Konno K, Nonaka K, Ueno A
Arzneimittelforschung. 1981;31(7):1072-5.
In renal hypertensive dogs, 1-[2-(1,3-dimethyl-2-butenylidene)hydrazino]phthalazine (budralazine) at doses of 1 and 2.5 mg/kg p.o. produced a gradual, progressive and significant fall in blood pressure which reached a maximum 3--4 h after dosing and persisted for 6--10 h. The hypotensive response to 1 mg/kg p.o. of budralazine was almost comparable to that to 2.5 mg/kg p.o. of reference drug hydralazine, but the duration of action of the former was much longer than that of the latter. At equihypotensive doses, budralazine was found to be approximately 3 times less potent than hydralazine in producing tachycardia. In normotensive dogs, budralazine at a dose of 1 mg/kg p.o. produced a significant increase in renal blood flow and a tendency for the increase in coronary blood flow associated with a significant and non-significant decrease in the peripheral vascular resistance. At this dose level, blood pressure remained almost unchanged.
在肾性高血压犬中,口服剂量为1和2.5mg/kg的1-[2-(1,3-二甲基-2-亚丁烯基)肼基]酞嗪(布屈嗪)可使血压逐渐、持续且显著下降,给药后3 - 4小时降至最低,持续6 - 10小时。口服1mg/kg布屈嗪的降压反应与口服2.5mg/kg参比药物肼屈嗪的降压反应几乎相当,但前者的作用持续时间比后者长得多。在等效降压剂量下,发现布屈嗪在引起心动过速方面的效力比肼屈嗪约低3倍。在正常血压犬中,口服1mg/kg布屈嗪可使肾血流量显著增加,冠状动脉血流量有增加趋势,同时外周血管阻力显著和非显著降低。在此剂量水平下,血压几乎保持不变。