Lefer D J, Lefer A M
Proc Soc Exp Biol Med. 1984 Feb;175(2):211-4. doi: 10.3181/00379727-175-41790.
Enalapril, a potent angiotensin converting enzyme inhibitor, effectively blocked the constrictor actions of angiotensin I in isolated perfused cat coronary arteries. Enalapril, at concentrations of 25 to 100 micrograms/ml, inhibited angiotensin I by 65 to 80%. Moreover, enalapril at 100 to 200 micrograms/ml, markedly antagonized the coronary vasoconstrictor effects of angiotensin II. At 150 micrograms/ml, enalapril blocked the angiotensin II response by 80 +/- 5%, and at 200 micrograms/ml, it was blocked by 95 +/- 4%. Enalaprilic acid at 0.5 to 1.0 microgram/ml also blocked the angiotensin II response by 94 +/- 5%. Captopril, up to 250 micrograms/ml, failed to significantly antagonize angiotensin II, although it readily blocked angiotensin I in this preparation. The duration of this angiotensin II blockade lasted about 60-90 min. This angiotensin II antagonism may help explain the beneficial effects of enalapril in situations such as acute myocardial ischemia.
依那普利是一种强效血管紧张素转换酶抑制剂,可有效阻断离体灌注猫冠状动脉中血管紧张素I的收缩作用。依那普利浓度为25至100微克/毫升时,对血管紧张素I的抑制率为65%至80%。此外,依那普利浓度为100至200微克/毫升时,可显著拮抗血管紧张素II的冠状动脉收缩作用。浓度为150微克/毫升时,依那普利对血管紧张素II反应的阻断率为80±5%,浓度为200微克/毫升时,阻断率为95±4%。浓度为0.5至1.0微克/毫升的依那普利拉对血管紧张素II反应的阻断率也为94±5%。卡托普利浓度高达250微克/毫升时,虽能在该制剂中轻易阻断血管紧张素I,但未能显著拮抗血管紧张素II。这种对血管紧张素II的阻断持续约60 - 90分钟。这种对血管紧张素II的拮抗作用可能有助于解释依那普利在急性心肌缺血等情况下的有益作用。