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NCI: A non-thiol angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, zabicipril is rapidly converted in vivo by de-esterification into its active form zabiciprilat. Zabiciprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Zabiciprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
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