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P2Y Receptor
P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. There are eight human P2Y receptor subtypes (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14. P2Y receptors are also found in many animal species indicating their development early in evolution. Almost all human cells express P2Y receptors. Human mast cells express P2Y12, an adenosine diphosphate receptor, and knockdown of this receptor impaired the LTE4-elicited production of MIP-1β and PGD2 in LAD2 human mast cells without altering their responses to LTD4. LTE4 induces the activation of ERK1/2 in CHO cells expressing P2Y12, which is sensitive to PTX. GPR99, which belongs to the P2Y receptor subfamily, was initially identified as a receptor for α-ketoglutarate. Because the α-ketoglutarate–dependent inositol phosphate formation in GPR99-expressing cells is insensitive to PTX, GPR99 seems to act via a Gq/11 pathway.
The ADP-induced platelet aggregation mediated by P2Y1 and P2Y12 receptors. Active metabolites of the thienopyridine compounds ticlopidine, clopidogrel and prasugrel as well as the nucleoside analogue ticagrelor block P2Y12 receptors and thereby platelet aggregation. These drugs are used for the prevention and therapy of cardiovascular events. P2Y receptors play important roles in the nervous system. Adenine nucleotides modulate neuronal activity and neuronal fibre outgrowth by activation of P2Y1 receptors and control migration of microglia by P2Y12 receptors. UDP triggers microglial phagocytosis through activation of P2Y6 receptors. Interestingly, recent findings reveal a prominent role for P2Y2 receptors in Alzheimer's disease pathology. Based on pharmacology, signal transduction and structural similarity, P2Y receptors are divided into two subfamilies. The receptors of the first subfamily (consisting of the P2Y1, P2Y2, P2Y4, P2Y6 and P2Y11 receptors) couple via Gq-proteins to stimulation of phospholipase C followed by increases in inositol phosphates and mobilisation of Ca2+ from intracellular stores. P2Y11 receptors couple in addition to Gs proteins followed by increased adenylate cyclase activity.
References
1.von Kügelgen I,et al. Neuropharmacology. 2016;104:50–61.
The ADP-induced platelet aggregation mediated by P2Y1 and P2Y12 receptors. Active metabolites of the thienopyridine compounds ticlopidine, clopidogrel and prasugrel as well as the nucleoside analogue ticagrelor block P2Y12 receptors and thereby platelet aggregation. These drugs are used for the prevention and therapy of cardiovascular events. P2Y receptors play important roles in the nervous system. Adenine nucleotides modulate neuronal activity and neuronal fibre outgrowth by activation of P2Y1 receptors and control migration of microglia by P2Y12 receptors. UDP triggers microglial phagocytosis through activation of P2Y6 receptors. Interestingly, recent findings reveal a prominent role for P2Y2 receptors in Alzheimer's disease pathology. Based on pharmacology, signal transduction and structural similarity, P2Y receptors are divided into two subfamilies. The receptors of the first subfamily (consisting of the P2Y1, P2Y2, P2Y4, P2Y6 and P2Y11 receptors) couple via Gq-proteins to stimulation of phospholipase C followed by increases in inositol phosphates and mobilisation of Ca2+ from intracellular stores. P2Y11 receptors couple in addition to Gs proteins followed by increased adenylate cyclase activity.
References
1.von Kügelgen I,et al. Neuropharmacology. 2016;104:50–61.
GPCR/G Protein
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P2Y Receptor
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SYL-4
产品货号 : M37336
cas no: 6222-65-7
SYL-4 is a potential P2Y12 receptor antagonist with a Ki value of 7.35 ± 1.72 for use in synthetic dyes.
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PPTN hydrochloride
产品货号 : M35725
cas no: 1992047-65-0
PPTN hydrochloride 是一种有效，高亲和力，竞争性和高选择性的 P2Y14 受体拮抗剂，KB 为 434 pM。PPTN hydrochloride 对 P2Y1，P2Y2，P2Y4，P2Y6，P2Y11，P2Y12 或 P2Y13 受体无激动剂或拮抗剂作用。具有抗炎和抗免疫活性。
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Regrelor disodium
产品货号 : M34691
cas no: 676251-22-2
Regrelor disodium (INS 50589) is a P2Y12 receptor antagonist that prevents thrombosis, effectively inhibits vascular smooth muscle cell contraction, curbs cell proliferation, and reduces inflammation.
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PSB-16133 sodium
产品货号 : M34386
cas no: 2089035-40-3
PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.
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PIT
产品货号 : M33909
cas no: 56583-49-4
PIT (2,2'-Pyridylisatogen tosylate) 是 P2Y1 受体 的选择性和非竞争性拮抗剂，对人 P2Y1 受体的 IC50 值为 0.14 μM。PIT 在不影响核苷酸结合的情况下拮抗 P2Y1 受体信号。PIT 是一些平滑肌中代谢性嘌呤受体 (P2Y 家族) 对 ATP 反应的不可逆拮抗剂。PIT 可用于慢性支气管炎和哮喘的研究。
