Chemical Name:2-Butyl-3,4-dihydro-N,N-dimethyl-4-oxo-3-[[2'-(1H-tetra
zol-5-yl)[1,1'-biphenyl-4-yl]methyl]-5H-imidazo[4,5-c]p
yridine-5-acetamide hydrochloride
Biological Activity:
Highly potent and very selective non-peptide
angiotensin AT1 receptor antagonist (IC50 values are 0.7
and > 10000 nM for AT1 and AT2 receptors
respectively). Potently inhibits angiotensin II-induced contractions in
isolated rabbit aorta (IC50 = 0.2 nM) and reduces blood pressure in
hypertensive rats.
Mederskiet al
(1994) Non-peptide angiotensin II receptor antagonists: synthesis and
biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine
derivatives. J.Med.Chem. 37 1632. Mederskiet al
(1995) 4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic
acid-derived AT1 antagonists with improved affinity for the AT2
receptor. Bioorg.Med.Chem.Lett. 5 2665.
