新型AT_1受体拮抗剂Ⅰb对大鼠的降压作用

Antihypertensive Effects of a New Angiotensin Type 1 Receptor Antagonist Ⅰb on Rats

目的:研究化合物Ⅰb作为一种AT1受体拮抗剂的拮抗活性。方法:分别以清醒自发性高血压大鼠、麻醉自发性高血压大鼠和肾性高血压大鼠为模型,测定化合物Ⅰb的降压活性。结果:在3种大鼠模型中,Ⅰb均可明显降低血压,最大降压幅度分别为17.1%,18.0%和18.0%,降压作用持续时间大约150 min。并且化合物Ⅰb在降压的同时对大鼠的心率无明显影响。结论:化合物Ⅰb作为一种新的抗高血压化合物具有广泛的研发前景。

AIM： To study the antagonistic effects of compound Ⅰb as a new angiotensin type 1 receptor antagonist. METHODS： Conscious spontaneously hypertensive rats （SHRs）, anesthetized spontaneously and renal hypertensive rats （RHRs） were used to evaluate the antagonistic effects of compound Ⅰb. RESULTS： It was shown that the blood pressure in conscious SHR, anesthetized SHR and RHR was significantly reduced after intravenous administration of compound Ⅰb. The maximal extents of attenuation were 17.1%, 18.0% and 18.0%, respectively. The effect lasted about 150 minutes without heart rate being increased. CONCLUSION： These results suggest that compound Ⅰb is a potent, active AT1 receptor antagonist and potent in the treatment of hypertension.