Bosentan (BioDeep_00000018421)
human metabolite blood metabolite
代谢物信息卡片
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide
化学式: C27H29N5O6S (551.1838)
中文名称: 波生坦
谱图信息:
最多检出来源 Homo sapiens(blood) 43.85%
分子结构信息
SMILES: CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC
InChI: InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32)
描述信息
Bosentan is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer®. Bosentan is used to treat pulmonary hypertension by blocking the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.
C - Cardiovascular system > C02 - Antihypertensives > C02K - Other antihypertensives > C02KX - Antihypertensives for pulmonary arterial hypertension
D002317 - Cardiovascular Agents > D000959 - Antihypertensive Agents
D065128 - Endothelin Receptor Antagonists
C28313 - Endothelin Receptor Antagonist
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
同义名列表
12 个代谢物同义名
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide; 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2-bipyrimidin)-4-yl) benzenesulphornamide; 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2-bipyrimidin)-4-yl) benzenesulfornamide; p-Tert-butyl-N-(6-(2-hydroxyethoxy)-5-(O-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl)benzenesulphonamide; p-Tert-butyl-N-(6-(2-hydroxyethoxy)-5-(O-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl)benzenesulfonamide; 4-t-Butyl-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2-bipyrimidin-4-yl)benzenesulfonamide; Bosentan monohydrate; Bosentan anhydrous; Bosentan hydrate; Bosentanum; Bosentan; Tracleer
数据库引用编号
13 个数据库交叉引用编号
- ChEBI: CHEBI:51450
- PubChem: 104865
- HMDB: HMDB0014699
- DrugBank: DB00559
- ChEMBL: CHEMBL957
- Wikipedia: Bosentan
- MeSH: Bosentan
- chemspider: 94651
- CAS: 1174918-31-0
- CAS: 147536-97-8
- CAS: 174227-18-0
- PMhub: MS000007860
- medchemexpress: HY-A0013
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
1 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
| 亚细胞结构定位 | 关联基因列表 |
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文献列表
- Duygu Yilmaz Usta, Burcu Timur, Zeynep Safak Teksin. Formulation development, optimization by Box-Behnken design, characterization, in vitro, ex-vivo, and in vivo evaluation of bosentan-loaded self-nanoemulsifying drug delivery system: A novel alternative dosage form for pulmonary arterial hypertension treatment.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.
2022 Jul; 174(?):106159. doi:
10.1016/j.ejps.2022.106159. [PMID: 35263632] - Cassandra C Derella, Anson M Blanks, Andy Nguyen, Jacob Looney, Matthew A Tucker, Jinhee Jeong, Paula Rodriguez-Miguelez, Jeffrey Thomas, Matthew Lyon, David M Pollock, Ryan A Harris. Dual endothelin receptor antagonism increases resting energy expenditure in people with increased adiposity.
American journal of physiology. Endocrinology and metabolism.
2022 06; 322(6):E508-E516. doi:
10.1152/ajpendo.00349.2021. [PMID: 35373585] - Di Chen, Tianyi Yuan, Yucai Chen, Huifang Zhang, Ziran Niu, Lianhua Fang, Guanhua Du. DL0805-1, a novel Rho-kinase inhibitor, attenuates lung injury and vasculopathy in a rat model of monocrotaline-induced pulmonary hypertension.
European journal of pharmacology.
2022 Mar; 919(?):174779. doi:
10.1016/j.ejphar.2022.174779. [PMID: 35092757] - Lisa Ferguson-Sells, Nieves Velez de Mendizabal, Baohui Li, David Small. Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Clinical pharmacokinetics.
2022 02; 61(2):249-262. doi:
10.1007/s40262-021-01052-8. [PMID: 34379314] - Koji Akita, Kikuo Isoda, Fumie Ohtomo, Sarasa Isobe, Tomiharu Niida, Yayoi Sato-Okabayashi, Motoaki Sano, Kazunori Shimada, Yoichiro Iwakura, Tohru Minamino. Blocking of interleukin-1 suppresses angiotensin II-induced renal injury.
Clinical science (London, England : 1979).
2021 09; 135(17):2035-2048. doi:
10.1042/cs20201406. [PMID: 34402864] - Marie-Camille Chaumais, Mohamed Reda Amar Djessas, Raphaël Thuillet, Amélie Cumont, Ly Tu, Guillaume Hebert, Pauline Gaignard, Alice Huertas, Laurent Savale, Marc Humbert, Christophe Guignabert. Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension.
Cardiovascular research.
2021 04; 117(5):1391-1401. doi:
10.1093/cvr/cvaa200. [PMID: 32653925] - Ashwani Kumar Sharma, Japneet Kaur, Tajpreet Kaur, Balbir Singh, Harlokesh Narayan Yadav, Devendra Pathak, Amrit Pal Singh. Ameliorative role of bosentan, an endothelin receptor antagonist, against sodium arsenite-induced renal dysfunction in rats.
Environmental science and pollution research international.
2021 Feb; 28(6):7180-7190. doi:
10.1007/s11356-020-11035-0. [PMID: 33026618] - Y Zhou, J Chi, Y Huang, B Dong, W Lv, Y G Wang. Efficacy and safety of endothelin receptor antagonists in type 2 diabetic kidney disease: A systematic review and meta-analysis of randomized controlled trials.
Diabetic medicine : a journal of the British Diabetic Association.
2021 01; 38(1):e14411. doi:
10.1111/dme.14411. [PMID: 33000477] - Makiko Kido-Nakahara, Bing Wang, Fumitaka Ohno, Gaku Tsuji, Dugarmaa Ulzii, Masaki Takemura, Masutaka Furue, Takeshi Nakahara. Inhibition of mite-induced dermatitis, pruritus, and nerve sprouting in mice by the endothelin receptor antagonist bosentan.
Allergy.
2021 01; 76(1):291-301. doi:
10.1111/all.14451. [PMID: 32535962] - Bryan Oronsky, Susan Knox, Pedro Cabrales, Arnold Oronsky, Tony R Reid. Desperate Times, Desperate Measures: The Case for RRx-001 in the Treatment of COVID-19.
Seminars in oncology.
2020 10; 47(5):305-308. doi:
10.1053/j.seminoncol.2020.07.002. [PMID: 32718560] - Kennosuke Yorifuji, Yuko Uemura, Shinji Horibata, Goh Tsuji, Yoko Suzuki, Kazuhiko Nakayama, Takashi Hatae, Shunichi Kumagai, Noriaki Emoto. Predictive model of bosentan-induced liver toxicity in Japanese patients with pulmonary arterial hypertension.
Canadian journal of physiology and pharmacology.
2020 Sep; 98(9):625-628. doi:
10.1139/cjpp-2019-0656. [PMID: 32433892] - S Javor, A Salsano. Why not consider an endothelin receptor antagonist against SARS-CoV-2?.
Medical hypotheses.
2020 08; 141(?):109792. doi:
10.1016/j.mehy.2020.109792. [PMID: 32361169] - Maria M Posada, Bridget L Morse, P Kellie Turner, Palaniappan Kulanthaivel, Stephen D Hall, Gemma L Dickinson. Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Journal of clinical pharmacology.
2020 07; 60(7):915-930. doi:
10.1002/jcph.1584. [PMID: 32080863] - Xiaoqing Fan, Jie Bai, Minwan Hu, Yanxia Xu, Shengyu Zhao, Yanhong Sun, Baolian Wang, Jinping Hu, Yan Li. Drug interaction study of flavonoids toward OATP1B1 and their 3D structure activity relationship analysis for predicting hepatoprotective effects.
Toxicology.
2020 05; 437(?):152445. doi:
10.1016/j.tox.2020.152445. [PMID: 32259555] - Natalie K Jones, Kevin Stewart, Alicja Czopek, Robert I Menzies, Adrian Thomson, Carmel M Moran, Carolynn Cairns, Bryan R Conway, Laura Denby, Dawn E W Livingstone, John Wiseman, Patrick W Hadoke, David J Webb, Neeraj Dhaun, James W Dear, John J Mullins, Matthew A Bailey. Endothelin-1 Mediates the Systemic and Renal Hemodynamic Effects of GPR81 Activation.
Hypertension (Dallas, Tex. : 1979).
2020 05; 75(5):1213-1222. doi:
10.1161/hypertensionaha.119.14308. [PMID: 32200679] - H Kazimoglu, E Uysal, M Dokur, A O Gurer, K Batcioglu, B A Uyumlu, E Petekkaya, M Karadag. Comparison of the protective effects of selective endothelin-a receptor antagonist, ambrisentan, and dual endothelin-A/B receptor antagonist, bosentan, in experimental renal ischemia reperfusion injury.
Bratislavske lekarske listy.
2020; 121(8):547-553. doi:
10.4149/bll_2020_091. [PMID: 32726116] - Lamei Yu, Weijian Li, Byung Mun Park, Gi-Ja Lee, Suhn Hee Kim. Hypoxia augments NaHS-induced ANP secretion via KATP channel, HIF-1α and PPAR-γ pathway.
Peptides.
2019 11; 121(?):170123. doi:
10.1016/j.peptides.2019.170123. [PMID: 31386893] - David Small, Lisa Ferguson-Sells, Nagib Dahdah, Damien Bonnet, John Landry, Baohui Li. Pharmacokinetics and safety of tadalafil in a paediatric population with pulmonary arterial hypertension: A multiple ascending-dose study.
British journal of clinical pharmacology.
2019 10; 85(10):2302-2309. doi:
10.1111/bcp.14039. [PMID: 31222765] - Zhen Wang, Xiangrui Jiang, Xianglei Zhang, Guanghui Tian, Rulei Yang, Jianzhong Wu, Xiaoli Zou, Zheng Liu, Xiaojun Yang, Chunhui Wu, Jing Shi, Jianfeng Li, Jin Suo, Yu Wang, Rongxia Zhang, Zhijian Xu, Xudong Gong, Yang He, Weiliang Zhu, Haji Akber Aisa, Hualiang Jiang, Yechun Xu, Jingshan Shen. Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Journal of medicinal chemistry.
2019 05; 62(10):4979-4990. doi:
10.1021/acs.jmedchem.9b00123. [PMID: 31021628] - Ryosuke Saigusa, Takashi Yamashita, Shunsuke Miura, Megumi Hirabayashi, Kouki Nakamura, Takuya Miyagawa, Yuki Fukui, Ayumi Yoshizaki, Shinichi Sato, Yoshihide Asano. A potential contribution of decreased galectin-7 expression in stratified epithelia to the development of cutaneous and oesophageal manifestations in systemic sclerosis.
Experimental dermatology.
2019 05; 28(5):536-542. doi:
10.1111/exd.13900. [PMID: 30739341] - Xiaona Xu, Zhiqiang Zhao, Guangping Li. The Protective Effect of Bosentan against Atherosclerosis in Apolipoprotein E-Deficient Mice Is Mediated by miRNA-21.
BioMed research international.
2019; 2019(?):8348430. doi:
10.1155/2019/8348430. [PMID: 31886257] - Sheng-Chang Yang, Ya-Jing Guo, Fu-Yang Yu, Ling-Ling Chen, Wen-Ya Li, En-Sheng Ji. [Bosentan ameliorates hypertension in rats exposed to chronic intermittent hypoxia through inhibiting renal sympathetic nerve activity].
Sheng li xue bao : [Acta physiologica Sinica].
2018 Aug; 70(4):354-360. doi:
NULL. [PMID: 30112560] - Muzaffar Iqbal, Essam Ezzeldin, Naser L Rezk, Amal A Bajrai, Khalid A Al-Rashood. A validated UPLC-MS/MS method for flibanserin in plasma and its pharmacokinetic interaction with bosentan in rats.
Bioanalysis.
2018 Jul; 10(14):1087-1097. doi:
10.4155/bio-2018-0065. [PMID: 29692180] - Jennifer Ryan, Ryan E Morgan, Yuan Chen, Laurie P Volak, Robert T Dunn, Kenneth W Dunn. Intravital Multiphoton Microscopy with Fluorescent Bile Salts in Rats as an In Vivo Biomarker for Hepatobiliary Transport Inhibition.
Drug metabolism and disposition: the biological fate of chemicals.
2018 05; 46(5):704-718. doi:
10.1124/dmd.117.079277. [PMID: 29467212] - Rui Li, Mark Niosi, Nathaniel Johnson, David A Tess, Emi Kimoto, Jian Lin, Xin Yang, Keith A Riccardi, Sangwoo Ryu, Ayman F El-Kattan, Tristan S Maurer, Larry M Tremaine, Li Di. A Study on Pharmacokinetics of Bosentan with Systems Modeling, Part 1: Translating Systemic Plasma Concentration to Liver Exposure in Healthy Subjects.
Drug metabolism and disposition: the biological fate of chemicals.
2018 04; 46(4):346-356. doi:
10.1124/dmd.117.078790. [PMID: 29330218] - Rui Li, Emi Kimoto, Mark Niosi, David A Tess, Jian Lin, Larry M Tremaine, Li Di. A Study on Pharmacokinetics of Bosentan with Systems Modeling, Part 2: Prospectively Predicting Systemic and Liver Exposure in Healthy Subjects.
Drug metabolism and disposition: the biological fate of chemicals.
2018 04; 46(4):357-366. doi:
10.1124/dmd.117.078808. [PMID: 29330219] - A Caires, G S Fernandes, A M Leme, B Castino, E A Pessoa, S M Fernandes, C D Fonseca, M F Vattimo, N Schor, F T Borges. Endothelin-1 receptor antagonists protect the kidney against the nephrotoxicity induced by cyclosporine-A in normotensive and hypertensive rats.
Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.
2017 Dec; 51(2):e6373. doi:
10.1590/1414-431x20176373. [PMID: 29267497] - Anke-Katrin Volz, Andreas Krause, Walter Emil Haefeli, Jasper Dingemanse, Thorsten Lehr. Target-Mediated Drug Disposition Pharmacokinetic-Pharmacodynamic Model of Bosentan and Endothelin-1.
Clinical pharmacokinetics.
2017 12; 56(12):1499-1511. doi:
10.1007/s40262-017-0534-4. [PMID: 28401480] - Bridget L Morse, Jamus G MacGuire, Anthony M Marino, Yue Zhao, Maxine Fox, Yueping Zhang, Hong Shen, W Griffith Humphreys, Punit Marathe, Yurong Lai. Physiologically Based Pharmacokinetic Modeling of Transporter-Mediated Hepatic Clearance and Liver Partitioning of OATP and OCT Substrates in Cynomolgus Monkeys.
The AAPS journal.
2017 11; 19(6):1878-1889. doi:
10.1208/s12248-017-0151-z. [PMID: 29019117] - Anna Russignan, Cecilia Spina, Nicola Tamassia, Adriana Cassaro, Antonella Rigo, Anna Bagnato, Laura Rosanò, Angela Bonalumi, Michele Gottardi, Lucia Zanatta, Alice Giacomazzi, Maria Teresa Scupoli, Martina Tinelli, Ugo Salvadori, Federico Mosna, Alberto Zamò, Marco A Cassatella, Fabrizio Vinante, Cristina Tecchio. Endothelin-1 receptor blockade as new possible therapeutic approach in multiple myeloma.
British journal of haematology.
2017 09; 178(5):781-793. doi:
10.1111/bjh.14771. [PMID: 28597546] - Rolf M F Berger, Martine Gehin, Maurice Beghetti, Dunbar Ivy, Andjela Kusic-Pajic, Peter Cornelisse, Simon Grill, Damien Bonnet. A bosentan pharmacokinetic study to investigate dosing regimens in paediatric patients with pulmonary arterial hypertension: FUTURE-3.
British journal of clinical pharmacology.
2017 08; 83(8):1734-1744. doi:
10.1111/bcp.13267. [PMID: 28213957] - Minyu Zhang, Hongwei Wu, Feifei Guo, Yangyang Yu, Junying Wei, Ya Geng, Shifeng Wang, Shiyou Li, Hongjun Yang. Identification of active components in Yixinshu Capsule with protective effects against myocardial dysfunction on human induced pluripotent stem cell-derived cardiomyocytes by an integrative approach.
Molecular bioSystems.
2017 Jul; 13(8):1469-1480. doi:
10.1039/c6mb00813e. [PMID: 28604846] - Major Singh, Atish Prakash. Possible role of endothelin receptor against hyperhomocysteinemia and β-amyloid induced AD type of vascular dementia in rats.
Brain research bulletin.
2017 Jul; 133(?):31-41. doi:
10.1016/j.brainresbull.2017.02.012. [PMID: 28274813] - Neslihan H Dikmenoğlu Falkmarken, Okan Arihan, Alper B Iskit. Comparison of endothelin and nitric oxide synthase blockers on hemorheological parameters in endotoxemic rats.
Turkish journal of medical sciences.
2017 Jun; 47(3):1045-1052. doi:
10.3906/sag-1607-19. [PMID: 28618763] - James A Angus, Paul F Soeding, Richard J A Hughes, Christine E Wright. Functional estimation of endothelin-1 receptor antagonism by bosentan, macitentan and ambrisentan in human pulmonary and radial arteries in vitro.
European journal of pharmacology.
2017 Jun; 804(?):111-116. doi:
10.1016/j.ejphar.2017.03.014. [PMID: 28300593] - Matthew Gibson Burbank, Ahmad Sharanek, Audrey Burban, Hervé Mialanne, Hélène Aerts, Christiane Guguen-Guillouzo, Richard John Weaver, André Guillouzo. From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells.
Toxicological sciences : an official journal of the Society of Toxicology.
2017 06; 157(2):451-464. doi:
10.1093/toxsci/kfx062. [PMID: 28369585] - Harini Chowdary Vadlamudi, Prasanna Raju Yalavarthi, Basaveswara Rao M V, Arun Rasheed, Tejeswari N. In vitro characterization studies of self-microemulsified bosentan systems.
Drug development and industrial pharmacy.
2017 Jun; 43(6):989-995. doi:
10.1080/03639045.2017.1287720. [PMID: 28121194] - Magali Vercauteren, Frederic Trensz, Anne Pasquali, Christophe Cattaneo, Daniel S Strasser, Patrick Hess, Marc Iglarz, Martine Clozel. Endothelin ETA Receptor Blockade, by Activating ETB Receptors, Increases Vascular Permeability and Induces Exaggerated Fluid Retention.
The Journal of pharmacology and experimental therapeutics.
2017 05; 361(2):322-333. doi:
10.1124/jpet.116.234930. [PMID: 28223322] - S B Sarsu, K Sahin, H Kilincaslan, S L Mirapoglu, N Buyukpınarbasili, M E Duz, I Aydogdu. Assessment of serum endothelin-1 levels in rat appendicitis model and the effects of bosentan.
European review for medical and pharmacological sciences.
2017 04; 21(7):1627-1634. doi:
NULL. [PMID: 28429342] - Cinzia Rotondo, Emanuela Praino, Mariangela Nivuori, Francesca di Serio, Giovanni Lapadula, Florenzo Iannone. No changes in N-terminal pro-brain natriuretic peptide in a longitudinal cohort of patients with systemic sclerosis-associated pulmonary arterial hypertension on therapy with bosentan.
International journal of rheumatic diseases.
2017 Jan; 20(1):90-96. doi:
10.1111/1756-185x.12721. [PMID: 26218502] - Ekkehard Grünig, Johanna Ohnesorge, Nicola Benjamin, Jürgen Burhenne, Yeliz Enderle, Benjamin Egenlauf, Christine Fischer, Satenik Harutyunova, Andrea Huppertz, Hans Klose, Walter E Haefeli. Plasma Drug Concentrations in Patients with Pulmonary Arterial Hypertension on Combination Treatment.
Respiration; international review of thoracic diseases.
2017; 94(1):26-37. doi:
10.1159/000470916. [PMID: 28494463] - Kouichi Nakau, Masaya Sugimoto, Hideharu Oka, Aya Kajihama, Jun Maeda, Hiroyuki Yamagishi, Naoya Kamiyama, Yoshikazu Tasaki, Hiroki Kajino, Hiroshi Azuma. Pharmacokinetics of drugs for pediatric pulmonary hypertension.
Pediatrics international : official journal of the Japan Pediatric Society.
2016 Nov; 58(11):1112-1117. doi:
10.1111/ped.12997. [PMID: 27038140] - Mengchun Chen, Wenjie Song, Shuanghu Wang, Qiulei Chen, Peipei Pan, Tao Xu, Guoxin Hu, Zhiqiang Zheng. Simultaneous Determination of Bosentan, Glimepiride, HYBOS and M1 in Rat Plasma by UPLC-MS-MS and its Application to Pharmacokinetic Study.
Journal of chromatographic science.
2016 Aug; 54(7):1159-65. doi:
10.1093/chromsci/bmw003. [PMID: 27240565] - Christian Jung, Michael Lichtenauer, Bernhard Wernly, Marcus Franz, Bjoern Goebel, Arnar Rafnsson, Hans-Reiner Figulla, John Pernow. Effect of endothelin-1 and endothelin receptor blockade on the release of microparticles.
European journal of clinical investigation.
2016 Aug; 46(8):707-13. doi:
10.1111/eci.12652. [PMID: 27322814] - Teresa M Seccia, Brasilina Caroccia, Francesca Gioco, Maria Piazza, Valentina Buccella, Diego Guidolin, Eugenia Guerzoni, Barbara Montini, Lucia Petrelli, Elisa Pagnin, Verdiana Ravarotto, Anna S Belloni, Lorenzo A Calò, Gian Paolo Rossi. Endothelin-1 Drives Epithelial-Mesenchymal Transition in Hypertensive Nephroangiosclerosis.
Journal of the American Heart Association.
2016 07; 5(7):. doi:
10.1161/jaha.116.003888. [PMID: 27444511] - Anne Briançon-Marjollet, Denis Monneret, Marion Henri, Florence Hazane-Puch, Jean-Louis Pepin, Patrice Faure, Diane Godin-Ribuot. Endothelin regulates intermittent hypoxia-induced lipolytic remodelling of adipose tissue and phosphorylation of hormone-sensitive lipase.
The Journal of physiology.
2016 Mar; 594(6):1727-40. doi:
10.1113/jp271321. [PMID: 26663321] - R Saigusa, Y Asano, T Yamashita, T Taniguchi, T Takahashi, Y Ichimura, T Toyama, A Yoshizaki, T Miyagaki, M Sugaya, S Sato. Fli1 deficiency contributes to the downregulation of endothelial protein C receptor in systemic sclerosis: a possible role in prothrombotic conditions.
The British journal of dermatology.
2016 Feb; 174(2):338-47. doi:
10.1111/bjd.14183. [PMID: 26399195] - A Hakamata, K Odagiri, S Miyakawa, H Irisawa, K Takeuchi, N Inui, S Tanaka, S Uchida, H Watanabe. Pharmacokinetic and Pharmacodynamic Comparison of Sildenafil-Bosentan and Sildenafil-Ambrisentan Combination Therapies for Pulmonary Hypertension.
Clinical and translational science.
2016 Feb; 9(1):29-35. doi:
10.1111/cts.12382. [PMID: 26756977] - Martine Géhin, Patricia N Sidharta, Jasper Dingemanse. Bosentan Pharmacokinetics in Pediatric Patients with Pulmonary Arterial Hypertension: Comparison of Dried Blood Spot and Plasma Analysis.
Pharmacology.
2016; 98(3-4):111-4. doi:
10.1159/000446583. [PMID: 27189212] - María F Albertoni Borghese, María C Ortiz, Sabrina Balonga, Rocío Moreira Szokalo, Mónica P Majowicz. The Role of Endothelin System in Renal Structure and Function during the Postnatal Development of the Rat Kidney.
PloS one.
2016; 11(2):e0148866. doi:
10.1371/journal.pone.0148866. [PMID: 26872270] - Yoon-Kyung Chang, Hyunsu Choi, Jin Young Jeong, Ki-Ryang Na, Kang Wook Lee, Dae Eun Choi. Co-inhibition of Angiotensin II Receptor and Endothelin-1 Attenuates Renal Injury in Unilateral Ureteral Obstructed Mice.
Kidney & blood pressure research.
2016; 41(4):450-9. doi:
10.1159/000443446. [PMID: 27415782] - Yeliz Enderle, Andreas D Meid, Jörg Friedrich, Ekkehard Grünig, Heinrike Wilkens, Walter E Haefeli, Jürgen Burhenne. Dried Blood Spot Technique for the Monitoring of Ambrisentan, Bosentan, Sildenafil, and Tadalafil in Patients with Pulmonary Arterial Hypertension.
Analytical chemistry.
2015 Dec; 87(24):12112-20. doi:
10.1021/acs.analchem.5b03077. [PMID: 26583764] - Didier Renard, Thomas Bouillon, Ping Zhou, Gerard Flesch, Debbie Quinn. Pharmacokinetic interactions among imatinib, bosentan and sildenafil, and their clinical implications in severe pulmonary arterial hypertension.
British journal of clinical pharmacology.
2015 Jul; 80(1):75-85. doi:
10.1111/bcp.12584. [PMID: 25581063] - Shanmuga Reddy Chilakapati, Mamatha Serasanambati, Prabhakar Vissavajjhala, Jagadeeshwara Reddy Kanala, Damodar Reddy Chilakapati. Amelioration of bleomycin-induced pulmonary fibrosis in a mouse model by a combination therapy of bosentan and imatinib.
Experimental lung research.
2015 May; 41(4):173-88. doi:
10.3109/01902148.2014.939312. [PMID: 25844688] - Agata Kowalczyk, Paulina Kleniewska, Michal Kolodziejczyk, Beata Skibska, Anna Goraca. The role of endothelin-1 and endothelin receptor antagonists in inflammatory response and sepsis.
Archivum immunologiae et therapiae experimentalis.
2015 Feb; 63(1):41-52. doi:
10.1007/s00005-014-0310-1. [PMID: 25288367] - J Gerry Kenna, Simone H Stahl, Julie A Eakins, Alison J Foster, Linda C Andersson, Jonas Bergare, Martin Billger, Marie Elebring, Charles S Elmore, Richard A Thompson. Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists.
The Journal of pharmacology and experimental therapeutics.
2015 Feb; 352(2):281-90. doi:
10.1124/jpet.114.220491. [PMID: 25467130] - Georgios S Vlachogeorgos, Nicholaos Daskalopoulos, Panayiotis Blatsiotis, Irene S Kourbeti, Ioannis Mantas, Georgios T Stathopoulos. Bosentan for patients with echocardiographic evidence of pulmonary hypertension due to long-standing rheumatic mitral stenosis.
Hellenic journal of cardiology : HJC = Hellenike kardiologike epitheorese.
2015 Jan; 56(1):36-43. doi:
NULL. [PMID: 25701970] - In-Sam Park. Efficacy of pulmonary vasodilator therapy in patients with functionally single ventricle.
International heart journal.
2015; 56 Suppl(?):S26-30. doi:
10.1536/ihj.14-392. [PMID: 25787795] - S Gong, Z Seng, W Wang, J Lv, Q Dong, B Yan, L Peng, X He. Bosentan protects the spinal cord from ischemia reperfusion injury in rats through vascular endothelial growth factor receptors.
Spinal cord.
2015 Jan; 53(1):19-23. doi:
10.1038/sc.2014.147. [PMID: 25179655] - M Nishikawa-Takahashi, S Ueno, K Kario. Long-term advanced therapy with bosentan improves symptoms and prevents deterioration of inoperable chronic thromboembolic pulmonary hypertension.
Life sciences.
2014 Nov; 118(2):410-3. doi:
10.1016/j.lfs.2014.03.024. [PMID: 24690389] - Kaori Sato, Tsutomu Saji, Taku Kaneko, Kei Takahashi, Kaoru Sugi. Unexpected pulmonary hypertensive crisis after surgery for ocular malignant melanoma.
Life sciences.
2014 Nov; 118(2):420-3. doi:
10.1016/j.lfs.2014.03.004. [PMID: 24632478] - Christoph Markert, Theresia Wirsching, Regina Hellwig, Jürgen Burhenne, Johanna Weiss, Klaus-Dieter Riedel, Gerd Mikus, Walter E Haefeli. Lack of a clinically significant interaction of grapefruit juice with ambrisentan and bosentan in healthy adults.
International journal of clinical pharmacology and therapeutics.
2014 Nov; 52(11):957-64. doi:
10.5414/cp202164. [PMID: 25207548] - Hiroyuki Kohno, Fukiko Ichida, Keiichi Hirono, Sayaka Ozawa, Naoki Yoshimura, Tsuneyuki Nakamura, Chisato Akita, Kazuya Ishida, Masato Taguchi. Plasma concentrations of tadalafil in children with pulmonary arterial hypertension.
Therapeutic drug monitoring.
2014 Oct; 36(5):576-83. doi:
10.1097/ftd.0000000000000055. [PMID: 24872209] - Mohamed Y Abd El Rahman, Axel Rentzsch, Philipp Scherber, Siegrun Mebus, Oliver Miera, Günther Balling, Petra Böttler, Karl-Otto Dubowy, Birgit Farahwaschy, Alfred Hager, Joachim Kreuder, Brigitte Peters, Felix Berger, Ingram Schulze-Neick, Hashim Abdul-Khaliq. Effect of bosentan therapy on ventricular and atrial function in adults with Eisenmenger syndrome. A prospective, multicenter study using conventional and Speckle tracking echocardiography.
Clinical research in cardiology : official journal of the German Cardiac Society.
2014 Sep; 103(9):701-10. doi:
10.1007/s00392-014-0703-5. [PMID: 24682249] - Gurpreet Singh, Bhupesh Sharma, Amteshwar Singh Jaggi, Nirmal Singh. Efficacy of bosentan, a dual ETA and ETB endothelin receptor antagonist, in experimental diabetes induced vascular endothelial dysfunction and associated dementia in rats.
Pharmacology, biochemistry, and behavior.
2014 Sep; 124(?):27-35. doi:
10.1016/j.pbb.2014.05.002. [PMID: 24836182] - Sei-Ichiro Motegi, Etsuko Okada, Akihiko Uchiyama, Kazuya Yamada, Sachiko Ogino, Yoko Yokoyama, Yuko Takeuchi, Fumiko Monma, Tamio Suzuki, Osamu Ishikawa. Role of endothelin-1/endothelin receptor signaling in fibrosis and calcification in nephrogenic systemic fibrosis.
Experimental dermatology.
2014 Sep; 23(9):664-9. doi:
10.1111/exd.12500. [PMID: 25048859] - Yavuz Pehlivan, Recep Dokuyucu, Tuncer Demir, Davut Sinan Kaplan, Ibrahim Koc, Mustafa Orkmez, Ibrahim Halil Turkbeyler, Ali Osman Ceribasi, Ediz Tutar, Seyithan Taysi, Bunyamin Kisacik, Ahmet Mesut Onat. Palosuran treatment effective as bosentan in the treatment model of pulmonary arterial hypertension.
Inflammation.
2014 Aug; 37(4):1280-8. doi:
10.1007/s10753-014-9855-8. [PMID: 24604341] - Alptug Atila, Murat Ozturk, Yucel Kadioglu, Zekai Halici, Didar Turkan, Muhammed Yayla, Harun Un. Development and validation of UFLC-MS/MS method for determination of bosentan in rat plasma.
Journal of pharmaceutical and biomedical analysis.
2014 Aug; 97(?):33-8. doi:
10.1016/j.jpba.2014.03.039. [PMID: 24803031] - Alexander Treiber, Päivi Äänismaa, Ruben de Kanter, Stephane Delahaye, Marianne Treher, Patrick Hess, Patricia Sidharta. Macitentan does not interfere with hepatic bile salt transport.
The Journal of pharmacology and experimental therapeutics.
2014 Jul; 350(1):130-43. doi:
10.1124/jpet.114.214106. [PMID: 24769543] - Xiangjun Qiu, Jianlong Zhao, Zhe Wang, Zhisheng Xu, Ren-ai Xu. Simultaneous determination of bosentan and glimepiride in human plasma by ultra performance liquid chromatography tandem mass spectrometry and its application to a pharmacokinetic study.
Journal of pharmaceutical and biomedical analysis.
2014 Jul; 95(?):207-12. doi:
10.1016/j.jpba.2014.03.011. [PMID: 24685726] - Neeraj Dhaun, Jean-Luc Vachiery, Raymond L Benza, Robert Naeije, Lie-Ju Hwang, Xuexuan Liu, Simon Teal, David J Webb. Endothelin antagonism and uric acid levels in pulmonary arterial hypertension: clinical associations.
The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation.
2014 May; 33(5):521-7. doi:
10.1016/j.healun.2014.01.853. [PMID: 24656288] - Dulce Fontoura, José Oliveira-Pinto, Marta Tavares-Silva, Sara Leite, Francisco Vasques-Nóvoa, Pedro Mendes-Ferreira, André P Lourenço, Adelino F Leite-Moreira. Myocardial and anti-inflammatory effects of chronic bosentan therapy in monocrotaline-induced pulmonary hypertension.
Revista portuguesa de cardiologia : orgao oficial da Sociedade Portuguesa de Cardiologia = Portuguese journal of cardiology : an official journal of the Portuguese Society of Cardiology.
2014 Apr; 33(4):213-22. doi:
10.1016/j.repc.2013.09.016. [PMID: 24780128] - N Puza, M G Papich, C Reinero, C H Chang, D-H Yu, C Sharp, A DeClue. Pharmacokinetics and preliminary safety data of a single oral dose of bosentan, a dual endothelin receptor antagonist, in cats.
Journal of veterinary pharmacology and therapeutics.
2014 Apr; 37(2):192-5. doi:
10.1111/jvp.12083. [PMID: 24745065] - Radica Z Alicic, Katherine R Tuttle. Novel therapies for diabetic kidney disease.
Advances in chronic kidney disease.
2014 Mar; 21(2):121-33. doi:
10.1053/j.ackd.2014.01.007. [PMID: 24602462] - Kacie M Dickinson, Peter M Clifton, Jennifer B Keogh. A reduction of 3 g/day from a usual 9 g/day salt diet improves endothelial function and decreases endothelin-1 in a randomised cross_over study in normotensive overweight and obese subjects.
Atherosclerosis.
2014 Mar; 233(1):32-8. doi:
10.1016/j.atherosclerosis.2013.11.078. [PMID: 24529119] - S Gong, L Peng, B Yan, Q Dong, Z Seng, W Wang, J Lv, X He. Bosentan reduces neuronal apoptosis following spinal cord ischemic reperfusion injury.
Spinal cord.
2014 Mar; 52(3):181-5. doi:
10.1038/sc.2013.133. [PMID: 24276417] - Yoshinari Yokoyama, Miho Tomatsuri, Hideki Hayashi, Keita Hirai, Yasuo Ono, Yuto Yamada, Kenichiro Todoroki, Toshimasa Toyo'oka, Hiroshi Yamada, Kunihiko Itoh. Simultaneous microdetermination of bosentan, ambrisentan, sildenafil, and tadalafil in plasma using liquid chromatography/tandem mass spectrometry for pediatric patients with pulmonary arterial hypertension.
Journal of pharmaceutical and biomedical analysis.
2014 Feb; 89(?):227-32. doi:
10.1016/j.jpba.2013.11.007. [PMID: 24309556] - Shin-ya Kawashiri, Yukitaka Ueki, Kaoru Terada, Satoshi Yamasaki, Kiyoshi Aoyagi, Atsushi Kawakami. Improvement of plasma endothelin-1 and nitric oxide in patients with systemic sclerosis by bosentan therapy.
Rheumatology international.
2014 Feb; 34(2):221-5. doi:
10.1007/s00296-013-2861-6. [PMID: 24071933] - Yoshinari Yokoyama, Ayaka Osano, Hideki Hayashi, Kunihiko Itoh, Takashi Okura, Yoshiharu Deguchi, Yoshihiko Ito, Shizuo Yamada. Endothelin-1 receptors in rat tissues: characterization by bosentan, ambrisentan and CI-1020.
Biological & pharmaceutical bulletin.
2014; 37(3):461-5. doi:
10.1248/bpb.b13-00881. [PMID: 24583865] - Christoph Markert, Yvonne Schweizer, Regina Hellwig, Theresia Wirsching, Klaus-Dieter Riedel, Juergen Burhenne, Johanna Weiss, Gerd Mikus, Walter E Haefeli. Clarithromycin substantially increases steady-state bosentan exposure in healthy volunteers.
British journal of clinical pharmacology.
2014 Jan; 77(1):141-8. doi:
10.1111/bcp.12177. [PMID: 23738582] - Frida Gustafsson, Alison J Foster, Sunil Sarda, Matthew H Bridgland-Taylor, J Gerry Kenna. A correlation between the in vitro drug toxicity of drugs to cell lines that express human P450s and their propensity to cause liver injury in humans.
Toxicological sciences : an official journal of the Society of Toxicology.
2014 Jan; 137(1):189-211. doi:
10.1093/toxsci/kft223. [PMID: 24085192] - F T Hammad, A M Wheatley, G Davis. Bosentan normalizes the GFR response to renal nerve stimulation following reversible unilateral ureteric obstruction in the rat.
Physiological research.
2014; 63(6):713-22. doi:
10.33549/physiolres.932667. [PMID: 25157662] - O Sengul, I Ferah, B Polat, Z Halici, Y Bayir, M Yilmaz, N Kilic, O N Keles. Blockade of endothelin receptors with bosentan limits ischaemia/reperfusion-induced injury in rat ovaries.
European journal of obstetrics, gynecology, and reproductive biology.
2013 Oct; 170(2):458-63. doi:
10.1016/j.ejogrb.2013.06.040. [PMID: 23880599] - Christian Jung, Arnar Rafnsson, Kerstin Brismar, John Pernow. Endothelial progenitor cells in relation to endothelin-1 and endothelin receptor blockade: a randomized, controlled trial.
International journal of cardiology.
2013 Sep; 168(2):1017-22. doi:
10.1016/j.ijcard.2012.10.032. [PMID: 23168014] - H Penn, N Quillinan, K Khan, K Chakravarty, V H Ong, A Burns, C P Denton. Targeting the endothelin axis in scleroderma renal crisis: rationale and feasibility.
QJM : monthly journal of the Association of Physicians.
2013 Sep; 106(9):839-48. doi:
10.1093/qjmed/hct111. [PMID: 23696678] - Hassane Izzedine, Philippe Rouvier, Gilbert Deray. Endothelin receptor antagonism-based treatment for scleroderma renal crisis.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2013 Aug; 62(2):394-5. doi:
10.1053/j.ajkd.2013.04.016. [PMID: 23769136] - Bekir Akgun, Metin Kaplan, Caner F Demir, Aysel Sarı, Hasan H Ozdemir, Said M Berilgen. Electrophysiological effects of bosentan in rats with induced cerebral ischemia-reperfusion.
Bosnian journal of basic medical sciences.
2013 Aug; 13(3):175-9. doi:
10.17305/bjbms.2013.2358. [PMID: 23988169] - Carmine Dario Vizza, Claudio Letizia, Roberto Badagliacca, Roberto Poscia, Beatrice Pezzuto, Cristina Gambardella, Alfred Nona, Silvia Papa, Serena Marcon, Massimo Mancone, Carlo Iacoboni, Valeria Riccieri, Maurzio Volterrani, Francesco Fedele. Relationship between baseline ET-1 plasma levels and outcome in patients with idiopathic pulmonary hypertension treated with bosentan.
International journal of cardiology.
2013 Jul; 167(1):220-4. doi:
10.1016/j.ijcard.2011.12.104. [PMID: 22265324] - Anders Hebert, Annette S Jensen, Lars Idorn, Keld E Sørensen, Lars Søndergaard. The effect of bosentan on exercise capacity in Fontan patients; rationale and design for the TEMPO study.
BMC cardiovascular disorders.
2013 May; 13(?):36. doi:
10.1186/1471-2261-13-36. [PMID: 23663658] - Cho-Ming Loi, Dennis A Smith, Deepak Dalvie. Which metabolites circulate?.
Drug metabolism and disposition: the biological fate of chemicals.
2013 May; 41(5):933-51. doi:
10.1124/dmd.112.050278. [PMID: 23454828] - C Fahrmayr, J König, D Auge, M Mieth, K Münch, J Segrestaa, T Pfeifer, A Treiber, Mf Fromm. Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line.
British journal of pharmacology.
2013 May; 169(1):21-33. doi:
10.1111/bph.12126. [PMID: 23387445] - Miguel D'haeseleer, Roel Beelen, Yves Fierens, Melissa Cambron, Anne-Marie Vanbinst, Christian Verborgh, Johan Demey, Jacques De Keyser. Cerebral hypoperfusion in multiple sclerosis is reversible and mediated by endothelin-1.
Proceedings of the National Academy of Sciences of the United States of America.
2013 Apr; 110(14):5654-8. doi:
10.1073/pnas.1222560110. [PMID: 23509249] - Shinichi Takatsuki, Erika B Rosenzweig, Warren Zuckerman, Daniela Brady, Michelle Calderbank, D Dunbar Ivy. Clinical safety, pharmacokinetics, and efficacy of ambrisentan therapy in children with pulmonary arterial hypertension.
Pediatric pulmonology.
2013 Jan; 48(1):27-34. doi:
10.1002/ppul.22555. [PMID: 22511577] - Laurent Savale, Romain Magnier, Jérôme Le Pavec, Xavier Jaïs, David Montani, Dermot S O'Callaghan, Marc Humbert, Jasper Dingemanse, Gérald Simonneau, Olivier Sitbon. Efficacy, safety and pharmacokinetics of bosentan in portopulmonary hypertension.
The European respiratory journal.
2013 Jan; 41(1):96-103. doi:
10.1183/09031936.00117511. [PMID: 22653773] - Zhongchen Zhang, Xiangdong Jian, Wei Zhang, Jieru Wang, Qian Zhou. Using bosentan to treat paraquat poisoning-induced acute lung injury in rats.
PloS one.
2013; 8(10):e75943. doi:
10.1371/journal.pone.0075943. [PMID: 24155875] - Jürgen Venitz, Julia Zack, Hunter Gillies, Martine Allard, Jean Regnault, Christopher Dufton. Clinical pharmacokinetics and drug-drug interactions of endothelin receptor antagonists in pulmonary arterial hypertension.
Journal of clinical pharmacology.
2012 Dec; 52(12):1784-805. doi:
10.1177/0091270011423662. [PMID: 22205719] - Daniel J Warner, Hongming Chen, Louis-David Cantin, J Gerry Kenna, Simone Stahl, Clare L Walker, Tobias Noeske. Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
Drug metabolism and disposition: the biological fate of chemicals.
2012 Dec; 40(12):2332-41. doi:
10.1124/dmd.112.047068. [PMID: 22961681] - Jignesh M Parekh, Dhaval K Shah, Mallika Sanyal, Manish Yadav, Pranav S Shrivastav. Development of an SPE-LC-MS/MS method for simultaneous quantification of bosentan and its active metabolite hydroxybosentan in human plasma to support a bioequivalence study.
Journal of pharmaceutical and biomedical analysis.
2012 Nov; 70(?):462-70. doi:
10.1016/j.jpba.2012.06.027. [PMID: 22789899] - Janet J Maguire, Rhoda E Kuc, Anthony P Davenport. Defining the affinity and receptor sub-type selectivity of four classes of endothelin antagonists in clinically relevant human cardiovascular tissues.
Life sciences.
2012 Oct; 91(13-14):681-6. doi:
10.1016/j.lfs.2012.05.008. [PMID: 22634326]
