Sato K, Kawasaki T, Hisamichi N, Taniuchi Y, Hirayama F, Koshio H, Ichihara M, Matsumoto Y
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical, Tsukuba, Ibaraki, Japan.
Eur J Pharmacol. 1998 May 29;350(1):87-91. doi: 10.1016/s0014-2999(98)00328-8.
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.
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。
