Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors.
The selective antagonist radioligand [(3)H]2-propylthioadenosine-5'-adenylic acid (1,1-dichloro-1-phosphonomethyl-1-phosphonyl) anhydride ([(3)H]PSB-0413) was prepared by catalytic hydrogenation of its propargyl precursor with a high specific radioactivity of 74Ci/mmol. In preliminary saturation binding studies, [(3)H]PSB-0413 showed high affinity for platelet P2Y(12) receptors with a K(D) value of 4.57nM. Human platelets had a high density of P2Y(12) receptors exhibiting a B(max) value of 7.66pmol/mg of protein.
El-Tayeb
Ali
A
Pharmaceutical Institute, Pharmaceutical Sciences Bonn (PSB), University of Bonn, Kreuzbergweg 26, D-53115 Bonn, Germany.
Griessmeier
Kerstin J
KJ
Müller
Christa E
CE
D000249:Adenosine Monophosphate / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000502:physiology*; D006801:Humans; D007700:Kinetics; D058919:Purinergic P2 Receptor Antagonists; D011869:Radioligand Assay; D018048:Receptors, Purinergic P2 / Q000097:blood; D058925:Receptors, Purinergic P2Y12; D013872:Thionucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D014316:Tritium
C548576:P2RY12 protein, human; C511278:PSB-0413; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058925:Receptors, Purinergic P2Y12; D013872:Thionucleosides; D014316:Tritium; D000249:Adenosine Monophosphate