Darusentan

ETA受体拮抗剂（大鼠主动脉血管平滑肌细胞中的Ki=13nM）；抑制大鼠主动脉环和肠系膜微血管中ET-1诱导的收缩（pA2s分别为8.1和7.97）；以50mg/kg降低DOCA盐高血压大鼠的收缩压；以1和5mg/kg降低正常血压猪的MAP和LVDP；降低猪LAD冠状动脉结扎诱发的缺血再灌注损伤模型中心肌梗死面积占风险面积的百分比。An ETA receptor antagonist (Ki = 13 nM in rat aortic vascular smooth muscle cells); inhibits ET-1-induced contractions in isolated rat aortic rings and mesenteric microvessels (pA2s = 8.1 and 7.97, respectively); decreases systolic blood pressure in DOCA-salt hypertensive rats at 50 mg/kg; decreases MAP and LVDP in normotensive pigs at 1 and 5 mg/kg; reduces myocardial infarct size as a percentage of the area at risk in a porcine model of LAD coronary artery ligation-induced ischemia-reperfusion injury.分子式C22H22N2O6分子量410.4COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1