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苯并吡喃类新化合物S103的药理作用初步研究结果表明:该化合物有较好的血管舒张活性,能浓度依赖性地抑制由KCl和去甲肾上腺素刺激引起的大鼠胸主动脉条的收缩,对低K+刺激引起收缩有较好的舒张作用(IC50为0.42±0.07μmol/L),其舒张作用被四乙铵和格列苯脲所拮抗;S103浓度依赖地抑制大鼠门静脉自发活动的收缩幅度;还能增加预先负载86Rb+的大鼠胸主动脉条的86Rb+外流;其作用特点和吡那地尔相似,表现出ATP敏感钾通道开放剂的特证。实验结果提示S103是一个新的ATP敏感钾通道开放剂。
The preliminary pharmacological effects of benzopyran novel compound S103 showed that the compound has good vasodilator activity and can inhibit the contraction of rat thoracic aortic strips in a concentration-dependent manner by KCl and norepinephrine stimulation , With a good relaxation effect on contractility induced by low K + stimulation (IC50 0.42 ± 0.07μmol / L), and its diastolic action was antagonized by tetraethylammonium and glibenclamide. S103 inhibited rat portal vein in a concentration-dependent manner Spontaneous contraction; and also increased 86Rb + efflux of the rat thoracic aortic strips preloaded with 86Rb +; its action profile is similar to pinacidil and evidence of ATP-sensitive potassium channel openers. The results suggest that S103 is a new ATP-sensitive potassium channel opener.