AVE 0991 is an orally active, non-peptide-based selective Ang (1-7) receptor (Mas, MasR) agonist with 5-times NO-inducing efficacy than Ang (1-7) in bovine aortic endothelial cell (BAEC) cultures (10 μM; BAEC) and 10-fold higher affinity (IC50 = 21 nM vs 220 nM, respectively, against 10 nM [125I]-Ang-(1-7) for BAEC membrane binding), exhibiting little affinity toward AT1 & AT2 receptors. AVE 0991 is a widely probing Mas-mediated responses in cultures (0.01-10 μM) and in animal disease models in vivo (0.3-10 mg/kg via ip., po. or intranasal; rats and mice).
Orally active, non-peptide-based selective Ang (1-7) receptor (Mas, MasR) agonist in vitro and in vivo.
Recent work has renewed interest in therapies targeting the renin-angiotensin system (RAS) to improve β-cell function in type 2 diabetes. Studies show that generation of angiotensin-(1-7) by ACE2 and its binding to the Mas receptor (MasR) improves glucose homeostasis, partly
Frontiers in pharmacology, 10, 146-146 (2019-03-12)
The MasR receptor (MasR) is an orphan G protein-coupled receptor proposed as a candidate for mediating the angiotensin (Ang)-converting enzyme 2-Ang-(1-7) protective axis of renin-angiotensin system. This receptor has been suggested to participate in several physiological processes including cardio- and
Recently, we demonstrated that the heptapeptide angiotensin-(1-7) (Ang-[1-7]) exhibits a favorable kinetic of nitric oxide (NO) release accompanied by extremely low superoxide (O2-) production. In this report we describe AVE 0991, a novel nonpeptide compound that evoked effects similar to
American journal of physiology. Heart and circulatory physiology, 312(5), H980-H991 (2017-04-16)
The objectives of the present study were to investigate the effect of ANG-(1-7) on the development of cardiac hypertrophy and to identify the intracellular mechanism underlying this action of ANG-(1-7). Blood pressure and heart rate were recorded using radiotelemetry before
During the aging process, chronic neuroinflammation induced by microglia is detrimental for the brain and contributes to the etiology of several aging-related neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. As a newly identified axis of renin-angiotensin system, ACE2/Ang-(1-7)/MAS1
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