Mentz P, Pawelski K E, Orlova Z R, Giessler C, Mest H J
Institut für Pharmakologie und Toxikologie, Martin-Luther-Universität Halle-Wittenberg.
Pharmazie. 1987 Jun;42(6):403-6.
Cardiac and coronary effects of trapidil (Rocornal) and some derivatives were investigated in isolated heart preparations and rabbit hearts in vivo. All substances showed a comparable increase of the coronary flow. Contrary to the cardiotonic influence of trapidil the trapidil derivates induced a negative inotropic effect, possibly due to a weak calcium antagonism. Heart rate was slightly diminished, but in some cases higher doses caused an acute tachycardia. I.v. application of the substances to rabbits in doses of 10 mg/kg and 30 mg/kg induced an initial depression of blood pressure normalizing within 3-5 min. An increase of the myocardial prostacyclin biosynthesis is only demonstrable under trapidil. The results indicate that the cardiac effects of trapidil derivatives are possibly caused by a direct influence on the contractile system and the membrane potential of the cardiac muscle cell.
在离体心脏标本和家兔活体心脏中研究了曲匹地尔（Rocornal）及其某些衍生物对心脏和冠状动脉的作用。所有物质均使冠状动脉血流量有类似增加。与曲匹地尔的强心作用相反，曲匹地尔衍生物产生负性肌力作用，这可能是由于其微弱的钙拮抗作用所致。心率略有降低，但在某些情况下，较高剂量会引起急性心动过速。静脉注射剂量为10mg/kg和30mg/kg的这些物质可使家兔血压最初下降，并在3 - 5分钟内恢复正常。仅在曲匹地尔作用下可证明心肌前列环素生物合成增加。结果表明，曲匹地尔衍生物对心脏的作用可能是直接影响心肌细胞的收缩系统和膜电位所致。
