Synthesis and preliminary evaluation of [H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors |
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Authors: | Ali El-Tayeb, Kerstin J. Griessmeier,Christa E. Mü ller, |
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Affiliation: | a Pharmaceutical Institute, Pharmaceutical Sciences Bonn (PSB), University of Bonn, Kreuzbergweg 26, D-53115 Bonn, Germany |
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Abstract: | The selective antagonist radioligand [3H]2-propylthioadenosine-5′-adenylic acid (1,1-dichloro-1-phosphonomethyl-1-phosphonyl) anhydride ([3H]PSB-0413) was prepared by catalytic hydrogenation of its propargyl precursor with a high specific radioactivity of 74 Ci/mmol. In preliminary saturation binding studies, [3H]PSB-0413 showed high affinity for platelet P2Y12 receptors with a KD value of 4.57 nM. Human platelets had a high density of P2Y12 receptors exhibiting a Bmax value of 7.66 pmol/mg of protein. |
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Keywords: | P2Y12 receptor Radioligand Platelets [3H]PSB-0413 Nucleotide analog AR-C67085MX |
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