Zofenopril

Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. IC50: 81 μM (ACE)[1]

Kinetic analyses demonstrate that enalapril inhibits the uptake of GlySar in a competitive manner (Ki approximately 6 mM). Fosinopril and Zofenopril have the greatest inhibitory potency (IC50 values of 55 and 81μM, respectively) while the other ACE inhibitors exhibit low-affinity interactions with the renal peptide transporter[1].

Zofenopril, a sulphydrylic compound, at doses higher than 70 mg/kg i.p. produces significant protection (i.e. at 70 mg/kg, P=0.044, F=2.17, d.f.=18; at higher concentration P<0.05) against the tonic phase of the audiogenic seizure response. Pretreatment with Zofenopril (15 mg/kg, i.p.) is able to produce a consistent shift to the left of the dose-response curves and a significant reduction of ED50 values against clonus of some AEDs with the exceptions of diazepam, felbamate, phenobarbital and phenytoin compare with concurrent groups, suggesting an increase in anticonvulsant activity[2].

[1]. Lin CJ, et al. Competitive inhibition of glycylsarcosine transport by enalapril in rabbit renal brush border membrane vesicles: interaction of ACE inhibitors with high-affinity H+/peptide symporter. Pharm Res. 1999 May;16(5):609-15. [2]. Sarro GD, et al. Fosinopril and zofenopril, two angiotensin-converting enzyme (ACE) inhibitors, potentiate the anticonvulsant activity of antiepileptic drugs against audiogenic seizures in DBA/2 mice. Pharmacol Res. 2012 Mar;65(3):285-96.