Abbildung 4: Angiotensin-I-Rezeptor
In vivo studies show that telmisartan is a potent and long-acting antagonist of the hypertensive effects of exogenously administered angiotensin II. In the rabbit aorta, the maximal contractile response to angiotensin II was dose-dependently decreased by 40% to 50% across a dose range of 10 to 1000 nM. No agonist activity was detected at any concentration.1 Even high concentrations of angiotensin II were unable to overcome the receptor blockade, demonstrating that telmisartan manifests an insurmountable AT1 receptor antagonism. 1. Wienen W, et al. Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br J Pharmacol 1993; 110: 245–252.