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Losartan, a nonpeptide angiotensin II (Ang II) receptor antagonist, inhibits neointima formation following balloon injury to rat carotid arteries.
TLDR
Losartan attenuated the vascular response to balloon catheter injury, and this effect was associated with functional block of vascular AT1 receptors, supporting a role for Ang II, acting via AT1 receptor, in myointimal thickening subsequent to balloon injury of rat carotid arteries. Expand
Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure
TLDR
A novel benzazepine compound evacetrapib is described, which is a potent and selective inhibitor of CETP both in vitro and in vivo, and is currently in phase II clinical development. Expand
Characterization of the ZDSD Rat: A Translational Model for the Study of Metabolic Syndrome and Type 2 Diabetes
TLDR
The ZDSD rat develops prediabetic metabolic syndrome and T2D in a manner that mirrors the development of metabolic syndrome in humans and will provide a novel, translational animal model for the study of human metabolic diseases and for theDevelopment of new therapies. Expand
3,3-Bisaryloxindoles as mineralocorticoid receptor antagonists.
Syntheses and SAR studies of 3,3-bisaryloxindole analogues provided potent mineralocorticoid receptor (MR) antagonists that were selective over other steroid nuclear hormone receptors.
Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1- yl]phenyl]methyl]imidazole derivatives and their in vitro activity.
A series of nonpeptide angiotensin II receptor antagonists was synthesized and tested in vitro to investigate requirements for recognition by and binding to AT1 receptors. Compared to a known seriesExpand
Rosiglitazone reverses endothelial dysfunction but not remodeling of femoral artery in Zucker diabetic fatty rats
TLDR
The endothelial dysfunction and mechanical remodeling are observed as early as 19 weeks of age in ZDF rat and Rosi treatment for 3 weeks improves endothelial function but not mechanical properties. Expand
Characterization of Distinct Angiotensin II Binding Sites in Rat Adrenal Gland and Bovine Cerebellum Using Selective Nonpeptide Antagonists
TLDR
The Ki values for DUP753 at the DUP753-sensitive binding site in rat adrenal glomerulosa and medulla are similar to the affinity of DUP753 for All receptors in rabbit aorta, suggesting a similarity among these sites. Expand
The relation between vascular relaxant and cardiac electrophysiological effects of pinacidil.
TLDR
It is concluded that pinacidil as well as nicorandil and BRL 34915 affect vascular and cardiac tissues by similar mechanisms, possibly by increases in potassium ion permeability, although other mechanisms may also play a role. Expand
Structural evolution and pharmacology of a novel series of triacid angiotensin II receptor antagonists.
TLDR
The most potent compound, cis-4-[4-(phosphonomethyl)phenoxy]-1-[1-oxo-2(R)-[4-[(2-sulfobenzoyl+ ++) amino]-1H-imidazol-1-yl]octyl]-L-proline (1e), inhibited the pressor response to exogenously administered Ang II for periods up to 8 h following oral dosing. Expand
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
TLDR
This compound represents the first MR antagonist in this class of molecules, exhibiting picomolar binding affinity and in vivo blood pressure lowering at pharmaceutically relevant doses. Expand
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