Department of Pharmacology and Toxicology, Pharma Center, University of Bonn, D-53127, Bonn, Germany.
Purinergic Signal. 2024 Apr;20(2):99-108. doi: 10.1007/s11302-023-09963-w. Epub 2023 Sep 12.
P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. There are eight mammalian P2Y receptor subtypes (P2Y, P2Y, P2Y, P2Y, P2Y, P2Y, P2Y, and P2Y). The widely expressed P2Y receptors play important roles in physiology and pathophysiology. This review summarizes the use of pharmacological tools to characterize the P2Y receptor subtypes involved in these responses. MRS2500 is a potent and selective antagonist acting at the P2Y receptor. AR-C118925 is useful for the selective antagonism of the P2Y receptor. PSB16133 blocks the P2Y receptor, MRS2578 is an antagonist at the P2Y receptor and NF157 as well as NF340 block the P2Y receptor. ADP-induced platelet aggregation is mediated by P2Y and P2Y receptors. A number of compounds or their active metabolites reduce ADP-induced platelet aggregation by blocking the P2Y receptor. These include the active metabolites of the thienopyridine compounds clopidogrel and prasugrel, the nucleoside analogue ticagrelor and the nucleotide analogue cangrelor. PSB0739 is also a potent antagonist at the P2Y receptor useful for both in vitro and in vivo studies. MRS2211 and MRS2603 inhibit P2Y mediated responses. PPTN is a very potent antagonist at the P2Y receptor.
P2Y 受体是细胞外核苷酸的 G 蛋白偶联受体 (GPCR)。哺乳动物有八种 P2Y 受体亚型 (P2Y、P2Y、P2Y、P2Y、P2Y、P2Y、P2Y 和 P2Y)。广泛表达的 P2Y 受体在生理和病理生理学中发挥重要作用。本文综述了使用药理学工具来描述参与这些反应的 P2Y 受体亚型的方法。MRS2500 是一种作用于 P2Y 受体的有效且选择性拮抗剂。AR-C118925 可用于选择性拮抗 P2Y 受体。PSB16133 阻断 P2Y 受体，MRS2578 是 P2Y 受体拮抗剂，NF157 和 NF340 阻断 P2Y 受体。ADP 诱导的血小板聚集由 P2Y 和 P2Y 受体介导。许多化合物或其活性代谢物通过阻断 P2Y 受体来减少 ADP 诱导的血小板聚集。这些包括噻吩并吡啶化合物氯吡格雷和普拉格雷的活性代谢物、核苷类似物替卡格雷和核苷酸类似物坎格雷洛。PSB0739 也是一种作用于 P2Y 受体的有效拮抗剂，可用于体外和体内研究。MRS2211 和 MRS2603 抑制 P2Y 介导的反应。PPTN 是一种非常有效的 P2Y 受体拮抗剂。
