SB-204741

5-HT2B受体拮抗剂；抑制5-HT诱发的大鼠胃底分离收缩(pA2=7.95)；对5-HT2B受体具有选择性，优于各种CNS受体(Kis=1-100µM)；以每天1mg/kg的剂量服用，可预防Bmpr2突变小鼠遗传性PAH模型中PAH的发生并降低血管僵硬性；降低DOCA盐高血压大鼠的血压。A 5-HT2B receptor antagonist; inhibits 5-HT-induced contraction of isolated rat stomach fundus (pA2 = 7.95); selective for 5-HT2B receptors over various CNS receptors (Kis = 1-100 µM); prevents the development of PAH and reduces vascular stiffness in a Bmpr2 mutant mouse model of hereditary PAH at 1 mg/kg per day; reduces blood pressure in DOCA-salt hypertensive rats.分子式C14H14N4OS分子量286.4O=C(NC1=CC(C=CN2C)=C2C=C1)NC3=CC(C)=NS3