Figure 2.

Differences in the inverse agonist activities of the six ARBs for WT‐ AT₁ receptors and the N111G‐ AT₁ receptor mutant, as measured by the IP assay. The concentration‐dependent inverse agonist activities of losartan, valsartan, candesartan, irbesartan, telmisartan and eprosartan for (A) WT‐ AT₁ receptors and (B) N111G‐ AT₁ receptors transfected into COS‐1 cells. Maximal inverse agonist activities of losartan, valsartan, candesartan, irbesartan, telmisartan and eprosartan for (C) WT‐ AT₁ receptors and (D) N111G‐ AT₁ receptors, measured at a concentration of 10 μM for each ARB. Data for losartan, valsartan and irbesartan are taken from our recent study and used with permission from Molecular Pharmacology (Takezako et al., 2015). The inverse agonist activities of the six ARBs are expressed as a percentage of the constitutive activity of vehicle‐treated WT‐ AT₁ receptor‐transfected and N111G‐AT₁ receptor‐transfected COS‐1 cells. The constitutive activities of vehicle‐treated cells expressing WT‐ AT₁ receptors and N111G‐ AT₁ receptors were defined as 0%. Data represent mean ± SEM of independent experiments (n = 6 for each groups). ^* P < 0.05, significant differences between the groups; one‐way ANOVA followed by Bonferroni's or Dunnett's post hoc tests.