A Series of Analogues to the ATR Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode.

We here report on our continued studies of ligands binding to the promising drug target angiotensin II type 2 receptor (ATR). Two series of compounds were synthesized and investigated. The first series explored the effects of adding small substituents to the phenyl ring of the known selective nonpeptide ATR antagonist , generating small but significant shifts in ATR affinity.

Anti-fibrotic Potential of AT Receptor Agonists.

There are a number of therapeutic targets to treat organ fibrosis that are under investigation in preclinical models. There is increasing evidence that stimulation of the angiotensin II type 2 receptor (ATR) is a novel anti-fibrotic strategy and we have reviewed the published preclinical data relating to the effects of compound 21 (C21), which is the only nonpeptide ATR agonist that is currently available for use in chronic preclinical studies. In particular, the differential influence of ATR on extracellular matrix status in various preclinical fibrotic models is discussed.

Efficacy of a low dose of estrogen on antioxidant defenses and heart rate variability.

This study tested whether a low dose (40% less than the pharmacological dose of 17-β estradiol) would be as effective as the pharmacological dose to improve cardiovascular parameters and decrease cardiac oxidative stress. Female Wistar rats (n = 9/group) were divided in three groups: (1) ovariectomized (Ovx), (2) ovariectomized animals treated for 21 days with low dose (LE; 0.2 mg), and (3) high dose (HE; 0.