阿替洛尔和普萘洛尔在自发性高血压大鼠体内对心脏与血管β受体的阻滞比率。
The ratio of cardiac to vascular beta-receptor blockade of atenolol and propranolol in spontaneously hypertensive rats in vivo.
作者信息
Kudo Y, Sokabe H
出版信息
J Pharmacobiodyn. 1982 Sep;5(9):745-7. doi: 10.1248/bpb1978.5.745.
Ratios of cardiac to vascular beta-receptor blockade (C:V ratios) of atenolol and propranolol were determined in pentobarbital anesthetized spontaneously hypertensive (SHR) rats. These values and the cardiovascular responses to isoproterenol were compared with those of age-matched normotensive control (Donryu, DON) rats reported previously. Mean blood pressure (BP) and heart rate (HR) were recorded. Full dose-response curves for isoproterenol were constructed in BP and HR. In vivo pD2 values of isoproterenol (potencies), were not different between DON and SHR rats, although the maximal responses to isoproterenol (efficacy) were significantly suppressed in SHR rats. C:V ratios of atenolol and propranolol in SHR rats were 7.95 and 0.44, respectively. As the values in DON rats were 9.77 and 1.20, respectively, C:V ratios of atenolol and propranolol were decreased in SHR rats. Markedly decreased C:V ratios of propranolol in SHR rats may explain its relatively weak antihypertensive action.
在戊巴比妥麻醉的自发性高血压（SHR）大鼠中测定了阿替洛尔和普萘洛尔的心脏与血管β受体阻滞率（C:V比率）。将这些值以及对异丙肾上腺素的心血管反应与先前报道的年龄匹配的正常血压对照（Donryu，DON）大鼠的进行比较。记录平均血压（BP）和心率（HR）。构建了异丙肾上腺素在血压和心率方面的全剂量反应曲线。尽管SHR大鼠对异丙肾上腺素的最大反应（效能）明显受到抑制，但DON大鼠和SHR大鼠之间异丙肾上腺素的体内pD2值（效价）并无差异。SHR大鼠中阿替洛尔和普萘洛尔的C:V比率分别为7.95和0.44。由于DON大鼠中的值分别为9.77和1.20，SHR大鼠中阿替洛尔和普萘洛尔的C:V比率降低。SHR大鼠中普萘洛尔的C:V比率显著降低可能解释了其相对较弱的降压作用。
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