Raz A
Thromb Haemost. 1983 Dec 30;50(4):784-6.
Mepacrine, in addition to its established antilipolytic activity, was also found to inhibit the conversion of 14C-arachidonic acid to 14C-thromboxane B2 in human washed platelets. In the concentration range of 3.33-33 microM, meparcrine exerted a dose dependent inhibition of arachidonate conversion to thromboxane B2 in parallel to inhibition of arachidonate-induced platelet aggregation. Mepacrine inhibition of thromboxane formation was not accompanied by a concomitant increase in other cyclooxygenase products. Furthermore, mepacrine did not affect platelet transformation of added prostaglandin H2 to thromboxane A2 and other products. These results indicate that mepacrine inhibits the cyclooxygenase enzyme and not thromboxane synthase. In washed platelets, mepacrine inhibition of arachidonic acid conversion to thromboxane A2 appears to be a major factor in the overall inhibitory effect of the compound on the combined process of arachidonate release from cellular phospholipids and its conversion to proaggregatory products.
除了其已确定的抗脂解活性外，还发现米帕林可抑制人洗涤血小板中14C-花生四烯酸向14C-血栓素B2的转化。在3.33 - 33微摩尔的浓度范围内，米帕林对花生四烯酸转化为血栓素B2具有剂量依赖性抑制作用，这与抑制花生四烯酸诱导的血小板聚集作用平行。米帕林对血栓素形成的抑制作用并未伴随着其他环氧化酶产物的相应增加。此外，米帕林不影响添加的前列腺素H2向血栓素A2和其他产物的血小板转化。这些结果表明，米帕林抑制环氧化酶而非血栓素合酶。在洗涤血小板中，米帕林抑制花生四烯酸转化为血栓素A2似乎是该化合物对细胞磷脂中花生四烯酸释放及其转化为促聚集产物的联合过程产生总体抑制作用的主要因素。
