin-1 antagonist that can be administered orally, has been shown to be effective in the treatment of idiopathic pulmonary arterial hypertension and may be of benefit to patients with the Eisenmenger syndrome. Bosentan 0-8 endothelin 1 Homo sapiens 13-25 15448709-11 2004 Our data demonstrates that high glucose-induced upregulation of FN messenger RNA and protein levels occur via activation of MAPK/ERK pathway, which was prevented by treatment of cells with bosentan, PD098059 and PKC blocker chelerythrine. Bosentan 189-197 fibronectin 1 Homo sapiens 64-66 15448709-11 2004 Our data demonstrates that high glucose-induced upregulation of FN messenger RNA and protein levels occur via activation of MAPK/ERK pathway, which was prevented by treatment of cells with bosentan, PD098059 and PKC blocker chelerythrine. Bosentan 189-197 mitogen-activated protein kinase 1 Homo sapiens 124-128 15448709-11 2004 Our data demonstrates that high glucose-induced upregulation of FN messenger RNA and protein levels occur via activation of MAPK/ERK pathway, which was prevented by treatment of cells with bosentan, PD098059 and PKC blocker chelerythrine. Bosentan 189-197 mitogen-activated protein kinase 1 Homo sapiens 129-132 15838329-3 2004 The inhibitory dissociation constant values of YM598, atrasentan and bosentan were 0.772, 0.0551 and 4.75 nM, respectively, for native human ETA receptors, and 143, 4.80 and 40.9 nM, respectively, for native human ETB subtypes. Bosentan 69-77 endothelin receptor type A Homo sapiens 141-144 15838329-3 2004 The inhibitory dissociation constant values of YM598, atrasentan and bosentan were 0.772, 0.0551 and 4.75 nM, respectively, for native human ETA receptors, and 143, 4.80 and 40.9 nM, respectively, for native human ETB subtypes. Bosentan 69-77 endothelin receptor type B Homo sapiens 214-217 15838329-4 2004 The calculated selectivity ratios of YM598, atrasentan and bosentan for ETA versus ETB receptors were 222, 136 and 13.0, respectively. Bosentan 59-67 endothelin receptor type A Homo sapiens 72-75 15838329-4 2004 The calculated selectivity ratios of YM598, atrasentan and bosentan for ETA versus ETB receptors were 222, 136 and 13.0, respectively. Bosentan 59-67 endothelin receptor type B Homo sapiens 83-86 15363992-3 2004 Ki values of YM598, atrasentan, and bosentan for native human endothelin ETA receptors were 0.772, 0.0551, and 4.75 nM, while those for native human endothelin ETB receptors were 143, 4.80, and 40.9 nM, respectively. Bosentan 36-44 endothelin receptor type A Homo sapiens 73-76 15363992-4 2004 The calculated selectivity ratios of YM598, atrasentan, and bosentan for endothelin ETA versus ETB receptors were 185, 87 and 8.6, respectively. Bosentan 60-68 endothelin receptor type A Homo sapiens 84-87 15334381-1 2004 Recent studies in our laboratory have demonstrated that bosentan, a mixed endothelin ET(A)/ET(B) receptor antagonist, prevented the upregulation of the arginine vasopressin (AVP) V(2) receptor in the inner medullary collecting duct (IMCD) of cardiomyopathic hamsters. Bosentan 56-64 endothelin receptor type B Rattus norvegicus 91-96 15063187-9 2004 Furthermore, bosentan, a pharmacological inhibitor of Endothelin-1 signaling caused a loss of I56i-lacZ expression in the most distal aspects of the expression domain, corresponding to the area of Dlx-6 expression previously shown to be under the control of Endothelin-1. Bosentan 13-21 endothelin 1 Homo sapiens 54-66 15180799-9 2004 The combined ET(A)/ET(B) antagonist Bosentan powerfully prevented the ET-1-induced decrease in G(aw) but did not alter its reduction in perfusion flow. Bosentan 36-44 endothelin receptor type A Rattus norvegicus 13-18 15180799-9 2004 The combined ET(A)/ET(B) antagonist Bosentan powerfully prevented the ET-1-induced decrease in G(aw) but did not alter its reduction in perfusion flow. Bosentan 36-44 endothelin receptor type B Rattus norvegicus 19-24 15180799-9 2004 The combined ET(A)/ET(B) antagonist Bosentan powerfully prevented the ET-1-induced decrease in G(aw) but did not alter its reduction in perfusion flow. Bosentan 36-44 endothelin 1 Rattus norvegicus 70-74 14693683-13 2004 In conclusion, the dual ETA/ETB receptor antagonist bosentan preserved endothelial and cardiac contractile function during ischemia and reperfusion via a mechanism dependent on endothelial NO production. Bosentan 52-60 endothelin receptor type A Rattus norvegicus 24-27 15093706-4 2004 Pretreatment with bosentan (ET-A and ET-B receptor antagonist), ET-B receptor antagonist BQ-788 or ET-A receptor antagonist BQ-485 completely inhibited the ET-3-induced decrease in the SMA blood flow. Bosentan 18-26 endothelin receptor type A Rattus norvegicus 28-32 15084165-5 2004 Inhibition of ET-1 action by a nonselective ET-1 receptor antagonist, bosentan, significantly decreased tracheal occlusion, which was linked to delayed epithelial necrosis, suppressed smooth muscle cell proliferation, and a marked reduction in the number of interleukin-1beta and interleukin-2 immunoreactive cells. Bosentan 70-78 endothelin 1 Rattus norvegicus 14-18 15084165-5 2004 Inhibition of ET-1 action by a nonselective ET-1 receptor antagonist, bosentan, significantly decreased tracheal occlusion, which was linked to delayed epithelial necrosis, suppressed smooth muscle cell proliferation, and a marked reduction in the number of interleukin-1beta and interleukin-2 immunoreactive cells. Bosentan 70-78 endothelin 1 Rattus norvegicus 44-48 15084165-5 2004 Inhibition of ET-1 action by a nonselective ET-1 receptor antagonist, bosentan, significantly decreased tracheal occlusion, which was linked to delayed epithelial necrosis, suppressed smooth muscle cell proliferation, and a marked reduction in the number of interleukin-1beta and interleukin-2 immunoreactive cells. Bosentan 70-78 interleukin 1 beta Rattus norvegicus 258-275 15084165-5 2004 Inhibition of ET-1 action by a nonselective ET-1 receptor antagonist, bosentan, significantly decreased tracheal occlusion, which was linked to delayed epithelial necrosis, suppressed smooth muscle cell proliferation, and a marked reduction in the number of interleukin-1beta and interleukin-2 immunoreactive cells. Bosentan 70-78 interleukin 2 Rattus norvegicus 280-293 15063187-9 2004 Furthermore, bosentan, a pharmacological inhibitor of Endothelin-1 signaling caused a loss of I56i-lacZ expression in the most distal aspects of the expression domain, corresponding to the area of Dlx-6 expression previously shown to be under the control of Endothelin-1. Bosentan 13-21 distal-less homeobox 6 Homo sapiens 197-202 15063187-9 2004 Furthermore, bosentan, a pharmacological inhibitor of Endothelin-1 signaling caused a loss of I56i-lacZ expression in the most distal aspects of the expression domain, corresponding to the area of Dlx-6 expression previously shown to be under the control of Endothelin-1. Bosentan 13-21 endothelin 1 Homo sapiens 258-270 15049280-8 2004 epoprostenol, nebulized iloprost, oral beraprost and oral bosentan, a dual endothelin-1 receptor antagonist. Bosentan 58-66 endothelin receptor type A Homo sapiens 75-96 14617681-4 2004 All known members of the organic anion transporting polypeptide (oatp) transport protein family expressed in rat liver, i.e., oatp1, oatp2, and oatp4, were shown to be involved in the uptake of bosentan. Bosentan 194-202 solute carrier organic anion transporter family, member 1a1 Rattus norvegicus 126-131 14617681-4 2004 All known members of the organic anion transporting polypeptide (oatp) transport protein family expressed in rat liver, i.e., oatp1, oatp2, and oatp4, were shown to be involved in the uptake of bosentan. Bosentan 194-202 solute carrier organic anion transporter family, member 1a4 Rattus norvegicus 133-138 14617681-4 2004 All known members of the organic anion transporting polypeptide (oatp) transport protein family expressed in rat liver, i.e., oatp1, oatp2, and oatp4, were shown to be involved in the uptake of bosentan. Bosentan 194-202 solute carrier organic anion transporter family member 1B2 Rattus norvegicus 144-149 14736539-9 2004 Bosentan, an orally active, dual ET-1 receptor antagonist has been shown to improve symptoms, exercise capacity, hemodynamics, echocardiographic parameters and the outcome of patients with severe PAH, and it has been approved for clinical use in many countries. Bosentan 0-8 endothelin 1 Homo sapiens 33-37 15568889-15 2004 Ketoconazole approximately doubles the exposure to bosentan because of inhibition of CYP3A4. Bosentan 51-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 15568889-16 2004 Bosentan decreases exposure to ciclosporin, glibenclamide, simvastatin (and beta-hydroxyacid simvastatin) and (R)- and (S)-warfarin by up to 50% because of induction of CYP3A4 and/or CYP2C9. Bosentan 0-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 15568889-16 2004 Bosentan decreases exposure to ciclosporin, glibenclamide, simvastatin (and beta-hydroxyacid simvastatin) and (R)- and (S)-warfarin by up to 50% because of induction of CYP3A4 and/or CYP2C9. Bosentan 0-8 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 183-189 15568889-20 2004 The possibility of reduced efficacy of CYP2C9 and 3A4 substrates should be considered when coadministered with bosentan. Bosentan 111-119 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 39-45 15568889-22 2004 In healthy subjects, bosentan doses >300 mg increase plasma levels of endothelin-1. Bosentan 21-29 endothelin 1 Homo sapiens 73-85 14748289-5 2004 Several clinical studies have revealed that ET-1 antagonists are clinically beneficial therapeutic agents for the treatment of several cardiovascular diseases, leading to the approval of bosentan (ETA/ETB antagonist) for the treatment of pulmonary hypertension. Bosentan 187-195 endothelin receptor type A Homo sapiens 197-200 14748289-5 2004 Several clinical studies have revealed that ET-1 antagonists are clinically beneficial therapeutic agents for the treatment of several cardiovascular diseases, leading to the approval of bosentan (ETA/ETB antagonist) for the treatment of pulmonary hypertension. Bosentan 187-195 endothelin receptor type B Homo sapiens 201-204 14615287-9 2003 Bosentan, an endothelin (ET) receptor antagonist, reduced Ang II-increased ICaT density without affecting the amount of CaV3.1 mRNA. Bosentan 0-8 angiotensinogen Rattus norvegicus 58-64 14638626-6 2004 In the SHR but not in the NWR the contralateral carotid was also depolarized, and this was prevented by the endothelin A/B receptor antagonist bosentan. Bosentan 143-151 endothelin receptor type A Rattus norvegicus 108-131 15658881-9 2004 The US FDA has approved a number of novel treatments, including long-acting oral ET-1 receptor antagonists such as bosentan and short-acting parenteral prostacyclin analogs, such as epoprostenol, for PAH. Bosentan 115-123 endothelin 1 Homo sapiens 81-85 15588125-6 2004 The survival rates in male and in female heterozygous TGR on the HS diet were 46 % and 80 %, respectively, and were significantly improved by administration of bosentan to 76 % and 97 %, respectively. Bosentan 160-168 thioredoxin reductase 3 Mus musculus 54-57 15588125-8 2004 Administration of bosentan in heterozygous TGR fed the HS diet markedly reduced proteinuria, glomerulosclerosis and attenuated the development of cardiac hypertrophy compared with untreated TGR. Bosentan 18-26 thioredoxin reductase 3 Mus musculus 43-46 14615287-10 2003 Finally, cotreatment with bosentan and UO126 abolished the Ang II-increased ICaT density. Bosentan 26-34 angiotensinogen Rattus norvegicus 59-65 14506620-3 2003 The goal of the present studies was to determine if ET-1 is involved in upregulating the expression of AVP V2 mRNA in the IMCD of CM by using a mixed ETA/ETB receptor antagonist bosentan. Bosentan 178-186 endothelin 1 Homo sapiens 52-56 14639097-9 2003 The statistical analysis of the results demonstrates that Bosentan has prevented the increase in urinary protein excretion and that of renal immunoreactive collagen I, fibronectin, and TGFbeta induced by diabetes without reducing blood pressure. Bosentan 58-66 fibronectin 1 Rattus norvegicus 168-179 14639097-9 2003 The statistical analysis of the results demonstrates that Bosentan has prevented the increase in urinary protein excretion and that of renal immunoreactive collagen I, fibronectin, and TGFbeta induced by diabetes without reducing blood pressure. Bosentan 58-66 transforming growth factor, beta 1 Rattus norvegicus 185-192 14506620-8 2003 The effect of bosentan in normalizing the expression of AVP V2 and AQP2 mRNA in the IMCD of CM was confirmed by in situ hybridization studies. Bosentan 14-22 aquaporin 2 Homo sapiens 67-71 14506620-0 2003 Attenuation of renal vasopressin V2 receptor upregulation by bosentan, an ETA/ETB receptor antagonist. Bosentan 61-69 arginine vasopressin receptor 2 Homo sapiens 21-44 14506620-0 2003 Attenuation of renal vasopressin V2 receptor upregulation by bosentan, an ETA/ETB receptor antagonist. Bosentan 61-69 endothelin receptor type A Homo sapiens 74-77 14506620-10 2003 This study demonstrated that AVP V2 and AQP2 mRNA are upregulated in CM hamsters and these upregulations are attenuated by bosentan treatment, suggesting that ET-1 plays a role in upregulating the expression of AVP V2 mRNA in CM hamsters. Bosentan 123-131 aquaporin 2 Homo sapiens 40-44 14506620-0 2003 Attenuation of renal vasopressin V2 receptor upregulation by bosentan, an ETA/ETB receptor antagonist. Bosentan 61-69 endothelin receptor type B Homo sapiens 78-81 14506620-10 2003 This study demonstrated that AVP V2 and AQP2 mRNA are upregulated in CM hamsters and these upregulations are attenuated by bosentan treatment, suggesting that ET-1 plays a role in upregulating the expression of AVP V2 mRNA in CM hamsters. Bosentan 123-131 endothelin 1 Homo sapiens 159-163 12686474-9 2003 On the other hand, bosentan and BQ788 caused a reduction in the numbers of endothelin-1-secreting cells. Bosentan 19-27 endothelin 1 Homo sapiens 75-87 14567928-0 2003 Effect of endothelin receptor antagonist bosentan on plasma leptin concentration in acute myocardial infarction in rats. Bosentan 41-49 leptin Rattus norvegicus 60-66 14567928-14 2003 Our results indicate that bosentan has an important effect on leptin concentration in ischemic cardiovascular pathology. Bosentan 26-34 leptin Rattus norvegicus 62-68 12841819-7 2003 Bosentan is an inducer of the isoenzymes CYP3A4 and 2C9. Bosentan 0-8 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-55 12853530-3 2003 DESIGN: The present study was an open-label extension to the preceding double-blind, placebo-controlled study of 32 patients with PAH (primary or associated with scleroderma) who received bosentan or placebo at 125 mg bid for 3 to 7 months. Bosentan 188-196 BH3 interacting domain death agonist Homo sapiens 218-221 12582013-5 2003 Increased FN expression was shown to be dependent on ET receptor-mediated signaling, as the increase was prevented by the dual ET receptor antagonist bosentan. Bosentan 150-158 fibronectin 1 Homo sapiens 10-12 14612185-10 2003 However, calcium content, 45Ca(2+) uptake and ALP activity in VDN plus bosentan group was 33, 36.7, and 40.4% lower than those in VDN group. Bosentan 71-79 alkaline phosphatase, placental Homo sapiens 46-49 12734647-6 2003 INTERVENTIONS: Nine pretreated dogs received an infusion of the endothelin A and B receptor antagonist bosentan (10 mg/kg) started before oleic acid. Bosentan 103-111 endothelin receptor type A Canis lupus familiaris 64-91 12686474-11 2003 The receptor antagonists, bosentan and BQ788, inhibited basal secretion of endothelin-1. Bosentan 26-34 endothelin 1 Homo sapiens 75-87 12887768-8 2003 The mRNA expressions of ColI, TGF-beta1 and TIMP-1 in renal tissue subjected to ureter ligation were significantly lower in the bosentan group then in the animal model group (all P < 0.05). Bosentan 128-136 transforming growth factor, beta 1 Rattus norvegicus 30-39 12887768-8 2003 The mRNA expressions of ColI, TGF-beta1 and TIMP-1 in renal tissue subjected to ureter ligation were significantly lower in the bosentan group then in the animal model group (all P < 0.05). Bosentan 128-136 TIMP metallopeptidase inhibitor 1 Rattus norvegicus 44-50 12887768-9 2003 The positive staining areas of ColI, TGF-beta1 and TIMP-1 in the tubulointerstitium were significantly smaller in bosentan group than in the animal model group (all P < 0.05). Bosentan 114-122 transforming growth factor, beta 1 Rattus norvegicus 37-46 12887768-9 2003 The positive staining areas of ColI, TGF-beta1 and TIMP-1 in the tubulointerstitium were significantly smaller in bosentan group than in the animal model group (all P < 0.05). Bosentan 114-122 TIMP metallopeptidase inhibitor 1 Rattus norvegicus 51-57 12628956-10 2003 CONCLUSIONS: Experimental overcirculation-induced pulmonary arterial hypertension appears to be causally related to an activation of the pulmonary ET-1 system and as such is completely prevented by the dual endothelin receptor antagonist bosentan. Bosentan 238-246 endothelin 1 Homo sapiens 147-151 12617929-1 2003 A series of compounds structurally related to bosentan 1 featuring an unsaturated side chain at position 6 of the core pyrimidine have been studied for their potential to block the ET(A) and ET(B) receptor. Bosentan 46-54 endothelin receptor type A Rattus norvegicus 181-186 12713683-7 2003 In addition, bosentan is not only a substrate but also an inducer of CYP3A4 and CYP2C9. Bosentan 13-21 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 80-86 12659977-11 2003 Clinical trials are underway examining the role of endothelin-1 receptor antagonists like bosentan in the prevention of graft atherosclerosis. Bosentan 90-98 endothelin receptor type A Homo sapiens 51-72 12547713-6 2003 Co-treatment with Bosentan abolished the actions of ET-1. Bosentan 18-26 endothelin 1 Homo sapiens 52-56 12631050-2 2003 We tested the hypothesis that the mixed endothelin-1 receptor antagonist bosentan would modify or prevent indomethacin-induced reduction of CBF in the anaesthetized pig. Bosentan 73-81 endothelin receptor type A Sus scrofa 40-61 12603176-1 2003 BACKGROUND: In vitro, bosentan has been shown to be a mild inducer of cytochrome P450 (CYP) 2C9 and 3A4. Bosentan 22-30 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 70-95 12616854-8 2003 Therapeutic treatment of patients suffering from the above-mentioned cardiovascular diseases with ET-receptor antagonists have also been taking place, and bosentan (ETA/ETB antagonist) was recently approved by the FDA as a formal therapeutic drug for pulmonary hypertension. Bosentan 155-163 endothelin receptor type A Homo sapiens 165-168 12616854-8 2003 Therapeutic treatment of patients suffering from the above-mentioned cardiovascular diseases with ET-receptor antagonists have also been taking place, and bosentan (ETA/ETB antagonist) was recently approved by the FDA as a formal therapeutic drug for pulmonary hypertension. Bosentan 155-163 endothelin receptor type B Homo sapiens 169-172 12509808-5 2003 Infusion of ET-1 induced a hypertrophy of ET(B)R/GFAP-IR astrocytes in the normal optic nerve, with no additional hypertrophy in the crushed nerve, whereas infusion of Bosentan induced a significant decrease in the hypertrophy of ET(B)R/GFAP-IR astrocytes in the crushed but not in the normal optic nerve. Bosentan 168-176 endothelin receptor type B Homo sapiens 230-236 12509808-5 2003 Infusion of ET-1 induced a hypertrophy of ET(B)R/GFAP-IR astrocytes in the normal optic nerve, with no additional hypertrophy in the crushed nerve, whereas infusion of Bosentan induced a significant decrease in the hypertrophy of ET(B)R/GFAP-IR astrocytes in the crushed but not in the normal optic nerve. Bosentan 168-176 glial fibrillary acidic protein Homo sapiens 237-241 12603176-9 2003 CONCLUSIONS: Concomitant treatment with bosentan reduces the exposure to simvastatin and beta-hydroxyacid simvastatin by approximately 40%, indicating that in vivo bosentan is also a mild inducer of CYP3A4. Bosentan 40-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 199-205 12603176-2 2003 PURPOSE: To investigate in vivo the mutual pharmacokinetic interactions between bosentan and simvastatin, a CYP3A4 substrate. Bosentan 80-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-114 12450064-0 2002 Exaggerated coronary reactivity to endothelin-1 in diabetes: reversal with bosentan. Bosentan 75-83 endothelin 1 Rattus norvegicus 35-47 12468266-2 2002 Group 1 was pre-treated only with lipopolysaccharide (LPS), group 2 was treated with lepirudin, a thrombin inhibitor, group 3 was pre-treated with bosentan, a dual inhibitor of ET-1 receptors. Bosentan 147-155 endothelin-1 Sus scrofa 177-181 12450064-1 2002 We previously demonstrated that chronic endothelin receptor blockade (with bosentan) improved functional cardiac performance in streptozotocin-diabetic rats, suggesting a novel role of endothelin-1 (ET-1) in modulating diabetic heart dysfunction. Bosentan 75-83 endothelin 1 Rattus norvegicus 199-203 12270740-3 2002 The aim of this study was to investigate the role of endothelin-1 (ET-1) in a cirrhotic rat model with endotoxin induced renal failure by mixed ET-1 receptor antagonist, bosentan. Bosentan 170-178 endothelin 1 Rattus norvegicus 53-65 12270740-3 2002 The aim of this study was to investigate the role of endothelin-1 (ET-1) in a cirrhotic rat model with endotoxin induced renal failure by mixed ET-1 receptor antagonist, bosentan. Bosentan 170-178 endothelin 1 Rattus norvegicus 67-71 12379507-9 2002 The endothelin ET-A/ET-B receptor antagonist, bosentan, the ET-B receptor antagonist, BQ-788, and anti-ET-1 serum decreased the percentage of endothelial cells that secreted adrenomedullin and CNP relative to control. Bosentan 46-54 adrenomedullin Homo sapiens 174-188 12379507-9 2002 The endothelin ET-A/ET-B receptor antagonist, bosentan, the ET-B receptor antagonist, BQ-788, and anti-ET-1 serum decreased the percentage of endothelial cells that secreted adrenomedullin and CNP relative to control. Bosentan 46-54 natriuretic peptide C Homo sapiens 193-196 12127422-0 2002 Contribution of mrp2 in alterations of canalicular bile formation by the endothelin antagonist bosentan. Bosentan 95-103 ATP binding cassette subfamily C member 2 Rattus norvegicus 16-20 12147293-3 2002 The effect of ET-1 was inhibited by bosentan and was insensitive to BQ788, suggesting the involvement of ETA receptor. Bosentan 36-44 endothelin 1 Rattus norvegicus 14-18 12206849-2 2002 The aim of the study was to investigate the effect of bosentan, its metabolites and glibenclamide on the activity of the pregnane X receptor, a nuclear receptor that regulates the transcription of CYP3A4. Bosentan 54-62 nuclear receptor subfamily 1 group I member 2 Homo sapiens 121-140 12206849-2 2002 The aim of the study was to investigate the effect of bosentan, its metabolites and glibenclamide on the activity of the pregnane X receptor, a nuclear receptor that regulates the transcription of CYP3A4. Bosentan 54-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 197-203 12127422-10 2002 CONCLUSIONS: Bosentan alters canalicular bile formation in major part via mrp2-mediated mechanisms. Bosentan 13-21 ATP binding cassette subfamily C member 2 Rattus norvegicus 74-78 12150723-10 2002 CONCLUSION: Bosentan combined with amlodipine can offer similar renoprotective effects on that of cilazapril and may be a potent therapy to attenuate renal injury by reducing renal protein levels of TGF-beta1 in diabetes with a hypertensive state. Bosentan 12-20 transforming growth factor, beta 1 Rattus norvegicus 199-208 12181591-2 2002 The present study was designed to investigate the role of endothelin in O2-induced contraction in the isolated ductal preparation of rabbit and rat, using the endothelin receptor antagonists, bosentan (antagonist for both ET-A and ET-B receptors) and BQ 485 (an ET-A selective antagonist). Bosentan 192-200 endothelin receptor type A Rattus norvegicus 222-226 12105391-6 2002 The treatment of the low calcium diet rats with bosentan was found to substantially reduce the number of PCNA-positive parathyroid cells, wet weight of parathyroid gland, and serum PTH level. Bosentan 48-56 parathyroid hormone Rattus norvegicus 181-184 11997273-10 2002 These proatherosclerotic effects of CRP were mediated, in part, via increased secretion of ET-1 and IL-6 (P<0.01) and were attenuated by both bosentan and IL-6 antagonism (P<0.01). Bosentan 145-153 C-reactive protein Homo sapiens 36-39 12047483-12 2002 In the presence of CYP3A4 inhibitors, bosentan concentrations may be increased 2-fold. Bosentan 38-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 12063458-4 2002 Therefore we studied the effects of endothelin receptor blockers (BQ-123 and bosentan) on hyperglycemia-induced endothelin-1 production and cellular injury after ischemia-reperfusion. Bosentan 77-85 endothelin 1 Homo sapiens 112-124 11973408-6 2002 Bosentan (10 microM, dual ETA/B receptor antagonist) reduced (p < 0.05) immunoreactive ET-1 content in control cells. Bosentan 0-8 endothelin receptor type A Homo sapiens 26-51 11973408-6 2002 Bosentan (10 microM, dual ETA/B receptor antagonist) reduced (p < 0.05) immunoreactive ET-1 content in control cells. Bosentan 0-8 endothelin 1 Homo sapiens 90-94 11973408-7 2002 Bosentan prevented exogenous ET-1-induced endothelial cell ET-1 loading, suggesting that exogenous ET-1 is partly recycled. Bosentan 0-8 endothelin 1 Homo sapiens 29-33 11973408-7 2002 Bosentan prevented exogenous ET-1-induced endothelial cell ET-1 loading, suggesting that exogenous ET-1 is partly recycled. Bosentan 0-8 endothelin 1 Homo sapiens 59-63 11973408-7 2002 Bosentan prevented exogenous ET-1-induced endothelial cell ET-1 loading, suggesting that exogenous ET-1 is partly recycled. Bosentan 0-8 endothelin 1 Homo sapiens 59-63 11973408-8 2002 PreproET-1 mRNA levels were reduced (p < 0.05) by exogenous ET-1 after 24 h, an effect blocked by BQ788 and bosentan. Bosentan 111-119 endothelin 1 Homo sapiens 6-10 11997273-13 2002 Bosentan may be useful in decreasing CRP-mediated vascular disease. Bosentan 0-8 C-reactive protein Homo sapiens 37-40 11953118-11 2002 CONCLUSION: Bosentan prevents the down-regulation of AT1 receptor in the kidneys of diabetic hypertensive rats. Bosentan 12-20 angiotensin II receptor, type 1a Rattus norvegicus 53-56 11849873-8 2002 Treatment with Bosentan, a mixed ET-1 receptor antagonist, significantly reduced the incidence and intensity of arteriosclerotic lesions in rat cardiac allografts, as well as total intragraft ET(A) and ET(B) mRNA expression and intimal cell ET-1 and receptor immunoreactivity. Bosentan 15-23 endothelin 1 Rattus norvegicus 33-37 11849873-8 2002 Treatment with Bosentan, a mixed ET-1 receptor antagonist, significantly reduced the incidence and intensity of arteriosclerotic lesions in rat cardiac allografts, as well as total intragraft ET(A) and ET(B) mRNA expression and intimal cell ET-1 and receptor immunoreactivity. Bosentan 15-23 endothelin receptor type B Rattus norvegicus 202-207 11849873-8 2002 Treatment with Bosentan, a mixed ET-1 receptor antagonist, significantly reduced the incidence and intensity of arteriosclerotic lesions in rat cardiac allografts, as well as total intragraft ET(A) and ET(B) mRNA expression and intimal cell ET-1 and receptor immunoreactivity. Bosentan 15-23 endothelin 1 Rattus norvegicus 241-258 11992503-6 2002 We report accurate TOF mass spectra of background-subtracted MS3 for protonated molecules reserpine (m/z 609), bosentan (m/z 1552), and taxol (m/z 854). Bosentan 111-119 MS3 Homo sapiens 61-64 14727963-1 2002 Bosentan is a nonpeptide, specific, competitive, dual antagonist at both endothelin receptor subtypes (ET(A) and ET(B)). Bosentan 0-8 endothelin receptor type B Homo sapiens 113-118 14727963-2 2002 Orally administered bosentan effectively prevents endothelin 1-induced vasoconstriction in pulmonary vessels in patients with pulmonary arterial hypertension. Bosentan 20-28 endothelin 1 Homo sapiens 50-62 11744810-12 2002 Bosentan prevented increased fibronectin and collagen alpha2(IV) mRNA expression, increased mesangial matrix deposition and GBM thickening. Bosentan 0-8 fibronectin 1 Homo sapiens 29-40 11447300-12 2001 Furthermore, the contribution of ET-1 to human hypertension appears more convincing since bosentan was shown to decrease blood pressure in hypertensive subjects. Bosentan 90-98 endothelin 1 Homo sapiens 33-37 11709418-4 2001 In contrast, the dose-related increases in total peripheral resistance evoked by vasopressin were blunted in both DOCA-salt hypertensive and sham normotensive rats, but this effect of bosentan was greater in the DOCA-salt hypertensive group. Bosentan 184-192 arginine vasopressin Rattus norvegicus 81-92 11709418-6 2001 The exaggerated vascular responsiveness (total peripheral resistance) of the DOCA-salt hypertensive group to vasopressin was largely abolished by bosentan. Bosentan 146-154 arginine vasopressin Rattus norvegicus 109-120 11447307-4 2001 Bosentan acutely and during short-term oral therapy markedly improved hemodynamics in patients in addition to standard heart failure therapy, including an ACE-inhibitor. Bosentan 0-8 angiotensin I converting enzyme Homo sapiens 155-158 11729239-7 2001 The AngII-induced effect on procol alpha 2(I) was completely inhibited by candesartan (AngII type 1 receptor antagonist) and substantially blunted by bosentan (dual ET receptor antagonist) (P < 0.01), whereas the ET-induced activation of collagen I gene was blocked only by bosentan. Bosentan 150-158 angiotensinogen (serpin peptidase inhibitor, clade A, member 8) Mus musculus 4-9 11729239-7 2001 The AngII-induced effect on procol alpha 2(I) was completely inhibited by candesartan (AngII type 1 receptor antagonist) and substantially blunted by bosentan (dual ET receptor antagonist) (P < 0.01), whereas the ET-induced activation of collagen I gene was blocked only by bosentan. Bosentan 277-285 angiotensinogen (serpin peptidase inhibitor, clade A, member 8) Mus musculus 4-9 11811379-3 2001 As both the mixed ETA/ETB-receptor antagonist bosentan and the selective ETA receptor antagonist BQ 123 acutely improved the haemodynamics of chronic heart failure patients, there seems to be good reason to believe that ET-1 receptor antagonism may also be of benefit in the setting of acute heart failure. Bosentan 46-54 endothelin receptor type A Homo sapiens 18-21 11736680-10 2001 A further increase in plasma endothelin-1-like immunoreactivity was seen in response to bosentan. Bosentan 88-96 endothelin-1 Sus scrofa 29-41 11696450-10 2001 The administration of the dual ETA/ETB antagonist bosentan to AT1(-/-) considerably reduced the interstitial infiltrates. Bosentan 50-58 endothelin receptor type A Mus musculus 31-34 11696450-10 2001 The administration of the dual ETA/ETB antagonist bosentan to AT1(-/-) considerably reduced the interstitial infiltrates. Bosentan 50-58 endothelin receptor type B Mus musculus 35-38 11696450-10 2001 The administration of the dual ETA/ETB antagonist bosentan to AT1(-/-) considerably reduced the interstitial infiltrates. Bosentan 50-58 angiotensin II receptor, type 1a Mus musculus 62-65 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). Bosentan 169-177 endothelin-1 Cricetulus griseus 28-32 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). Bosentan 169-177 endothelin-1 Cricetulus griseus 74-78 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). Bosentan 169-177 endothelin-1 Cricetulus griseus 74-78 11566958-16 2001 A greater blood pressure-lowering effect of bosentan (ET(A)/ET(B) blocker) was observed in OVX-DOCA rats. Bosentan 44-52 endothelin receptor type B Rattus norvegicus 60-65 11597932-8 2001 Conversely, bosentan induced a marked increase in vessel density at 3 and 28 days (1.4-fold and 1.7-fold, respectively, compared with no treatment; P<0.05), which was associated with an increase in VEGF and endothelial NO synthase levels in ischemic legs (by 31+/-8% and 45+/-23%, respectively, at 3 days and by 65+/-13% and 55+/-15%, respectively, at 28 days; P<0.05 versus nontreated rats). Bosentan 12-20 vascular endothelial growth factor A Rattus norvegicus 201-205 11566958-17 2001 The observation that OVX worsens hypertension as well as the altered ET(B) receptor-mediated responses and the effects of bosentan in female DOCA rats supports our suggestion that the ovarian hormones modulate ET-1/ET(B) receptor vascular responses/expression in DOCA-salt hypertension. Bosentan 122-130 endothelin 1 Rattus norvegicus 210-214 11463769-4 2001 In the presence of bosentan, pressor and renal vasoconstrictor responses to low-dose angiotensin II were blunted (P<0.02 and P<0.01, respectively), and the results with BQ-123 were similar. Bosentan 19-27 angiotensinogen Rattus norvegicus 85-99 11515898-8 2001 Bosentan reduced the hypoxia and reoxygenation-induced elevation of ET-1 and iNOS mRNA at the end of recovery (p < 0.05). Bosentan 0-8 endothelin 1 Homo sapiens 68-72 11515898-8 2001 Bosentan reduced the hypoxia and reoxygenation-induced elevation of ET-1 and iNOS mRNA at the end of recovery (p < 0.05). Bosentan 0-8 inositol-3-phosphate synthase 1 Homo sapiens 77-81 11463769-6 2001 In contrast, high-dose angiotensin II caused natriuretic and diuretic effects that were completely prevented by bosentan. Bosentan 112-120 angiotensinogen Rattus norvegicus 23-37 11407110-6 2001 Vasopeptidase inhibitor, such as omapatrilat, and endothelin-1 antagonist, such as bosentan, may become future agents approved for the reduction of morbidity and mortality with hypertension. Bosentan 83-91 endothelin 1 Homo sapiens 50-62 11459133-0 2001 Endothelium-dependent relaxation in response to low concentrations of bradykinin is enhanced by phosphoramidon, bosentan and BQ-123 in bovine coronary arteries in vitro. Bosentan 112-120 kininogen 1 Bos taurus 70-80 11386616-5 2001 A novel finding was that AE-ITU also prevented the GAS-induced marked increase in plasma ET-1 at 6 h. Short-term (7-h) survival was improved by both AE-ITU and by bosentan. Bosentan 163-171 endothelin 1 Rattus norvegicus 89-93 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 198-207 endothelin receptor type A Rattus norvegicus 75-80 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 198-207 endothelin receptor type A Rattus norvegicus 160-165 11360057-12 2001 Pathology scores for factor VIII immunohistochemical staining were 2.3-fold higher in the bosentan-treated livers as compared to untreated livers (P < 0.05). Bosentan 90-98 coagulation factor VIII Sus scrofa 21-32 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 198-207 endothelin receptor type B Rattus norvegicus 166-171 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 209-217 endothelin receptor type A Rattus norvegicus 75-80 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 209-217 endothelin receptor type A Rattus norvegicus 160-165 11383615-1 2001 In the present article we wish to report the discovery of a novel class of ET(A)-selective endothelin (ET) receptor antagonists through the modification of the ET(A)/ET(B) non-selective antagonist, Ro47-0203 (Bosentan, 1). Bosentan 209-217 endothelin receptor type B Rattus norvegicus 166-171 11264238-10 2001 In study 1, infusion of bosentan reduced TPR and BP dramatically in DOCA-salt hypertensive rats but not in SHAM control rats, and this effect was greater when the AVP system had been blocked. Bosentan 24-32 arginine vasopressin Rattus norvegicus 163-166 11309550-2 2001 In this study we investigated whether inhibition of the hepatocanalicular bile salt export pump (rodents, Bsep; humans, BSEP ABCB11) could account for bosentan-induced liver injury. Bosentan 151-159 ATP binding cassette subfamily B member 11 Homo sapiens 120-124 11309550-7 2001 In vitro, Bsep-mediated taurocholate transport was inhibited by bosentan (inhibition constant, approximately 12 micromol/L) and metabolites (inhibition constant, approximately 8.5 micromol/L for metabolite Ro 47-8634). Bosentan 64-72 ATP binding cassette subfamily B member 11 Homo sapiens 10-14 11309550-8 2001 CONCLUSIONS: These results indicate that bosentan-induced liver injury is mediated, at least in part, by inhibition of Bsep/BSEP-causing intracellular accumulation of cytotoxic bile salts and bile salt induced liver cell damage. Bosentan 41-49 ATP binding cassette subfamily B member 11 Homo sapiens 119-123 11309550-8 2001 CONCLUSIONS: These results indicate that bosentan-induced liver injury is mediated, at least in part, by inhibition of Bsep/BSEP-causing intracellular accumulation of cytotoxic bile salts and bile salt induced liver cell damage. Bosentan 41-49 ATP binding cassette subfamily B member 11 Homo sapiens 124-128 11330884-9 2001 Strikingly, responses to NE and ET-1 (in arteries with endothelium) were completely normalized following long-term bosentan treatment. Bosentan 115-123 endothelin 1 Rattus norvegicus 32-36 11238005-6 2001 Treatment of the animals with the ET receptor antagonist bosentan resulted in a substantial decrease in the concentrations of tumor necrosis factor-alpha, IL-4, IL-1beta, interferon-gamma, and ET-1 in bronchoalveolar lavage fluid. Bosentan 57-65 tumor necrosis factor Homo sapiens 126-153 11238005-6 2001 Treatment of the animals with the ET receptor antagonist bosentan resulted in a substantial decrease in the concentrations of tumor necrosis factor-alpha, IL-4, IL-1beta, interferon-gamma, and ET-1 in bronchoalveolar lavage fluid. Bosentan 57-65 interleukin 4 Homo sapiens 155-159 11238005-6 2001 Treatment of the animals with the ET receptor antagonist bosentan resulted in a substantial decrease in the concentrations of tumor necrosis factor-alpha, IL-4, IL-1beta, interferon-gamma, and ET-1 in bronchoalveolar lavage fluid. Bosentan 57-65 interleukin 1 beta Homo sapiens 161-169 11238005-6 2001 Treatment of the animals with the ET receptor antagonist bosentan resulted in a substantial decrease in the concentrations of tumor necrosis factor-alpha, IL-4, IL-1beta, interferon-gamma, and ET-1 in bronchoalveolar lavage fluid. Bosentan 57-65 interferon gamma Homo sapiens 171-187 11238005-6 2001 Treatment of the animals with the ET receptor antagonist bosentan resulted in a substantial decrease in the concentrations of tumor necrosis factor-alpha, IL-4, IL-1beta, interferon-gamma, and ET-1 in bronchoalveolar lavage fluid. Bosentan 57-65 endothelin 1 Homo sapiens 193-197 11304520-7 2001 The administration of the ACE inhibitor quinapril plus the ET(A)/ET(B) receptor antagonist bosentan during 28 days to BSA-overloaded animals diminished proteinuria, renal lesions, and NF-kappaB activity more markedly than single drugs. Bosentan 91-99 endothelin receptor type B Rattus norvegicus 65-70 11093481-5 2000 In 2-week-old pigs, ET-1 elevated PAP (19,009 +/- 1,834 versus 21,935 +/- 2,104; p = 0.003) and PVR (1,624 +/- 254 versus 2,302 +/- 416; p = 0.001), whereas bosentan abolished the ET-1 induced pulmonary and systemic vasoconstriction. Bosentan 157-165 endothelin-1 Sus scrofa 20-24 11230326-11 2001 Bosentan also blocked Ang II-induced hypertension (from 135+/-4 to 139+/-3 mm Hg) but did not decrease isoprostanes (146+/-14 pg/mL). Bosentan 0-8 angiotensinogen Rattus norvegicus 22-28 11152109-9 2000 The inhibition of ET with bosentan prevented the increase of both hepatic and plasma TNF, thus attenuating the liver and lung injury, whereas TNF addition abolished the benefits of bosentan. Bosentan 181-189 tumor necrosis factor-like Rattus norvegicus 142-145 11152109-10 2000 CONCLUSIONS: These findings suggest that both bosentan and preconditioning, by inhibition of ET could attenuate the microvascular disorders and the deleterious effect of TNF on the liver and lung elicited by hepatic I/R. Bosentan 46-54 tumor necrosis factor-like Rattus norvegicus 170-173 11093786-10 2000 They accelerated the relaxing action of BQ-123 and bosentan in ET-1-treated aortic rings. Bosentan 51-59 endothelin 1 Rattus norvegicus 63-67 11156886-7 2001 The mixed endothelin-1 ET(A)/ET(B) receptor antagonist bosentan but not the angiotensin II type 1 receptor antagonist losartan completely inhibited the pressure overload-induced increase in left ventricular BNP GATA4 binding activity. Bosentan 55-63 endothelin 1 Rattus norvegicus 10-22 11156886-7 2001 The mixed endothelin-1 ET(A)/ET(B) receptor antagonist bosentan but not the angiotensin II type 1 receptor antagonist losartan completely inhibited the pressure overload-induced increase in left ventricular BNP GATA4 binding activity. Bosentan 55-63 natriuretic peptide B Rattus norvegicus 207-210 11156886-7 2001 The mixed endothelin-1 ET(A)/ET(B) receptor antagonist bosentan but not the angiotensin II type 1 receptor antagonist losartan completely inhibited the pressure overload-induced increase in left ventricular BNP GATA4 binding activity. Bosentan 55-63 GATA binding protein 4 Rattus norvegicus 211-216 11230293-9 2001 In addition, insulin evoked vasorelaxation in aortas isolated from rats after long-term bosentan treatment (100 mg. kg(-1). Bosentan 88-96 insulin Homo sapiens 13-20 11156582-5 2001 Bosentan (antagonist for ET(A) and ET(B) receptors, 1 microM based on concentration-response curves of ET-1), SQ 30,741 (antagonist of TXA(2) receptors, 0.1 microM), or the combination thereof was administered to isolated perfused rat hearts undergoing 15 min of global ischaemia and 60 min of reperfusion. Bosentan 0-8 endothelin receptor type A Rattus norvegicus 25-30 11152109-9 2000 The inhibition of ET with bosentan prevented the increase of both hepatic and plasma TNF, thus attenuating the liver and lung injury, whereas TNF addition abolished the benefits of bosentan. Bosentan 26-34 tumor necrosis factor-like Rattus norvegicus 85-88 11093481-7 2000 CONCLUSIONS: ET-1 caused a pulmonary depressor response in 48-hour-old pigs and a constrictor response in 2-week-old pigs, whereas bosentan inhibited the ET-1 induced pulmonary arteriolar vasoconstriction in 2-week-old pigs. Bosentan 131-139 endothelin-1 Sus scrofa 154-158 11093481-9 2000 These data suggest that bosentan may have potential clinical application in the treatment of newborn pulmonary hypertensive episodes as it ablated ET-1 induced pulmonary vasoconstriction, while maintaining systemic pressure. Bosentan 24-32 endothelin-1 Sus scrofa 147-151 11078409-0 2000 Bosentan the mixed endothelin-A- and -B-receptor antagonist suppresses intrapericardial endothelin-1-induced ventricular arrhythmias. Bosentan 0-8 endothelin 1 Canis lupus familiaris 88-100 11082120-6 2000 Pre-treatment with the selective ET(A) receptor antagonists, LBL 031 or PD 156707, or the mixed ET(A/B) receptor antagonist, bosentan (each at 30 mg kg(-1)), reduced ET-1-induced leakage to baseline levels. Bosentan 125-133 endothelin 1 Rattus norvegicus 166-170 11187978-7 2000 Bosentan, the non-selective ET(A)/ET(B) antagonist, when given by dialysis at the site of injection, reduced the area of both the ET-1-induced pallor and surrounding flare by 41 and 26%, respectively. Bosentan 0-8 endothelin receptor type B Homo sapiens 34-39 11187978-7 2000 Bosentan, the non-selective ET(A)/ET(B) antagonist, when given by dialysis at the site of injection, reduced the area of both the ET-1-induced pallor and surrounding flare by 41 and 26%, respectively. Bosentan 0-8 endothelin 1 Homo sapiens 130-134 11078348-10 2000 Bosentan, an ET(A)/ET(B)-receptor antagonist, induced a greater decrease in mean arterial blood pressure in male than in female DOCA-salt hypertensive rats. Bosentan 0-8 endothelin receptor type B Rattus norvegicus 19-24 11078409-4 2000 The aim of this study was to test the antiarrhythmic and anti-ischemic efficacy of the mixed endothelin-A- and -B- (ETA/B) receptor antagonist bosentan (BOS) on ET-1-induced arrhythmias on six mongrel dogs. Bosentan 143-151 endothelin 1 Canis lupus familiaris 161-165 11078423-0 2000 Mixed endothelin ET(A) and ET(B) antagonist bosentan inhibits oleic acid-induced lung plasma extravasation in mouse. Bosentan 44-52 endothelin receptor type B Mus musculus 27-32 11078409-4 2000 The aim of this study was to test the antiarrhythmic and anti-ischemic efficacy of the mixed endothelin-A- and -B- (ETA/B) receptor antagonist bosentan (BOS) on ET-1-induced arrhythmias on six mongrel dogs. Bosentan 153-156 endothelin 1 Canis lupus familiaris 161-165 11078423-4 2000 Pretreatment with the mixed endothelin-ET(A) and ET(B) (ET(A)/ET(B)) receptor antagonist bosentan (30 mg/kg, i.v., 30 min before oleic acid) markedly reduced lung Evans blue content (to 0.24 +/- 0.04), as did pretreatments with prazosin (1 mg/kg), meloxicam (5 mg/kg) and dexamethasone (1 mg/kg/day, for 3 days). Bosentan 89-97 endothelin receptor type B Mus musculus 49-54 11092528-6 2000 Bosentan, a mixed ET(A) and ET(B) receptor antagonist, induced apoptosis in these cell lines in a dose-dependent manner. Bosentan 0-8 endothelin receptor type A Homo sapiens 18-23 11078418-8 2000 After application of 0.1 mg/kg of bosentan, sinusoids remained constricted (89.7 +/- 9.9%, AST 255.0 +/- 12.8 U/l). Bosentan 34-42 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 91-94 11078418-9 2000 Blocking ET receptors with 1 mg/kg bosentan avoided sinusoidal constriction (99.0 +/- 8.8%, p < 0.05) and led to the most effective reduction of AST level peak after 6 h of reperfusion (244.0 +/- 34.2 U/l vs 422.9 +/- 163.3 U/l in untreated ischemia). Bosentan 35-43 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 148-151 11078419-4 2000 Bosentan, a mixed endothelin-A- and -B- (ET(A)/ET(B)) receptor antagonist, potentiated FasL- (APO-1, CD95) induced apoptosis in these cells. Bosentan 0-8 Fas ligand Homo sapiens 87-91 11078419-4 2000 Bosentan, a mixed endothelin-A- and -B- (ET(A)/ET(B)) receptor antagonist, potentiated FasL- (APO-1, CD95) induced apoptosis in these cells. Bosentan 0-8 Fas cell surface death receptor Homo sapiens 94-99 11078419-4 2000 Bosentan, a mixed endothelin-A- and -B- (ET(A)/ET(B)) receptor antagonist, potentiated FasL- (APO-1, CD95) induced apoptosis in these cells. Bosentan 0-8 Fas cell surface death receptor Homo sapiens 101-105 10961375-11 2000 With respect to ET-1-induced bronchoconstriction, in the IPL bosentan in concentrations of up to 10 microM aggravated ET-1-induced bronchoconstriction probably due to the blockade of bronchodilatory ET(A)-receptors (IC50 0.3 microM) and even at 100 microM showed only very little protection from ET- -induced bronchoconstriction in the IPL and in the PCLS. Bosentan 61-69 endothelin receptor type A Rattus norvegicus 199-204 10966825-11 2000 In keeping with focal fibrosis, myocardium from diabetic rats further showed significantly increased mRNA expression of two extracellular matrix protein transcripts, fibronectin and collagen alpha 1(IV) which were completely prevented by treatment with bosentan. Bosentan 253-261 fibronectin 1 Rattus norvegicus 166-177 10948091-0 2000 Effect of bosentan on NF-kappaB, inflammation, and tissue factor in angiotensin II-induced end-organ damage. Bosentan 10-18 coagulation factor III, tissue factor Homo sapiens 51-64 10948091-0 2000 Effect of bosentan on NF-kappaB, inflammation, and tissue factor in angiotensin II-induced end-organ damage. Bosentan 10-18 angiotensinogen Homo sapiens 68-82 10948091-2 2000 We tested the hypothesis that endothelin (ET)(A/B) receptor blockade with bosentan (100 mg/kg by gavage after age 4 weeks) ameliorates cardiac and renal damage by decreasing inflammation in rats harboring both human renin and angiotensinogen genes (dTGR). Bosentan 74-82 renin Homo sapiens 216-221 10948091-3 2000 Furthermore, we elucidated the effect of bosentan on tissue factor (TF), which is a key regulator of the extrinsic coagulation cascade. Bosentan 41-49 coagulation factor III, tissue factor Homo sapiens 53-66 10948091-3 2000 Furthermore, we elucidated the effect of bosentan on tissue factor (TF), which is a key regulator of the extrinsic coagulation cascade. Bosentan 41-49 coagulation factor III, tissue factor Homo sapiens 68-70 10948091-13 2000 Renal vasculopathy was accompanied by increased tissue factor expression on macrophages and vessels of untreated and hydralazine-treated dTGR, which was markedly reduced by bosentan. Bosentan 173-181 coagulation factor III, tissue factor Homo sapiens 48-61 10961375-2 2000 Recently, the non-peptide mixed ET(A)/ET(B) endothelin receptor antagonist bosentan has been successfully tested in the treatment of cardiovascular diseases. Bosentan 75-83 endothelin receptor type A Rattus norvegicus 32-37 10961375-3 2000 It was the aim of the present study to characterize the effects of bosentan on the pulmonary actions of endothelin- (ET-1), endothelin-3 (ET-3) and the ET(B)-receptor agonist IRL1620 in the isolated perfused and ventilated rat lung (IPL) and in precision-cut lung slices (PCLS). Bosentan 67-75 endothelin 3 Rattus norvegicus 124-136 10961375-5 2000 The inhibition by bosentan of ET-1-elicited vasoconstriction showed a biphasic course, reflecting the inhibition of ET(A)-and ET(B)-mediated vasoconstriction (IC50 0.2 microM and 19 microM, respectively). Bosentan 18-26 endothelin receptor type A Rattus norvegicus 116-121 10989742-9 2000 Similarly, bosentan prevented and reversed the effect of angiotensin II on cardiovascular structure independently of arterial pressure. Bosentan 11-19 angiotensinogen Homo sapiens 57-71 10989742-11 2000 The influence of bosentan suggests that endothelin plays an important role in local action of angiotensin II independently of blood pressure level. Bosentan 17-25 angiotensinogen Homo sapiens 94-108 10780753-10 2000 Pulmonary vascular remodelling, associated with elevated plasma endothelin-1 levels and positive endothelin-1 immunoreactivity in lung tissue is attenuated by the endothelin receptor antagonist, bosentan. Bosentan 195-203 endothelin 1 Canis lupus familiaris 64-76 10908213-2 2000 This trial was designed to assess the hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with PHT, in which local overproduction of endothelin-1 (ET-1) is thought to play a pathogenic role. Bosentan 61-69 endothelin 1 Homo sapiens 161-173 10908213-2 2000 This trial was designed to assess the hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with PHT, in which local overproduction of endothelin-1 (ET-1) is thought to play a pathogenic role. Bosentan 61-69 endothelin 1 Homo sapiens 175-179 10886569-7 2000 Bosentan treatment in the obstructed group prevented these Ang II-induced effects and did not have any effect on the sham-operated kidney. Bosentan 0-8 angiotensinogen Rattus norvegicus 59-65 10807679-6 2000 The simultaneous administration of BQ 123 and BQ 788, the respective antagonists of ET(A) and ET(B) endothelin receptors, or that of bosentan, a mixed ET(A)/ET(B) antagonist, antagonized the vasoconstrictor effect of 10% xenogeneic human serum, as well as that of 10(-9) M endothelin-1. Bosentan 133-141 endothelin receptor type A Homo sapiens 151-156 10807679-6 2000 The simultaneous administration of BQ 123 and BQ 788, the respective antagonists of ET(A) and ET(B) endothelin receptors, or that of bosentan, a mixed ET(A)/ET(B) antagonist, antagonized the vasoconstrictor effect of 10% xenogeneic human serum, as well as that of 10(-9) M endothelin-1. Bosentan 133-141 endothelin receptor type B Homo sapiens 157-162 10738244-6 2000 Bosentan, a mixed ET(A)/ET(B) receptor antagonist, potentiated FasL-induced apoptosis in these cells. Bosentan 0-8 Fas ligand Rattus norvegicus 63-67 10738244-7 2000 At low concentrations (10(-13) to 10(-10) M), ET-1 dose-dependently reversed bosentan-induced apoptosis. Bosentan 77-85 endothelin 1 Rattus norvegicus 46-50 10738244-8 2000 Bosentan sensitization to FasL-induced apoptosis was not mediated by increased expression of Fas receptor and was blocked by the caspase inhibitor zVAD-fmk. Bosentan 0-8 Fas ligand Rattus norvegicus 26-30 10760337-3 2000 On day 1, angiotensin II increased from 16.1+/-17.9 to 27.6+/-5.6 ng/L (p <0.05) with bosentan and similarly with placebo (15.5+/-9.3 and 36.0+/-49.1 ng/L, p = 0.06) after the morning dose of diuretics and digoxin. Bosentan 89-97 angiotensinogen Homo sapiens 10-24 10780753-10 2000 Pulmonary vascular remodelling, associated with elevated plasma endothelin-1 levels and positive endothelin-1 immunoreactivity in lung tissue is attenuated by the endothelin receptor antagonist, bosentan. Bosentan 195-203 endothelin 1 Canis lupus familiaris 97-109 10637124-6 1999 When tissues are incubated in the presence of endothelin 1 (ET-1) (10(-7) M), NOS activity is higher in C pancreas, while the ET-receptor antagonist bosentan (B) decreases NOS levels in D but not in C tissues. Bosentan 149-157 endothelin 1 Rattus norvegicus 46-58 10858017-6 2000 BQ-123 and bosentan also inhibited LPS increases in neutrophil (by 67 and 40%) and eosinophil (by 63 and 74%) at 24 h. CONCLUSIONS: Endothelins, acting via ETA receptors, play a role in late eosinophil and neutrophil accumulation (24 h), but not in the acute (4 h) neutrophilic response. Bosentan 11-19 toll-like receptor 4 Mus musculus 35-38 10726713-6 2000 Acute inhibition of both ETA and ETB receptors with bosentan dramatically prolonged 125I-ET-1 plasma half-life and shifted tissue uptake from lung to liver and kidneys. Bosentan 52-60 endothelin receptor type A Rattus norvegicus 25-28 10726713-6 2000 Acute inhibition of both ETA and ETB receptors with bosentan dramatically prolonged 125I-ET-1 plasma half-life and shifted tissue uptake from lung to liver and kidneys. Bosentan 52-60 endothelin receptor type B Rattus norvegicus 33-36 10726713-6 2000 Acute inhibition of both ETA and ETB receptors with bosentan dramatically prolonged 125I-ET-1 plasma half-life and shifted tissue uptake from lung to liver and kidneys. Bosentan 52-60 endothelin 1 Rattus norvegicus 89-93 10666411-7 2000 Bosentan treatment significantly reduced mesenteric weight, wall-to-lumen ratio, mast cell infiltration, matrix deposition, and EGF mRNA but did not prevent the overexpression of transforming growth factor-beta(1) mRNA in diabetic rats. Bosentan 0-8 epidermal growth factor like 1 Rattus norvegicus 128-131 10732291-6 1999 The mixed endothelin A and endothelin B receptor antagonist bosentan (20 mg/kg b.w.) Bosentan 60-68 endothelin receptor type B Rattus norvegicus 27-48 10732291-14 1999 CONCLUSION: Therapy with the mixed endothelin A and endothelin B receptor antagonist bosentan does not influence the outcome after severe experimental pancreatitis. Bosentan 85-93 endothelin receptor type B Rattus norvegicus 52-73 10703878-10 1999 Moreover, bosentan reduced glomerular hypertrophy and deposits of collagen and fibronectin in the kidney and cardiac deposits of collagen III. Bosentan 10-18 fibronectin 1 Rattus norvegicus 79-90 10619183-6 1999 Moreover, bosentan (from 2.5 mg kg(-1) to 10 mg kg(-1)), an ET(A)/ET(B) receptor antagonist, also inhibited the bronchial hyperresponsiveness achieved 24 h following endothelin-1 challenge (P<0.01), but with no difference from FR 139317. Bosentan 10-18 endothelin-1 Oryctolagus cuniculus 166-178 10666080-2 2000 Mean ANF responses to slow infusions (3 x 3.3 ml/8 min) were dose dependently reduced (P < 0.05) by bosentan (nonselective ET-receptor antagonist) from 64.1 +/- 18.1 (SE) pg/ml (control) to 52.6 +/- 16.1 (0.033 mg bosentan/rat), 16.1 +/- 7.6 (0. Bosentan 103-111 natriuretic peptide A Rattus norvegicus 5-8 10953665-17 2000 Th non-selective ETA/ETB blocker bosentan is in the stage of clinical tests and seems to be safe and perspective. Bosentan 33-41 endothelin receptor type A Homo sapiens 17-20 10953665-17 2000 Th non-selective ETA/ETB blocker bosentan is in the stage of clinical tests and seems to be safe and perspective. Bosentan 33-41 endothelin receptor type B Homo sapiens 21-24 10637124-6 1999 When tissues are incubated in the presence of endothelin 1 (ET-1) (10(-7) M), NOS activity is higher in C pancreas, while the ET-receptor antagonist bosentan (B) decreases NOS levels in D but not in C tissues. Bosentan 149-157 endothelin 1 Rattus norvegicus 60-64 10393673-7 1999 Most of the potentiating effects (88%) were blocked by the ETA receptor antagonist LU135252 and slightly further blocked by the ETA/B receptor antagonist bosentan (P<0.05). Bosentan 154-162 endothelin receptor type A Homo sapiens 128-131 10534471-7 1999 Oral bosentan, a mixed ET-1 receptor antagonist, was administered after virus inoculation in doses of 0 (control group), 10, or 100 mg. kg(-1). Bosentan 5-13 endothelin 1 Mus musculus 23-27 10523377-6 1999 The ET(A/B) antagonist bosentan induced blood-pressure reductions in mildly hypertensive patients similar to those achieved with an angiotensin-converting enzyme inhibitor. Bosentan 23-31 endothelin receptor type A Homo sapiens 4-10 10474778-10 1999 Bosentan significantly attenuated the endothelin-1-induced blood pressure rise at 0.125 nmol/kg (P < 0.05), but not at higher doses. Bosentan 0-8 endothelin 1 Rattus norvegicus 38-50 10474778-12 1999 Bosentan at a dose which attenuated endothelin-1-induced blood pressure increase had no effect on either blood pressure or metabolic parameters in ACTH-treated rats. Bosentan 0-8 endothelin 1 Rattus norvegicus 36-48 10585047-4 1999 This study was carried out using an established model of hypoxia and reoxygenation to determine whether endothelin-1 blockade with Bosentan could prevent hypoxia-reoxygenation-induced pulmonary hypertension and reoxygenation injury. Bosentan 131-139 endothelin 1 Homo sapiens 104-116 10585047-6 1999 Control animals (n = 12) received no drug treatment, whereas the treatment group (n = 8) received the endothelin-1 receptor antagonist, Bosentan, throughout hypoxia. Bosentan 136-144 endothelin receptor type A Homo sapiens 102-123 10585047-10 1999 Consequently, animals in the Bosentan group had better postreoxygenation pulmonary vascular resistance, A-a gradient, and airway resistance along with lower myeloperoxidase levels than controls. Bosentan 29-37 myeloperoxidase Homo sapiens 157-172 10063923-12 1999 Bosentan effectively prevented ET-1 elevation but could not reverse creatinine or bilirubin elevation. Bosentan 0-8 endothelin 1 Rattus norvegicus 31-35 10233186-0 1999 Protection against aspirin-induced human gastric mucosal injury by bosentan, a new endothelin-1 receptor antagonist. Bosentan 67-75 endothelin receptor type A Homo sapiens 83-104 10233186-5 1999 AIM: To investigate whether acute gastroduodenal injury induced in humans by aspirin can be prevented by the endothelin-1 antagonist, bosentan. Bosentan 134-142 endothelin 1 Homo sapiens 109-121 10385252-10 1999 The spasm induced by TEA and ET-1 was amplified by the ETA antagonist, EMD94246, and suppressed by the ET(A)-ET(B) antagonist, bosentan. Bosentan 127-135 endothelin-1 Cavia porcellus 29-33 10101112-4 1999 All these effects were blocked by the ETA/ETB receptor antagonist bosentan (5 mg kg-1). Bosentan 67-75 endothelin receptor type A Homo sapiens 39-42 10101112-4 1999 All these effects were blocked by the ETA/ETB receptor antagonist bosentan (5 mg kg-1). Bosentan 67-75 endothelin receptor type B Homo sapiens 43-46 10215740-10 1999 Bosentan also caused complete reduction of MPO activity. Bosentan 0-8 myeloperoxidase Rattus norvegicus 43-46 10215740-11 1999 In indomethacin-induced gastric damage, 100 mg/kg bosentan attenuated gastric damage by 45% and 61% as measured by the gastric lesion index and MPO activity respectively. Bosentan 50-58 myeloperoxidase Rattus norvegicus 144-147 10220306-12 1999 Bosentan increased ET-1 levels 2.7 times higher in septic than in nonseptic sheep. Bosentan 0-8 EDN1 Ovis aries 19-23 10220306-13 1999 We conclude that during sepsis, the NO scavenger PHP unmasks an underlying ET-1 mediated vasoconstriction, and its effect is antagonized by L-arginine and bosentan. Bosentan 155-163 EDN1 Ovis aries 75-79 10433505-10 1999 These actions of ET-1 were almost completely prevented by the ET(A) receptor antagonist FR 139317 (1 microM) and the ET(A)/ET(B) receptor antagonist bosentan (10 microM), whereas the ET(B) receptor antagonist BQ 788 (1 microM) had no effect. Bosentan 149-157 endothelin 1 Homo sapiens 17-21 10433505-10 1999 These actions of ET-1 were almost completely prevented by the ET(A) receptor antagonist FR 139317 (1 microM) and the ET(A)/ET(B) receptor antagonist bosentan (10 microM), whereas the ET(B) receptor antagonist BQ 788 (1 microM) had no effect. Bosentan 149-157 endothelin receptor type A Homo sapiens 117-122 10354287-7 1999 The increases in systemic blood pressure (BP), glomerular BP (PGC), RA, and RE and the reduction in Kf seen with systemic NOS inhibition were attenuated by either bosentan or losartan. Bosentan 163-171 progastricsin Rattus norvegicus 62-65 10535692-4 1999 Bosentan markedly reduced the pressor effects elicited by DCLHb, L-NAME, and ET-1, but not those evoked by NA. Bosentan 0-8 endothelin 1 Rattus norvegicus 77-81 10535692-9 1999 They suggest also that nonpeptide endothelin receptor antagonists such as bosentan or LU-135252 may be useful to counteract endothelin-mediated undesirable hemodynamic effects of drugs that inhibit the activity of the NO system. Bosentan 74-82 endothelin 1 Rattus norvegicus 34-44 9792992-1 1998 BACKGROUND: As endothelin-1 exerts positive inotropic effects, the present study evaluated whether the hypotensive effects of the endothelin-1 receptor antagonist bosentan were partially related to a decrease in myocardial performance. Bosentan 163-171 endothelin receptor type A Canis lupus familiaris 130-151 9886874-9 1998 In a 4-week trial the combined ETA/ETB antagonist bosentan reduced the blood pressure of essential hypertensive patients equally to enalapril. Bosentan 50-58 endothelin receptor type B Homo sapiens 35-38 9826312-12 1998 Plasma ET-1 levels increased after bosentan, but baseline levels of the other hormones were unchanged. Bosentan 35-43 endothelin 1 Homo sapiens 7-11 9861300-0 1998 Acute effects of an endothelin-1 receptor antagonist bosentan at different stages of heart failure in conscious dogs. Bosentan 53-61 endothelin receptor type A Canis lupus familiaris 20-41 9777021-5 1998 Contractions induced by endothelin-1 were antagonized by FR 139,317 and bosentan, but not by BQ 788. Bosentan 72-80 endothelin 1 Homo sapiens 24-36 9731554-0 1998 Beneficial hemodynamic effects of bosentan, a mixed ET(A) and ET(B) receptor antagonist, in portal hypertensive rats. Bosentan 34-42 endothelin receptor type A Rattus norvegicus 52-57 9789575-3 1998 Pre-treatment with the non-selective ETA/ETB receptor antagonist bosentan (1 and 10 microM) attenuated this reduction in coronary flow to 16% (P < 0.05) and 8% (P < 0.01), respectively. Bosentan 65-73 endothelin receptor type A Rattus norvegicus 37-40 9605569-12 1998 Bosentan (non-peptide mixed ET(A)/ET(B) receptor antagonist) increased the potency of ET-1 in control rat vessels but was without effect in the pulmonary hypertensive rat vessels. Bosentan 0-8 endothelin 1 Rattus norvegicus 86-90 9693206-7 1998 Myeloperoxidase activity showed a significant increase in ER (7.07 +/- 85.70 U/g; p < 0.001) compared to control (281.16 +/- 43.23 U/g), but BOS had no effect on this increase. Bosentan 144-147 myeloperoxidase Rattus norvegicus 0-15 15992023-2 1998 Bosentan is a combined and competitive antagonist of both ETA and ETB receptors that is selective for the endothelin system. Bosentan 0-8 endothelin receptor type A Rattus norvegicus 58-61 9663924-1 1998 OBJECTIVE: To evaluate whether the cumulative hypotensive effect of the endothelin-1 receptor antagonist bosentan, previously demonstrated in the presence of an angiotensin converting enzyme inhibitor, persists under angiotensin II receptor blockade with losartan. Bosentan 105-113 endothelin receptor type A Canis lupus familiaris 72-93 9663924-7 1998 CONCLUSION: The cumulative hypotensive effect of bosentan suggests that, besides angiotensin II, endothelin-1 is independently involved in the pathophysiology of hypertension, which presents new therapeutic perspectives. Bosentan 49-57 endothelin 1 Canis lupus familiaris 97-109 9672179-8 1998 At this dose, endothelin-1 markedly decreased extravascular albumin space in both controls and micronodular cirrhosis; this could be antagonized by Bosentan 10(-5) mol/l. Bosentan 148-156 endothelin 1 Rattus norvegicus 14-26 9635152-3 1998 The vasodilator and vasoconstrictor components of the biphasic responses to endothelin-1 and sarafotoxin 6c were reduced by bosentan, and the endothelin receptor antagonist reduced baseline systemic arterial and hind-limb perfusion pressures. Bosentan 124-132 endothelin 1 Homo sapiens 76-88 9593320-3 1998 These experiments involved acutely blocking endogenous ET with Bosentan (a non-peptide mixed antagonist to both ET receptor types ETA and ETB), in Sprague-Dawley male rats of various ages: young (4 5 months), middle-aged (12-13 months) and old (19-20 months). Bosentan 63-71 endothelin receptor type B Rattus norvegicus 112-141 9535432-5 1998 ET-induced contraction was shifted to the right in ET-1-treated animals and not modified by BQ123 (an ET(A) receptor antagonist); bosentan (ET(A/B) receptor antagonist) prevented ET-1-induced contraction in both groups. Bosentan 130-138 endothelin 1 Rattus norvegicus 179-183 9535432-13 1998 In cerebral vessels, endothelial alpha2-adrenoceptor-dependent stimulation induced greater contractile responses in treated rats which were sensitive to bosentan, suggesting that oxymetazoline stimulates ET-1 release from the endothelium. Bosentan 153-161 endothelin 1 Rattus norvegicus 204-208 9635152-6 1998 The results of the present study show that bosentan attenuates vasodilator and vasoconstrictor responses to endothelin-1 and sarafotoxin 6c and vasoconstrictor responses to lower doses of angiotensin II in the hind-limb vascular bed of the cat. Bosentan 43-51 endothelin 1 Homo sapiens 108-120 9635152-4 1998 Bosentan decreased vasoconstrictor responses to lower doses of angiotensin II, whereas responses to higher doses of angiotensin II and responses to vasopressin, U46619, BAY K8644, norepinephrine, acetylcholine, bradykinin, levcromakalim, PGE1, adrenomedullin, and calcitonin gene-related peptide were not altered. Bosentan 0-8 angiotensinogen Homo sapiens 63-77 9635152-6 1998 The results of the present study show that bosentan attenuates vasodilator and vasoconstrictor responses to endothelin-1 and sarafotoxin 6c and vasoconstrictor responses to lower doses of angiotensin II in the hind-limb vascular bed of the cat. Bosentan 43-51 angiotensinogen Homo sapiens 188-202 9635152-4 1998 Bosentan decreased vasoconstrictor responses to lower doses of angiotensin II, whereas responses to higher doses of angiotensin II and responses to vasopressin, U46619, BAY K8644, norepinephrine, acetylcholine, bradykinin, levcromakalim, PGE1, adrenomedullin, and calcitonin gene-related peptide were not altered. Bosentan 0-8 kininogen 1 Homo sapiens 211-221 9830507-11 1998 In a study of mild hypertensive patients, the ETA/B antagonist bosentan reduced blood pressure similarly to an ACE inhibitor. Bosentan 63-71 endothelin receptor type A Rattus norvegicus 46-49 9537672-7 1998 Taken together, results from this study implicate the endogenous peptide, ET-1, as a powerful mediator of stress-evoked gastro-duodenal mucosal damage and, moreover, present bosentan as a potential protector against hyperacidity and mucosal erosion that occur as a consequence of stress. Bosentan 174-182 endothelin 1 Rattus norvegicus 74-78 9539881-12 1998 In fresh mesenteric arterial segments FR139317 (ETA receptor antagonist) and bosentan (ETA/ETB receptor antagonist) but not IRL 2500 (ETB receptor antagonist) shifted the ET-1-induced concentration-response curve in parallel to the right. Bosentan 77-85 endothelin receptor type A Rattus norvegicus 87-90 9539881-12 1998 In fresh mesenteric arterial segments FR139317 (ETA receptor antagonist) and bosentan (ETA/ETB receptor antagonist) but not IRL 2500 (ETB receptor antagonist) shifted the ET-1-induced concentration-response curve in parallel to the right. Bosentan 77-85 endothelin receptor type B Rattus norvegicus 91-94 9449383-4 1998 Although bosentan alone did not affect SAP, the development of Ang II-induced hypertension was entirely prevented by the endothelin antagonist. Bosentan 9-17 angiotensinogen Rattus norvegicus 63-69 9449383-5 1998 In addition, the reduction in renal blood flow induced by Ang II (4.9+/-0.3 versus 7.4+/-0.2 mL x min-1 x g-1 in control rats) was prevented by concomitant administration of bosentan (8.8+/-0.8 mL x min-1 x g-1). Bosentan 174-182 angiogenin Rattus norvegicus 58-61 9449383-6 1998 The marked increase in albuminuria observed in rats infused with Ang II (2524+/-961 versus 91+/-6 microg/24 h in control rats) was prevented by bosentan. Bosentan 144-152 angiotensinogen Rattus norvegicus 65-71 9449383-7 1998 Similarly, bosentan abolished the increase in heart weight index (from 2.96+/-0.03 to 3.41+/-0.08 mg/g body weight) and carotid media thickness (from 73+/-14 to 108+/-6 microm) induced by Ang II infusion. Bosentan 11-19 angiotensinogen Rattus norvegicus 188-194 9403621-7 1997 Chronic bosentan treatment also decreased ET-1 levels (390+/-33 versus 475+/-22 pg/g tissue, P<.05) and density of ET-1 receptors (262+/-24 versus 346+/-31 fmol/mg protein, P<.05) in left ventricular myocardium. Bosentan 8-16 endothelin 1 Rattus norvegicus 42-46 9595437-10 1998 The nonselective antagonist bosentan attenuated both phases of the ET-1 response in all three strains. Bosentan 28-36 endothelin 1 Rattus norvegicus 67-71 9553399-15 1998 Endothelin- converting enzyme inhibitor (phosphoramidon) and ET-A/B r antagonists (bosentan, BQ-123, FR139317) may have potential role as vasodilators in the treatment of hypertension. Bosentan 83-91 endothelin receptor type A Homo sapiens 61-67 9595538-4 1998 Fibroblast ET-1 binding sites were measured using 125I-labeled ET-1, and the modulation of ICAM-1 function by ET-1 was determined by measuring the binding of human U937 cells to fibroblasts in the presence of a mixed ETA/B receptor antagonist (bosentan) or a neutralizing anti-ICAM-1 antibody. Bosentan 244-252 intercellular adhesion molecule 1 Homo sapiens 91-97 9595538-7 1998 RT-PCR demonstrated that ICAM-1 mRNA was upregulated by ET-1, and results from binding studies showed fibroblasts exposed to ET-1 supported more U937 cells than controls, a process that could be inhibited by bosentan and ICAM-1 neutralizing antibody. Bosentan 208-216 intercellular adhesion molecule 1 Homo sapiens 25-31 9595538-7 1998 RT-PCR demonstrated that ICAM-1 mRNA was upregulated by ET-1, and results from binding studies showed fibroblasts exposed to ET-1 supported more U937 cells than controls, a process that could be inhibited by bosentan and ICAM-1 neutralizing antibody. Bosentan 208-216 intercellular adhesion molecule 1 Homo sapiens 221-227 9403621-7 1997 Chronic bosentan treatment also decreased ET-1 levels (390+/-33 versus 475+/-22 pg/g tissue, P<.05) and density of ET-1 receptors (262+/-24 versus 346+/-31 fmol/mg protein, P<.05) in left ventricular myocardium. Bosentan 8-16 endothelin 1 Rattus norvegicus 118-122 9324107-13 1997 Chronic bosentan treatment of the F group restored the maximum tension responses of arteries to ET-1 [(+) in the FB group: 1.88 +/- 0.12 g/mm3 v C, P > .05, (-): 1.95 +/- 0.05 g/mm3 v C, P > .05] but had no effect on the responses of the CB group. Bosentan 8-16 endothelin 1 Rattus norvegicus 96-100 9403591-0 1997 Bosentan prevents preglomerular alterations during angiotensin II hypertension. Bosentan 0-8 angiotensinogen Rattus norvegicus 51-65 9403591-10 1997 AR were inhibited in Ang II-treated rats along ILA and AA; Ang II-induced AR changes were prevented by bosentan. Bosentan 103-111 angiotensinogen Rattus norvegicus 21-27 9403591-10 1997 AR were inhibited in Ang II-treated rats along ILA and AA; Ang II-induced AR changes were prevented by bosentan. Bosentan 103-111 angiotensinogen Rattus norvegicus 59-65 9386175-4 1997 Bolus injections of bosentan (mixed ET(A)/ET(B) receptor antagonist, 10 mg/kg I.V.) Bosentan 20-28 endothelin receptor type A Rattus norvegicus 36-41 9386175-4 1997 Bolus injections of bosentan (mixed ET(A)/ET(B) receptor antagonist, 10 mg/kg I.V.) Bosentan 20-28 endothelin receptor type B Rattus norvegicus 42-47 9386175-7 1997 In an isolated perfused rat heart preparation, infusion of bosentan (1 micromol/L) for 2 hours inhibited the mechanical stretch-induced increase in BNP mRNA levels in the right atria, whereas an AT1 receptor antagonist, CV-11974 (10 nmol/L), had no effect. Bosentan 59-67 natriuretic peptide B Rattus norvegicus 148-151 9401758-14 1997 The AII-induced femoral vasodilatation was suppressed by blockade of nitric oxide (NO) synthesis with NG-nitro-L-arginine methyl ester (L-NAME, 40 mumol kg-1) and reversed to vasoconstriction when L-NAME was combined with indomethacin (30 mumol kg-1), but was left unaltered by antagonism of endothelin ETA/B receptors with bosentan (37 mumol kg-1). Bosentan 324-332 angiotensinogen Rattus norvegicus 4-7 9401760-19 1997 Bosentan is more efficacious than PD 142893 in inhibiting the venous effects of ET-1. Bosentan 0-8 endothelin 1 Rattus norvegicus 80-84 9338430-3 1997 A single dose of the nonspecific ET blocker bosentan (100 mg/kg) given to intact rats by gavage completely blocked the pulmonary vasoconstrictor actions of Big ET-1 and partially blunted hypoxic pulmonary vasoconstriction. Bosentan 44-52 endothelin 1 Rattus norvegicus 160-164 9338430-6 1997 Bosentan raised plasma ET-1 levels but had no effect on lung ET-1 levels. Bosentan 0-8 endothelin 1 Rattus norvegicus 23-27 9294120-9 1997 Finally, in vivo administration of bosentan, an endothelin receptor antagonist, totally prevented lethality in Vim-/- mice. Bosentan 35-43 vimentin Mus musculus 111-114 9346328-3 1997 Pretreatment with bosentan failed to change hemodynamic responses of WKY to vasopressin, but it blunted the increases in blood pressure and the decreases in conductance evoked by vasopressin in SHR. Bosentan 18-26 arginine vasopressin Rattus norvegicus 179-190 9346328-5 1997 Except at the highest dose of vasopressin, bosentan abolished the exaggerated pressor responsiveness of the SHR to vasopressin. Bosentan 43-51 arginine vasopressin Rattus norvegicus 115-126 9324107-14 1997 In arteries with intact endothelium, bosentan treatment restored the sensitivity of the F arteries to ET-1 (pD2 values FB 8.82 +/- 0.05 v C, P < .05). Bosentan 37-45 endothelin 1 Rattus norvegicus 102-106 9324107-16 1997 These data suggest that mesenteric arteries from FH demonstrate a specific alteration towards the reactivity to ET-1, which is restored by long-term bosentan treatment. Bosentan 149-157 endothelin 1 Rattus norvegicus 112-116 9404419-0 1997 [Bosentan attenuates the hypertensive effect of angiotensin II in rats]. Bosentan 1-9 angiotensinogen Rattus norvegicus 48-62 9404419-4 1997 [table: see text] Tail-cuff pressure increased from 126 +/- 4 to 164 +/- 8 mmHg in rats infused with AngII alone whereas it did not change (basal: 132 +/- 3 and final: 135 +/- 3 mmHg: p = NS) when bosentan was coadministered with AngII. Bosentan 197-205 angiotensinogen Rattus norvegicus 101-106 9404419-6 1997 In AngII-perfused rats, CO, RBF, TPR and RVR were restored by bosentan to values observed in untreated rats. Bosentan 62-70 angiotensinogen Rattus norvegicus 3-8 9404419-6 1997 In AngII-perfused rats, CO, RBF, TPR and RVR were restored by bosentan to values observed in untreated rats. Bosentan 62-70 translocated promoter region, nuclear basket protein Rattus norvegicus 33-36 9404419-7 1997 These results indicate that blockade of endothelin A and B receptors by bosentan prevents the development of AngII-induced hypertension through attenuation of the effect of AngII on vascular tone and suggest that endothelin is an important mediator of the vasoconstrictor action of angiotensin II in rats. Bosentan 72-80 angiotensinogen Rattus norvegicus 109-114 9404419-7 1997 These results indicate that blockade of endothelin A and B receptors by bosentan prevents the development of AngII-induced hypertension through attenuation of the effect of AngII on vascular tone and suggest that endothelin is an important mediator of the vasoconstrictor action of angiotensin II in rats. Bosentan 72-80 angiotensinogen Rattus norvegicus 173-178 9246031-7 1997 However, the greater protection observed with bosentan than with radical scavengers might reflect a preferential role of endothelin-1 in this type of injury. Bosentan 46-54 endothelin 1 Rattus norvegicus 121-133 9176305-3 1997 Despite this increase in ET-1 production, there was no difference in baseline systemic or pulmonary arterial pressures between control and endotoxin-treated rats, and, furthermore, combined ETA/ETB receptor antagonism using bosentan produced reductions in systemic and pulmonary arterial pressures that were not greater than the modest fall seen in controls. Bosentan 224-232 endothelin 1 Rattus norvegicus 25-29 9201101-2 1997 In this study we investigated the influence of a mixed ETA-, ETB-receptor antagonist (Bosentan) on ischemia-reperfusion damage of the liver by means of intravital fluorescence microscopy (IVM). Bosentan 86-94 endothelin receptor type A Rattus norvegicus 55-58 9186867-12 1997 In addition, bosentan coadministered with L-NAME in vivo blunted the inhibitory effect of L-NAME and restored the increases in renin mRNA level, synthesis and secretion. Bosentan 13-21 renin Rattus norvegicus 127-132 9176269-6 1997 The combined ETA-ETB antagonist, bosentan, also inhibited ET-1-induced mitogenesis (IC50 = 20 nM, slope of 0.60). Bosentan 33-41 endothelin receptor type A Homo sapiens 13-16 9176269-6 1997 The combined ETA-ETB antagonist, bosentan, also inhibited ET-1-induced mitogenesis (IC50 = 20 nM, slope of 0.60). Bosentan 33-41 endothelin receptor type B Homo sapiens 17-20 9176269-6 1997 The combined ETA-ETB antagonist, bosentan, also inhibited ET-1-induced mitogenesis (IC50 = 20 nM, slope of 0.60). Bosentan 33-41 endothelin 1 Homo sapiens 58-62 9176269-7 1997 The effects of BQ-788 and bosentan appear to be mediated via the same receptor (ETB), as their slopes are comparable. Bosentan 26-34 endothelin receptor type B Homo sapiens 80-83 9146895-8 1997 Both effects were antagonized by the ETA/ETB-receptor antagonist bosentan and the ETA-receptor antagonist BQ-123, but not affected by the ETB-receptor antagonist IRL 1038 and the AT1-receptor antagonist losartan. Bosentan 65-73 endothelin receptor type A Rattus norvegicus 37-53 9146895-8 1997 Both effects were antagonized by the ETA/ETB-receptor antagonist bosentan and the ETA-receptor antagonist BQ-123, but not affected by the ETB-receptor antagonist IRL 1038 and the AT1-receptor antagonist losartan. Bosentan 65-73 endothelin receptor type A Rattus norvegicus 37-40 9196318-2 1997 We tested the hypothesis that inhibition of ET synthesis during cardioplegic arrest using phosphoramidon (an ET converting enzyme inhibitor) or blockade of ET receptors using bosentan (a mixed ET(A)/ET(B) antagonist), might improve the postischaemic recovery of coronary flow. Bosentan 175-183 endothelin receptor type B Rattus norvegicus 199-204 9176305-3 1997 Despite this increase in ET-1 production, there was no difference in baseline systemic or pulmonary arterial pressures between control and endotoxin-treated rats, and, furthermore, combined ETA/ETB receptor antagonism using bosentan produced reductions in systemic and pulmonary arterial pressures that were not greater than the modest fall seen in controls. Bosentan 224-232 endothelin receptor type A Rattus norvegicus 190-193 9176305-3 1997 Despite this increase in ET-1 production, there was no difference in baseline systemic or pulmonary arterial pressures between control and endotoxin-treated rats, and, furthermore, combined ETA/ETB receptor antagonism using bosentan produced reductions in systemic and pulmonary arterial pressures that were not greater than the modest fall seen in controls. Bosentan 224-232 endothelin receptor type B Rattus norvegicus 194-197 9176305-4 1997 However, bosentan completely antagonized the hemodynamic effects of exogenous ET-1 in controls but only weakly antagonized its effects in LPS animals. Bosentan 9-17 endothelin 1 Rattus norvegicus 78-82 9145775-3 1997 Bosentan and FR 139317 (each 10 microM) produced a small shift in response curves to endothelin-1 (1.6- and 1.5-fold, respectively). Bosentan 0-8 endothelin 1 Homo sapiens 85-97 9068974-7 1997 The combined ETA/B receptor blocker bosentan (Ro 47-0203) eliminated the ET-3-evoked neuronal effect. Bosentan 36-44 endothelin 3 Rattus norvegicus 73-77 9085162-0 1997 Bosentan, a novel synthetic mixed-type endothelin receptor antagonist, attenuates acute gastric mucosal lesions induced by indomethacin and HCl in the rat: role of endogenous endothelin-1. Bosentan 0-8 endothelin 1 Rattus norvegicus 175-187 8978330-4 1997 Both the ETA receptor antagonist BQ-123 and ETA/ETB receptor antagonist bosentan decreased plasma ANP and NT-ANP responses to volume load (P < .05 to .001), whereas the AT1 receptor antagonist losartan had no significant effect on this response. Bosentan 72-80 endothelin receptor type A Rattus norvegicus 44-47 9110115-0 1997 Acute and short-term effects of the nonpeptide endothelin-1 receptor antagonist bosentan in humans. Bosentan 80-88 endothelin receptor type A Homo sapiens 47-68 9107557-8 1997 Similarly, the ETA/ETB receptor antagonist, bosentan (0.1, 10 and 1,000 nM), induced a concentration-dependent decrease in the contraction. Bosentan 44-52 endothelin receptor type A Rattus norvegicus 15-18 9107557-8 1997 Similarly, the ETA/ETB receptor antagonist, bosentan (0.1, 10 and 1,000 nM), induced a concentration-dependent decrease in the contraction. Bosentan 44-52 endothelin receptor type B Rattus norvegicus 19-22 9016927-5 1996 In the spleen, both the extraction and vascular effects of exogenous endothelin-1 were attenuated by both bosentan and PD155080 whereas renal extraction and vascular effects in the kidney were unaffected by both drugs. Bosentan 106-114 endothelin-1 Sus scrofa 69-81 9380222-5 1997 The ETA/ETB receptor blocker bosentan restored GFR and the renal concentrating ability. Bosentan 29-37 endothelin receptor type A Homo sapiens 4-7 9380222-5 1997 The ETA/ETB receptor blocker bosentan restored GFR and the renal concentrating ability. Bosentan 29-37 endothelin receptor type B Homo sapiens 8-11 9265559-6 1997 The dose-dependent systemic vasoconstriction evoked by ET-1 infusion was reduced after administration of the combined ETA and ETB receptor antagonist bosentan as well as the selective ETA receptor blockers BMS-182874 and TBC-11251 indicating that this effect is primarily mediated by ETA receptors. Bosentan 150-158 endothelin 1 Homo sapiens 55-59 9265559-6 1997 The dose-dependent systemic vasoconstriction evoked by ET-1 infusion was reduced after administration of the combined ETA and ETB receptor antagonist bosentan as well as the selective ETA receptor blockers BMS-182874 and TBC-11251 indicating that this effect is primarily mediated by ETA receptors. Bosentan 150-158 endothelin receptor type A Homo sapiens 118-121 9265559-6 1997 The dose-dependent systemic vasoconstriction evoked by ET-1 infusion was reduced after administration of the combined ETA and ETB receptor antagonist bosentan as well as the selective ETA receptor blockers BMS-182874 and TBC-11251 indicating that this effect is primarily mediated by ETA receptors. Bosentan 150-158 endothelin receptor type B Sus scrofa 126-129 9265559-12 1997 The plasma levels of ET-1 increased following the non-selective ET receptor antagonist bosentan but were unaffected by selective ETA receptor antagonism. Bosentan 87-95 endothelin 1 Homo sapiens 21-25 9265559-24 1997 The concentration-dependent contraction evoked by ET-1 in human vessels in vitro (LAD, IMA, PA, SV) was reduced after incubation with BQ-123 and bosentan. Bosentan 145-153 endothelin 1 Homo sapiens 50-54 9444527-3 1997 In human intralobar artery and rat main pulmonary artery, bosentan (3 and 10 microM) shifted the endothelin-1 concentration response curve to a higher concentration range (endothelin-1 concentration ratios, in human intralobar and rat main pulmonary artery, respectively: 3 microM bosentan, 4.5 and 8.1; 10 microM bosentan, 13.5 and 19.5), but caused no significant block of endothelin-1 in rat intralobar artery. Bosentan 58-66 endothelin 1 Rattus norvegicus 97-109 9444527-3 1997 In human intralobar artery and rat main pulmonary artery, bosentan (3 and 10 microM) shifted the endothelin-1 concentration response curve to a higher concentration range (endothelin-1 concentration ratios, in human intralobar and rat main pulmonary artery, respectively: 3 microM bosentan, 4.5 and 8.1; 10 microM bosentan, 13.5 and 19.5), but caused no significant block of endothelin-1 in rat intralobar artery. Bosentan 58-66 endothelin 1 Rattus norvegicus 172-184 9444527-3 1997 In human intralobar artery and rat main pulmonary artery, bosentan (3 and 10 microM) shifted the endothelin-1 concentration response curve to a higher concentration range (endothelin-1 concentration ratios, in human intralobar and rat main pulmonary artery, respectively: 3 microM bosentan, 4.5 and 8.1; 10 microM bosentan, 13.5 and 19.5), but caused no significant block of endothelin-1 in rat intralobar artery. Bosentan 58-66 endothelin 1 Rattus norvegicus 172-184 9444527-4 1997 The latter finding may be due to the reported presence of ETB receptors in rat intralobar arteries and the higher potency of bosentan on ETA than on ETB receptors. Bosentan 125-133 endothelin receptor type A Rattus norvegicus 137-140 9444527-4 1997 The latter finding may be due to the reported presence of ETB receptors in rat intralobar arteries and the higher potency of bosentan on ETA than on ETB receptors. Bosentan 125-133 endothelin receptor type B Rattus norvegicus 149-152 9069452-5 1997 The mitogenic effect of endothelial cells in coculture resulted from ET-1 production since it was suppressed by bosentan, a mixed specific ET-1 receptor antagonist. Bosentan 112-120 endothelin 1 Homo sapiens 69-73 9069452-5 1997 The mitogenic effect of endothelial cells in coculture resulted from ET-1 production since it was suppressed by bosentan, a mixed specific ET-1 receptor antagonist. Bosentan 112-120 endothelin 1 Homo sapiens 139-143 9016927-6 1996 In the lung, only bosentan decreased pulmonary extraction of endothelin-1. Bosentan 18-26 endothelin-1 Sus scrofa 61-73 9016927-7 1996 In conclusion, the bosentan-induced increase of circulating endothelin-1 seems to be related to blockade of endothelin-1 binding to endothelin ET(B) receptors. Bosentan 19-27 endothelin-1 Sus scrofa 60-72 9016927-7 1996 In conclusion, the bosentan-induced increase of circulating endothelin-1 seems to be related to blockade of endothelin-1 binding to endothelin ET(B) receptors. Bosentan 19-27 endothelin-1 Sus scrofa 108-120 8997390-4 1996 The medullary vasodilation induced by ET-1 was observed with doses lower than that required to produce cortical vasoconstriction; was completely blocked by bosentan, a mixed ETA/B-receptor antagonist; and was mimicked by IRL-1620, a specific ETB-receptor agonist. Bosentan 156-164 endothelin 1 Rattus norvegicus 38-42 8997390-4 1996 The medullary vasodilation induced by ET-1 was observed with doses lower than that required to produce cortical vasoconstriction; was completely blocked by bosentan, a mixed ETA/B-receptor antagonist; and was mimicked by IRL-1620, a specific ETB-receptor agonist. Bosentan 156-164 endothelin receptor type B Rattus norvegicus 242-245 8916269-3 1996 Binding of [3H]bosentan was inhibited by unlabelled bosentan and endothelin-1 at high concentrations, suggesting specific binding of the antagonist. Bosentan 15-23 endothelin 1 Rattus norvegicus 65-77 8944823-8 1996 Both the nonselective ETA/ETB receptor antagonist bosentan (1 microM) and the ET(A)-receptor-selective antagonist BQ 123 (2 microM) abolished protection from ET-1 (infarct size: 43.3 +/- 3.5 and 41.3 +/- 3.3%, respectively), as did the PKC inhibitor chelerythrine (2 microM) (infarct size: 41.1 +/- 5.2%) and the KATP blocker 5-hydroxydecanoate (infarct size: 41.7 +/- 2.9%). Bosentan 50-58 endothelin receptor type A Rattus norvegicus 22-25 8940346-12 1996 Endothelin-1, a vasoconstrictor peptide that is known to promote fibroblast-embedded collagen gel contraction, appeared to be partially involved in the IGF-I- and IGFBP-1-induced gel contraction, because the addition of an endothelin receptor antagonist (Bosentan or BE-18257B at 1 microg/ml) moderately suppressed the IGF-I- and IGFBP-1-induced gel contraction (P < 0.01). Bosentan 255-263 endothelin 1 Homo sapiens 0-12 8940346-12 1996 Endothelin-1, a vasoconstrictor peptide that is known to promote fibroblast-embedded collagen gel contraction, appeared to be partially involved in the IGF-I- and IGFBP-1-induced gel contraction, because the addition of an endothelin receptor antagonist (Bosentan or BE-18257B at 1 microg/ml) moderately suppressed the IGF-I- and IGFBP-1-induced gel contraction (P < 0.01). Bosentan 255-263 insulin like growth factor 1 Homo sapiens 152-157 8940346-12 1996 Endothelin-1, a vasoconstrictor peptide that is known to promote fibroblast-embedded collagen gel contraction, appeared to be partially involved in the IGF-I- and IGFBP-1-induced gel contraction, because the addition of an endothelin receptor antagonist (Bosentan or BE-18257B at 1 microg/ml) moderately suppressed the IGF-I- and IGFBP-1-induced gel contraction (P < 0.01). Bosentan 255-263 insulin like growth factor binding protein 1 Homo sapiens 163-170 8901827-5 1996 Strikingly, bosentan pretreatment blunted the increases in blood pressure, the fall in cardiac output, and the decreases in conductance evoked by lower doses of Ang II but not higher doses of the peptide. Bosentan 12-20 angiotensinogen Rattus norvegicus 161-167 8874149-10 1996 Daily treatment with bosentan dose-dependently reduced colonic damage and myeloperoxidase activity when bosentan was given prior to induction of colitis. Bosentan 21-29 myeloperoxidase Rattus norvegicus 74-89 8899066-4 1996 Pre-treatment with Bosentan reduced ET-1-LI content in the lung parenchyma but increased ET-1-LI levels in BALF, possibly indicating an effective displacement of ET-1 from its receptors. Bosentan 19-27 endothelin 1 Rattus norvegicus 36-40 8899066-4 1996 Pre-treatment with Bosentan reduced ET-1-LI content in the lung parenchyma but increased ET-1-LI levels in BALF, possibly indicating an effective displacement of ET-1 from its receptors. Bosentan 19-27 endothelin 1 Rattus norvegicus 89-93 8899066-4 1996 Pre-treatment with Bosentan reduced ET-1-LI content in the lung parenchyma but increased ET-1-LI levels in BALF, possibly indicating an effective displacement of ET-1 from its receptors. Bosentan 19-27 endothelin 1 Rattus norvegicus 89-93 8899066-7 1996 If anything, Bosentan enhanced the oedema formation in parallel with increased ET-1-LI in BALF. Bosentan 13-21 endothelin 1 Rattus norvegicus 79-83 8873714-5 1996 After administration of bosentan, the vasopressor effect of endothelin-1 during normoxia was significantly attenuated and the pulmonary vasodilatory effect of endothelin-1 during hypoxia was reduced. Bosentan 24-32 endothelin-1 Sus scrofa 60-72 8873714-5 1996 After administration of bosentan, the vasopressor effect of endothelin-1 during normoxia was significantly attenuated and the pulmonary vasodilatory effect of endothelin-1 during hypoxia was reduced. Bosentan 24-32 endothelin-1 Sus scrofa 159-171 8823303-9 1996 Bosentan reduced levels of type I collagen and cellular fibronectin mRNAs in whole-liver tissue extracts in both models. Bosentan 0-8 fibronectin 1 Homo sapiens 56-67 8872972-6 1996 The administration of bosentan, an ETA/ETB receptor antagonist, had a beneficial effect on the evolution of nephritis preventing the appearance of intense proteinuria (76 +/- 35 vs. 380 +/- 77 mg/24 hr, N = 4 to 5, P < 0.05), the morphological lesions and the renal function impairment (creatinine clearance 367 +/- 46 vs. 268 +/- 33 microliters/min/100 g, N = 4 to 5). Bosentan 22-30 endothelin receptor type A Rattus norvegicus 35-38 8872972-6 1996 The administration of bosentan, an ETA/ETB receptor antagonist, had a beneficial effect on the evolution of nephritis preventing the appearance of intense proteinuria (76 +/- 35 vs. 380 +/- 77 mg/24 hr, N = 4 to 5, P < 0.05), the morphological lesions and the renal function impairment (creatinine clearance 367 +/- 46 vs. 268 +/- 33 microliters/min/100 g, N = 4 to 5). Bosentan 22-30 endothelin receptor type B Rattus norvegicus 39-42 8772702-2 1996 In the present study, we examined the effects of intravenous bosentan, a nonpeptide, competitive endothelin-1 receptor antagonist, on hemodynamics in dogs with chronic heart failure. Bosentan 61-69 endothelin receptor type A Canis lupus familiaris 97-118 8864526-14 1996 The ETA receptor antagonist, BQ123, did not affect these depressor responses whereas the mixed ETA/ETB antagonist, bosentan, blocked them. Bosentan 115-123 endothelin receptor type A Rattus norvegicus 95-98 8864526-14 1996 The ETA receptor antagonist, BQ123, did not affect these depressor responses whereas the mixed ETA/ETB antagonist, bosentan, blocked them. Bosentan 115-123 endothelin receptor type B Rattus norvegicus 99-102 8681627-11 1996 This was reduced to 4 +/- 17% (p < 0.01, n = 6) in rings treated with both 10(-8) mol/L endothelin-1 and 10(-5) mol/L bosentan. Bosentan 121-129 endothelin 1 Rattus norvegicus 91-110 8823230-8 1996 Plasma ET-1 increased maximally twofold (oral) and threefold (intravenous), and this increase was directly related to bosentan plasma concentrations according to an Emax model. Bosentan 118-126 endothelin 1 Homo sapiens 7-11 8823230-9 1996 Bosentan reversed the vasoconstrictor effect of ET-1 measured in the skin microcirculation. Bosentan 0-8 endothelin 1 Homo sapiens 48-52 8823230-13 1996 CONCLUSION: Bosentan is an orally bioavailable, well-tolerated, and active ET-1 antagonist with a low clearance and a moderate volume of distribution. Bosentan 12-20 endothelin 1 Homo sapiens 75-79 8751489-10 1996 Furthermore, contractions evoked by endothelin-1 in the left anterior descending coronary and pulmonary arteries were antagonized by the combined endothelinA- and endothelinB-receptor blocker bosentan. Bosentan 192-200 endothelin 1 Homo sapiens 36-48 8751489-10 1996 Furthermore, contractions evoked by endothelin-1 in the left anterior descending coronary and pulmonary arteries were antagonized by the combined endothelinA- and endothelinB-receptor blocker bosentan. Bosentan 192-200 endothelin receptor type B Homo sapiens 146-183 8832068-5 1996 When vessels were preincubated with bosentan, an endothelinA- and endothelinB-receptor antagonist, in addition to L-NAME, acetylcholine-induced contraction was reduced to 8 +/- 2% (P < 0.01) of KCl contractions. Bosentan 36-44 endothelin receptor type B Rattus norvegicus 49-86 8762086-0 1996 Bosentan-improved cardiopulmonary vascular performance and increased plasma levels of endothelin-1 in porcine endotoxin shock. Bosentan 0-8 endothelin-1 Sus scrofa 86-98 8707268-9 1996 Finally, the mixed endothelin-A (ETA) and ETB receptor antagonist, bosentan, reduced portal pressure in portal hypertensive animals, consistent with its inhibitory effect on stellate cell contraction. Bosentan 67-75 endothelin receptor type B Rattus norvegicus 42-54 8798262-5 1996 Therefore, we studied and compared the changes in pulmonary hemodynamics associated with in utero O2 ventilation with and without ET-1 receptor blockade induced by an infusion of Ro 47-0203 (Bosentan, a nonselective ET receptor antagonist), in 13 late-gestation fetal lambs. Bosentan 179-189 EDN1 Ovis aries 130-134 8828566-2 1996 This effect could be abolished by pretreatment with either the endothelin ETA/B receptor antagonist bosentan (1 nmol, intrastriatally) or the dopamine D2 receptor antagonist raclopride (0.1 mg/kg, s.c.) suggesting that endothelin is acting at endothelin receptors to evoke ipsilateral turning behaviour and that this response is mediated by dopamine. Bosentan 100-108 endothelin receptor type A Rattus norvegicus 74-77 8762086-16 1996 Bosentan caused an increase of the basal arterial plasma levels of ET-1-like immunoreactivity (LI), from 16.8 +/- 1.3 pM to 49.6 +/- 10.0 pM (n = 6, P < 0.01). Bosentan 0-8 endothelin-1 Sus scrofa 67-71 8762086-18 1996 Repeated administration of bosentan during LPS infusion caused an additional increase of ET-1-LI levels. Bosentan 27-35 endothelin-1 Sus scrofa 89-93 8528554-0 1995 Effects of the ETA/ETB receptor antagonist, bosentan on endothelin-1-induced myocardial ischaemia and oedema in the rat. Bosentan 44-52 endothelin 1 Rattus norvegicus 56-68 8640984-1 1996 Acute effects of bosentan, an orally active, mixed endothelin ETA and ETB receptor antagonist. Bosentan 17-25 endothelin receptor type A Rattus norvegicus 62-65 8640984-12 1996 Bosentan attenuated norepinephrine-induced increases in ventricular weight, ratio of RNA to protein, and expression of skeletal alpha-actin mRNA and beta-myosin heavy chain mRNA at 5 days, but it did not attenuate increased ventricular expression of atrial natriuretic factor mRNA. Bosentan 0-8 myosin heavy chain 7 Rattus norvegicus 149-172 8662290-7 1996 BQ123, an inhibitor of ETA receptors, did not prevent ET-1-mediated signalling in BBM, but an ETA,B antagonist, bosentan, inhibited ET-3-mediated signalling in BBM. Bosentan 112-120 endothelin receptor type A Rattus norvegicus 94-97 8689641-9 1996 The blockade of both ETA and ETB by bosentan had no further effect on MAP reduction or RBF increase in SHR compared to the ETA blockade by BQ 123. Bosentan 36-44 endothelin receptor type B Rattus norvegicus 29-32 8689641-10 1996 The ETA antagonist BQ 123 had no effect on GFR either in SHR or in WKY, whereas the combined blockade of ETA and ETB by bosentan significantly decreased GFR in SHR by about 50% but not in WKY. Bosentan 120-128 endothelin receptor type A Rattus norvegicus 105-108 8689641-10 1996 The ETA antagonist BQ 123 had no effect on GFR either in SHR or in WKY, whereas the combined blockade of ETA and ETB by bosentan significantly decreased GFR in SHR by about 50% but not in WKY. Bosentan 120-128 endothelin receptor type B Rattus norvegicus 113-116 8748689-7 1995 Bosentan treatment of rats undergoing CCl4 inhalation resulted in a significant protection against elevation of ALT, AST, LDH and bilirubin. Bosentan 0-8 C-C motif chemokine ligand 4 Rattus norvegicus 38-42 8748689-7 1995 Bosentan treatment of rats undergoing CCl4 inhalation resulted in a significant protection against elevation of ALT, AST, LDH and bilirubin. Bosentan 0-8 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 117-120 7658874-2 1995 The role of endogenously released endothelin-1 in the maintenance of vascular tone in chronic heart failure was assessed by acute administration of an endothelin receptor antagonist, bosentan. Bosentan 183-191 endothelin 1 Homo sapiens 34-46 7658874-8 1995 Plasma endothelin-1 concentrations rose more than twofold from baseline in bosentan recipients while big-endothelin-1 concentrations were unchanged. Bosentan 75-83 endothelin 1 Homo sapiens 7-19 8528554-15 1995 Pretreatment of the animals with bosentan (10 mg kg-1) inhibited by 71 and 90% the depressor and pressor actions of ET-1 (1 nmol kg-1) and the accompanying tachycardia and bradycardia, respectively. Bosentan 33-41 endothelin 1 Rattus norvegicus 116-120 8528554-17 1995 ET-1-induced albumin extravasation was completely inhibited by bosentan (10 mg kg-1) both in the left ventricle and right atrium, compared to the 86% inhibition observed with FR 139317 (2.5 mg kg-1).6. Bosentan 63-71 endothelin 1 Rattus norvegicus 0-4 8528554-21 1995 These results indicate that ETB receptors, albeit to a lesser extent than ETA receptors, are also involved in mediating ET-1-induced myocardial ischaemia and oedema in the rat, and suggest the therapeutic potential for bosentan in the treatment of ischaemic myocardial diseases. Bosentan 219-227 endothelin receptor type B Rattus norvegicus 28-31 8528554-21 1995 These results indicate that ETB receptors, albeit to a lesser extent than ETA receptors, are also involved in mediating ET-1-induced myocardial ischaemia and oedema in the rat, and suggest the therapeutic potential for bosentan in the treatment of ischaemic myocardial diseases. Bosentan 219-227 endothelin 1 Rattus norvegicus 120-124 8621208-7 1996 Ccr was remarkably improved in CsA-treated rats that received bosentan, the combined antagonist of both endothelin A and endothelin B receptors. Bosentan 62-70 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 31-34 8602109-2 1996 Preinjection (10 min before) of BQ-788 (an ETB receptor selective antagonist; 5 nmol) or bosentan (an ETA/ETB receptor non-selective antagonist; 10 nmol) to the PAG reduced the behavioral response to ET-1. Bosentan 89-97 endothelin receptor type A Rattus norvegicus 102-105 8602109-2 1996 Preinjection (10 min before) of BQ-788 (an ETB receptor selective antagonist; 5 nmol) or bosentan (an ETA/ETB receptor non-selective antagonist; 10 nmol) to the PAG reduced the behavioral response to ET-1. Bosentan 89-97 endothelin receptor type B Rattus norvegicus 106-109 8602109-2 1996 Preinjection (10 min before) of BQ-788 (an ETB receptor selective antagonist; 5 nmol) or bosentan (an ETA/ETB receptor non-selective antagonist; 10 nmol) to the PAG reduced the behavioral response to ET-1. Bosentan 89-97 endothelin 1 Rattus norvegicus 200-204 8876667-4 1996 The results show that the sensitivity of basilar artery to Bay K 8644 was increased by salt load and that this hypersensitivity was blunted by bosentan, an ETA/ETB antagonist. Bosentan 143-151 endothelin receptor type A Rattus norvegicus 156-159 8876667-4 1996 The results show that the sensitivity of basilar artery to Bay K 8644 was increased by salt load and that this hypersensitivity was blunted by bosentan, an ETA/ETB antagonist. Bosentan 143-151 endothelin receptor type B Rattus norvegicus 160-163 8748689-2 1995 Wistar Kyoto rats were divided into four groups: a bosentan (mixed endothelin ETA and ETB receptor antagonist) treated group with CCl4 intoxication, a vehicle treated group with CCl4 intoxication, a nontreated control group and a bosentan treated control group. Bosentan 51-59 C-C motif chemokine ligand 4 Rattus norvegicus 130-134 9072349-9 1995 Treatment of DOCA-salt hypertensive rats with the combined ETA/ETB endothelin antagonist bosentan lowered blood pressure slightly, but vascular hypertrophy regressed almost completely and any hypertrophy remaining could be explained by the residual elevated blood pressure. Bosentan 89-97 endothelin receptor type A Rattus norvegicus 59-62 7485537-8 1995 Both ramipril (an angiotensin-converting enzyme inhibitor, 7.5 mg/kg daily) and bosentan (a nonselective ET receptor antagonist, 100 mg/kg daily) substantially reduced the elevation in ET-1 mRNA seen in the clipped kidney after 2 days, suggesting that the generation of angiotensin II and the action of ET itself are involved in the mechanism by which clipping stimulates ET-1 expression. Bosentan 80-88 endothelin 1 Rattus norvegicus 185-189 7485537-8 1995 Both ramipril (an angiotensin-converting enzyme inhibitor, 7.5 mg/kg daily) and bosentan (a nonselective ET receptor antagonist, 100 mg/kg daily) substantially reduced the elevation in ET-1 mRNA seen in the clipped kidney after 2 days, suggesting that the generation of angiotensin II and the action of ET itself are involved in the mechanism by which clipping stimulates ET-1 expression. Bosentan 80-88 angiotensinogen Rattus norvegicus 270-284 7485537-8 1995 Both ramipril (an angiotensin-converting enzyme inhibitor, 7.5 mg/kg daily) and bosentan (a nonselective ET receptor antagonist, 100 mg/kg daily) substantially reduced the elevation in ET-1 mRNA seen in the clipped kidney after 2 days, suggesting that the generation of angiotensin II and the action of ET itself are involved in the mechanism by which clipping stimulates ET-1 expression. Bosentan 80-88 endothelin 1 Rattus norvegicus 372-376 7498305-2 1995 Endothelin-1 (0.012-0.4 nmol) evoked dose-dependent reduction in coronary flow, which was attenuated by bosentan (1.0-10 microM) in a concentration-related fashion. Bosentan 104-112 endothelin 1 Rattus norvegicus 0-12 8528554-2 1995 The purpose of this study were to assess the role of ETB receptors in mediating endothelin-1 (ET-1)-induced myocardial ischaemia and oedema in rats and to study the inhibitory action of the novel nonpeptide ETA/ETB receptor antagonist, bosentan on these actions of ET-1. Bosentan 236-244 endothelin receptor type A Rattus norvegicus 207-210 8546870-3 1995 Application of bosentan (10 microM; and ETA and ETB receptor antagonist) and FR 139317 (1-10 microM; a selective ETA receptor antagonist) prevented initiation of inward currents or enhancement of Iout by ET-1. Bosentan 15-23 endothelin receptor type A Rattus norvegicus 40-43 8546870-3 1995 Application of bosentan (10 microM; and ETA and ETB receptor antagonist) and FR 139317 (1-10 microM; a selective ETA receptor antagonist) prevented initiation of inward currents or enhancement of Iout by ET-1. Bosentan 15-23 endothelin receptor type A Rattus norvegicus 113-116 8546870-3 1995 Application of bosentan (10 microM; and ETA and ETB receptor antagonist) and FR 139317 (1-10 microM; a selective ETA receptor antagonist) prevented initiation of inward currents or enhancement of Iout by ET-1. Bosentan 15-23 endothelin 1 Rattus norvegicus 204-208 7663155-4 1995 This was confirmed by experiments in which the binding activity of endothelin-1 to various chimeric endothelin receptors was monitored in the presence and absence of competitive endothelin receptor antagonists such as BQ-123 and bosentan. Bosentan 229-237 endothelin 1 Homo sapiens 67-79 7653672-3 1995 Blockade of ETA and ETB receptors with Bosentan produced a small fall in systemic blood pressure and a large fall in glomerular blood pressure due to a significant increase in preglomerular (afferent) arteriolar resistance. Bosentan 39-47 endothelin receptor type A Rattus norvegicus 12-15 8564194-3 1995 Bosentan, a mixed ETA/ETB endothelin receptor antagonist, blunts the development of elevated blood pressure of DOCA-salt hypertensive rats but not in SHR. Bosentan 0-8 endothelin receptor type A Rattus norvegicus 18-21 8564194-16 1995 They also support the hypothesis that an antihypertensive effect of the mixed ETA/ETB endothelin receptor antagonist, bosentan, is found when experimental hypertensive animals exhibit enhanced endothelin-1 gene expression in blood vessels. Bosentan 118-126 endothelin receptor type A Rattus norvegicus 78-81 8564194-16 1995 They also support the hypothesis that an antihypertensive effect of the mixed ETA/ETB endothelin receptor antagonist, bosentan, is found when experimental hypertensive animals exhibit enhanced endothelin-1 gene expression in blood vessels. Bosentan 118-126 endothelin 1 Rattus norvegicus 193-205 7788903-13 1995 Plasma endothelin-1 levels, similar under basal conditions in healthy and hypertensive dogs, increased 30-fold with bosentan (P = .0001). Bosentan 116-124 endothelin 1 Canis lupus familiaris 7-19 7788903-17 1995 The increase of plasma endothelin-1 with bosentan, due either to a displacement of endothelin-1 from its receptor or to a feedback mechanism, does not prevent this blood pressure reduction. Bosentan 41-49 endothelin 1 Canis lupus familiaris 23-35 7656284-5 1995 The effect of bosentan on endothelin-1 induced vasoconstriction was evaluated in isolated diagonal branches of left anterior descending coronary artery. Bosentan 14-22 endothelin-1 Sus scrofa 26-38 7656284-11 1995 Bosentan effectively antagonised the endothelin-1 induced but not the serotonin induced, contractions of isolated coronary arteries and reversed the established contraction induced by endothelin-1. Bosentan 0-8 endothelin-1 Sus scrofa 37-49 7656284-11 1995 Bosentan effectively antagonised the endothelin-1 induced but not the serotonin induced, contractions of isolated coronary arteries and reversed the established contraction induced by endothelin-1. Bosentan 0-8 endothelin-1 Sus scrofa 184-196 7656284-12 1995 CONCLUSIONS: The non-peptide endothelin receptor antagonist bosentan markedly protects the myocardium from ischaemia/reperfusion injury and improves blood flow to the reperfused area, indicating the involvement of endogenous endothelin-1 and the therapeutic value of bosentan in the treatment of ischaemia/reperfusion injury. Bosentan 60-68 endothelin-1 Sus scrofa 225-237 7582486-9 1995 The mixed ET receptor antagonist, bosentan (5 microM), markedly attenuated the responses of ET-1 and SX6C on PPP and lung weight, further implicating activation of both ETA and ETB receptors in these responses. Bosentan 34-42 endothelin 1 Rattus norvegicus 92-96 7582486-9 1995 The mixed ET receptor antagonist, bosentan (5 microM), markedly attenuated the responses of ET-1 and SX6C on PPP and lung weight, further implicating activation of both ETA and ETB receptors in these responses. Bosentan 34-42 endothelin receptor type A Rattus norvegicus 169-172 7582486-9 1995 The mixed ET receptor antagonist, bosentan (5 microM), markedly attenuated the responses of ET-1 and SX6C on PPP and lung weight, further implicating activation of both ETA and ETB receptors in these responses. Bosentan 34-42 endothelin receptor type B Rattus norvegicus 177-180 7582486-21 1995 Differences in the bronchoconstrictor potency of SX6C (compared to ETs) and the antagonism by bosentan may indicate ETB receptor heterogeneity in the airways. Bosentan 94-102 endothelin receptor type B Rattus norvegicus 116-119 7663155-4 1995 This was confirmed by experiments in which the binding activity of endothelin-1 to various chimeric endothelin receptors was monitored in the presence and absence of competitive endothelin receptor antagonists such as BQ-123 and bosentan. Bosentan 229-237 endothelin 1 Homo sapiens 67-77 7670725-11 1995 The ETA/ETB receptor antagonist, bosentan (10 mg kg-1) almost completely inhibited the pressor, haemoconcentration and permeability effects of both ET-1 and IRL 1620. Bosentan 33-41 endothelin-1 Cavia porcellus 148-152 7670725-14 1995 ET-1 (1 nmol kg-1)-induced neutropenia was prevented by pretreatment of the animals with FR 139317 (2.5 mg kg-1), bosentan (10 mg kg-1) or adrenaline (90 nmol kg-1), indicating that ET-1 caused intravascular sequestration of neutrophil granulocytes. Bosentan 114-122 endothelin-1 Cavia porcellus 0-4 7670740-2 1995 The effects of the non-selective endothelin (ET) receptor (ETA/ETB) antagonist, bosentan, on sciatic nerve dysfunction in experimental diabetes were investigated. Bosentan 80-88 endothelin receptor type A Rattus norvegicus 59-62 7670740-2 1995 The effects of the non-selective endothelin (ET) receptor (ETA/ETB) antagonist, bosentan, on sciatic nerve dysfunction in experimental diabetes were investigated. Bosentan 80-88 endothelin receptor type B Rattus norvegicus 63-66 7737710-2 1995 To this end, we studied the effects of the orally active endothelin antagonist Ro 47-0203 (100 mg/kg per day) for 2 days on plasma renin activity and renal renin mRNA levels in normal rats and rats with unilateral renal artery clips (0.2 mm). Bosentan 79-89 renin Rattus norvegicus 131-136 7721389-2 1995 Treatment with the combined endothelin type A/endothelin type B receptor antagonist bosentan moderately reduced blood pressure rise and nearly completely blunted the development of vascular hypertrophy, particularly in small arteries, in the deoxycorticosterone acetate-salt hypertensive model, suggesting a paracrine role for vascular endothelin-1 in the induction of blood vessel hypertrophy in some forms of experimental hypertension. Bosentan 84-92 endothelin 1 Rattus norvegicus 336-348 7721425-10 1995 The response induced by a single bolus of endothelin-3 (10(-9) mol/L) was antagonized by bosentan but not by FR139317, confirming that endothelin B receptors were involved. Bosentan 89-97 endothelin 3 Rattus norvegicus 42-54 7721425-11 1995 In endothelium-intact arteries half-maximally precontracted with norepinephrine, bosentan but not FR139317 inhibited the relaxations induced by intraluminally applied endothelin-3. Bosentan 81-89 endothelin 3 Rattus norvegicus 167-179 7721390-5 1995 In old (and less so in adult) SHR, cumulative concentration-contraction curves to endothelin-1 showed a small contraction resistant to FR139317 (10(-5) mol/L) at 3 x 10(-9) to 10(-8) mol/L endothelin-1, which was completely inhibited by bosentan (10(-5) mol/L). Bosentan 237-245 endothelin 1 Rattus norvegicus 82-94 7864210-4 1995 In lungs from normoxic rats, bosentan (10(-5) M) abolished the vasodilator responses to ET-1 (10(-10) M) or to the ETB-selective agonist IRL-1620 (10(-10) M) and attenuated the vasoconstrictor responses to 10(-9) M ET-1 (from 8.7 +/- 0.7 to 1.8 +/- 0.3 mmHg, P < 0.01) or 10(-9) M IRL-1620 (from 1.5 +/- 0.4 to 0.4 +/- 0.1 mmHg, P < 0.05). Bosentan 29-37 endothelin receptor type B Rattus norvegicus 115-118 7544236-0 1995 Endothelin-1 expression in blood vessels of DOCA-salt hypertensive rats treated with the combined ETA/ETB endothelin receptor antagonist bosentan. Bosentan 137-145 endothelin 1 Rattus norvegicus 0-12 7544236-2 1995 DOCA-salt hypertensive rats respond to treatment with the combined ETA/ETB endothelin receptor antagonist bosentan with lowering of blood pressure. Bosentan 106-114 endothelin receptor type A Rattus norvegicus 67-70 7544236-3 1995 In the present study, we investigated the ir-ET-1 levels and the expression of the ET-1 gene in blood vessels of DOCA-salt hypertensive rats treated or not treated with bosentan. Bosentan 169-177 endothelin 1 Rattus norvegicus 83-87 7544236-5 1995 Plasma ir-ET-1 concentration was slightly but significantly elevated (p < 0.01) in DOCA-salt hypertensive rats compared with uninephrectomized control rats, and was further increased (p < 0.01) in bosentan-treated rats. Bosentan 203-211 endothelin 1 Rattus norvegicus 10-14 7544236-7 1995 The abundance of ET-1 mRNA measured by Northern blot analysis in thoracic aorta and the ir-ET-1 content were attenuated by bosentan treatment. Bosentan 123-131 endothelin 1 Rattus norvegicus 17-21 7544236-7 1995 The abundance of ET-1 mRNA measured by Northern blot analysis in thoracic aorta and the ir-ET-1 content were attenuated by bosentan treatment. Bosentan 123-131 endothelin 1 Rattus norvegicus 91-95 7828305-6 1995 L-NAME induced a dose-dependent increase in mean arterial pressure (percent increase from baseline after 3 mg.kg-1, 25 +/- 5%), and this was reduced by bosentan (13 +/- 3%; P < .05) or by the selective ETA antagonist BQ-123 (3 mg.kg-1: controls, 25 +/- 4%; BQ-123, 14 +/- 5%; P < .01). Bosentan 152-160 endothelin receptor type A Rattus norvegicus 205-208 7840293-3 1995 Big ET induced peripheral and coronary vasoconstriction, which occurred before significant elevations in plasma ET and which was nearly completely blocked by bosentan, a new nonpeptidic mixed (ETA and ETB) ET receptor antagonist. Bosentan 158-166 endothelin receptor type A Canis lupus familiaris 193-196 7864865-5 1995 BQ-123, an ETA antagonist, minimally inhibited ET-1 induced contraction, while bosentan, a mixed, nonpeptide ETA/ETB antagonist, inhibited ET-1 and sarafotoxin S6C mediated contraction in a similar fashion. Bosentan 79-87 endothelin receptor type A Rattus norvegicus 109-112 7864865-5 1995 BQ-123, an ETA antagonist, minimally inhibited ET-1 induced contraction, while bosentan, a mixed, nonpeptide ETA/ETB antagonist, inhibited ET-1 and sarafotoxin S6C mediated contraction in a similar fashion. Bosentan 79-87 endothelin receptor type B Rattus norvegicus 113-116 7843769-13 1995 Bosentan, a combined endothelin-A/endothelin-B receptor antagonist, inhibited endothelin-1 markedly, especially in SHR (P < .05). Bosentan 0-8 endothelin 1 Rattus norvegicus 78-90 7840293-3 1995 Big ET induced peripheral and coronary vasoconstriction, which occurred before significant elevations in plasma ET and which was nearly completely blocked by bosentan, a new nonpeptidic mixed (ETA and ETB) ET receptor antagonist. Bosentan 158-166 endothelin receptor type B Canis lupus familiaris 201-204 7840293-4 1995 Bosentan also prevented the peripheral dilatation caused by the specific ETB receptor agonist, sarafotoxin S6c, but did not prevent the peripheral vasoconstriction induced by angiotensin II. Bosentan 0-8 endothelin receptor type B Canis lupus familiaris 73-76 8587339-3 1995 Contraction was potentiated by the ETA receptor antagonist BQ 123 (10 microM) and the mixed antagonist bosentan (10 microM), suggesting that ET-1 also activates ETA and ETB receptors that inhibit contraction. Bosentan 103-111 endothelin 1 Rattus norvegicus 141-145 8587353-6 1995 In control rats, responses to ET-1 were unaffected by FR 139317 (1 microM) and were potentiated by BMS 182874 (1 microM) and by the mixed ETA/ETB receptor antagonist bosentan (1 microM). Bosentan 166-174 endothelin receptor type A Rattus norvegicus 138-141 8587339-3 1995 Contraction was potentiated by the ETA receptor antagonist BQ 123 (10 microM) and the mixed antagonist bosentan (10 microM), suggesting that ET-1 also activates ETA and ETB receptors that inhibit contraction. Bosentan 103-111 endothelin receptor type A Rattus norvegicus 161-164 8587353-6 1995 In control rats, responses to ET-1 were unaffected by FR 139317 (1 microM) and were potentiated by BMS 182874 (1 microM) and by the mixed ETA/ETB receptor antagonist bosentan (1 microM). Bosentan 166-174 endothelin receptor type B Rattus norvegicus 142-145 8587339-3 1995 Contraction was potentiated by the ETA receptor antagonist BQ 123 (10 microM) and the mixed antagonist bosentan (10 microM), suggesting that ET-1 also activates ETA and ETB receptors that inhibit contraction. Bosentan 103-111 endothelin receptor type B Rattus norvegicus 169-172 8587341-7 1995 Bosentan treatment of rats undergoing CCl4 inhalation resulted in significant protection against elevation of ALT, AST, LDH, and bilirubin. Bosentan 0-8 glutamic-oxaloacetic transaminase 2 Rattus norvegicus 115-118 8587362-5 1995 Higher concentrations of ET-1 (> or = 1 nM) were able to re-induce SPC in rings in which SPCs had been abolished by BQ-123 or bosentan. Bosentan 129-137 proline rich protein gene cluster Homo sapiens 70-73 8587449-8 1995 Blockade of ETA and ETB receptors in SHR with bosentan as well as with BQ 123 led to a significant decrease in MAP and a significant increase in RBF, indicating that the ETA receptor plays a major role in the maintenance of high blood pressure and the regulation of RBF in SHRs. Bosentan 46-54 endothelin receptor type A Rattus norvegicus 12-15 8587434-2 1995 Pretreatment with the broad spectrum ETA and ETB antagonist bosentan (17 mumol/kg) had minimal effect on postischemic hypoperfusion, as measured by hydrogen clearance, in the caudate nucleus and the parietal cortex during 3 h after bilateral common carotid artery occlusion with concomitant hemorrhagic hypotension (transient global ischemia). Bosentan 60-68 endothelin receptor type B Rattus norvegicus 45-48 8587420-1 1995 The binding characteristics and localization of bosentan, an orally active endothelin-1 (ET-1) antagonist, were studied on sections of human coronary artery by in vitro autoradiography. Bosentan 48-56 endothelin 1 Homo sapiens 75-87 8587449-8 1995 Blockade of ETA and ETB receptors in SHR with bosentan as well as with BQ 123 led to a significant decrease in MAP and a significant increase in RBF, indicating that the ETA receptor plays a major role in the maintenance of high blood pressure and the regulation of RBF in SHRs. Bosentan 46-54 endothelin receptor type B Rattus norvegicus 20-23 8587420-1 1995 The binding characteristics and localization of bosentan, an orally active endothelin-1 (ET-1) antagonist, were studied on sections of human coronary artery by in vitro autoradiography. Bosentan 48-56 endothelin 1 Homo sapiens 89-93 8587420-2 1995 Competition studies were performed to determine the ability of bosentan to prevent [125I]ET-1 binding to the coronary vasculature. Bosentan 63-71 endothelin 1 Homo sapiens 89-93 8587420-3 1995 The effects of bosentan on ET-1-induced contraction of the coronary artery were also studied in vitro. Bosentan 15-23 endothelin 1 Homo sapiens 27-31 8587420-5 1995 Unlabeled bosentan prevented [125I]ET-1 binding to this vessel in a concentration-dependent manner, and functional studies indicated that bosentan antagonizes ET-1--induced constriction. Bosentan 10-18 endothelin 1 Homo sapiens 35-39 8587420-5 1995 Unlabeled bosentan prevented [125I]ET-1 binding to this vessel in a concentration-dependent manner, and functional studies indicated that bosentan antagonizes ET-1--induced constriction. Bosentan 138-146 endothelin 1 Homo sapiens 159-163 8587420-6 1995 These data show that bosentan is able to reduce ET-1 binding to the human coronary artery and ET-1 constrictor effects in vitro. Bosentan 21-29 endothelin 1 Homo sapiens 48-52 8587420-6 1995 These data show that bosentan is able to reduce ET-1 binding to the human coronary artery and ET-1 constrictor effects in vitro. Bosentan 21-29 endothelin 1 Homo sapiens 94-98 8587420-7 1995 Bosentan is an orally active ET-1 antagonist, and these results suggest that this compound might be used to block the effects of locally released ET-1 in pathologic conditions, such as atherosclerosis, angina, and myocardial ischemia. Bosentan 0-8 endothelin 1 Homo sapiens 29-33 8587420-7 1995 Bosentan is an orally active ET-1 antagonist, and these results suggest that this compound might be used to block the effects of locally released ET-1 in pathologic conditions, such as atherosclerosis, angina, and myocardial ischemia. Bosentan 0-8 endothelin 1 Homo sapiens 146-150 8587449-8 1995 Blockade of ETA and ETB receptors in SHR with bosentan as well as with BQ 123 led to a significant decrease in MAP and a significant increase in RBF, indicating that the ETA receptor plays a major role in the maintenance of high blood pressure and the regulation of RBF in SHRs. Bosentan 46-54 endothelin receptor type A Rattus norvegicus 170-173 8587449-9 1995 The blockade of both ETA and ETB receptors by bosentan has no further effect on MAP reduction or increase in RBF in SHRs compared to ETA blockade by BQ 123. Bosentan 46-54 endothelin receptor type B Rattus norvegicus 29-32 8587449-10 1995 In contrast, combined blockade of ETA and ETB receptors by bosentan significantly decreased GFR in SHRs, whereas no effect on GFR was observed in WKY rats, suggesting that the glomerular ETB overexpression in SHRs is of pathophysiologic relevance. Bosentan 59-67 endothelin receptor type A Rattus norvegicus 34-37 8587449-10 1995 In contrast, combined blockade of ETA and ETB receptors by bosentan significantly decreased GFR in SHRs, whereas no effect on GFR was observed in WKY rats, suggesting that the glomerular ETB overexpression in SHRs is of pathophysiologic relevance. Bosentan 59-67 endothelin receptor type B Rattus norvegicus 42-45 8587458-8 1995 In DOCA/salt hypertensive rats and DOCA/salt SHRs treated with the combined ETA/ETB endothelin receptor antagonist bosentan, vascular morphometry correlated more closely with blood pressure, even though the blood pressure was only slightly lower than that of untreated rats. Bosentan 115-123 endothelin receptor type A Rattus norvegicus 76-79 7869843-0 1995 Bosentan antagonizes the effects of endothelin-1 on rat gastric blood flow and mucosal integrity. Bosentan 0-8 endothelin 1 Rattus norvegicus 36-48 7869843-1 1995 Bosentan, a new type of orally effective, mixed (ETA+ETB) endothelin receptor antagonist has been recently introduced and tested in a variety of experimental models. Bosentan 0-8 endothelin receptor type A Rattus norvegicus 49-52 7869843-1 1995 Bosentan, a new type of orally effective, mixed (ETA+ETB) endothelin receptor antagonist has been recently introduced and tested in a variety of experimental models. Bosentan 0-8 endothelin receptor type B Rattus norvegicus 53-56 7869843-3 1995 Bosentan (10 mg/kg iv) pretreated rats were injected with endothelin-1 (500-1000-2000 pmol/kg, iv) and gastric mucosal hemodynamics were monitored. Bosentan 0-8 endothelin 1 Rattus norvegicus 58-70 7869843-5 1995 Bosentan antagonized the vasodilator, vasoconstrictor and ulcerogenic effects of endothelin-1 in the rat gastric mucosa. Bosentan 0-8 endothelin 1 Rattus norvegicus 81-93 7955209-8 1994 At weeks 2 through 8, oral administration of the mixed (ETA and ETB) endothelin receptor antagonist bosentan significantly decreased mean arterial pressure in conscious CHF rats, an effect that increased over time. Bosentan 100-108 endothelin receptor type A Rattus norvegicus 56-59 7858876-13 1994 FR 139317 and bosentan (10 mg kg-1) inhibited ET-1-induced bradycardia by 79% and 71%, respectively.ET-l-induced tachycardia was significantly attenuated by bosentan,but not FR 139317.3. Bosentan 14-22 endothelin 1 Rattus norvegicus 46-50 7858876-13 1994 FR 139317 and bosentan (10 mg kg-1) inhibited ET-1-induced bradycardia by 79% and 71%, respectively.ET-l-induced tachycardia was significantly attenuated by bosentan,but not FR 139317.3. Bosentan 157-165 endothelin 1 Rattus norvegicus 46-50 7858879-9 1994 Bosentan, administered at a dose which virtually abolished the pressor response to big ET-1 (3 mg kg-1, i.v. Bosentan 0-8 endothelin 1 Rattus norvegicus 87-91 7955209-8 1994 At weeks 2 through 8, oral administration of the mixed (ETA and ETB) endothelin receptor antagonist bosentan significantly decreased mean arterial pressure in conscious CHF rats, an effect that increased over time. Bosentan 100-108 endothelin receptor type B Rattus norvegicus 64-67 7957619-3 1994 Ro 47-0203 (bosentan, 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2,2"-bipyr imidin-4 - yl]-benzene-sulfonamide) has been evaluated on local microvascular responses to endothelin-1 and endothelin-3, measured by a multiple site 133Xe clearance technique in rat skin in vivo. Bosentan 0-10 endothelin 1 Rattus norvegicus 183-195 7980530-6 1994 The ETA/ETB-receptor antagonist bosentan shifted the entire concentration response curve to the right. Bosentan 32-40 endothelin receptor type A Homo sapiens 4-7 7957619-3 1994 Ro 47-0203 (bosentan, 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2,2"-bipyr imidin-4 - yl]-benzene-sulfonamide) has been evaluated on local microvascular responses to endothelin-1 and endothelin-3, measured by a multiple site 133Xe clearance technique in rat skin in vivo. Bosentan 0-10 endothelin 3 Rattus norvegicus 200-212 7957619-6 1994 Bosentan (3-1000 pmol/site), a new non-peptide mixed antagonist of endothelin ETA and endothelin ETB receptors, significantly reduced the vasoconstriction induced by endothelin-1 but was less effective than BQ-123. Bosentan 0-8 endothelin 1 Rattus norvegicus 166-178 8035319-4 1994 Contractions induced by ET-1 in isolated rat aorta (ETA) and by the selective ETB agonist sarafotoxin S6C in rat trachea were competitively inhibited by bosentan (pA2 = 7.2 and 6.0, respectively), as was the endothelium-dependent relaxation to sarafotoxin S6C in rabbit superior mesenteric artery (pA2 = 6.7). Bosentan 153-161 endothelin 1 Rattus norvegicus 24-28 7921608-4 1994 Bosentan blocked the initial depressor, tachycardic and hindquarters hyperaemic vasodilator effects of ET-1, -2 and -3, and substantially curtailed the primary renal and secondary hindquarters vasoconstrictor responses. Bosentan 0-8 endothelin 1 Rattus norvegicus 103-118 7921608-11 1994 The most straightforward explanation of the results is that the major haemodynamic effects of ET-1, -2 and -3, and all the effects of big ET-1, are mediated through ETA- and/or ETB-receptors that are effectively antagonized by bosentan. Bosentan 227-235 endothelin 1 Rattus norvegicus 94-109 8035319-4 1994 Contractions induced by ET-1 in isolated rat aorta (ETA) and by the selective ETB agonist sarafotoxin S6C in rat trachea were competitively inhibited by bosentan (pA2 = 7.2 and 6.0, respectively), as was the endothelium-dependent relaxation to sarafotoxin S6C in rabbit superior mesenteric artery (pA2 = 6.7). Bosentan 153-161 endothelin receptor type B Rattus norvegicus 78-81 8035319-6 1994 In vivo, bosentan inhibited the pressor response to big ET-1 both after i.v. Bosentan 9-17 endothelin 1 Homo sapiens 56-60 8124808-9 1994 The ETA/ETB receptor antagonist bosentan caused a parallel shift of the concentration-contraction curve to the right at all concentrations of endothelin. Bosentan 32-40 endothelin receptor type A Homo sapiens 4-7 8124808-9 1994 The ETA/ETB receptor antagonist bosentan caused a parallel shift of the concentration-contraction curve to the right at all concentrations of endothelin. Bosentan 32-40 endothelin receptor type B Homo sapiens 8-11 34800596-10 2022 Interestingly, co-administration of bosentan could ameliorate 5-FU-induced cardiotoxicity via improving the detected biochemical and histopathological changes besides modulation of TLR4/MyD88/NFkappaB signaling pathway, eNOS, and endothelin receptors. Bosentan 36-44 toll-like receptor 4 Rattus norvegicus 181-185 8035662-3 1994 In vitro, bosentan was a potent (pA2 = 7.5) and competitive endothelin receptor antagonist as shown by the parallel rightward shift of the concentration-response curve for endothelin-1 on guinea pig aortic rings in presence of increasing concentrations of bosentan. Bosentan 10-18 endothelin-1 Cavia porcellus 172-184 34800596-10 2022 Interestingly, co-administration of bosentan could ameliorate 5-FU-induced cardiotoxicity via improving the detected biochemical and histopathological changes besides modulation of TLR4/MyD88/NFkappaB signaling pathway, eNOS, and endothelin receptors. Bosentan 36-44 MYD88, innate immune signal transduction adaptor Rattus norvegicus 186-191 34800596-10 2022 Interestingly, co-administration of bosentan could ameliorate 5-FU-induced cardiotoxicity via improving the detected biochemical and histopathological changes besides modulation of TLR4/MyD88/NFkappaB signaling pathway, eNOS, and endothelin receptors. Bosentan 36-44 nitric oxide synthase 3 Rattus norvegicus 220-224 34546411-3 2021 We herein present the case of an 11-year-old boy previously diagnosed with an ACTA2 gene mutation who developed repetitive transient ischemic attacks and treated with bosentan, an oral endothelin receptor antagonist. Bosentan 167-175 actin alpha 2, smooth muscle Homo sapiens 78-83 34060401-9 2021 Bosentan + Iloprost and Bosentan + Sildenafil were better for mPAP. Bosentan 0-8 phospholipid phosphatase 1 Mus musculus 62-66 34837677-5 2021 Results: ET-1 (100 nM) and EGF (100 ng/ml) stimulated ERK1/2 phosphorylation and inhibited in the presence of bosentan (ET receptor inhibitor), AG1478 (EGFR inhibitor), and DPI (NOX antagonist). Bosentan 110-118 endothelin 1 Homo sapiens 9-13 34837677-5 2021 Results: ET-1 (100 nM) and EGF (100 ng/ml) stimulated ERK1/2 phosphorylation and inhibited in the presence of bosentan (ET receptor inhibitor), AG1478 (EGFR inhibitor), and DPI (NOX antagonist). Bosentan 110-118 epidermal growth factor Homo sapiens 27-30 34837677-6 2021 Also, ET-1 treatment increased CHSY1 enzyme level; this response was suppressed by bosentan, AG1478, DPI, and SB431542, TGF-beta receptor antagonist. Bosentan 83-91 endothelin 1 Homo sapiens 6-10 34837677-6 2021 Also, ET-1 treatment increased CHSY1 enzyme level; this response was suppressed by bosentan, AG1478, DPI, and SB431542, TGF-beta receptor antagonist. Bosentan 83-91 chondroitin sulfate synthase 1 Homo sapiens 31-36 34800000-4 2022 To account for co-dosing of the commonly prescribed moderate CYP3A4 inducer bosentan, predicted exposures were increased by a factor of 1.54 based on changes in exposure in adults with PAH. Bosentan 76-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-67 34840823-8 2021 Bosentan inhibited ET-1 expression in plasma (P < 0.05) and RPE/choroid/sclera complexes at P28 in rd10 mice. Bosentan 0-8 endothelin 1 Mus musculus 19-23 34546411-9 2021 Bosentan might be beneficial for treating cerebral ischemia associated with ACTA2 cerebral arteriopathy by maintaining the dilatation of stenotic vessels and adequate systemic blood flow and should be considered before performing revascularization surgery. Bosentan 0-8 actin alpha 2, smooth muscle Homo sapiens 76-81 34278410-6 2021 Flow cytometric analyses of eWAT indicated that HFD mice had significantly higher percentages of both CD4+ and CD8+ T cells compared to NMD mice, which was attenuated by treatment with atrasentan or bosentan. Bosentan 199-207 CD4 antigen Mus musculus 102-105 34086873-11 2021 Furthermore, the effects of BMP9 on vasoconstriction were inhibited by bosentan, an endothelin receptor antagonist, in a chick chorioallantoic membrane assay. Bosentan 71-79 growth differentiation factor 2 Mus musculus 28-32 35527471-5 2022 The TGF-beta receptor antagonist, SB431542 and the mixed ETA and ETB receptor antagonist bosentan, inhibited ET-1-mediated phospho-Smad2L level. Bosentan 89-97 endothelin 1 Homo sapiens 109-113 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin converting enzyme 1 Homo sapiens 35-40 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin 1 Homo sapiens 41-53 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin 1 Homo sapiens 55-59 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 heme oxygenase 1 Homo sapiens 120-124 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 tumor protein p53 Homo sapiens 128-131 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin receptor type A Homo sapiens 218-222 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin receptor type B Homo sapiens 227-231 34199777-5 2021 Carbon monoxide (CO) activated the ECE-1/endothelin-1 (ET-1) pathway, which could account for the protumoral effects of HO-1 in p53 wild-type cells, as demonstrated after treatment with bosentan (an antagonist of both ETRA and ETRB endothelin-1 receptors). Bosentan 186-194 endothelin 1 Homo sapiens 232-244 34199777-6 2021 Surprisingly, in cells with a non-active p53 or a mutated p53 with gain-of-function, ECE-1-produced ET-1 acted as a protective molecule, since treatment with bosentan led to increased efficiency for spheres formation and percentage of cancer stem cells (CSCs) markers. Bosentan 158-166 tumor protein p53 Homo sapiens 58-61 34199777-6 2021 Surprisingly, in cells with a non-active p53 or a mutated p53 with gain-of-function, ECE-1-produced ET-1 acted as a protective molecule, since treatment with bosentan led to increased efficiency for spheres formation and percentage of cancer stem cells (CSCs) markers. Bosentan 158-166 endothelin converting enzyme 1 Homo sapiens 85-90 34199777-6 2021 Surprisingly, in cells with a non-active p53 or a mutated p53 with gain-of-function, ECE-1-produced ET-1 acted as a protective molecule, since treatment with bosentan led to increased efficiency for spheres formation and percentage of cancer stem cells (CSCs) markers. Bosentan 158-166 endothelin 1 Homo sapiens 100-104 34199777-7 2021 In these cells, HO-1 could activate or inactivate certain unknown routes that could induce these contrary responses after treatment with bosentan in our cell model. Bosentan 137-145 heme oxygenase 1 Homo sapiens 16-20 34894846-5 2021 Intraperitoneal administration of bosentan, a dual ETA/ETB receptor antagonist, effectively blocked the development or prevented the onset of both cold allodynia and mechanical allodynia. Bosentan 34-42 endothelin receptor type A Rattus norvegicus 51-54 34894846-5 2021 Intraperitoneal administration of bosentan, a dual ETA/ETB receptor antagonist, effectively blocked the development or prevented the onset of both cold allodynia and mechanical allodynia. Bosentan 34-42 endothelin receptor type B Rattus norvegicus 55-58 35373585-7 2022 RESULTS: Treatment with bosentan increased plasma ET-1 in both OB and HW groups. Bosentan 24-32 endothelin 1 Homo sapiens 50-54 35373585-10 2022 Overall, absolute plasma concentrations of ET-1 following treatment with bosentan were significantly associated with kcal/day of fat (r=0.488, p=0.005), percentage of fat utilization (r=0.415, p=0.020), and inversely associated with the percentage of carbohydrates (r=-0.419, p=0.019), and respiratory exchange ratio (r=-0.407, p=0.023). Bosentan 73-81 endothelin 1 Homo sapiens 43-47 35609831-6 2022 The chemical stability of milled bosentan was evaluated using ATR-IR and 1 H NMR as well. Bosentan 33-41 ATR serine/threonine kinase Homo sapiens 62-65 35370222-1 2022 We encountered cases in which the anticoagulant effects of warfarin (CYP2C9 substrate) were reversibly attenuated by the concomitant administration of rifampicin or bosentan, which are potent pregnane X receptor (PXR) ligands. Bosentan 165-173 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 69-75 35370222-1 2022 We encountered cases in which the anticoagulant effects of warfarin (CYP2C9 substrate) were reversibly attenuated by the concomitant administration of rifampicin or bosentan, which are potent pregnane X receptor (PXR) ligands. Bosentan 165-173 nuclear receptor subfamily 1 group I member 2 Homo sapiens 192-211 35370222-1 2022 We encountered cases in which the anticoagulant effects of warfarin (CYP2C9 substrate) were reversibly attenuated by the concomitant administration of rifampicin or bosentan, which are potent pregnane X receptor (PXR) ligands. Bosentan 165-173 nuclear receptor subfamily 1 group I member 2 Homo sapiens 213-216 35370222-11 2022 This study suggests not only the possibility of heterogeneity in the response to PXR activation and deactivation, but also the importance of long-term monitoring of drug-drug interactions when switching from bosentan to macitentan. Bosentan 208-216 nuclear receptor subfamily 1 group I member 2 Homo sapiens 81-84 35609831-6 2022 The chemical stability of milled bosentan was evaluated using ATR-IR and 1 H NMR as well. Bosentan 33-41 insulin receptor Homo sapiens 66-74 34982346-9 2022 ET-1 mediated mRNA expression of GAG synthesizing enzymes C4ST-1 and ChSy-1 was also blocked by TGBFR1 antagonists, SB431542, broad spectrum ET receptor antagonist bosentan, DPI and ROS scavenger N-acetyl-L-cysteine. Bosentan 164-172 endothelin 1 Homo sapiens 0-4 34982346-9 2022 ET-1 mediated mRNA expression of GAG synthesizing enzymes C4ST-1 and ChSy-1 was also blocked by TGBFR1 antagonists, SB431542, broad spectrum ET receptor antagonist bosentan, DPI and ROS scavenger N-acetyl-L-cysteine. Bosentan 164-172 carbohydrate sulfotransferase 11 Homo sapiens 58-64 34982346-9 2022 ET-1 mediated mRNA expression of GAG synthesizing enzymes C4ST-1 and ChSy-1 was also blocked by TGBFR1 antagonists, SB431542, broad spectrum ET receptor antagonist bosentan, DPI and ROS scavenger N-acetyl-L-cysteine. Bosentan 164-172 chondroitin sulfate synthase 1 Homo sapiens 69-75