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- W934197824 abstract "Losartan is the prototype of a new class of orally active, nonpeptide angiotensin II (AII) receptor antagonists. Losartan inhibits specifically the renin-angiotensin system (RAS) without the agonist effects of the peptide receptor antagonists or the bradykinin (BK) potentiating effects of the angiotensin-converting enzyme (ACE) inhibitors. The BK potentiation effects of ACE inhibitors, however, have given rise to the mechanistic issues. Losartan, by contrast, is selective for the AII AT1 receptor subtype, which mediates all of the known biological effects of AII. Because of its specificity and selectivity of action, losartan is being used to define the functional role of AII in many physiological or pathophysiological settings. This chapter discusses the methods and strategies by which the prototype nonpeptide AII receptor antagonist losartan was (1) synthesized, (2) characterized in vitro, (3) characterized in vivo, (4) analyzed in blood or urine, and (5) evaluated in man. At present, these methods/strategies are being applied to the discovery of a new class of inhibitors of the renin-angiotensin system." @default.
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- W934197824 date "1993-01-01" @default.
- W934197824 modified "2023-10-15" @default.
- W934197824 title "Nonpeptide Angiotensin II Receptor Antagonist: Losartan" @default.
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- W934197824 doi "https://doi.org/10.1016/b978-0-12-185275-7.50021-4" @default.
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