- 生物活性
Daltroban (BM-13505) 是一种选择性和特异性血栓素 A2 (TXA2) 受体拮抗剂。Daltroban 增加血管平滑肌细胞内钙。Daltroban 对再灌注损伤有保护作用。
- 靶点
TXA
2
- 体内研究
Daltroban (BM-13505) (1 mg/kg; i.v.; per hour) exerts protective effect in reperfusion injury following acute myocardial ischemia in cats.
In comparison with vehicle (physiological saline)-treated cats, Daltroban (20 mg/kg per hour i.v.) reduces the ischaemia-induced rise in the ST segment and prevented the development of a Q-wave in the ECG during reperfusion. Daltroban protects the myocardium from ischaemic injury and that this effect involves prevention of ischaemia-induced leukocytosis.
Animal Model:
Adult male cats (2.8 to 4.6 kg; anesthetized cat model)
Dosage:
1 mg/kg
Administration:
i.v.; 30 minutes before reperfusion at a rate of 1 mg/kg followed by 1 mg/kg/hour
Result:
Significantly reduced the area of ischemic tissue as a percent of total left ventricular mass and total area at risk, without altering basic hemodynamics and thereby not influencing myocardial oxygen demand.
- 化学性质
从含水乙醇得白色结晶，熔点138～140℃。
- 为血栓素A2受体的特异性强效拮抗剂，有抑制血小板聚集，影响血栓形成，防止猝死等作用。用于治疗心肌缺血、出血性休克、内毒性休克、心肺性猝死、急性肾衰竭、动脉粥样硬化等。
医药
4-氰甲基苯乙酸溶于无水乙醇，加入氯化钯和浓盐酸，在室温和0.5MPa通氢。滤除催化剂，滤液减压蒸出溶剂。加入水，充分溶解，过滤，滤液为化合物(I)的溶液。往该溶液中，加入碳酸钾，再在80℃加入对氯苯磺酰氯。加毕，在80℃搅拌。冷却，用2mol/L盐酸酸化至Ph值2。滤集固体，水洗，干燥。再用66%乙醇重结晶，得达曲班，熔点138～140℃。
