Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) induces a similar level of inhibition (87±4%) of the pressor responses to angiotensin I[3]. Intravenous Losartan Carboxylic Acid (0.1 mg/kg+0.01 mg/kg/min) is infused in anesthetized dogs with recent (8.1±0.4 days) anterior myocardial infarction. Electrolytic injury of the left circumflex coronary artery to induce thrombotic occlusion and posterolateral ischemia is initiated 1 h after the start of treatment[4]. Animal Model: Mongrel dogs of either sex, weighing 15-25 kg[3] Dosage: 0.1 mg/kg (followed by 0.02 mg/kg/h) Administration: i.v. for 5.5 hours Result: The pressor response was reduced by 87±4%.
In Vitro
The specific binding of [125I]-angiotensin II to VSMC is inhibited by Losartan Carboxylic Acid (E-3174) with an IC50 of 1.1 nM. Losartan Carboxylic Acid abolishes the angiotensin II-induced formation of inositolphosphates in VSMC. Losartan Carboxylic Acid inhibits the angiotensin II-induced elevation of intracellular cytosolic Ca2+ concentration with an IC50 of 5 nM. Losartan Carboxylic Acid is more effective than losartan in blocking the angiotensin II-induced increase in Egr-1 mRNA. Losartan Carboxylic Acid inhibits the angiotensin II-induced cell protein synthesis with an IC50 of 3 nM[1].
Kinase Assay
Cell Assay
Animal Administration
References
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