Block H U, Gabbasov Z A, Pozin E Y, Popov E G, Mest H J
Institute of Pharmacology and Toxicology, Martin Luther University, Halle, GDR.
Biomed Biochim Acta. 1988;47(12):1093-7.
The antianginal drug trapidil (5-methyl-7-diethylamino-s-triazolo-(1.5-a)pyrimidine) and its derivative AR 12463 (5-piperidino-7-(N-(n-amyl)-N-(beta-hydroxyethyl)-amino)-s-triazolo(1.5- a) pyrimidine) inhibit the thromboxane A2 agonist (U-46619)-induced mobilization of intracellular platelet-free Ca++ as measured with the fluorescent Ca++ indicator Indo-1. This inhibitory effect is independent of extracellular Ca++ concentration, and AR 12463 is about 70-fold more active than trapidil itself.
抗心绞痛药物曲匹地尔（5-甲基-7-二乙氨基-s-三唑并-(1.5-a)嘧啶）及其衍生物AR 12463（5-哌啶基-7-（N-（正戊基）-N-（β-羟乙基）-氨基）-s-三唑并(1.5-a)嘧啶）可抑制血栓素A2激动剂（U-46619）诱导的细胞内游离血小板钙的动员，这是通过荧光钙指示剂Indo-1进行测量的。这种抑制作用与细胞外钙浓度无关，并且AR 12463的活性比曲匹地尔本身高约70倍。
