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P2Y₁₂ receptor (P2Y₁₂)
- Target
- P2Y₁₂
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The P2Y₁₂ receptor is a G protein-coupled purinergic receptor expressed on platelets and is essential for ADP-mediated platelet activation and aggregation. Antagonists of this receptor, including ticagrelor and its equipotent active metabolite AR-C124910XX, inhibit platelet aggregation and are used clinically to reduce the risk of thrombotic cardiovascular events such as myocardial infarction and stroke, particularly in acute coronary syndrome. Unlike thienopyridines, ticagrelor and AR-C124910XX bind reversibly and do not require hepatic metabolic activation, allowing for a more rapid and predictable antiplatelet effect[1][3][4][5][6][7][8].
- Other names
- P2Y12 purinoceptorP2Y12 platelet receptorP2RY12
02
Mechanism of action
Reversible inhibition of ADP-induced activation of the P2Y₁₂ receptor to block platelet aggregation[1][3][5][7][8] Antagonism (competitive or allosteric) at the P2Y₁₂ receptor
03
Biological functions
Signal transductionPlatelet aggregationHemostasis
04
Disease associations
Cardiovascular diseaseThrombosisMyocardial infarctionAcute coronary syndrome
05
Safety considerations
Bleeding risk (including major bleeding)DyspneaBradyarrhythmiasDrug-drug interactions (notably with CYP3A4 inhibitors/inducers)[1][3][5][6]
06
Interacting drugs
Ticagrelor
5 more in the full profile.
07
Biomarkers
Platelet function tests (e.g., ADP-induced platelet aggregation)P2Y₁₂ reaction units (PRU; e.g., VerifyNow assay)
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