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本品为白色或类白色结晶性粉末。无臭,无味,微溶于水、乙醇、生理食盐水,溶于稀甲醇。药理作用:本品是选择性作用于突触后α-肾上腺素能受体的阻断剂。它对血管平滑肌具有直接松弛作用,能降低小动脉阻力,也能扩张小静脉,减低心脏前负荷和后负荷。实验证明,本品通过抑制细胞膜下的磷酸二酯酶,从而增加细胞内环磷酸腺苷(cAMP)的含量,而cAMP 则是松弛血管平滑肌的一种介质,故能发挥扩血管作用。当切除交感神经后,本品即无血管扩张作用。口服本品1mg 的降舒张压作用相当于肼苯哒嗪的20mg。在狗的实验中,本品除高剂量组能引起反
This product is white or almost white crystalline powder. Odorless, tasteless, slightly soluble in water, ethanol, saline, soluble in dilute methanol. Pharmacological effects: This product is selectively acting on the postsynaptic α-adrenergic receptor blockers. It has a direct relaxation of vascular smooth muscle, can reduce arteriolar resistance, but also dilate the small veins, reduce pre-cardiac load and afterload. Experiments show that this product by inhibiting cell membrane phosphodiesterase, thereby increasing intracellular cyclic AMP (cAMP) content, while cAMP is a mediator of relaxation of vascular smooth muscle, it can play a vasodilator effect. When the excision of the sympathetic nerve, this product is no vasodilatation. Oral 1mg of oral antihypertensive effect of the equivalent of hydralazine 20mg. In the dog’s experiment, this product can cause anti-high-dose group