Description

MRS2578 is an antagonist of the purinergic P2Y₆ receptor (IC₅₀s = 37 and 98 nM for human and rat receptors, respectively). It is without effect at other purinergic receptors. MRS2578 is used to study the cellular and physiological roles of P2Y₆.

Uses

MRS 2578 is a selective P2Y66?receptor antagonist.

Uses

MRS 2578 has been used an antagonist of purinoceptor P2Y6:

• to study the role of purinergic receptor in Up4A-induced relaxation in coronary small arteries from swine
• in P. aeruginosa infected mice to test its effect on the inflammatory responses
• to test its inhibition on neutrophil extracellular traps and monosodium urate (MSU) crystals formation in polymorphonuclear leukocytes

Biological Activity

Selective antagonist of P2Y 6 nucleotide receptors; IC 50 values are 37 and 98 nM at human and rat P2Y 6 receptors respectively. Displays no activity at P2Y 1 , P2Y 2 , P2Y 4 and P2Y 11 receptors (IC 50 > 10 μ M). Inhibits agonist-induced cardiomyocyte contraction and UDP-induced phagocytosis.

Biochem/physiol Actions

MRS 2578 elicits cytoprotective functionality in neuroblastoma cells and prevents dopaminergic neuron death under in vitro and in vivo conditions. It also protects microglia by delaying lipopolysaccharide-induced death.

storage

-20°C (desiccate)

References

[1] mamedova l k, joshi b v, gao z g, et al. diisothiocyanate derivatives as potent, insurmountable antagonists of p2y6 nucleotide receptors[j]. biochemical pharmacology, 2004, 67(9): 1763-1770.