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Updated: Jul 5, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
P2Y1 receptor antagonists as novel antithrombotic agents
Jeffrey A Pfefferkorn1, Chulho Choi, Thomas Winters
1Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, 28/2099E, Ann Arbor, MI 48105, USA. jeffrey.a.pfefferkorn@pfizer.com
Abstract:
The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable.
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