Ram N, Heilman R D, Greenslade F C
Arch Int Pharmacodyn Ther. 1976 Nov;224(1):102-8.
Studies were carried out to determine the antihypertensive effects of the 5-hydroxy derivative (ORF 12,592) of propranolol. Acute administration of ORF 12,592 produced a reduction in mean systolic blood pressure in desoxycorticosterone acetate (DOCA) rats and in spontaneously hypertensive rats (SHR). Propranolol was not effective in DOCA rats and produced a significant blood pressure reduction in SHR 48 hr after acute administration. These results demonstrated antihypertensive activity of an analog of propranolol and support the concept that the antihypertensive effects of propranolol may be mediated through a metabolite.
开展了多项研究以确定普萘洛尔的5-羟基衍生物(ORF 12,592)的降压作用。急性给予ORF 12,592可使醋酸去氧皮质酮(DOCA)大鼠和自发性高血压大鼠(SHR)的平均收缩压降低。普萘洛尔对DOCA大鼠无效,急性给药48小时后可使SHR的血压显著降低。这些结果证明了普萘洛尔类似物的降压活性,并支持普萘洛尔的降压作用可能通过一种代谢产物介导的观点。