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 IC
50 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 (Item No.
15558), zofenopril does not affect bronchoalveolar lavage fluid (BALF) levels of bradykinin or prostaglandin E
2 (PGE
2; Item No.
14010) or increase coughing induced by citric acid in guinea pigs.
3