Thiemermann C, Ney P, Schrör K
Institut für Pharmakologie, Universität Düsseldorf, F.R.G.
Eur J Pharmacol. 1988 Oct 11;155(1-2):57-67. doi: 10.1016/0014-2999(88)90402-5.
The cardioprotective action of the new selective inhibitor of thromboxane receptors, daltroban (BM 13.505), was studied in cats subjected to 3 h of coronary artery ligation followed by 2 h of reperfusion. In comparison with vehicle (physiological saline)-treated cats, daltroban (20 mg/kg per h i.v.) reduced the ischaemia-induced rise in the ST segment and prevented the development of a Q-wave in the ECG during reperfusion. This was paralleled by a significantly improved preservation of creatine-phosphokinase activity in the ischaemic myocardium. Daltroban significantly attenuated platelet ATP secretion, the U-46.619-induced contraction of the cat thoracic aorta ex vivo and the myeloperoxidase-associated generation of reactive oxygen species ex vivo. These effects could be largely attributed to the inhibition of ischaemia-induced leukocytosis. It is concluded that daltroban protects the myocardium from ischaemic injury and that this effect involves prevention of ischaemia-induced leukocytosis.
研究了新型血栓素受体选择性抑制剂达曲班(BM 13.505)对结扎冠状动脉3小时后再灌注2小时的猫的心脏保护作用。与用赋形剂(生理盐水)处理的猫相比,达曲班(每小时20毫克/千克静脉注射)可降低缺血诱导的ST段抬高,并防止再灌注期间心电图中出现Q波。这与缺血心肌中肌酸磷酸激酶活性的显著改善的保存情况平行。达曲班显著减弱血小板ATP分泌、U-46.619诱导的离体猫胸主动脉收缩以及离体髓过氧化物酶相关的活性氧生成。这些作用很大程度上可归因于对缺血诱导的白细胞增多的抑制。得出结论,达曲班可保护心肌免受缺血性损伤,且这种作用涉及预防缺血诱导的白细胞增多。