The P2Y12 receptor: no active metabolite, no party.
Poor responders to clopidogrel have low levels of circulating active metabolite. However, in vitro experiments have shown that blood platelets from poor responders are fully inhibited by the active metabolite of this prodrug. Impaired platelet inhibition reflects inadequate plasma levels of active metabolites, and not differences in platelet P2Y12 receptor function.
Patrono
Carlo
C
Department of Pharmacology, Catholic University School of Medicine, Largo F. Vito 1, Rome, Italy. carlo.patrono@rm.unicatt.it
D001189:Aryl Hydrocarbon Hydroxylases / Q000235:genetics / Q000378:metabolism; D001682:Biological Availability; D001711:Biotransformation; D000077144:Clopidogrel; D065731:Cytochrome P-450 CYP2C19; D004347:Drug Interactions; D004351:Drug Resistance; D014644:Genetic Variation; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010979:Platelet Function Tests; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2 / Q000097:blood; D058925:Receptors, Purinergic P2Y12; D013988:Ticlopidine / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D017211:Treatment Failure
C548576:P2RY12 protein, human; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058925:Receptors, Purinergic P2Y12; D000077144:Clopidogrel; D001189:Aryl Hydrocarbon Hydroxylases; C045793:CYP2C19 protein, human; D065731:Cytochrome P-450 CYP2C19; D013988:Ticlopidine