Eprosartan (mesylate)

Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC₅₀s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively^[1]. In Vitro: Eprosartan (SKF-108566J) inhibits [¹²⁵I]AII binding to human liver membranes (IC₅₀ of 1.7 nM) and to rat mesenteric artery membranes (IC₅₀ of 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca²⁺ levels^[1]. In Vivo: In conscious normotensive rats, i.v. administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Administration of Eprosartan (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^[1].