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YM-60828在豚鼠三种血栓形成模型中的抗血栓作用。

Antithrombotic effects of YM-60828 in three thrombosis models in guinea pigs.

作者信息

Sato K, Kawasaki T, Hisamichi N, Taniuchi Y, Hirayama F, Koshio H, Ichihara M, Matsumoto Y

机构信息

Institute for Drug Discovery Research, Yamanouchi Pharmaceutical, Tsukuba, Ibaraki, Japan.

出版信息

Eur J Pharmacol. 1998 May 29;350(1):87-91. doi: 10.1016/s0014-2999(98)00328-8.

Abstract

The antithrombotic effects of a novel factor Xa inhibitor, YM-60828 ([N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]-N-[(7-amidino-2-nap hthyl)methyl]sulfamoyl]acetic acid dihydrochloride), in three thrombosis models in guinea pigs were studied in comparison with its effect on bleeding time. The antithrombotic effects of YM-60828 were most pronounced in the venous thrombosis and the arterio-venous shunt models but YM-60828 showed 10-fold weaker effects in the carotid thrombosis model. However, YM-60828 prolonged bleeding time at a much higher dose than that required in all thrombosis models. In conclusion, YM-60828 exerted its antithrombotic effects without prolonging bleeding time in all thrombosis models and may be of clinical value not only in venous thrombosis but also in arterial thrombosis.

摘要

研究了新型Xa因子抑制剂YM-60828([N-[4-[(1-乙酰亚胺基-4-哌啶基)氧基]苯基]-N-[(7-脒基-2-萘基)甲基]氨磺酰基]乙酸二盐酸盐)在豚鼠三种血栓形成模型中的抗血栓作用,并与其对出血时间的影响进行了比较。YM-60828的抗血栓作用在静脉血栓形成和动静脉分流模型中最为明显,但在颈动脉血栓形成模型中其作用弱10倍。然而,YM-60828延长出血时间的剂量远高于所有血栓形成模型所需的剂量。总之,YM-60828在所有血栓形成模型中均发挥抗血栓作用而不延长出血时间,不仅在静脉血栓形成中,而且在动脉血栓形成中可能具有临床价值。

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