生物活性

• 靶点	Angiotensin Receptor IC50:20nM

• 描述The numerous effects of Angiotensin II (AII), including its roles in vasoconstriction, secretion of aldosterone and vasopressin, cellular proliferation, and hypertrophy are dominantly mediated through the activation of the angiotensin type 1 (AT₁) receptor, a member of the superfamily of G protein-coupled receptors. Losartan Potassium is an AII receptor antagonist that competitively binds the AT₁ receptor with IC₅₀ of 20 nM. Male cynomolgus monkeys were given losartan (180 mg/d, n=6) or vehicle (n=8) for 6 weeks. Losartan caused significant (P<0.05) increases in plasma AII and angiotensin-(1-7). Compared with vehicle-treated controls, losartan reduced the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% (P<0.05). A significant (P<0.05) reduction in the susceptibility of low-density lipoprotein (LDL) to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression were also associated with losartan treatment.

• 动物研究
  剂量	Mice[3]: 0.1 mg/kg - 5 mg/kg (i.p.); 3 mg/kg, 30 mg/kg (p.o.) Rat[4]: 10 mg/kg (p.o.)
  给药途径	i.p., p.o.
  动物药代数据	Animal Rats[4] Dose 10 mg/kg Administration p.o. T1/2 3.27 ± 0.45 h Tmax 0.73 ± 0.16 h Cmax 1.33 ± 0.21 mg/L AUC0→t 7.34 ± 0.75 mg·h/L