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给正常大鼠静脉注射3μg/Kg内皮素,可引起动脉血压下降和心肌收缩力减弱,使LVPSP和±LV dP/dtmax呈显著而持久的降低。给利血平和阿托品化的大鼠注射同样剂量的内皮素,使血压一过性升高。用不同剂量的内皮素灌流心脏,可引起冠状动脉收缩,使灌流压升高,并有强大的抑制心功能的作用,使LVPSP和±LV dp/dt max显著降低,且具有剂效关系。在浓度为10~(-8)M时,可出现心肌挛缩和心律失常,内皮素具有强大的收缩主动脉环的作用,其ED_(50)为3×10~8M,较NE强约5倍。提示内皮素可能是在机体严重损伤(如休克、缺血、缺氧)等条件下,血管内皮细胞产生、释放或漏出的一种致病因子,参与某些疾病的发病过程。
Intravenous injection of 3 μg / Kg of endothelin to normal rats caused a decrease in arterial blood pressure and decreased myocardial contractility, resulting in a significant and sustained decrease in LVPSP and ± LV dP / dtmax. Reserpine and atropine in rats injected with the same dose of endothelin, the blood pressure transiently increased. Perfusion of the heart with different doses of endothelin led to coronary artery contractions, increased perfusion pressure, and a strong inhibition of cardiac function, LVPSP and ± LV dp / dt max were significantly reduced, and with a dose-response relationship. Myocardial contracture and arrhythmia may occur at concentrations of 10 -8 M, and endothelin has a strong systolic aortic ring with an ED 50 of 3 × 10 -8 M, which is about 5 times stronger than that of NE . Tip endothelin may be in the body of severe injury (such as shock, ischemia, hypoxia) and other conditions, vascular endothelial cells produce, release or leakage of a causal agent involved in the pathogenesis of certain diseases.