Tamao Y, Hara H, Umezu K, Ito J, Doi A, Sudo A, Hirata T, Mineo K, Tobe A
Nihon Yakurigaku Zasshi. 1986 Feb;87(2):161-7. doi: 10.1254/fpj.87.161.
MCI-2016 showed little influence on coagulation (APTT) and fibrinolysis (plasma clot lysis activated by urokinase) at doses (concentrations) as high as 300 mg/kg, p.o. or 8.6 X 10(-4) M. Hemolytic action of MCI-2016 was only observed at the concentrations above 2 mM. The drug also showed no influence on blood glucose level (30-300 mg/kg, p.o.). Effects of MCI-2016 on hemorheological properties were studied either in vitro or ex vivo. Above the doses (concentrations) of 100 mg/kg, p.o. and 10 microM, MCI-2016 suppressed the mechanical hemolysis and accelerated the membrane filtration rate. These effects of MCI-2016 were superior to those of cinepazide, Ca-hopantenate, meclofenoxate and pentoxyfylline. MCI-2016 also inhibited platelet aggregation induced by collagen with the IC 50 of 35 to 60 microM (rabbit and human platelets). Secondary aggregations of ADP and epinephrine were also inhibited by MCI-2016. As for reference drugs, bencyclane showed inhibitory patterns similar to MCI-2016. Other drugs examined exhibited little effect. In summary, it may be suggested that MCI-2016 exhibits beneficial influences in the clinical fields of cerebrovascular diseases.
MCI - 2016经口服给予高达300毫克/千克的剂量(浓度)或8.6×10(-4)M时,对凝血(活化部分凝血活酶时间)和纤维蛋白溶解(尿激酶激活的血浆凝块溶解)几乎没有影响。仅在浓度高于2毫摩尔时才观察到MCI - 2016的溶血作用。该药物对血糖水平也无影响(口服30 - 300毫克/千克)。对MCI - 2016在血液流变学性质方面的影响进行了体外或离体研究。口服剂量(浓度)高于100毫克/千克及10微摩尔时,MCI - 2016可抑制机械性溶血并加快膜过滤速率。MCI - 2016的这些作用优于桂哌齐特、钙泛酸盐、氯酯醒和己酮可可碱。MCI - 2016还可抑制胶原蛋白诱导的血小板聚集,其对兔和人血小板的半数抑制浓度(IC 50)为35至60微摩尔。MCI - 2016还可抑制二磷酸腺苷(ADP)和肾上腺素引起的继发性聚集。作为参比药物,苄环烷显示出与MCI - 2016相似的抑制模式。所检测的其他药物几乎没有作用。总之,提示MCI - 2016在脑血管疾病临床领域具有有益影响。