High affinity and selective P2Y14 antagonist (KB = 434 pM). Exhibits >10,000-fold selectivity for P2Y14 over other P2Y receptors. Inhibits UDP-glucose and MRS 2690-induced porcine pancreatic artery contraction ex vivo. Also blocks UDP-glucose-induced chemotaxis of HL-60 leukemia cells in vitro.
Gao et al (2013) The role of P2Y14 and other P2Y receptors in degranulation of human LAD2 mast cells. Purinergic Signal. 9 31 PMID:22825617 |Alsaqati et al (2014) Novel vasocontractile role of the P2Y14 receptor: characterization of its signalling in porcine isolated pancreatic arteries. Br.J.Pharmacol. 171 701 PMID:24138077 |Barrett et al (2013) A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Mol.Pharmacol. 84 41 PMID:23592514