In Vitro Binding of [³H]PSB-0413 to P2Y₁₂ Receptors.
Fiche publication
Date publication
décembre 2015
Journal
Current protocols in pharmacology
Auteurs
Membres identifiés du Cancéropôle Est :
Dr GACHET Christian
Tous les auteurs :
Dupuis A, Heim V, Ohlmann P, Gachet C
Lien Pubmed
Résumé
The P2Y₁₂/ADP receptor plays a central role in platelet activation. Characterization of this receptor is mandatory for studying disorders associated with a P2Y₁₂ receptor defect and for evaluating P2Y₁₂ receptor agonists and antagonists. In the absence of suitable anti-P2Y₁₂ antibodies, radioligand binding assays are the only way to conduct such studies. While various radioligands were employed in the past for this purpose, none were found to be suitable for routine use. Described in this unit are protocols for quantitatively and qualitatively assessing P2Y₁₂ receptors with [³H]PSB-0413, a selective antagonist for this site. The saturation and competition assays described herein make possible the determination of P2Y₁₂ receptor density on cells, as well as the potencies and affinities of test agents at this site.
Mots clés
Adenosine Monophosphate, analogs & derivatives, Blood Platelets, drug effects, Competitive Bidding, methods, Humans, Purinergic P2Y Receptor Antagonists, pharmacology, Radioligand Assay, methods, Receptors, Purinergic P2, metabolism, Receptors, Purinergic P2Y12, metabolism, Thionucleosides, pharmacology
Référence
Curr Protoc Pharmacol. 2015 Dec;71:1.35.1-19