Preclinical pharmacology of zofenopril, an inhibitor of angiotensin I converting enzyme

Journal of Cardiovascular Pharmacology
J M DeForrestE W Petrillo

Abstract

Zofenopril calcium (one-half calcium salt) is a prodrug ester analog of captopril whose biological effects are manifested by its active component, SQ 26,333. Because of the relative insolubilities of both zofenopril calcium and SQ 26,333, zofenopril potassium salt and SQ 26,703, the arginine salt of the active ACE (angiotensin I converting enzyme) inhibitory moiety of zofenopril, were employed in many of the following studies. The in vitro and in vivo pharmacological effects of zofenopril have been evaluated and comparisons have been made to captopril. In vitro, SQ 26,703 was more potent than captopril as an inhibitor of rabbit lung ACE (IC50 = 8 vs. 23 nM). SQ 26,703 was also a potent inhibitor of angiotensin I (AI)-induced contractions (EC50 = 3 nM) and a potentiator of bradykinin-induced contractions (EC50 = 1 nM) of isolated guinea pig ileum, while it had no effect on the inotropic effects of angiotensin II, BaCl2, PGE1, histamine, serotonin, or acetycholine in the same tissue, signifying that zofenopril is a specific inhibitor of ACE. In vivo, the potency of SQ 26,703 was equal to or greater than that of captopril as an inhibitor of an AI pressor response when given intravenously to rats, dogs, and monkeys. After oral admi...Continue Reading

Citations

Dec 9, 2003·European Journal of Pharmacology·Anne Ward ScribnerClaudio Napoli
Nov 24, 2011·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Giovambattista De SarroEmilio Russo
Jan 18, 2005·The Journal of International Medical Research·S Evangelista, S Manzini
Aug 28, 2010·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Alessandra Del FiorentinoRoberto Pedrinelli
Aug 28, 2004·Expert Opinion on Pharmacotherapy·Claudio BorghiEttore Ambrosioni
Jul 7, 2016·Journal of the American Heart Association·Erminia DonnarummaTraci T Goodchild
Aug 10, 2020·Advances in Therapy·Claudio Borghi, Stefano Omboni
Nov 25, 2016·Molecular and Cellular Biochemistry·Petar RisticVladimir Lj Jakovljevic
Jul 18, 2018·European Journal of Pharmacology·Paolo FagoneFerdinando Nicoletti

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