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业已证明,以阿司匹林为代表药物的抗血小板疗法对脑缺血、不稳定型心绞痛和心肌梗塞等心脑血管疾病的防治有肯定疗效。其作用机理主要是抑制血小板血栓素A_2(thromboxane A_2,TxA_2)的合成。但阿司匹林的作用选择性差,在抑制血小板TxA_2合成的同时,血管内皮细胞中具有抗血小板活性的前列环素(prostacyclin,PGI_2)的合成亦被抑制,使其疗效受到限制。因此,近年来人们一直致力于寻找具有选择性抗TxA_2活性的药物,并已取得较大进展。
It has been proven that antiplatelet therapy with aspirin as a representative drug has a definite effect on the prevention and treatment of cardiovascular and cerebrovascular diseases such as cerebral ischemia, unstable angina and myocardial infarction. Its mechanism of action is mainly to inhibit the synthesis of thromboxane A_2 (TxA_2). However, the poor selectivity of aspirin inhibits the synthesis of TxA_2 on platelets and inhibits the synthesis of prostacyclin (PGI_2) with anti-platelet activity in vascular endothelial cells, which limits its efficacy. Therefore, in recent years, people are always looking for drugs with selective anti-TxA2 activity and great progress has been made.