摘要
目的:观察一氧化氮(NO)供体型苯骈吡喃类化合物Ⅱ-7对清醒自发性高血压大鼠(SHR)血压的影响及体外NO释放活性.方法:NO供体型苯骈吡喃类化合物Ⅱ-7分别一次性及重复多次(连续7 d)对SHR灌胃给药,测定其尾动脉收缩压(SAP)、舒张压(DAP)及心率(HR);采用Griess法测定Ⅱ-7体外NO释放量.结果:Ⅱ-7在6.0 mg/kg的剂量下一次性及连续7 d经口给药,均可非常显著地降低SHR的SAP和DAP(P＜0.01),一次性给药在降压的同时显著增加SHR的HR值(P＜0.05).体外NO释放试验结果显示,Ⅱ-7在体外能缓慢且稳定地释放NO,2.5～5.0 h内维持在较恒定的水平(0.265～0.284μg/mL).结论:NO供体型苯骈吡喃类化合物Ⅱ-7单次及重复灌胃7 d均能明显降低SHR的血压,降压作用具有一定的剂量相关性,其在体外能缓慢稳定地释放NO.
AIM:To study the effect of NO donating-benzopyran compound——Ⅱ-7 on the awake spontaneously hypertensive rats (SHR) and the nitric oxide (NO) release in vitro.METHODS:Systolic artery pressure(SAP),diastolic artery pressure(DAP) and heart rate(HR) were measured after single oral administration and 7-day repeated oral administration of Ⅱ-7.The quantity of NO releasing was determined by Griess method.RESULTS:Single oral administration of Ⅱ-7 at 6.0 mg/kg decreased the SAP and DAP very significantly (P<0.01 vs control) while increasing the HR remarkably (P<0.05 vs control).After 7-day repeated administration of Ⅱ-7 (6.0,2.0 mg/kg),with no difference in SAP and DAP being observed in the (2.0 mg/kg) group (P>0.05 vs control),the compound showed a dose-dependent effect while those of the 6.0 mg/kg group were decreased very significantly(P<0.01 vs control).It was also found that NO was slowly released and even remained at a rather stable level between 0.265～0.284 μg/mL in 2.5 h with the maximal release of 0.286 μg/mL being reached.CONCLUSION:Single or 7-day repeated oral administration of NO donating-benzopyran compound (Ⅱ-7) could significantly decrease the blood pressure of SHR release NO slowly while remaining at a rather stable level in vitro.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2005年第4期359-362,共4页
Journal of China Pharmaceutical University
