Morita A, Endo K, Mori M, Akiyama K, Kohata K, Kobayashi S
Arzneimittelforschung. 1986 Apr;36(4):676-9.
Antithrombotic effects of sodium salt of 17(R)-methyl-20-isopropylidenecarbacyclin (CS-570), a chemically stable prostaglandin I2 (PGI2, epoprostenol, prostacyclin) derivative, were investigated in the arteriole of the hamster cheek pouch. A microthrombus was produced by a slight mechanical injury followed by iontophoretic application of adenosine diphosphate (ADP) to an arteriole of 70 to 100 micron in diameter. The platelet thrombus size was determined with a video image processor. With this technique, a reproducible and quantitatively measurable periodical thrombus was obtained. CS-570 inhibited the thrombus formation dose-dependently. The potency of CS-570 was about 1/8 that of PGI2 and 6 times that of carbacyclin when infused i.v. CS-570 also decomposed an established thrombus. Alprostadil (PGE1), dipyridamole and ticlopidine failed to show inhibitory effects. The antithrombotic effect of CS-570 was definitely demonstrated.
研究了化学稳定的前列腺素I2(PGI2,依前列醇,前列环素)衍生物17(R)-甲基-20-异亚丙基卡前列环素(CS-570)钠盐在仓鼠颊囊小动脉中的抗血栓形成作用。通过轻微机械损伤,然后向直径70至100微米的小动脉中离子电渗法施加二磷酸腺苷(ADP)来形成微血栓。用视频图像处理器测定血小板血栓大小。用这种技术,获得了可重复且可定量测量的周期性血栓。CS-570剂量依赖性地抑制血栓形成。静脉注射时,CS-570的效力约为PGI2的1/8,是卡前列环素的6倍。CS-570还能分解已形成的血栓。前列地尔(PGE1)、双嘧达莫和噻氯匹定未显示出抑制作用。CS-570的抗血栓形成作用得到了明确证实。