Darusentan

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Darusentan Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist with Ki of 1.4 nM for ET-A receptor and 184 nM for ET-B receptor , the selectivity of ETA receptors is more than 100 times higher than that of ETB receptors. It competes for binding of radiolabeled endothelin in the membrane of rat aortic vascular smooth muscle cells (RAVSMs) with a Ki of 13 nM.

• in vitro

  Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K _i =13 nM . In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA ₂ =8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.

• in vivo

  Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats. < /p>

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  Animal Model:	Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g
  Dosage:	30 mg/kg
  Administration:	Administered orally in rat food for weeks 3 and 4
  Result:	Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg).

Darusentan Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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