Takeda K, Nakagawa Y, Hashimoto T, Sakurai H, Imai S
Jpn J Pharmacol. 1979 Apr;29(2):171-8. doi: 10.1254/jjp.29.171.
Antihypertensive effects of chronic oral administration of adrenergic beta-blocking agents were assessed in SHR. Propranolol, pindolol, oxprenolol, atenolol and labetalol were used as beta-blockers and the effects of these compounds on the blood pressure and the heart rate were compared with those of hydralazine, a representative vasodilating antihypertensive agent. Propranolol, oxprenolol and atenolol produced a definite decrease in the heart rate; the development of hypertension was retarded. Pindolol produced antihypertensive effects only after a longer period of administration and such were associated with insignificant decrease in heart rate. With a shorter period of administration the drug produced only an insignificant fall of blood pressure with practically no change in the heart rate. With labetalol, a beta-blocker with alpha-blocking action, a fall of blood pressure appeared earlier and was of greater magnitude. Hydralazine produced a definite antihypertensive effect, which appeared immediately after administration and was associated with a tachycardia. In pithed rats, only pindolol produced a definite fall of blood pressure. On the basis of these findings, possible mechanisms of antihypertensive effects of beta-blockers were discussed.
在自发性高血压大鼠(SHR)中评估了慢性口服肾上腺素能β受体阻滞剂的降压作用。普萘洛尔、吲哚洛尔、氧烯洛尔、阿替洛尔和拉贝洛尔用作β受体阻滞剂,并将这些化合物对血压和心率的影响与代表性血管舒张性抗高血压药物肼屈嗪的影响进行了比较。普萘洛尔、氧烯洛尔和阿替洛尔使心率明显降低;高血压的发展受到抑制。吲哚洛尔仅在较长时间给药后才产生降压作用,且与心率的轻微降低有关。给药时间较短时,该药物仅使血压轻微下降,心率几乎无变化。具有α受体阻滞作用的β受体阻滞剂拉贝洛尔,血压下降出现得更早且幅度更大。肼屈嗪产生明确的降压作用,给药后立即出现,并伴有心动过速。在脊髓麻醉大鼠中,只有吲哚洛尔使血压明显下降。基于这些发现,讨论了β受体阻滞剂降压作用的可能机制。