Quinaprilat (Synonyms: CI-928)

Quinaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC₅₀ = 0.06 nM) and an active metabolite of the ACE inhibitor prodrug quinapril .^1,2 It inhibits calcium overload and rod to round cell shape change induced by lysophosphatidylcholine (LPC) in isolated rat cardiomyocytes when used at concentrations of 20 and 50 µM.² Quinaprilat (3 µg/kg) reduces the frequency of ventricular fibrillation in a dog model of myocardial ischemia and reperfusion injury.³ It also reduces blood pressure and proteinuria in rat models of uranyl nitrate- or 5/6 nephrectomy-induced chronic renal failure when administered at a dose of 0.1 mg/kg.⁴

1.Perich, R.B., Jackson, B., and Johnston, C.I.Structural constraints of inhibitors for binding at two active sites on somatic angiotensin converting enzymeEur. J. Pharmacol.266(3)201-211(1994) 2.Ma, H., Hashizume, H., Hara, A., et al.Protective effect of quinaprilat, an active metabolite of quinapril, on Ca2+-overload induced by lysophosphatidylcholine in isolated rat cardiomyocytesJpn. J. Pharmacol.79(1)17-24(1999) 3.Fujinaga, H., Wakatsuki, T., Nishikado, A., et al.Electrophysiologic effects of quinaprilat in dogs during acute myocardial ischemia and following reperfusionCoron. Artery Dis.9(10)697-701(1998) 4.Appenroth, D., Beutinger, R., Lupp, A., et al.Effects of a therapy with losartan and quinaprilat on the progression of chronic renal failure in rats after a single dose of uranyl nitrate or 5/6 nephrectomyExp. Toxicol. Pathol.54(5-6)359-366(2003)