Description
Angiotensin-converting enzyme (ACE) converts angiotensin I to angiotensin II, a peptide hormone that impacts vascular smooth muscle tone and renal salt exchange, driving hypertension. Enalaprilat is the active metabolite of enalapril , an ACE inhibitor with roles in the management of hypertension, congestive heart failure, myocardial infarction, and diabetic nephropathies.. Enalaprilat is esterified with ethanol to produce enalapril in order to enable oral activity and subsequently metabolized
in vivo to the active form by various esterases. Enalaprilat is reported to inhibit ACE activity with an IC
50 value of 5.8 nM
in vitro.
Chemical Properties
White Solid
Uses
Active metabolite of Enalapril. A nonsulfhydryl dipeptide angiotensin converting enzyme (ACE) inhibitor. Enalapril EP Impurity C (Dihydrate).
Definition
ChEBI: The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients wi
h nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.
Biochem/physiol Actions
Enalapril, the ethyl ester of?enalaprilat exhibits slight pharmacological activity until it is hydrolyzed in the liver to?enalaprilat. Enalaprilat, a IV form of an angiotensin-converting-enzyme inhibitor (ACE) prevents the transformation of angiotensin I to angiotensin II, a potent vasoconstrictor.
