The P2Y₁₂ receptor is one of eight known P2Y receptor subtypes, and belongs to the G-protein-coupled receptor (GPCR) family. The P2Y₁₂ receptor is highly expressed on blood platelets and in the brain. Potent, selective, peripherally acting antagonists for the P2Y₁₂ receptor are used clinically as antithrombotic drugs. Several different scaffolds have been identified as P2Y₁₂ receptor antagonists, including irreversibly acting thienotetrahydropyridines (prodrugs), and reversible competitive antagonists, including adenine nucleotide analogs, piperazinyl-glutamate-quinolines, -pyridines, and -pyrimidines, and anthraquinone derivatives. Here, we provide an overview of the different scaffolds that have been developed as P2Y₁₂ receptor antagonists, some of which have become important therapeutics.

P2Y ₁₂受体是八种已知的P2Y受体亚型之一，属于G蛋白偶联受体（GPCR）家族。P2Y ₁₂受体在血小板和大脑中高表达。P2Y ₁₂受体的有效，选择性，作用于周围的拮抗剂在临床上用作抗血栓形成药物。几种不同的支架已被鉴定为P2Y ₁₂受体拮抗剂，包括不可逆作用的硫代四氢吡啶类（前药）和可逆竞争性拮抗剂，包括腺嘌呤核苷酸类似物，哌嗪基-谷氨酸喹啉，-吡啶和-嘧啶和蒽醌衍生物。在这里，我们提供了已被开发为P2Y ₁₂的不同支架的概述。 受体拮抗剂，其中一些已成为重要的治疗剂。