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Anti-thrombotic Activity of KBT-3022 in Experimental Models of Thrombosis

机译：KBT-3022在血栓形成实验模型中的抗血栓形成活性

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References(36) Cited-By(11) In this study, we investigated the effects of KBT-3022 (ethyl 2-[4, 5-bis(4-methoxyphenyl)-thiazol-2-yl]pyrrol-1-ylacetate), a potent and long-lasting anti-platelet agent, in several experimental thrombosis models and compared them with those of other anti-platelet drugs. Oral administration of KBT-3022 prevented arachidonic acid-induced death due to pulmonary embolism in mice and rabbits with respective ED50 values of 0.29 and 0.12 mg/kg. The protective effect of acetylsalicylic acid (ASA) against mortality was weaker than that of KBT-3022, and ticlopidine hydrochloride (TP) showed no such effect in these models. In a guinea pig arterio-venous shunt model, the inhibition by KBT-3022 of thrombus formation on a silk thread inserted into the shunt was dose-dependent and 300 and 30 times more potent than the inhibition obtained with ASA and indomethacin, respectively. In a model of aortic thrombosis induced by perivascular application of 20% silver nitrate solution, KBT-3022 (1 mg/kg, p.o.) inhibited thrombus formation significantly, ASA (100 mg/kg, p.o.) tended to inhibit it, and TP had no effect. However, in a stasisinduced venous thrombosis model in guinea pigs, TP inhibited thrombus formation significantly, but KBT-3022 and ASA were ineffective. These results suggest that KBT-3022 may be a useful drug for the treatment and/or prophylaxis of thrombus formation in shunts and aortic thrombosis.
机译：参考文献（36）被引用者（11）在本研究中，我们研究了KBT-3022（2- [4,5-双（4-甲氧基苯基）-噻唑-2-基]吡咯-1-基乙酸乙酯）的作用。是一种有效且持久的抗血小板药，它在几种实验性血栓形成模型中进行了比较，并与其他抗血小板药物进行了比较。口服KBT-3022可预防小鼠和兔子中肺栓塞引起的花生四烯酸诱导的死亡，ED50分别为0.29和0.12 mg / kg。乙酰水杨酸（ASA）对死亡率的保护作用比KBT-3022弱，而噻氯匹定盐酸盐（TP）在这些模型中没有这种作用。在豚鼠动静脉分流模型中，KBT-3022对插入分流器的丝线上的血栓形成的抑制作用是剂量依赖性的，分别比ASA和消炎痛的抑制作用强300和30倍。在血管周围应用20％硝酸银溶液引起的主动脉血栓形成模型中，KBT-3022（1 mg / kg，po）显着抑制血栓形成，ASA（100 mg / kg，po）倾向于抑制血栓形成，而TP具有没有效果。然而，在豚鼠的瘀阻性静脉血栓形成模型中，TP显着抑制血栓形成，但KBT-3022和ASA无效。这些结果表明，KBT-3022可能是治疗和/或预防分流和主动脉血栓形成中血栓形成的有用药物。

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