Tezosentan

  • N-{6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1H-tetrazol-5-yl)-4-pyridyl]pyrimidin-4-yl}-5-isopropylpyridin-2-sulfonamid (IUPAC)
  • RITZ 1 ( Actelion / Genentech)
  • Tezosentanum (Latin )

Endothelin antagonist

Template: Infobox chemical / molecular formula search available

Tezosentan is a potential drug that is being developed under the name Veletri of the Swiss pharmaceutical company Actelion. It should be used for the treatment of acute heart failure. Medicinally, the disodium salt is used.

Pharmacology

Mechanism of Action

Tezosentan is a competitive antagonist of endothelin receptors A and B, by inhibition of binding of endothelin -1, endothelin-3 and sarafotoxin on endothelin receptors A and B, tezosentan prevents constriction of the smooth muscle.

Properties

The plasma half-life of 3-5 minutes, and the plasma protein binding of 0.2 to 60 ug / ml.

CAS registry number PubChem Receptor antagonist Active ingredient Smooth muscle tissue Xenobiotica JAMA (journal) PubMed Central
766923
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