Losartan Carboxylic Acid (Synonyms: E-3174,EXP-3174) |
カタログ番号GC12512 |
ロサルタンの活性カルボン酸代謝産物であるロサルタンカルボン酸 (E-3174) は、アンギオテンシン II 受容体タイプ 1 (AT1) 拮抗薬です。
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Cas No.: 124750-92-1
Sample solution is provided at 25 µL, 10mM.
Ki = 5-20 nM
Losartan Carboxylic Acid, also named E-3174, a physiologically active metabolite of losartan, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. AII is the primary mediator of the reninangiotensin system, which regulates the blood pressure and body-fluid balance and may be associated with the development of cardiovascular diseases via increasing contractility and cell growth in vascular smooth muscle cells (VSMC).
In vitro: E-3174 potently blocked the specific binding of [125I]-AII to VSMC isolated from rat aorta. E-3174 was able to dampen the platelet-derived growth factor-induced increase in cell DNA synthesis and protein, which led to the blockade of the AII-induced increase in cell protein [1].
In vivo: Rats were administrated E-3174 intravenously at a dose of l.0 mg/kg. After 6 hours, E-3174 markedly attenuated the cardiovascular effects of AII in rats. E-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2].
References:
[1]. Li, X. & Widdop, R. Angiotensin Type I Receptor Antagonists CY-11974 and EXP 3174 Cause Selective Renal Vasodilatation in Conscious Spontaneously Hypertensive Rats. Clinical Science, 1996; 91(2): 147-154.
[2]. Sachinidis, A., Ko, Y., Weisser, P., zu BricBkwedde, M., Dsing, R., & Christian, R. et al. EXP3174, a metabolite of losartan (MK954, DuP753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. Journal of Hypertension. 1993; 11(2): 155-162.
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