Taube C, Steinborn C, Mest H J
Institut für Pharmakologie und Toxikologie, Bereichs Medizin, Martin-Luther-Universität Halle-Wittenberg.
Pharmazie. 1987 May;42(5):334-6.
The trapidil derivative AR 12463 has a much more stronger inhibiting effect than trapidil on different atherosclerotic parameters of the cell cultures obtained from normal intima and fatty streaks of human aorta, on thromboxane (TX) formation and on the aggregation of human platelets in vitro, and on the activity of phosphodiesterase. In addition to these present results, AR 12463 reduced significantly the mean arterial blood pressure of spontaneously hypertensive rats (at a dosage of 20 mg/kg/d administered orally for 2 weeks) in contrast to the same dosage of trapidil. Simultaneously, TX formation is significantly reduced in serum by 48% in aorta thoracica by 29%, and in aorta abdominalis by 19%. Due to these properties, AR 12463 seems to be suitable for a therapeutic and prophylactic strategy in chronic ischemic diseases.
曲匹地尔衍生物AR 12463对从人主动脉正常内膜和脂肪条纹获得的细胞培养物的不同动脉粥样硬化参数、对血栓素（TX）的形成、对人血小板的体外聚集以及对磷酸二酯酶的活性具有比曲匹地尔更强得多的抑制作用。除了这些现有结果外，与相同剂量的曲匹地尔相比，AR 12463显著降低了自发性高血压大鼠的平均动脉血压（以20mg/kg/d的剂量口服给药2周）。同时，血清中TX的形成显著降低48%，胸主动脉中降低29%，腹主动脉中降低19%。由于这些特性，AR 12463似乎适用于慢性缺血性疾病的治疗和预防策略。
