Losartan Carboxylic Acid (E-3174), the active metabolite of Losartan featuring carboxylic acid, acts as an antagonist to the angiotensin II receptor type 1 (AT1). It displays Ki values of 0.97, 0.57, and 0.67 nM for rat AT1B/AT1A and human AT1, respectively. This compound inhibits angiotensin II-induced effects in vascular smooth muscle cells (VSMC) and increases plasma renin activity while lowering mean arterial pressure[1][2][3][4].
Losartan Carboxylic Acid/氯沙坦羧酸 动物研究
Animal study
Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) produces a comparable degree of suppression (87±4%) of the pressor responses to angiotensin I[3].Intravenous administration of Losartan Carboxylic Acid (0.1 mg/kg followed by 0.01 mg/kg/min) is delivered to anesthetized dogs experiencing recent (8.1±0.4 days) anterior myocardial infarction. Thrombotic occlusion and posterolateral ischemia are induced by electrolytic injury to the left circumflex coronary artery, starting one hour after treatment begins[4].
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