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内皮素A受体阻滞剂可抑制内皮素引起血管暂时舒张后的持续性收缩,使血管舒张,可治疗与内皮素有关的血管收缩性疾病。SB209670除抑制ETAR,ETB1R外,还能抑制介导收缩反应的ETB2R,能更全面地阻滞收缩反应;BQ-153和BQ-123等扩张血管时不影响血压;FR13931抑制平滑肌细胞增殖,可能对ET-1引起的肺动脉高压有效;具有口服活性的L-744453,L-754142,A-127722,PD012527,PD155080,SB217242,SB209670,BMS-18274等治疗更方便;PD151242可形成放射性结合物,使其应用更广。
Endothelin A receptor blocker can inhibit endothelins caused by sustained vasoconstriction of the blood vessels after a temporary contraction, so that vasodilatation can be treated with endothelin-related vasoconstrictive disease. In addition to ETAR and ETB1R inhibition, SB209670 can inhibit ETB2R that mediates contractile response, which can more completely block the contractile response; BQ-153 and BQ-123 do not affect blood pressure when dilated blood vessels; FR13931 inhibits smooth muscle cell proliferation, ET-1-induced pulmonary hypertension; oral administration of L-744453, L-754142, A-127722, PD012527, PD155080, SB217242, SB209670, BMS-18274 and other treatment more convenient; PD151242 can form radioactive conjugates, More widely used.