Figure 1 | Scientific Reports

Figure 1

From: Effects of 4(1H)-quinolinone derivative, a novel non-nucleotide allosteric purinergic P2Y 2 agonist, on cardiomyocytes in neonatal rats

Figure 1

Compound 89 displays selective agonist activity for P2Y2 in P2Y-overexpressing 1321N1 cells. (a) The chemical structure of the 4(1H)-quinolinone derivative Compound 89: 2-((ethyl(4-fluorobenzyl)amino)methyl)-7,8-dimethylquinolin-4(1H)-one. (b) Agonistic activity against human and mouse P2Y2 receptors in a FLIPR Ca2+ mobilization assay using 1321N1 cells that were transiently-expressing hP2Y2 receptors (hP2Y2-1321N1) and stably-expressing mP2Y2 receptors (mP2Y2-1321N1). The activity of 10 μM ATP was normalized to 100%. (c) Agonistic activity against human P2Y1, P2Y4, P2Y6, and P2Y11 receptors in FLIPR Ca2+ mobilization assays utilising their respective transiently-expressing 1321N1 cells. The agonistic activity of 10 μM ADP for hP2Y1, UTP for hP2Y4, UDP for hP2Y6, and ATP for hP2Y11 was normalized to 100%. (d) Agonistic activity against human P2Y12 receptor in a cAMP accumulation assay using stably-expressing hP2Y12-1321N1 cells. The activity of 1 μM ADP was normalized to 100%. All data points represent the mean in duplicate or quadruplicate and comparable results were obtained from another independent experiment.

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