Target intelligence / Profile preview

P2Y₁₂ purinoceptor (P2Y₁₂ receptor) (P2Y₁₂)

Target
P2Y₁₂
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The P2Y₁₂ purinoceptor is a G protein-coupled ADP receptor found on platelets, mediating ADP-induced platelet activation and aggregation—a central component of hemostasis and thrombosis. Ticagrelor is an orally active, reversible antagonist of the P2Y₁₂ receptor; its major active metabolite AR-C124910XX shares this action. These agents block ADP-induced signal transduction, thereby preventing platelet activation and reducing risk of arterial thrombotic events, including myocardial infarction and stroke. In contrast to the thienopyridine class, ticagrelor and AR-C124910XX bind reversibly and do not require metabolic activation for efficacy.

Other names
P2Y₁₂ receptorP2Y₁₂ ADP receptorPurinergic receptor P2Y₁₂P2RY12
02

Mechanism of action

Reversible, non-competitive antagonism of the P2Y₁₂ receptor, preventing ADP-mediated platelet activation and aggregation (for ticagrelor and its active metabolite); Irreversible antagonism of P2Y₁₂ receptor (for thienopyridines: clopidogrel, prasugrel, ticlopidine).

03

Biological functions

Signal transductionPlatelet activationPlatelet aggregationHemostasis
04

Disease associations

Cardiovascular diseaseThrombosisMyocardial infarctionStroke
05

Safety considerations

Increased risk of bleeding (major and minor hemorrhage)Dyspnea (shortness of breath)BradyarrhythmiasContraindication with strong CYP3A4 inhibitors/inducers (affecting ticagrelor and its metabolite exposure)Not recommended in patients with active pathological bleeding, history of intracranial hemorrhage
06

Interacting drugs

Ticagrelor

5 more in the full profile.

07

Biomarkers

P2Y₁₂ receptor function (e.g., platelet reactivity assays)Platelet aggregation/IPA (inhibition of platelet aggregation) testingCYP2C19 genotype is relevant for clopidogrel (not for ticagrelor, which is not dependent on CYP2C19 for activation)

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