Figure 2

The carboxyl group and the hydroxyl group are critical structures in olmesartan's inverse agonist activity that allow it to suppress basal c-fos promoter activity. The basal activities of the AT1-N111G mutant receptor were evaluated by a luciferase assay examining c-fos promoter activity in HEK293 cells expressing AT1-N111G. Cells were treated with indicated concentrations of olmesartan, R-239470 or R-90929. *P<0.01 vs. that of pMT3-transfected cells, #P<0.01 vs. that of untreated AT1-N111G-transfected cells, §P<0.05 vs. that of AT1-N111G-transfected cells treated with olmesartan (10−7 M). AT1, angiotensin II type 1.