Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent. It exhibits inhibitory effects on angiotensin II receptors with IC50 values of 9.2 nM in rat adrenocortical membranes and 3.9 nM in human adrenocortical membranes.

[125I] binding to human liver membranes:1.7 nM, Mesenteric artery membranes (rat):1.5 nM

Eprosartan (SKF-108566J) inhibits [125I]AII binding to human liver membranes with an IC50 of 1.7 nM and to rat mesenteric artery membranes with an IC50 of 1.5 nM. In rabbit aortic smooth muscle cells, Eprosartan causes a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[1]

In conscious normotensive rats, intravenous administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Intragastric or intraduodenal administration of Eprosartan (3-10 mg/kg) to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). Significant inhibition of the pressor response to AII was observed for 3 hours at a dose of 10 mg/kg, intraduodenally[1].