A prodrug form of zofenoprilat
Zofenopril is a prodrug form of the angiotensin-converting enzyme (ACE) inhibitor zofenoprilat.1 Zofenopril is hydrolyzed by cardiac esterases in vivo to form zofenoprilat. It inhibits ACE with an IC50 value of 0.9 nM in heart tissue homogenates and inhibits cardiac ACE activity in isolated perfused rat hearts. It reduces mean arterial blood pressure in two kidney-one clip renal hypertensive (2K-1C) rats and spontaneously hypertensive rats (SHRs) when administered at doses of 2.2, 6.6, and 22 mg/kg.2 Unlike the ACE inhibitor ramipril , zofenopril does not affect bronchoalveolar lavage fluid (BALF) levels of bradykinin or prostaglandin E2 or increase coughing induced by citric acid in guinea pigs.3
1.Grover, G.J., Sleph, P.G., Dzwonczyk, S., et al.Effects of different angiotensin-converting enzyme (ACE) inhibitors on ischemic isolated rat hearts: Relationship between cardiac ACE inhibition and cardioprotectionJ. Pharmacol. Exp. Ther.257(3)919-929(1991) 2.DeForrest, J.M., Waldron, T.L., Krapcho, J., et al.Preclinical pharmacology of zofenopril, an inhibitor of angiotensin I converting enzymeJ. Cardiovasc. Pharmacol.13(6)887-894(1989) 3.Cialdai, C., Giuliani, S., Valenti, C., et al.Differences between zofenopril and ramipril, two ACE inhibitors, on cough induced by citric acid in guinea pigs: Role of bradykinin and PGE2Naunyn Schmiedebergs Arch. Pharmacol.382(5-6)455-461(2010)
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