Storck J, Ochs J G, Kirsten R
Institut für klinische Pharmakologie, J.W-Goethe-Universität Frankfurt, FRG.
Int J Clin Pharmacol Ther Toxicol. 1990 Jul;28(7):303-8.
Urapidil inhibits the 5HT induced human platelet aggregation and the 5HT uptake by platelets in vitro and ex vivo. The aggregation was inhibited with a KI-value of 8.8 microM and the 5HT uptake in a noncompetitive way with KI1 = 15.3 microM and K12 = 10.6 microM. In vivo, the 5HT induced platelet aggregation was increased 4 h after oral administration of 60 mg urapidil. Subsequently, the aggregation decreased and reached a minimum at various times in the different volunteers. Eight h after oral administration of 60 mg urapidil, the 5HT uptake velocity was reduced approximately 40%.
乌拉地尔在体内外均可抑制5-羟色胺（5HT）诱导的人血小板聚集及血小板对5HT的摄取。其对血小板聚集的抑制作用的抑制常数（KI）值为8.8微摩尔，对5HT摄取的抑制作用呈非竞争性，其中KI1 = 15.3微摩尔，K12 = 10.6微摩尔。在体内，口服60毫克乌拉地尔4小时后，5HT诱导的血小板聚集增加。随后，聚集作用下降，并在不同志愿者的不同时间达到最小值。口服60毫克乌拉地尔8小时后，5HT摄取速度降低约40%。
