Overview
- Konieczka, K. et al. (2011) Curr. Eye Res. 36, 118.
Alomone Labs Avosentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.Dose-response curve of Avosentan (#A-355) inhibition of ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 2.79 nM. Cells were loaded with Calcium 6 dye, incubated with Avosentan, and stimulated with 15 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
Avosentan is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. It was initially developed for the treatment of diabetic nephropathy1,2. Studies show that inhibition of ET-A receptors can be protective in chronic kidney disease through several processes including vasodilation, attenuation of proteinuria, and increasing diuresis2.
ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides3.
