Purinergic (P2Y) Receptors

Prasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI.

Cangrelor Tetrasodium is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion.

Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis.

TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.

Clopidogrel thiolactone is a P2Y12 receptor inhibitor, is a potent antiplatelet agent.

N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM).

Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.

HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC50 of 26 pM. This compound effectively blocks the activation of hepatic stellate cells by inhibiting the PKA/Raf1/MEK/ERK signaling pathway associated with P2Y14R, thereby mitigating the progression of liver fibrosis. HDB-1 is valuable for research into the mechanisms underlying liver fibrosis and the development of potential therapeutic strategies.

(±)-Clopidogrel bisulfate is an inhibitor of the platelet P2Y12 receptor and serves as an adenosine diphosphate (ADP) receptor antagonist. By blocking ADP binding to its receptors on platelet membranes, (±)-Clopidogrel bisulfate effectively attenuates ADP-mediated glycoprotein GPIIb/IIIa complex activation. This compound is utilized in research investigating its role in reducing vascular inflammation and mitigating the progression of angiotensin II-induced abdominal aortic aneurysms, as well as exploring its anti-inflammatory properties.

PSB-16133 sodium is a potent P2Y receptor inhibitor that selectively targets various P2Y receptor subtypes. This compound is valuable for studying purinergic signaling pathways and understanding their roles in physiological and pathological processes. PSB-16133 sodium can be utilized in research applications focusing on inflammation, cardiovascular disorders, and neuronal signaling.

R-138727 is a potent and selective irreversible antagonist of the P2Y12 receptor, functioning as a key inhibitor with an IC50 of 2.5 μM. This compound covalently binds to the P2Y12 receptor present on platelet surfaces, effectively blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 is valuable for research applications targeting stroke, cerebral infarction, and associated neurological deficits.

NF340 is a selective inhibitor of the P2Y11 receptor, achieving a pIC50 of 7.3-7.7 in human cells. It effectively blocks nociceptive signaling and alleviates the upregulation of P2Y11 receptors in the spinal dorsal horn following spinal cord injury. NF340 further inhibits the NFκB signaling pathway induced by IL-1β, leading to a reduction in pro-inflammatory cytokine expression and a decrease in intracellular ROS levels. Additionally, it suppresses ATP-induced calcium influx and cell migration in human hepatocellular carcinoma cells. NF340 is relevant for research into neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma.