Angiotensin-converting enzyme (ACE) removes the C-terminal dipeptide from angiotensin I to form angiotensin II, a powerful vasoconstrictor. ACE is a key regulator of the renin-angiotensin system and an important drug target for the treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications in diabetes.1 Lisinopril is a potent ACE inhibitor that blocks the formation of angiotensin I with an IC50 value of 1.2 nM (ovine) and displays ID50 values of 2.3 and 6.5 µg/kg in rat and canine, respectively.2 At 0.1 nM lisinopril reduces the formation of endothelin-1 and increases nitric oxide in human vascular endothelial cells.3
1
Zaman, M.A., Oparil, S., and Calhoun, D.A. Drugs targeting the renin-angiotensin-aldosterone system. Nat Rev Drug Discov1621-636(2002).
2
Patchett, A.A., Harris, E., Tristram, E.W., et al. A new class of angiotensin-converting enzyme inhibitors. Nature288280-283(1980).
3
Desideri, G., Grassi, D., Croce, G., et al. Different effects of angiotensin converting enzyme inhibitors on endothelin-1 and nitric oxide balance in human vascular endothelial cells: Evidence of an oxidant-sensitive pathway. Mediators Inflamm(2008).
Desideri, G., Grassi, D., Croce, G., et al. Different effects of angiotensin converting enzyme inhibitors on endothelin-1 and nitric oxide balance in human vascular endothelial cells: Evidence of an oxidant-sensitive pathway. Mediators Inflamm(2008).
Zaman, M.A., Oparil, S., and Calhoun, D.A. Drugs targeting the renin-angiotensin-aldosterone system. Nat Rev Drug Discov1621-636(2002).
Patchett, A.A., Harris, E., Tristram, E.W., et al. A new class of angiotensin-converting enzyme inhibitors. Nature288280-283(1980).
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