Internalization of constitutively active N111G mutant of AT1 receptor induced by angiotensin II-receptor antagonists candesartan, losartan, and telmisartan: Comparison with valsartan

Abstract

Based on radioligand binding and signal transduction assays in our previous study, we have determined the binding pattern and functional efficacy of the constitutively active mutant N111G of angiotensin II type 1 (AT1) receptor. We have also shown that the N111G mutant induces homologous internalization through mediation of the AT1-receptor antagonist valsartan. In this study we demonstrated that other AT1-receptor antagonists, candesartan, losartan, and telmisartan, also stimulate internalization of N111G mutant receptor to the same extent. We further showed that the internalization pattern is also similar for all the AT1-receptor antagonists. ©2010 The Japanese Pharmacological Society.