一种前体激素血管紧张素拮抗剂的合成与药理学
Synthesis and pharmacology of a prohormone angiotensin antagonist.
作者信息
Chiu A T, Sutherland J C, Day A R, Freer R J
出版信息
Eur J Pharmacol. 1979 Feb 15;54(1-2):177-80. doi: 10.1016/0014-2999(79)90421-7.
PMID:421740
Abstract
A prohormone angiotensin antagonist, Sarcosyl1-Alanyl8-angiotensin I (Sar1-Ala8-A-I) was synthesized and its pharmacological properties were evaluated in three biological systems. It was found to be a good inhibitor in vivo in the rat blood pressure assay, somewhat less active in guinea pig ileum and a relatively weak antagonist in rat uterus. In vivo the inhibitory effect was greatly attenuated by the presence of the converting enzyme inhibitor BPP5alpha.
摘要
一种前体激素血管紧张素拮抗剂，肌氨酸1 - 丙氨酰8 - 血管紧张素I（Sar1 - Ala8 - A - I）被合成出来，并在三个生物系统中评估了其药理特性。发现在大鼠血压测定中它在体内是一种良好的抑制剂，在豚鼠回肠中活性稍低，而在大鼠子宫中是相对较弱的拮抗剂。在体内，由于存在转化酶抑制剂BPP5α，其抑制作用大大减弱。
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