Figure 6 | Hypertension Research

Figure 6

From: Multivalent ligand–receptor interactions elicit inverse agonist activity of AT1 receptor blockers against stretch-induced AT1 receptor activation

Figure 6

Specific drug–receptor interactions are required for olmesartan's inverse agonist activity against stretch-induced extracellular signal-regulated protein kinase (ERK) activation. (a) HEK293 cells expressing AT1-WT, -Y113F, -K199Q, -H256A or -Q257A mutant receptors were pretreated with 10−7 M olmesartan and stimulated by mechanical stretch. The activation of ERKs was then determined. *P<0.01 vs. that of wild-type AT1-WT. (b) The chemical structures of olmesartan and R-88145, which has a carboxyl group (circled COOH) instead of a tetrazole group. (c) HEK293-AT1 cells were pretreated with indicated concentrations of olmesartan or R-88145 and were stimulated by 10−7 M AngII (left) or mechanical stretch (right). The activation of ERKs was then determined. AT1, angiotensin II type 1.

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