Ticagrelor Inhibits Adenosine Uptake In Vitro and Enhances Adenosine-Mediated Hyperemia Responses in a Canine Model:

作者: J. J. J. van Giezen , James Sidaway , Philip Glaves , Ian Kirk , Jan-Arne Björkman

DOI: 10.1177/1074248411410883

关键词: In vitroIn vivoBlood flowMedicinePharmacologyReactive hyperemiaDipyridamoleInternal medicineArteryCardiologyAdenosineTicagrelor

摘要: Aims: A routine secondary pharmacology screen indicated that reversibly binding oral P2Y12 receptor antagonist ticagrelor could inhibit adenosine uptake in human erythrocytes, suggesting may potentiate adenosine-mediated responses vivo. The aim of this study was to further characterize the inhibition vitro and possible physiological consequences by an anesthetized dog model coronary blood flow compared dipyridamole. Methods Results: We measured [2-3H]adenosine purified erythrocytes several cell lines presence or known inhibitor dipyridamole as a comparator. Using open-chest (beagles), we left anterior descending (LAD) artery during reactive hyperemia after 1 minute occlusion intracoronary infusion before administration vehicle, ticagrelor, (each n = 8). Ticagrelor co...

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