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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

In vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors.

L-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.[1]


  1. In vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors. Kivlighn, S.D., Zingaro, G.J., Gabel, R.A., Broten, T.P., Chang, R.S., Ondeyka, D.L., Mantlo, N.B., Gibson, R.E., Greenlee, W.J., Siegl, P.K. Eur. J. Pharmacol. (1995) [Pubmed]
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