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  • Title: Inhibition of cytosolic Ca++ mobilization in human platelets by the antianginal drug trapidil and its derivative AR 12463.
    Author: Block HU, Gabbasov ZA, Pozin EY, Popov EG, Mest HJ.
    Journal: Biomed Biochim Acta; 1988; 47(12):1093-7. PubMed ID: 2855396.
    Abstract:
    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.
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