Mizuno K, Hashimoto S, Kunii N, Tani M, Niimura S, Yabe R, Watari H, Fukuchi S
Res Commun Chem Pathol Pharmacol. 1985 Aug;49(2):175-87.
In 15 patients with mild-to-moderate essential hypertension a new orally active angiotensin converting enzyme inhibitor, 1-(D-3-acetylthio-2-methylpropanoyl)-L-prolyl-L-phenylalanine (Alacepril), was administered with a single oral dose of 50 mg to evaluate its antihypertensive effect. Following Alacepril plasma angiotensin converting enzyme (ACE) activity was inhibited by approximately 75% within 2 h. Plasma renin activity increased slightly whereas plasma levels of aldosterone decreased significantly. Blood pressure fell markedly not only in patients with high renin levels but also in those with low renin levels. Nevertheless, the magnitude of blood pressure reduction was correlated with the pre-treatment plasma renin values (r = -0.602, p less than 0.05 systolic, r = -0.667, p less than 0.01 diastolic). No relevant changes in pulse rate was observed. These findings demonstrate that in essential hypertension the novel orally active ACE inhibitor Alacepril exerts marked antihypertensive effect, which may offer a new effective approach to treatment of hypertension.
对15例轻至中度原发性高血压患者给予一种新型口服活性血管紧张素转换酶抑制剂1-(D-3-乙酰硫基-2-甲基丙酰基)-L-脯氨酰-L-苯丙氨酸(阿拉普利),单次口服剂量为50mg,以评估其降压效果。服用阿拉普利后,血浆血管紧张素转换酶(ACE)活性在2小时内被抑制约75%。血浆肾素活性略有升高,而醛固酮血浆水平显著降低。血压不仅在高肾素水平患者中明显下降,在低肾素水平患者中也明显下降。然而,血压降低的幅度与治疗前血浆肾素值相关(收缩压r = -0.602,p < 0.05;舒张压r = -0.667,p < 0.01)。未观察到脉搏率有相关变化。这些发现表明,在原发性高血压中,新型口服活性ACE抑制剂阿拉普利具有显著的降压作用,这可能为高血压治疗提供一种新的有效方法。