Darusentan (BioDeep_00000690688)

   


代谢物信息卡片


Darusentan

化学式: C22H22N2O6 (410.1477792)
中文名称: 达芦生坦
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: COC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC
InChI: InChI=1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1

描述信息

C78274 - Agent Affecting Cardiovascular System > C270 - Antihypertensive Agent
D065128 - Endothelin Receptor Antagonists
C28313 - Endothelin Receptor Antagonist
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors[1]. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM[2].

同义名列表

2 个代谢物同义名

Darusentan; Lu-135252



数据库引用编号

5 个数据库交叉引用编号

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)

0 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。



文献列表

  • Yu Sun, Jinwen Liu, Bo Yang, Xiaoyong Sai, Tiande Li, Dong Wang, Rongbin Zhou. Inhibitory effect of co-administration of atorvastatin and endothelin-1 receptor antagonist on the progression of atherosclerosis in rabbit. APMIS : acta pathologica, microbiologica, et immunologica Scandinavica. 2014 Jun; 122(6):556-64. doi: 10.1111/apm.12185. [PMID: 24164644]
  • Yohann Rautureau, Ernesto L Schiffrin. Endothelin in hypertension: an update. Current opinion in nephrology and hypertension. 2012 Mar; 21(2):128-36. doi: 10.1097/mnh.0b013e32834f0092. [PMID: 22257795]
  • Ovidiu Constantin Baltatu, Radu Iliescu, Christian E Zaugg, Jane F Reckelhoff, Pat Louie, Christoph Schumacher, Luciana Aparecida Campos. Antidiuretic effects of the endothelin receptor antagonist avosentan. Frontiers in physiology. 2012; 3(?):103. doi: 10.3389/fphys.2012.00103. [PMID: 22529820]
  • Patricia N Sidharta, Paul L M van Giersbergen, Atef Halabi, Jasper Dingemanse. Macitentan: entry-into-humans study with a new endothelin receptor antagonist. European journal of clinical pharmacology. 2011 Oct; 67(10):977-84. doi: 10.1007/s00228-011-1043-2. [PMID: 21541781]
  • Jianmin Gu, Xiaowei Shi, Yumin Du, Wei Wang, Xiufang Du, Lantong Zhang. Determination of darusentan enantiomers in rat plasma by enantioselective liquid chromatography with tandem mass spectrometry using cellulose-based chiral stationary phase. Journal of separation science. 2011 Oct; 34(19):2680-5. doi: 10.1002/jssc.201100433. [PMID: 21823235]
  • Z Khawaja, C S Wilcox. Role of the kidneys in resistant hypertension. International journal of hypertension. 2011 Mar; 2011(?):143471. doi: 10.4061/2011/143471. [PMID: 21461391]
  • Charles Faselis, Michael Doumas, Vasilios Papademetriou. Common secondary causes of resistant hypertension and rational for treatment. International journal of hypertension. 2011 Mar; 2011(?):236239. doi: 10.4061/2011/236239. [PMID: 21423678]
  • Ivana Lazich, George L Bakris. Endothelin antagonism in patients with resistant hypertension and hypertension nephropathy. Contributions to nephrology. 2011; 172(?):223-234. doi: 10.1159/000328988. [PMID: 21894002]
  • Matthias Barton. Endothelin antagonism and reversal of proteinuric renal disease in humans. Contributions to nephrology. 2011; 172(?):210-222. doi: 10.1159/000328702. [PMID: 21894001]
  • Donald E Wesson, Jan Simoni. Acid retention during kidney failure induces endothelin and aldosterone production which lead to progressive GFR decline, a situation ameliorated by alkali diet. Kidney international. 2010 Dec; 78(11):1128-35. doi: 10.1038/ki.2010.348. [PMID: 20861823]
  • Kyoung Ah Lim, Kwan Chang Kim, Min-Sun Cho, Bo En Lee, Hae Soon Kim, Young Mi Hong. Gene expression of endothelin-1 and endothelin receptor a on monocrotaline-induced pulmonary hypertension in rats after bosentan treatment. Korean circulation journal. 2010 Sep; 40(9):459-64. doi: 10.4070/kcj.2010.40.9.459. [PMID: 20967148]
  • Darren M Allcock, James R Sowers. Best strategies for hypertension management in type 2 diabetes and obesity. Current diabetes reports. 2010 Apr; 10(2):139-44. doi: 10.1007/s11892-010-0100-z. [PMID: 20425573]
  • Michael A Weber, Henry Black, George Bakris, Henry Krum, Stuart Linas, Robert Weiss, Jennifer V Linseman, Brian L Wiens, Marshelle S Warren, Lars H Lindholm. A selective endothelin-receptor antagonist to reduce blood pressure in patients with treatment-resistant hypertension: a randomised, double-blind, placebo-controlled trial. Lancet (London, England). 2009 Oct; 374(9699):1423-31. doi: 10.1016/s0140-6736(09)61500-2. [PMID: 19748665]
  • Jennifer Frank, David Sommerfeld. Clinical approach in treatment of resistant hypertension. Integrated blood pressure control. 2009; 2(?):9-23. doi: 10.2147/ibpc.s4315. [PMID: 21966229]
  • Stephan J L Bakker, Rijk O B Gans, Gerjan Navis. Dietary alkalinization and darusentan for prevention of decline in glomerular filtration rate in rats fed a casein diet. Kidney international. 2008 Dec; 74(12):1625-6; author reply 1626. doi: 10.1038/ki.2008.434. [PMID: 19034308]
  • Philipp Kalk, Philine Senf, Maria Deja, Bodil Petersen, Thilo Busch, Christian Bauer, Willehad Boemke, Udo Kaisers, Berthold Hocher. Inhalation of an endothelin receptor A antagonist attenuates pulmonary inflammation in experimental acute lung injury. Canadian journal of physiology and pharmacology. 2008 Aug; 86(8):511-5. doi: 10.1139/y08-046. [PMID: 18758498]
  • Bodil Petersen, Maria Deja, Roland Bartholdy, Bernd Donaubauer, Sven Laudi, Roland C E Francis, Willehad Boemke, Udo Kaisers, Thilo Busch. Inhalation of the ETA receptor antagonist LU-135252 selectively attenuates hypoxic pulmonary vasoconstriction. American journal of physiology. Regulatory, integrative and comparative physiology. 2008 Feb; 294(2):R601-5. doi: 10.1152/ajpregu.00739.2007. [PMID: 18077516]
  • D E Wesson, T Nathan, T Rose, J Simoni, R M Tran. Dietary protein induces endothelin-mediated kidney injury through enhanced intrinsic acid production. Kidney international. 2007 Feb; 71(3):210-7. doi: 10.1038/sj.ki.5002036. [PMID: 17164833]
  • Stephan R Orth, Günter Schiele, Bernhard Banas, Eberhard Ritz, Kerstin Amann. Effect of a selective endothelin receptor A blocker on cardiovascular remodeling in uninephrectomized spontaneously hypertensive rats of the stroke-prone strain. Kidney & blood pressure research. 2007; 30(6):400-7. doi: 10.1159/000108626. [PMID: 17890870]
  • Jana Ortmann, Philipp C Nett, Jennifer Celeiro, Regina Hofmann-Lehmann, Luigi Tornillo, Luigi M Terracciano, Matthias Barton. Downregulation of renal endothelin-converting enzyme 2 expression in early autoimmune diabetes. Experimental biology and medicine (Maywood, N.J.). 2006 Jun; 231(6):1030-3. doi: . [PMID: 16741043]
  • Bernd Donaubauer, Thilo Busch, Robert Lachmann, Maria Deja, Bodil Petersen, Roland Francis, Annette Träger, Michael Ebsen, Willehad Boemke, Udo Kaisers. Low-dose inhalation of an endothelin-A receptor antagonist in experimental acute lung injury: ET-1 plasma concentration and pulmonary inflammation. Experimental biology and medicine (Maywood, N.J.). 2006 Jun; 231(6):960-6. doi: NULL. [PMID: 16741031]
  • Sebastian J Buss, Johannes Backs, Michael M Kreusser, Stefan E Hardt, Christiane Maser-Gluth, Hugo A Katus, Markus Haass. Spironolactone preserves cardiac norepinephrine reuptake in salt-sensitive Dahl rats. Endocrinology. 2006 May; 147(5):2526-34. doi: 10.1210/en.2005-1167. [PMID: 16439456]
  • Tobias Traupe, Jana Ortmann, Elvira Haas, Klaus Münter, Niranjan Parekh, Regina Hofmann-Lehmann, Karin Baumann, Matthias Barton. Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. Journal of cardiovascular pharmacology. 2006 Mar; 47(3):456-62. doi: 10.1097/01.fjc.0000211709.10735.32. [PMID: 16633090]
  • Johannes Backs, Elke Bresch, Matthias Lutz, Arnt V Kristen, Markus Haass. Endothelin-1 inhibits the neuronal norepinephrine transporter in hearts of male rats. Cardiovascular research. 2005 Aug; 67(2):283-90. doi: 10.1016/j.cardiores.2005.03.018. [PMID: 16005303]
  • Thomas Lattmann, Marc Hein, Sibylle Horber, Jana Ortmann, Mauro M Teixeira, Danielle G Souza, Elvira Haas, Luigi Tornillo, Klaus Münter, Wilhelm Vetter, Matthias Barton. Activation of pro-inflammatory and anti-inflammatory cytokines in host organs during chronic allograft rejection: role of endothelin receptor signaling. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2005 May; 5(5):1042-9. doi: 10.1111/j.1600-6143.2005.00807.x. [PMID: 15816884]
  • Cipy Hofman, Efraim Gabai, Edna Peleg, Klaus Munter, Talma Rosenthal. Endothelin A antagonist LU-135252 and trandolapril in the treatment of the Cohen-Rosenthal diabetic hypertensive rat. Blood pressure. 2005; 14(2):114-9. doi: 10.1080/08037050510008913. [PMID: 16036489]
  • Jana Ortmann, Kerstin Amann, Ralf P Brandes, Matthias Kretzler, Klaus Münter, Niranjan Parekh, Tobias Traupe, Melanie Lange, Thomas Lattmann, Matthias Barton. Role of podocytes for reversal of glomerulosclerosis and proteinuria in the aging kidney after endothelin inhibition. Hypertension (Dallas, Tex. : 1979). 2004 Dec; 44(6):974-81. doi: 10.1161/01.hyp.0000149249.09147.b4. [PMID: 15545511]
  • Maria Deja, Thilo Busch, Steffen Wolf, Bernd Donaubauer, Bodil Petersen, Joerg Skomrock, Willehad Boemke, Udo Kaisers. Inhalation of the endothelin-A receptor antagonist LU-135252 at various doses in experimental acute lung injury. Journal of cardiovascular pharmacology. 2004 Nov; 44 Suppl 1(?):S151-5. doi: 10.1097/01.fjc.0000166261.42723.b7. [PMID: 15838267]
  • Anna Mitchell, Birte Lückebergfeld, Sandra Bührmann, Uljana Rushentsova, Jens Nürnberger, Winfried Siffert, Rafael F Schäfers, Thomas Philipp, René R Wenzel. Effects of systemic endothelin A receptor antagonism in various vascular beds in men: in vivo interactions of the major blood pressure-regulating systems and associations with the GNB3 C825T polymorphism. Clinical pharmacology and therapeutics. 2004 Nov; 76(5):396-408. doi: 10.1016/j.clpt.2004.07.011. [PMID: 15536455]
  • John A Schirger, Horng H Chen, Michihisa Jougasaki, Ondrej Lisy, Guido Boerrigter, Alessandro Cataliotti, John C Burnett. Endothelin A receptor antagonism in experimental congestive heart failure results in augmentation of the renin-angiotensin system and sustained sodium retention. Circulation. 2004 Jan; 109(2):249-54. doi: 10.1161/01.cir.0000109139.69775.eb. [PMID: 14691038]
  • Jutta Bergler-Klein, Richard Pacher, Rudolf Berger, Anda Bojic, Brigitte Stanek. Neurohumoral and hemodynamic effects of the selective endothelin antagonist darusentan in advanced chronic heart failure. The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation. 2004 Jan; 23(1):20-7. doi: 10.1016/s1053-2498(03)00062-7. [PMID: 14734123]
  • Georg Ertl, Johann Bauersachs. Endothelin receptor antagonists in heart failure: current status and future directions. Drugs. 2004; 64(10):1029-40. doi: 10.2165/00003495-200464100-00001. [PMID: 15139784]
  • Lars Rothermund, Peter Kossmehl, Hans-H Neumayer, Martin Paul, Reinhold Kreutz. Renal damage is not improved by blockade of endothelin receptors in primary renin-dependent hypertension. Journal of hypertension. 2003 Dec; 21(12):2389-97. doi: 10.1097/00004872-200312000-00028. [PMID: 14654760]
  • Marie-Luise Gross, Eberhard Ritz, Arne Schoof, Burkhard Helmke, Amy Parkman, Orien Tulp, Klaus Münter, Kerstin Amann. Renal damage in the SHR/N-cp type 2 diabetes model: comparison of an angiotensin-converting enzyme inhibitor and endothelin receptor blocker. Laboratory investigation; a journal of technical methods and pathology. 2003 Sep; 83(9):1267-77. doi: 10.1097/01.lab.0000085188.23709.29. [PMID: 13679434]
  • M-L Gross, A El-Shakmak, A Szábó, A Koch, A Kuhlmann, K Münter, E Ritz, K Amann. ACE-inhibitors but not endothelin receptor blockers prevent podocyte loss in early diabetic nephropathy. Diabetologia. 2003 Jun; 46(6):856-68. doi: 10.1007/s00125-003-1106-8. [PMID: 12802493]
  • Lars Rothermund, Tobias Traupe, Maike Dieterich, Peter Kossmehl, Chana Yagil, Yoram Yagil, Reinhold Kreutz. Nephroprotective effects of the endothelin ET(A) receptor antagonist darusentan in salt-sensitive genetic hypertension. European journal of pharmacology. 2003 May; 468(3):209-16. doi: 10.1016/s0014-2999(03)01714-x. [PMID: 12754059]
  • M Rigol, M Heras, N Solanes, F Epelde, E Roig, F Pérez-Villa, M Roqué, G Sanz. Enalaprilat, losartan and LU 135252 in coronary blood flow regulation. European journal of clinical investigation. 2003 May; 33(5):363-9. doi: 10.1046/j.1365-2362.2003.01160.x. [PMID: 12713448]
  • Berthold Hocher, Philipp Kalk, Torsten Slowinski, Michael Godes, Alexander Mach, Sophia Herzfeld, Doreen Wiesner, Petra Clara Arck, Hans-H Neumayer, Benno Nafz. ETA receptor blockade induces tubular cell proliferation and cyst growth in rats with polycystic kidney disease. Journal of the American Society of Nephrology : JASN. 2003 Feb; 14(2):367-76. doi: 10.1097/01.asn.0000042165.63601.65. [PMID: 12538737]
  • Thomas Quaschning, Frank Ruschitzka, Thomas Stallmach, Sidney Shaw, Henning Morawietz, Winfried Goettsch, Matthias Hermann, Torsten Slowinski, Franz Theuring, Berthold Hocher, Thomas F Lüscher, Max Gassmann. Erythropoietin-induced excessive erythrocytosis activates the tissue endothelin system in mice. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 2003 Feb; 17(2):259-61. doi: 10.1096/fj.02-0296fje. [PMID: 12490547]
  • Friedrich C Blumberg, Konrad Wolf, Michael Arzt, Cornelia Lorenz, Günter A J Riegger, Michael Pfeifer. Effects of ET-A receptor blockade on eNOS gene expression in chronic hypoxic rat lungs. Journal of applied physiology (Bethesda, Md. : 1985). 2003 Feb; 94(2):446-52. doi: 10.1152/japplphysiol.00239.2002. [PMID: 12391096]
  • Tobias Saam, Heimo Ehmke, Christian Haas, Eberhard Ritz, Kerstin Amann. Effect of endothelin blockade on early cardiovascular remodeling in the one-clip-two-kidney hypertension of the rat. Kidney & blood pressure research. 2003; 26(5-6):325-32. doi: 10.1159/000073938. [PMID: 14610336]
  • Thomas F Lüscher, Frank Enseleit, Richard Pacher, Veselin Mitrovic, Matthias R Schulze, Roland Willenbrock, Rainer Dietz, Valentin Rousson, David Hürlimann, Sebastian Philipp, Thomas Notter, Georg Noll, Frank Ruschitzka. Hemodynamic and neurohumoral effects of selective endothelin A (ET(A)) receptor blockade in chronic heart failure: the Heart Failure ET(A) Receptor Blockade Trial (HEAT). Circulation. 2002 Nov; 106(21):2666-72. doi: 10.1161/01.cir.0000038497.80095.e1. [PMID: 12438291]
  • Jörg Trenkner, Friedrich Priem, Christian Bauer, Hans-Hellmut Neumayer, Manfred Raschak, Berthold Hocher. Endothelin receptor A blockade reduces proteinuria and vascular hypertrophy in spontaneously hypertensive rats on high-salt diet in a blood-pressure-independent manner. Clinical science (London, England : 1979). 2002 Aug; 103 Suppl 48(?):385S-388S. doi: 10.1042/cs103s385s. [PMID: 12193128]
  • Sebastian Philipp, Jan Monti, Ines Pagel, Thomas Langenickel, Thomas Notter, Frank Ruschitzka, Thomas Lüscher, Rainer Dietz, Roland Willenbrock. Treatment with darusentan over 21 days improved cGMP generation in patients with chronic heart failure. Clinical science (London, England : 1979). 2002 Aug; 103 Suppl 48(?):249S-253S. doi: 10.1042/cs103s249s. [PMID: 12193097]
  • Terézia B Andrási, Violetta Kékesi, Anna Blázovics, István Dóbi, Gábor Szabó, Alexander Juhász-Nagy. ET(A) receptor blockade protects the small intestine against ischaemia/reperfusion injury in dogs via an enhancement of antioxidant defences. Clinical science (London, England : 1979). 2002 Aug; 103 Suppl 48(?):59S-63S. doi: 10.1042/cs103s059s. [PMID: 12193055]
  • Friedrich C Blumberg, Cornelia Lorenz, Konrad Wolf, Peter Sandner, Günter A J Riegger, Michael Pfeifer. Increased pulmonary prostacyclin synthesis in rats with chronic hypoxic pulmonary hypertension. Cardiovascular research. 2002 Jul; 55(1):171-7. doi: 10.1016/s0008-6363(02)00318-8. [PMID: 12062720]
  • Gunnar Tepe, Ute Brehme, Harald Seeger, Manfred Raschack, Claus D Claussen, Stephan H Duda. Endothelin A receptor antagonist LU 135252 inhibits hypercholesterolemia-induced, but not deendothelialization-induced, atherosclerosis in rabbit arteries. Investigative radiology. 2002 Jun; 37(6):349-55. doi: 10.1097/00004424-200206000-00007. [PMID: 12021592]
  • Livius V d'Uscio, Matthias Barton, Sidney Shaw, Thomas F Lüscher. Chronic ET(A) receptor blockade prevents endothelial dysfunction of small arteries in apolipoprotein E-deficient mice. Cardiovascular research. 2002 Feb; 53(2):487-95. doi: 10.1016/s0008-6363(01)00469-2. [PMID: 11827700]
  • Jan P Loennechen, Odd G Nilsen, Ingerid Arbo, Petter Aadahl, Turid Nilsen, Helge L Waldum, Arne K Sandvik, O Ellingsen. Chronic exposure to carbon monoxide and nicotine: endothelin ET(A) receptor antagonism attenuates carbon monoxide-induced myocardial hypertrophy in rat. Toxicology and applied pharmacology. 2002 Jan; 178(1):8-14. doi: 10.1006/taap.2001.9300. [PMID: 11781074]
  • L E Spieker, G Noll, F T Ruschitzka, T F Lüscher. Endothelin receptor antagonists in congestive heart failure: a new therapeutic principle for the future?. Journal of the American College of Cardiology. 2001 May; 37(6):1493-505. doi: 10.1016/s0735-1097(01)01210-4. [PMID: 11345356]
  • W Boemke, B Hocher, N Schleyer, M O Krebs, G Kaczmarczyk. Hemodynamic, renal, and endocrine responses to acute ET(A) blockade at different ANG II plasma levels. American journal of physiology. Regulatory, integrative and comparative physiology. 2001 May; 280(5):R1322-31. doi: 10.1152/ajpregu.2001.280.5.r1322. [PMID: 11294750]
  • T Knoll, S Schult, R Birck, C Braun, M S Michel, S Bross, K P Juenemann, M Kirchengast, P Rohmeiss. Therapeutic administration of an endothelin-A receptor antagonist after acute ischemic renal failure dose-dependently improves recovery of renal function. Journal of cardiovascular pharmacology. 2001 Apr; 37(4):483-8. doi: 10.1097/00005344-200104000-00015. [PMID: 11300661]
  • R Berger, B Stanek, M Hülsmann, B Frey, S Heher, R Pacher, T Neunteufl. Effects of endothelin a receptor blockade on endothelial function in patients with chronic heart failure. Circulation. 2001 Feb; 103(7):981-6. doi: 10.1161/01.cir.103.7.981. [PMID: 11181473]
  • B Hocher, A Schwarz, D Reinbacher, J Jacobi, A Lun, F Priem, C Bauer, H H Neumayer, M Raschack. Effects of endothelin receptor antagonists on the progression of diabetic nephropathy. Nephron. 2001 Feb; 87(2):161-9. doi: 10.1159/000045906. [PMID: 11244312]
  • F Schweda, A Schweda, M Pfeifer, F C Blumberg, M C Kammerl, S R Holmer, G A Riegger, B K Krämer. Role of endothelins for the regulation of renal renin gene expression. Journal of cardiovascular pharmacology. 2000 Nov; 36(5 Suppl 1):S187-90. doi: 10.1097/00005344-200036051-00057. [PMID: 11078373]
  • F Schweda, F C Blumberg, A Schweda, C Nabel, S R Holmer, G A Riegger, M Pfeifer, B K Krämer. Effects of chronic hypoxia on renal PDGF-A, PDGF-B, and VEGF gene expression in rats. Nephron. 2000 Oct; 86(2):161-6. doi: 10.1159/000045735. [PMID: 11014986]
  • J Bauersachs, C Braun, D Fraccarollo, J Widder, G Ertl, L Schilling, M Kirchengast, P Rohmeiss. Improvement of renal dysfunction in rats with chronic heart failure after myocardial infarction by treatment with the endothelin A receptor antagonist, LU 135252. Journal of hypertension. 2000 Oct; 18(10):1507-14. doi: 10.1097/00004872-200018100-00020. [PMID: 11057440]
  • T Foitzik, G Eibl, H G Hotz, J Faulhaber, M Kirchengast, H J Buhr. Endothelin receptor blockade in severe acute pancreatitis leads to systemic enhancement of microcirculation, stabilization of capillary permeability, and improved survival rates. Surgery. 2000 Sep; 128(3):399-407. doi: 10.1067/msy.2000.107104. [PMID: 10965310]
  • J Bauersachs, D Fraccarollo, P Galuppo, J Widder, G Ertl. Endothelin-receptor blockade improves endothelial vasomotor dysfunction in heart failure. Cardiovascular research. 2000 Jul; 47(1):142-9. doi: 10.1016/s0008-6363(00)00083-3. [PMID: 10869540]
  • C Braun, S Vetter, T Conzelmann, M Schaub, M Kirchengast, F J van der Woude, P Rohmeiss. Improved recovery following posttransplant acute renal failure in rat renal isografts with an oral endothelin-A receptor antagonist. Experimental nephrology. 2000 Jul; 8(4-5):283-90. doi: 10.1159/000020680. [PMID: 10940728]
  • J J Cho, B Hocher, H Herbst, J D Jia, M Ruehl, E G Hahn, E O Riecken, D Schuppan. An oral endothelin-A receptor antagonist blocks collagen synthesis and deposition in advanced rat liver fibrosis. Gastroenterology. 2000 Jun; 118(6):1169-78. doi: 10.1016/s0016-5085(00)70370-2. [PMID: 10833492]
  • L E Spieker, V Mitrovic, G Noll, R Pacher, M R Schulze, J Muntwyler, C Schalcher, W Kiowski, T F Lüscher. Acute hemodynamic and neurohumoral effects of selective ET(A) receptor blockade in patients with congestive heart failure. ET 003 Investigators. Journal of the American College of Cardiology. 2000 Jun; 35(7):1745-52. doi: 10.1016/s0735-1097(00)00649-5. [PMID: 10841220]
  • T Foitzik, G Eibl, H J Buhr. Therapy for microcirculatory disorders in severe acute pancreatitis: comparison of delayed therapy with ICAM-1 antibodies and a specific endothelin A receptor antagonist. Journal of gastrointestinal surgery : official journal of the Society for Surgery of the Alimentary Tract. 2000 May; 4(3):240-6; discussion 247. doi: 10.1016/s1091-255x(00)80072-4. [PMID: 10769086]
  • S Dhein, S Hochreuther, C Aus Dem Spring, K Bollig, C Hufnagel, M Raschack. Long-term effects of the endothelin(A) receptor antagonist LU 135252 and the angiotensin-converting enzyme inhibitor trandolapril on diabetic angiopathy and nephropathy in a chronic type I diabetes mellitus rat model. The Journal of pharmacology and experimental therapeutics. 2000 May; 293(2):351-9. doi: NULL. [PMID: 10773002]
  • Matthias Barton, Ingrid Vos, Sidney Shaw, Peter Boer, Livius V D'Uscio, Hermann-Josef Gröne, Ton J Rabelink, Thomas Lattmann, Pierre Moreau, Thomas F Lüscher. Dysfunctional renal nitric oxide synthase as a determinant of salt-sensitive hypertension: mechanisms of renal artery endothelial dysfunction and role of endothelin for vascular hypertrophy and Glomerulosclerosis. Journal of the American Society of Nephrology : JASN. 2000 May; 11(5):835-845. doi: 10.1681/asn.v115835. [PMID: 10770961]
  • M Burkhardt, M Barton, S G Shaw. Receptor- and non-receptor-mediated clearance of big-endothelin and endothelin-1: differential effects of acute and chronic ETA receptor blockade. Journal of hypertension. 2000 Mar; 18(3):273-9. doi: 10.1097/00004872-200018030-00006. [PMID: 10726713]
  • F Schweda, F C Blumberg, A Schweda, M Kammerl, S R Holmer, G A Riegger, M Pfeifer, B K Krämer. Effects of chronic hypoxia on renal renin gene expression in rats. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association. 2000 Jan; 15(1):11-5. doi: 10.1093/ndt/15.1.11. [PMID: 10607761]
  • M Barton, R Carmona, H Morawietz, L V d'Uscio, W Goettsch, H Hillen, C C Haudenschild, J E Krieger, K Münter, T Lattmann, T F Lüscher, S Shaw. Obesity is associated with tissue-specific activation of renal angiotensin-converting enzyme in vivo: evidence for a regulatory role of endothelin. Hypertension (Dallas, Tex. : 1979). 2000 Jan; 35(1 Pt 2):329-36. doi: 10.1161/01.hyp.35.1.329. [PMID: 10642320]
  • H Berthold, A Just, H R Kirchheim, H Ehmke. Interaction between nitric oxide and endogenous vasoconstrictors in control of renal blood flow. Hypertension (Dallas, Tex. : 1979). 1999 Dec; 34(6):1254-8. doi: 10.1161/01.hyp.34.6.1254. [PMID: 10601127]
  • J Schmect, P Krafft, A Gröschler, A Heller, H Neuhof, K van Ackern, T Koch. Characterization and distribution of endothelin receptors in the pulmonary circulation: investigation of isolated, perfused, and ventilated rabbit lungs. Shock (Augusta, Ga.). 1999 Oct; 12(4):247-54. doi: 10.1097/00024382-199910000-00001. [PMID: 10509625]
  • C Braun, T Conzelmann, S Vetter, M Schaub, W E Back, B Yard, M Kirchengast, S G Tullius, P Schnülle, F J van der Woude, P Rohmeiss. Prevention of chronic renal allograft rejection in rats with an oral endothelin A receptor antagonist. Transplantation. 1999 Sep; 68(6):739-46. doi: 10.1097/00007890-199909270-00005. [PMID: 10515373]
  • E Brochu, S Lacasse, C Moreau, M Lebel, I Kingma, J H Grose, R Larivière. Endothelin ET(A) receptor blockade prevents the progression of renal failure and hypertension in uraemic rats. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association. 1999 Aug; 14(8):1881-8. doi: 10.1093/ndt/14.8.1881. [PMID: 10462266]
  • E Brochu, S Lacasse, R Larivière, I Kingma, J H Grose, M Lebel. Differential effects of endothelin-1 antagonists on erythropoietin-induced hypertension in renal failure. Journal of the American Society of Nephrology : JASN. 1999 Jul; 10(7):1440-6. doi: 10.1681/asn.v1071440. [PMID: 10405199]
  • H Berthold, K Münter, A Just, H R Kirchheim, H Ehmke. Stimulation of the renin-angiotensin system by endothelin subtype A receptor blockade in conscious dogs. Hypertension (Dallas, Tex. : 1979). 1999 Jun; 33(6):1420-4. doi: 10.1161/01.hyp.33.6.1420. [PMID: 10373226]
  • H Ehmke, J Faulhaber, K Münter, M Kirchengast, R J Wiesner. Chronic ETA receptor blockade attenuates cardiac hypertrophy independently of blood pressure effects in renovascular hypertensive rats. Hypertension (Dallas, Tex. : 1979). 1999 Apr; 33(4):954-60. doi: 10.1161/01.hyp.33.4.954. [PMID: 10205230]
  • H Berthold, K Münter, A Just, H R Kirchheim, H Ehmke. Contribution of endothelin to renal vascular tone and autoregulation in the conscious dog. The American journal of physiology. 1999 03; 276(3):F417-24. doi: 10.1152/ajprenal.1999.276.3.f417. [PMID: 10070165]
  • S R Orth, G Odoni, K Amann, P Strzelczyk, M Raschack, E Ritz. The ET(A) receptor blocker LU 135252 prevents chronic transplant nephropathy in the 'Fisher to Lewis' model. Journal of the American Society of Nephrology : JASN. 1999 Feb; 10(2):387-91. doi: 10.1681/asn.v102387. [PMID: 10215340]
  • M Barton, C C Haudenschild, L V d'Uscio, S Shaw, K Münter, T F Lüscher. Endothelin ETA receptor blockade restores NO-mediated endothelial function and inhibits atherosclerosis in apolipoprotein E-deficient mice. Proceedings of the National Academy of Sciences of the United States of America. 1998 Nov; 95(24):14367-72. doi: 10.1073/pnas.95.24.14367. [PMID: 9826706]
  • J Schmeck, R Janzen, K Münter, H Neuhof, T Koch, R Janzen. Endothelin-1 and thromboxane A2 increase pulmonary vascular resistance in granulocyte-mediated lung injury. Critical care medicine. 1998 Nov; 26(11):1868-74. doi: 10.1097/00003246-199811000-00031. [PMID: 9824081]
  • T Foitzik, J Faulhaber, H G Hotz, M Kirchengast, H J Buhr. Endothelin receptor blockade improves fluid sequestration, pancreatic capillary blood flow, and survival in severe experimental pancreatitis. Annals of surgery. 1998 Nov; 228(5):670-5. doi: 10.1097/00000658-199811000-00006. [PMID: 9833805]
  • G W Moe, A Albernaz, G O Naik, M Kirchengast, D J Stewart. Beneficial effects of long-term selective endothelin type A receptor blockade in canine experimental heart failure. Cardiovascular research. 1998 Sep; 39(3):571-9. doi: 10.1016/s0008-6363(98)00169-2. [PMID: 9861299]
  • A T Gonon, Q D Wang, J Pernow. The endothelin A receptor antagonist LU 135252 protects the myocardium from neutrophil injury during ischaemia/reperfusion. Cardiovascular research. 1998 Sep; 39(3):674-82. doi: 10.1016/s0008-6363(98)00167-9. [PMID: 9861311]
  • P Cernacek, L Franchi, J Dupuis, J L Rouleau, M Levy. Radioreceptor assay of an endothelin A receptor antagonist in plasma and urine. Clinical chemistry. 1998 Aug; 44(8 Pt 1):1666-73. doi: 10.1093/clinchem/44.8.1666. [PMID: 9702953]
  • A Benigni, D Corna, R Maffi, G Benedetti, C Zoja, G Remuzzi. Renoprotective effect of contemporary blocking of angiotensin II and endothelin-1 in rats with membranous nephropathy. Kidney international. 1998 Aug; 54(2):353-9. doi: 10.1046/j.1523-1755.1998.00011.x. [PMID: 9690201]
  • R Birck, T Knoll, C Braun, M Kirchengast, K Münter, F J van der Woude, P Rohmeiss. Improvement of postischemic acute renal failure with the novel orally active endothelin-A receptor antagonist LU 135252 in the rat. Journal of cardiovascular pharmacology. 1998 Jul; 32(1):80-6. doi: 10.1097/00005344-199807000-00013. [PMID: 9676725]
  • T Foitzik, H G Hotz, B Hot, M Kirchengast, H J Buhr. Endothelin-1 mediates the alcohol-induced reduction of pancreatic capillary blood flow. Journal of gastrointestinal surgery : official journal of the Society for Surgery of the Alimentary Tract. 1998 Jul; 2(4):379-84. doi: 10.1016/s1091-255x(98)80078-4. [PMID: 9841996]
  • S R Orth, J P Esslinger, K Amann, U Schwarz, M Raschack, E Ritz. Nephroprotection of an ET(A)-receptor blocker (LU 135252) in salt-loaded uninephrectomized stroke-prone spontaneously hypertensive rats. Hypertension (Dallas, Tex. : 1979). 1998 Apr; 31(4):995-1001. doi: 10.1161/01.hyp.31.4.995. [PMID: 9535426]
  • K Huntington, P Picard, G Moe, D J Stewart, A Albernaz, J C Monge. Increased cardiac and pulmonary endothelin-1 mRNA expression in canine pacing-induced heart failure. Journal of cardiovascular pharmacology. 1998; 31 Suppl 1(?):S424-6. doi: 10.1097/00005344-199800001-00121. [PMID: 9595502]
  • B Hocher, A Lun, F Priem, H H Neumayer, M Raschack. Renal endothelin system in diabetes: comparison of angiotensin-converting enzyme inhibition and endothelin-A antagonism. Journal of cardiovascular pharmacology. 1998; 31 Suppl 1(?):S492-5. doi: 10.1097/00005344-199800001-00141. [PMID: 9595522]
  • K Münter, S Hergenröder, M Kirchengast. Endothelin-A receptor antagonist combined with hydralazine improves survival and renal function in hypertensive rats. Journal of cardiovascular pharmacology. 1998; 31 Suppl 1(?):S245-8. doi: 10.1097/00005344-199800001-00069. [PMID: 9595450]
  • M Barton, S Shaw, L V d'Uscio, P Moreau, T F Lüscher. Differential modulation of the renal and myocardial endothelin system by angiotensin II in Vivo. Effects of chronic selective ETA receptor blockade. Journal of cardiovascular pharmacology. 1998; 31 Suppl 1(?):S265-8. doi: 10.1097/00005344-199800001-00075. [PMID: 9595456]
  • L V d'Uscio, M Barton, S Shaw, P Moreau, T F Lüscher. Structure and function of small arteries in salt-induced hypertension: effects of chronic endothelin-subtype-A-receptor blockade. Hypertension (Dallas, Tex. : 1979). 1997 Oct; 30(4):905-11. doi: 10.1161/01.hyp.30.4.905. [PMID: 9336391]
  • M Barton, S Shaw, L V d'Uscio, P Moreau, T F Lüscher. Angiotensin II increases vascular and renal endothelin-1 and functional endothelin converting enzyme activity in vivo: role of ETA receptors for endothelin regulation. Biochemical and biophysical research communications. 1997 Sep; 238(3):861-5. doi: 10.1006/bbrc.1997.7394. [PMID: 9325182]
  • S Prié, T K Leung, P Cernacek, J W Ryan, J Dupuis. The orally active ET(A) receptor antagonist (+)-(S)-2-(4,6-dimethoxy-pyrimidin-2-yloxy)-3-methoxy-3,3-diphe nyl-propionic acid (LU 135252) prevents the development of pulmonary hypertension and endothelial metabolic dysfunction in monocrotaline-treated rats. The Journal of pharmacology and experimental therapeutics. 1997 Sep; 282(3):1312-8. doi: NULL. [PMID: 9316840]
  • E L Schiffrin, A Turgeon, L Y Deng. Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in rats. British journal of pharmacology. 1997 Jul; 121(5):935-40. doi: 10.1038/sj.bjp.0701224. [PMID: 9222550]
  • . . . . doi: . [PMID: 19920913]