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CAS No. : 144143-96-4
MCE 国际站:Eprosartan mesylate
产品活性:Eprosartan mesylate (SKF-108566J) 是一种选择性,竞争性,非肽和具有口服活性的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,可用作降压剂。Eprosartan mesylate 结合血管紧张素 II 受体,在大鼠和人类肾上腺皮质膜中的 IC50 值分别为 9.2 nM 和 3.9 nM。
研究领域:GPCR/G Protein
作用靶点:Angiotensin Receptor
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.
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.
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