Takami N, Sugawara K, Ozaki M
Nihon Yakurigaku Zasshi. 1979 Oct;75(7):747-54.
The effects of acebutolol, a cardioselective beta-adrenoceptor blocking agent, on the systolic blood pressure and heart rate were investigated in conscious Kyoto Wistar normotensive rats (WKY), spontaneously hypertensive rats (SHR) and DOCA-NaCl hypertensive rats (DOCA rats) and the results compared with those of propranolol and practolol. In WKY and DOCA rats, the intraperitoneal administration of acebutolol, propranolol and practolol (0.5 approximately 20 mg/kg) produced a hypotensive action, however, these effects were observed only with restricted doses and there was no evidence of a dose-dependency. The heart rate was decreased by acebutolol and propranolol, but was increased by practolol which possesses an intrinsic sympathomimetic activity. In SHR, propranolol produced a dual action, a slight rise followed by a slight fall, the change not being significant, while practolol induced a slight hypertension. On the other hand, acebutolol in high doses induced a dose-dependent hypotensive action. The heart rate was markedly and dose-dependently decreased by these three agents. Thus, while propranolol and practolol produced hypotensive effects in WKY and DOCA rats, acebutolol produced hypotensive effects in WKY, SHR and DOCA rats. These results suggest that acebutolol is a beta-adrenoceptor blocking agent which possesses hypotensive activity in hypertensive rats.
在清醒的京都Wistar正常血压大鼠(WKY)、自发性高血压大鼠(SHR)和DOCA-氯化钠高血压大鼠(DOCA大鼠)中研究了心脏选择性β-肾上腺素受体阻滞剂醋丁洛尔对收缩压和心率的影响,并将结果与普萘洛尔和普拉洛尔的结果进行比较。在WKY大鼠和DOCA大鼠中,腹腔注射醋丁洛尔、普萘洛尔和普拉洛尔(0.5至20mg/kg)产生降压作用,然而,这些作用仅在受限剂量下观察到,且没有剂量依赖性的证据。醋丁洛尔和普萘洛尔使心率降低,但具有内在拟交感活性的普拉洛尔使心率升高。在SHR中,普萘洛尔产生双重作用,先有轻微升高,随后轻微下降,变化不显著,而普拉洛尔引起轻微高血压。另一方面,高剂量的醋丁洛尔诱导剂量依赖性降压作用。这三种药物均使心率显著且剂量依赖性地降低。因此,虽然普萘洛尔和普拉洛尔在WKY大鼠和DOCA大鼠中产生降压作用,但醋丁洛尔在WKY大鼠、SHR大鼠和DOCA大鼠中均产生降压作用。这些结果表明,醋丁洛尔是一种在高血压大鼠中具有降压活性的β-肾上腺素受体阻滞剂。