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乃舒匹林(2-(乙酰氧基)苯甲酸-3-(硝氧基)丙酯)是一种新型的阿司匹林硝酸酯衍生物,初步实验提示该药除可能具有抑制环加氧酶而产生抗炎等作用外,在体内还能释放一氧化氮(NO)基团,可能对胃肠粘膜提供一定的保护作用,并能通过NO对心血管等系统产生其他作用如血管舒张效应等。本实验研究了乃舒匹林对离体兔胸主动脉的舒张作用,结果表叫乃舒匹林对于内应完整和去除内皮的血管均有剂量依赖的舒张作用(EC_(50);分别为7.26×10~(-6)mol·L-1和 125×10-5 mol·L~(-1)),与硝酸甘油(EC50分别为4.69×10~(-6)mol·L~(-1)和5.3×10~(-6)mol·L~(-1))。相比,差异无显著性(P>0.05)。阿司匹林对离体血管无显著的舒张作用(浓度范围1x10~(-8)mol·L~(-1)至1x10~(-4)mol·L~(-1))研究结果表明乃舒匹林可不依赖于内皮细胞地扩张离体血管,这种血管舒张效应可能与提供NO,作用于血管平滑肌有关。
Nesugustine (2- (acetoxy) benzoate-3- (nitroxyphenyl) benzoate) is a novel aspirin nitrate derivative. Preliminary experiments suggest that this drug may not only inhibit cyclooxygenase It can release nitric oxide (NO) group in the body, which may provide certain protective effect on the gastrointestinal mucosa and can exert other functions such as vasodilation effect on the cardiovascular system through NO. In this study, we investigated the relaxation effect of norgexapine on the thoracic aorta of isolated rabbit. The results showed that naloxipram had a dose-dependent relaxation effect on intact and endothelial-evacuated blood vessels (EC 50; .6 × 10 ~ (-6) mol·L-1 and 125 × 10-5 mol·L-1), and the EC50 values were 4.69 × 10 ~ (-6) mol·L ~ (-1) and 5.3 × 10 ~ (-6) mol·L -1). Compared with no significant difference (P> 0.05). Aspirin showed no significant relaxation effect on isolated blood vessels (concentration range of 1 × 10 -8 mol·L -1 to 1 × 10 -4 mol·L -1) Vasodilation can be independent of endothelial cells, this vasodilatation may be related to the provision of NO, acting on vascular smooth muscle.