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.
MRS 2578 is a selective P2Y66?receptor antagonist.
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
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.
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.
[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.
