Date published: 2025-9-12

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P2Y12 Inhibitors

P2Y12 inhibitors form a diverse class of compounds meticulously designed to modulate platelet function by targeting the P2Y12 receptor, a pivotal player in adenosine diphosphate (ADP)-mediated platelet activation. This receptor is a critical component in the intricate web of signaling pathways governing platelet aggregation, making it a prime target for intervention in cardiovascular diseases. Within the realm of P2Y12 inhibitors, there exists a fundamental categorization into thienopyridines and non-thienopyridines, each wielding its inhibitory effects through distinctive mechanisms. Thienopyridines, typified by clopidogrel, prasugrel, and ticlopidine, represent prodrugs necessitating metabolic activation to engender an active form capable of irreversibly binding to the P2Y12 receptor. In contrast, non-thienopyridine P2Y12 inhibitors, exemplified by ticagrelor, operate by directly and reversibly binding to the P2Y12 receptor. This mechanism obviates the need for metabolic conversion, offering a distinct pharmacological profile. This subclass also encompasses compounds like cangrelor, AZD1283, and ticagrelor ditosylate, each endowed with unique attributes such as a rapid onset of action or investigational potential, enriching the armamentarium of antiplatelet agents. Additionally, compounds like MRS2395, PSB-0739, MRS2211, MRS2500, and AR-C69931MX contribute significantly to ongoing research endeavors by selectively inhibiting P2Y12 receptors. These compounds serve as valuable tools for probing the intricacies of platelet activation and the broader purinergic signaling network, advancing our understanding of these processes

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