Fujita K, Matsumura Y, Miyazaki Y, Hashimoto N, Takaoka M, Morimoto S
Department of Pharmacology, Osaka University of Pharmaceutical Sciences, Japan.
Life Sci. 1996;58(1):PL1-7. doi: 10.1016/0024-3205(95)02259-7.
Renal effects of FR139317, an endothelin ETA receptor antagonist, were examined using anesthetized normotensive and deoxycorticosterone acetate (DOCA)-salt hypertensive rats. The intravenous bolus injection of FR139317 (10 mg/kg) produced a slight decrease in mean blood pressure (MAP; -13%) in the control rats and this hypotension was accompanied by a moderate renal vasodilation (renal vascular resistance: RVR; -12%). In the DOCA-salt hypertensive rat, FR139317 had a more pronounced hypotensive effect (MAP; -26%) accompanied by a potent renal vasodilation (RVR; -33%). FR139317 significantly increased renal blood flow only in the DOCA-salt rats. In contrast, FR139317 produced a significant decrease in urine flow and urinary sodium excretion only in control rats. Northern blot analysis revealed that the renal prepro endothelin-1 (ET-1) mRNA level was significantly increased in DOCA-salt hypertensive rats. Thus, it seems likely that endogenous ET-1 is responsible for the maintenance of DOCA-salt-induced hypertension. We also suggest that at least in part, ET-1 and ETA receptors are involved in renal hemodynamic abnormalities in DOCA-salt-induced hypertension. The augmentation of renal ET-1 production may possibly have a function in the development and maintenance of DOCA-salt-induced hypertension.
使用麻醉的正常血压大鼠和醋酸脱氧皮质酮(DOCA)-盐高血压大鼠,研究了内皮素ETA受体拮抗剂FR139317对肾脏的影响。在对照大鼠中静脉推注FR139317(10mg/kg)导致平均血压(MAP)略有下降(-13%),这种低血压伴随着中度肾血管舒张(肾血管阻力:RVR;-12%)。在DOCA-盐高血压大鼠中,FR139317具有更明显的降压作用(MAP;-26%),同时伴有强力的肾血管舒张(RVR;-33%)。FR139317仅在DOCA-盐大鼠中显著增加肾血流量。相反,FR139317仅在对照大鼠中使尿流量和尿钠排泄显著减少。Northern印迹分析显示,DOCA-盐高血压大鼠肾前内皮素-1(ET-1)mRNA水平显著升高。因此,内源性ET-1似乎是DOCA-盐诱导高血压维持的原因。我们还认为,ET-1和ETA受体至少部分参与了DOCA-盐诱导高血压中的肾血流动力学异常。肾ET-1产生的增加可能在DOCA-盐诱导高血压的发生和维持中起作用。