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Ticagrelor inhibits adenosine uptake in vitro and enhances adenosine-mediated hyperemia responses in a canine model.
van Giezen JJ, Sidaway J, Glaves P, Kirk I, Björkman JA. van Giezen JJ, et al. J Cardiovasc Pharmacol Ther. 2012 Jun;17(2):164-72. doi: 10.1177/1074248411410883. Epub 2011 Jun 22. J Cardiovasc Pharmacol Ther. 2012. PMID: 21697355
Role of newly formed platelets in thrombus formation in rat after clopidogrel treatment: comparison to the reversible binding P2Y₁₂ antagonist ticagrelor.
Kuijpers MJ, Megens RT, Nikookhesal E, Feijge MA, De Mey JG, oude Egbrink MG, van Giezen JJ, Heemskerk JW. Kuijpers MJ, et al. Among authors: van giezen jj. Thromb Haemost. 2011 Dec;106(6):1179-88. doi: 10.1160/TH11-04-0252. Epub 2011 Nov 10. Thromb Haemost. 2011. PMID: 22071958
Characterization of the adenosine pharmacology of ticagrelor reveals therapeutically relevant inhibition of equilibrative nucleoside transporter 1.
Armstrong D, Summers C, Ewart L, Nylander S, Sidaway JE, van Giezen JJ. Armstrong D, et al. Among authors: van giezen jj. J Cardiovasc Pharmacol Ther. 2014 Mar;19(2):209-19. doi: 10.1177/1074248413511693. Epub 2014 Jan 10. J Cardiovasc Pharmacol Ther. 2014. PMID: 24414167
Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations.
Giordanetto F, Bach P, Zetterberg F, Antonsson T, Bylund R, Johansson J, Sellén M, Brown D, Hideståhl L, Berntsson P, Hovdal D, Zachrisson H, Björkman JA, van Giezen JJ. Giordanetto F, et al. Among authors: van giezen jj. Bioorg Med Chem Lett. 2014 Jul 1;24(13):2963-8. doi: 10.1016/j.bmcl.2014.04.001. Epub 2014 Apr 12. Bioorg Med Chem Lett. 2014. PMID: 24835983
Gradual increase in thrombogenicity of juvenile platelets formed upon offset of prasugrel medication.
Baaten CC, Veenstra LF, Wetzels R, van Geffen JP, Swieringa F, de Witt SM, Henskens YM, Crijns H, Nylander S, van Giezen JJ, Heemskerk JW, van der Meijden PE. Baaten CC, et al. Among authors: van giezen jj. Haematologica. 2015 Sep;100(9):1131-8. doi: 10.3324/haematol.2014.122457. Epub 2015 Jun 25. Haematologica. 2015. PMID: 26113418 Free PMC article. Clinical Trial.
Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.
Bach P, Antonsson T, Bylund R, Björkman JA, Österlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. Bach P, et al. Among authors: van giezen jj. J Med Chem. 2013 Sep 12;56(17):7015-24. doi: 10.1021/jm400820m. Epub 2013 Aug 29. J Med Chem. 2013. PMID: 23899349
Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y₁₂ receptor.
Bach P, Boström J, Brickmann K, van Giezen JJ, Groneberg RD, Harvey DM, O'Sullivan M, Zetterberg F. Bach P, et al. Among authors: van giezen jj. Eur J Med Chem. 2013 Jul;65:360-75. doi: 10.1016/j.ejmech.2013.04.007. Epub 2013 May 15. Eur J Med Chem. 2013. PMID: 23747805
Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model.
Ravnefjord A, Weilitz J, Emanuelsson BM, van Giezen JJ. Ravnefjord A, et al. Among authors: van giezen jj. Thromb Res. 2012 Oct;130(4):622-8. doi: 10.1016/j.thromres.2012.07.021. Epub 2012 Aug 19. Thromb Res. 2012. PMID: 22909827
A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor.
Bach P, Boström J, Brickmann K, van Giezen JJ, Hovland R, Petersson AU, Ray A, Zetterberg F. Bach P, et al. Among authors: van giezen jj. Bioorg Med Chem Lett. 2011 May 15;21(10):2877-81. doi: 10.1016/j.bmcl.2011.03.088. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21507636
Ticagrelor binds to human P2Y(12) independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation.
VAN Giezen JJ, Nilsson L, Berntsson P, Wissing BM, Giordanetto F, Tomlinson W, Greasley PJ. VAN Giezen JJ, et al. J Thromb Haemost. 2009 Sep;7(9):1556-65. doi: 10.1111/j.1538-7836.2009.03527.x. Epub 2009 Jun 23. J Thromb Haemost. 2009. PMID: 19552634
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