Abstract: Objective To investigate the effects of olmesartan, zofenopril and eplerenone on angiotensin Ⅱ type 1 receptor （AT1R） and antibody against AT1R （AT1R-Ab） in two-kidney one clip （2K1C） renovascular hypertensive rats. Methods One hundred and twenty male Sprague-Dawly rats were randomly divided into Sham, 2K1C, 2K1C+olmesartan（O）, 2K1C+zofenopril（Z） and 2K1C+eplerenone group（E）, with 24 rats in each group. 2K1C hypertensive model was established in the last four groups. Four weeks after operation, rats in O, Z and E group were treated with olmesartan （3 mg/kg）, zofenopril （10 mg/kg） and eplerenone（100 mg/kg） by gavage respectively, while rats in Sham and 2K1C group were treated with equal-volume distilled water. The myocardial structure and function were detected by ultrasonography, and the plasma AT1R, AT1R-Ab were evaluated by ELISA at 8, 12 and 14 weeks after operation. Results At 8 weeks after operation, the level of plasma AT1R in 2K1C group was not significantly different from that in sham group, while it was increased in O, Z and E groups （all P＜0.05）. At 12 or 14 weeks after operation, the level of plasma AT1R in 2K1C group was higher than that in sham group and lower than that in Z and E groups 12 week （67.56±1.67） vs （74.63±0.83）, （75.85±3.09） ng/L; 14 week （73.90±1.98） vs （78.29±0.31）, （78.05±1.12）ng/L, respectively, all P＜0.05. While, there was no significant difference between 2K1C group and O group in plasma AT1R levels. Compared with sham group, plasma AT1R-Ab levels in 2K1C group were higher at 8 weeks after operation, which was decreased at 12 and 14 weeks. The levels of plasma AT1R-Ab in Z and E groups were lower than that in 2K1C group at each time points 8 week （2.10±0.10）,（2.13±0.18）vs（2.75±0.13）ng/L; 12 week（2.00±0.10）,（2.03±0.1）vs（2.32±0.10）ng/L; 14 week（1.99±0.16）,（2.00±0.09）vs（2.23±0.23）ng/L; all P＜0.05. While, there was no significant difference between 2K1C group and O group in plasma AT1R-Ab levels. Conclusion Plasma levels of AT1R, AT1R-Ab, and blood pressure were always changing with time in renovascular hypertensive rats. Olmesartan, zofenopril and eplerenone decreased blood pressure and the thickness of left ventricle, but up-regulated the plasma AT1R. Zofenopril and eplerenone but not olmesartan reduced the levels of AT1R-Ab.