Darusentan (BioDeep_00000690688)
代谢物信息卡片
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
数据库引用编号
5 个数据库交叉引用编号
- PubChem: 177236
- DrugBank: DB04883
- ChEMBL: CHEMBL23261
- CAS: 171714-84-4
- medchemexpress: HY-15404
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
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Current opinion in nephrology and hypertension.
2012 Mar; 21(2):128-36. doi:
10.1097/mnh.0b013e32834f0092
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Frontiers in physiology.
2012; 3(?):103. doi:
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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:
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International journal of hypertension.
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International journal of hypertension.
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Kidney international.
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Korean circulation journal.
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Canadian journal of physiology and pharmacology.
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American journal of physiology. Regulatory, integrative and comparative physiology.
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Kidney international.
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Kidney & blood pressure research.
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Experimental biology and medicine (Maywood, N.J.).
2006 Jun; 231(6):1030-3. doi:
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Experimental biology and medicine (Maywood, N.J.).
2006 Jun; 231(6):960-6. doi:
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Endocrinology.
2006 May; 147(5):2526-34. doi:
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Journal of cardiovascular pharmacology.
2006 Mar; 47(3):456-62. doi:
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Cardiovascular research.
2005 Aug; 67(2):283-90. doi:
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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:
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. [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:
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Hypertension (Dallas, Tex. : 1979).
2004 Dec; 44(6):974-81. doi:
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Journal of cardiovascular pharmacology.
2004 Nov; 44 Suppl 1(?):S151-5. doi:
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Clinical pharmacology and therapeutics.
2004 Nov; 76(5):396-408. doi:
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Circulation.
2004 Jan; 109(2):249-54. doi:
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The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation.
2004 Jan; 23(1):20-7. doi:
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Drugs.
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Journal of hypertension.
2003 Dec; 21(12):2389-97. doi:
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Laboratory investigation; a journal of technical methods and pathology.
2003 Sep; 83(9):1267-77. doi:
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Diabetologia.
2003 Jun; 46(6):856-68. doi:
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European journal of pharmacology.
2003 May; 468(3):209-16. doi:
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. [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.
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FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
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Journal of applied physiology (Bethesda, Md. : 1985).
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Kidney & blood pressure research.
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Circulation.
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Clinical science (London, England : 1979).
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Clinical science (London, England : 1979).
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Investigative radiology.
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Cardiovascular research.
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Toxicology and applied pharmacology.
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American journal of physiology. Regulatory, integrative and comparative physiology.
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Nephron.
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Nephron.
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Journal of hypertension.
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Cardiovascular research.
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Experimental nephrology.
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Gastroenterology.
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Journal of the American College of Cardiology.
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