Ticagrelor inverse agonist activity at the P2Y₁₂ receptor is non-reversible versus its endogenous agonist adenosine 5´-diphosphate.

ABSTRACT:

Background and purpose

Ticagrelor is labelled as a reversible, direct-acting platelet P2Y₁₂ receptor (P2Y₁₂ R) antagonist that is indicated clinically for the prevention of thrombotic events in patients with acute coronary syndrome (ACS). As with many antiplatelet drugs, ticagrelor therapy increases bleeding risk in patients, which may require platelet transfusion in emergency situations. The aim of this study was to further examine the reversibility of ticagrelor at the P2Y₁₂ R.

Experimental approach

Studies were performed in human platelets, with P2Y₁₂ R-stimulated GTPase activity and platelet aggregation assessed. Cell-based bioluminescence resonance energy transfer (BRET) assays were undertaken to assess G protein-subunit activ

SUBMITTER: Khalil J 

PROVIDER: S-EPMC10953389 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature