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Description: EXP-3174 (also known as losartan aarboxylic acid), a physiologically active metabolite of losartan produced by cytochrome P450 isoforms in the liver, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. Like the parent compound losartan, EXP-3174 is a potent AT1 antagonist with Kis of 0.57 and 0.67 nM for rat and human forms, respectively. It produces a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability.
References: Clinical Science, 1996; 91(2): 147-154; Journal of Hypertension. 1993; 11(2): 155-162.
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