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根据尼卡地平结构特征，设计并合成了三个衍生物，化合物代号分别为９２０１、９２０２和９２０３。在体外血管、工作心脏和清醒大鼠多种实验模型上，研究这三个新化合物对心血管系统的作用特点。在大鼠主动脉环上，尼卡地平、９２０１、９２０２和９２０３抗氯化钾４０ｍｍｏｌ／Ｌ缩血管作用的ＥＣ５０值分别为１．１，０．４，１．２，７．２μｍｏｌ／Ｌ；抗氯化钙２５ｍｍｏｌ／Ｌ缩血管作用的ＥＣ５０值分别为４６，６，１．１，２．８μｍｏｌ／Ｌ；浓度在０．１～１００μｍｏｌ／Ｌ范围内，不对抗去甲肾上腺素５．５μｍｏｌ／Ｌ诱发血管收缩的作用；浓度增至１０ｍｍｏｌ／Ｌ也不对抗去甲肾上腺素０．６μｍｏｌ／Ｌ在无钙孵育液中的缩血管效应。在大鼠工作心脏上，９２０２作用强度与尼卡地平相当，浓度在０．１～１．０μｍｏｌ／Ｌ时可减慢心率，抑制心脏收缩和舒张功能，９２０１和９２０３的作用比尼卡地平弱９０％以上。在清醒大鼠上，灌胃给予尼卡地平及其三个衍生物３ｍｇ／ｋｇ均可使收缩压下降２．０～２．７ｋＰａ，降压至少可持续３ｈ，且对心率的影响轻。提示尼卡地平及这三个衍生物具有较强的扩血管作用，其中９２０１和９２０３对心脏的作用较轻，口服可产生确切的降压效应。
According to the structural characteristics of nicardipine, three derivatives were designed and synthesized with compound codes of 9201, 9202 and 9203, respectively. In vitro vascular, working heart and awake rats on a variety of experimental models to study the three new compounds on the cardiovascular system. In rat aortic rings, EC50 values of nicardipine, 9201, 9202 and 9203 anti-potassium chloride 40mmol / L vasoconstriction were 1.1,0.4,1.2,7.2μmol / L, The EC50 values of anti-calcium chloride 25mmol / L vasoconstriction were 46, 6, 1.1 and 2.8μmol / L, respectively. The concentrations of anti-calcium norepinephrine / L induced vasoconstriction; the concentration increased to 10mmol / L nor anti-norepinephrine 0.6μmol / L in calcium-free incubation of vasoconstrictor effect. In the working heart of rats, the intensity of 9202 is comparable with that of nicardipine, the heart rate can be slowed down and the cardiac systolic and diastolic function can be slowed down when the concentration is 0.1 ~ 1.0μmol / L. The effect of 9201 and 9203 is weaker than that of nicardipine More than 90%. In awake rats, intragastric administration of nicardipine and its three derivatives 3mg / kg systolic blood pressure can be reduced by 2.0 ~ 2.7kPa, blood pressure can be sustained for at least 3h, and the impact on heart rate is light. These findings suggest that nicardipine and these three derivatives have a strong vasodilator effect, of which 9201 and 9203 have less effect on the heart, and oral can produce the exact antihypertensive effect.