Angiotensin receptor is a G protein coupled receptor with angiotensin as ligand, which can trigger various signal cascades after being activated. Eprosartan mesylate (SKF-108566J) is a nonpeptide angiotensin receptor antagonist[3]. In rat and human adrenal cortical membranes, rat mesenteric artery membranes and human liver membranes, Eprosartan Mesylate specifically displaced angiotensin receptor ligand, [125I] angiotensin II (AII), with IC50 of 9.2, 3.9, 1.5 and 1.7 nM, respectively[3]. In rabbit aortic smooth muscle cells, Eprosartan Mesylate caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[3]. In vivo assay, administration of Eprosartan mesylate (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[3].
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