Comparative studies of tissue inhibition by angiotensin converting enzyme inhibitors

Abstract

There is increasing evidence that inhibition of tissue angiotensin converting enzyme (ACE) is important for the pharmacokinetics and pharmacodynamic effects of ACE inhibitors. Radioligand inhibitor binding methods using 125I-351A and either tissue homogenates or in vitro autoradiography have allowed in vitro and ex vivo quantitation of tissue ACE inhibition by a variety of ACE inhibitors. The rank order of potency against plasma as well as lung, kidney, and cardiac homogenates was quinaprilat = benazeprilat > perindoprilat > lisinopril > enalaprilat > fosinoprilat. The highest concentration of ACE in the heart was found in the cardiac valves followed by the right and left atria, then the rig..