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17(R)-甲基-20-异亚丙基卡前列素钠盐对仓鼠颊囊小动脉的抗血栓形成作用。

Antithrombotic effects of sodium salt of 17(R)-methyl-20-isopropylidenecarbacyclin in the arteriole of the hamster cheek pouch.

作者信息

Morita A, Endo K, Mori M, Akiyama K, Kohata K, Kobayashi S

出版信息

Arzneimittelforschung. 1986 Apr;36(4):676-9.

PMID:3521615
Abstract

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.

摘要

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。

相似文献

1
Antithrombotic effects of sodium salt of 17(R)-methyl-20-isopropylidenecarbacyclin in the arteriole of the hamster cheek pouch.17(R)-甲基-20-异亚丙基卡前列素钠盐对仓鼠颊囊小动脉的抗血栓形成作用。
Arzneimittelforschung. 1986 Apr;36(4):676-9.
2
Effect of a stable prostacyclin analogue on platelet function and experimentally-induced thrombosis in the microcirculation.一种稳定的前列环素类似物对血小板功能及实验性诱导的微循环血栓形成的影响。
Arzneimittelforschung. 1985;35(12):1816-8.
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Prostacyclin (PGI2) inhibits the formation of platelet thrombi in arterioles and venules of the hamster cheek pouch.前列环素(PGI2)抑制仓鼠颊囊小动脉和小静脉中血小板血栓的形成。
Br J Pharmacol. 1978 Jul;63(3):535-9. doi: 10.1111/j.1476-5381.1978.tb07809.x.
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