Bradshaw D, Franz P H, Sugden A L
Br J Pharmacol. 1982 May;76(1):163-8. doi: 10.1111/j.1476-5381.1982.tb09202.x.
1 The effect of the angiotensin converting enzyme inhibitor, MK 421 (N-((S)-1-(ethoxycarbonyl)-3-phenylpropyl)L-Ala-L-Pro), on the blood pressure of two-kidney Goldblatt hypertensive rats has been investigated in relation to he initial plasma renin activity (PRA) and the initial blood pressure of the individual animals. 2 Blood pressure was monitored by an indirect tail-cuff method at 1, 3, 6 and 24 h after dosing. MK 421 produced a fall in blood pressure in the majority of animals, but the extent of this reduction varied considerably between individuals. 3 The change in blood pressure showed a significant correlation with both the initial PRA and the initial blood pressures of the animals. However, only a modest correlation was found between the initial PRA and the degree of hypertension. 4 MK 421 (10 mg/kg, orally) produced a mean blood pressure change which was statistically significant (P less than 0.001) at all times tested. 5 It is concluded that the degree of antihypertensive activity of MK 421 is related to the degree of activity of the renin-angiotensin system which, in this model at least, is reflected by the PRA.
1 研究了血管紧张素转换酶抑制剂MK 421(N-((S)-1-(乙氧羰基)-3-苯基丙基)-L-丙氨酰-L-脯氨酸)对二肾型Goldblatt高血压大鼠血压的影响,并与个体动物的初始血浆肾素活性(PRA)和初始血压相关联。2 给药后1、3、6和24小时,通过间接尾袖法监测血压。MK 421使大多数动物的血压下降,但个体间这种降低的程度差异很大。3 血压变化与动物的初始PRA和初始血压均呈显著相关。然而,初始PRA与高血压程度之间仅发现适度相关性。4 MK 421(10mg/kg,口服)在所有测试时间点均产生了具有统计学意义(P小于0.001)的平均血压变化。5 得出结论,MK 421的降压活性程度与肾素-血管紧张素系统的活性程度相关,至少在该模型中,PRA反映了这种活性。