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

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

Eprosartan（SKF-108566J）在抑制[125I]AII与人类肝膜结合方面的IC50为1.7 nM，而抑制其与大鼠肠系膜动脉膜结合的IC50为1.5 nM。在兔主动脉平滑肌细胞中，Eprosartan能够浓度依赖性地抑制AII引起的细胞内Ca2+水平增加[1]。

在清醒的正常血压大鼠中，静脉给予Eprosartan（0.01-0.3 mg/kg）会导致剂量依赖性的平行位移，在AII增压剂量-反应曲线上表现出来。通过胃管或十二指肠给药Eprosartan（3-10 mg/kg）亦可在这些大鼠体内产生对AII（250 ng/kg，静脉给药）增压反应的剂量依赖性抑制。尤其是当剂量达到10 mg/kg，经十二指肠给药时，在3小时内观察到对AII增压反应的显著抑制[1]。