Tezosentan

Tezosentan is a non-selective ETA and ETB receptor antagonist.[1] It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events.[2]

Tezosentan
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • N-[6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-propan-2-ylpyridine-2-sulfonamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H27N9O6S
Molar mass605.624 g·mol−1
3D model (JSmol)
SMILES
  • O=S(=O)(c1ncc(cc1)C(C)C)Nc3nc(nc(OCCO)c3Oc2ccccc2OC)c5ccnc(c4n[nH]nn4)c5
InChI
  • InChI=1S/C27H27N9O6S/c1-16(2)18-8-9-22(29-15-18)43(38,39)34-26-23(42-21-7-5-4-6-20(21)40-3)27(41-13-12-37)31-24(30-26)17-10-11-28-19(14-17)25-32-35-36-33-25/h4-11,14-16,37H,12-13H2,1-3H3,(H,30,31,34)(H,32,33,35,36) Y
  • Key:TUYWTLTWNJOZNY-UHFFFAOYSA-N Y
  (verify)

References
  1. Urbanowicz W, Sogni P, Moreau R, Tazi KA, Barriere E, Poirel O, et al. (December 2004). "Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats". Gut. BMJ Publishing Group Ltd & British Society of Gastroenterology. 53 (12): 1844–9. doi:10.1136/gut.2003.036517. PMC 1774327. PMID 15542526.
  2. "Tezosentan does not appear to improve symptoms for patients with acute heart failure". Medical Studies/Trials. news-medical.net. 7 Nov 2007. Retrieved 2007-11-24.


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