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pubmed-article:8750704pubmed:abstractTextL-163,017 (6-[benzoylamino]-7-methyl-2-propyl-3-[[2'-(N-(3-methyl-1-butoxy) carbonylaminosulfonyl)[1,1']-biphenyl-4-yl]methyl]-3H-imidazo[4,5- b]pyridine) is a potent, orally active, nonpeptide angiotensin II receptor antagonist. Conscious rats and dogs were dosed p.o. and i.v.; in both species the plasma bioequivalents are similar at the angiotensin AT1 and AT2 receptor sites indicating balanced activity is maintained in vivo. L-163,017 prevents the pressor response to intravenous (i.v.) angiotensin II in the conscious rat, dog, and rhesus monkey. L-163,017 also significantly reduces blood pressure in a renin-dependent model of hypertension, similar to an angiotensin converting enzyme inhibitor (Enalapril) and an angiotensin AT1 receptor-selective antagonist (L-159,282). These studies indicate that neither the angiotensin AT2 receptor nor bradykinin is important in the acute antihypertensive activity of angiotensin converting enzyme inhibitors or angiotensin II receptor antagonists.lld:pubmed
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pubmed-article:8750704pubmed:articleTitleIn vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors.lld:pubmed
pubmed-article:8750704pubmed:affiliationDepartment of Cardiovascular Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA.lld:pubmed
pubmed-article:8750704pubmed:publicationTypeJournal Articlelld:pubmed