Raĭnova L, Georgieva A, Staneva-Stoĭcheva D
Eksp Med Morfol. 1978;17(1):37-43.
The report describes the hypotensive and antihypertensive activity of the compound N-(trans-3-hydroxy-1,2,3,4-tetrahydro-2-naphtyl)-N'-(3-oxo-3-phenylpropyl) piperazine dihydrochloride (P11). The work is made on normotensive cats and rats as well as on spontaneous and experimental (metacorticoid) hypertension. The studies were carried out under the conditions of acute and chronic experiment as the arteria pressure was recorded by blood and bloodless method. The compound P11 show a manifested hypotensive activity with favourable duration and therapeutic width. Its antihypertensive activity is revealed in rats with spontaneous and metacorticoid hypertension both after single and chronic applciation of the compound. The influence on the blood pressure weakens after reserpinization of the animals. The compound possesses slight ganglion-blocking action and manifested alpha and beta adreno-blocking activity: diminishes noradrenaline, adrenaline and isoprenaline responses on the arterial pressure and heart activity in anesthetised cats and rats, shifts to the right the cumulative dose-response curve of noradrenaline on vas deferens of a rat, ect. The hypotensive and antihypertensive effect of the compound P11 is discussed on the basis of its alpha and beta adrenoblocking action and its specific sedative effect.
该报告描述了化合物N-(反式-3-羟基-1,2,3,4-四氢-2-萘基)-N'-(3-氧代-3-苯基丙基)哌嗪二盐酸盐(P11)的降压和抗高血压活性。研究对象为血压正常的猫和大鼠,以及自发性和实验性(皮质激素性)高血压动物。研究在急性和慢性实验条件下进行,采用血液和无血方法记录动脉血压。化合物P11表现出明显的降压活性,作用持续时间适宜,治疗窗良好。在自发性和皮质激素性高血压大鼠中,单次和长期应用该化合物后均显示出抗高血压活性。动物利血平化后,其对血压的影响减弱。该化合物具有轻微的神经节阻断作用,并表现出α和β肾上腺素阻断活性:降低麻醉猫和大鼠动脉血压和心脏活动对去甲肾上腺素、肾上腺素和异丙肾上腺素的反应,使大鼠输精管上去甲肾上腺素的累积剂量-反应曲线右移等。基于其α和β肾上腺素阻断作用及其特定的镇静作用,对化合物P11的降压和抗高血压作用进行了讨论。