| Autor: |
S D, Kivlighn, G J, Zingaro, R A, Gabel, T P, Broten, R S, Chang, D L, Ondeyka, N B, Mantlo, R E, Gibson, W J, Greenlee, P K, Siegl |
| Rok vydání: |
1995 |
| Předmět: |
|
| Zdroj: |
European journal of pharmacology. 294(2-3) |
| ISSN: |
0014-2999 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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