Chiba S, Furukawa Y, Saegusa K, Ohba Y
Department of Pharmacology, Shinshu University School of Medicine, Matsumoto, Japan.
Jpn Heart J. 1988 Nov;29(6):841-8. doi: 10.1536/ihj.29.841.
The effects of calcium (-)-N-[(S)-3(N-cyclohexylcarbonyl-D-alanyl)-thio]-2-methylpropion] -L- prolinate (MC-838, altiopril calcium), an inhibitor of angiotensin converting enzyme, were investigated in 9 isolated atrial preparations and 7 intact anesthetized donor dogs. In 7 intact dogs, 1-10 mg/Kg of MC-838 caused a decrease in systemic blood pressure, but no significant influence on heart rate was observed. At the same time, in isolated atria perfused with donor's blood, significant increases in developed tension and slight increases in sinus rate were observed with 3 and 10 mg/Kg of MC-838. Intraarterial MC-838 at 10-300 micrograms did not induce significant cardiac effects and MC-838 at 1-3 mg caused an increase in developed tension and a slight increase in sinus rate. The positive inotropic and chronotropic effects were not blocked by adequate doses of propranolol, which significantly blocked norepinephrine-induced positive chronotropic and inotropic effects. It is concluded that a large amount of MC-838 has slight cardiotonic properties which are not mediated via a beta-adrenergic mechanism.
研究了血管紧张素转换酶抑制剂（-）-N-[(S)-3(N-环己基羰基-D-丙氨酰基)-硫代]-2-甲基丙酸]-L-脯氨酸钙（MC-838，阿尔替普利钙）对9个离体心房标本和7只完整麻醉供体犬的作用。在7只完整犬中，1-10mg/kg的MC-838可使全身血压降低，但未观察到对心率有显著影响。同时，在用供体血液灌注的离体心房中，3mg/kg和10mg/kg的MC-838可使舒张张力显著增加，窦性心率略有增加。动脉内注射10-300微克的MC-838未引起明显的心脏效应，而1-3mg的MC-838可使舒张张力增加，窦性心率略有增加。普萘洛尔适当剂量不能阻断其正性肌力和变时性作用，而普萘洛尔能显著阻断去甲肾上腺素引起的正性变时性和正性肌力作用。结论是，大量的MC-838具有轻微的强心特性，其作用不是通过β-肾上腺素能机制介导的。
