Yamamoto J, Sekiya A, Maekawa H
Jpn J Pharmacol. 1975 Aug;25(4):465-71. doi: 10.1254/jjp.25.465.
Effects of practolol, alprenolol and pindolol on blood pressure in the rat were studied. Also effects of these three beta-blocking agents on blood pressure and heart rate in spinal rats during adrenaline infusion were studied and compared with those of propranolol. The beta-blocking agents produced a sustained pressor action in the rat, and in the spinal rat infused with adrenaline. The magnitude of the pressor action induced by the beta-blockers was in the following order: pindolol larger than or equal to propranolol larger than or equal to alprenolol greater than practolol. Minimum doses of these beta-blockers required to cause a pressor action in the spinal rat infused with adrenaline were in the following order; practolol greater than alprenolol larger than or equal to propranolol larger than or equal to pindolol. The magnitude of the pressor action produced by the same dose of these beta-blockers and minimum doses of these beta-blockers required to cause a pressor action in the spinal rat infused with adrenaline seemed to be roughly proportional to their beta-receptor blocking activities. It was concluded that the minimum doses of these beta-blockers required to cause a pressor action and the magnitude of the pressor action induced by the beta-blockers in the spinal rat infused with adrenaline could be used to compare their beta-blocking activities and that practolol, a cardioselective beta-blocker, seems to block not only cardiac beta-receptor but to some extent also peripheral vascular beta-receptors.
研究了心得宁、烯丙洛尔和吲哚洛尔对大鼠血压的影响。还研究了这三种β受体阻滞剂在给脊髓大鼠输注肾上腺素期间对血压和心率的影响,并与普萘洛尔的影响进行了比较。这些β受体阻滞剂在大鼠以及输注了肾上腺素的脊髓大鼠中产生了持续的升压作用。β受体阻滞剂引起的升压作用强度顺序如下:吲哚洛尔≥普萘洛尔≥烯丙洛尔>心得宁。在输注了肾上腺素的脊髓大鼠中引起升压作用所需的这些β受体阻滞剂的最小剂量顺序如下:心得宁>烯丙洛尔≥普萘洛尔≥吲哚洛尔。相同剂量的这些β受体阻滞剂产生的升压作用强度以及在输注了肾上腺素的脊髓大鼠中引起升压作用所需的这些β受体阻滞剂的最小剂量似乎与其β受体阻断活性大致成正比。得出的结论是,在输注了肾上腺素的脊髓大鼠中引起升压作用所需的这些β受体阻滞剂的最小剂量以及β受体阻滞剂引起的升压作用强度可用于比较它们的β受体阻断活性,并且心得宁,一种心脏选择性β受体阻滞剂,似乎不仅阻断心脏β受体,而且在一定程度上还阻断外周血管β受体。