MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

PPTN hydrochloride is a potent, high-affinity, competitive, highly selective P2Y14 receptor antagonist (KB: 434 pM), but no agonist or antagonist activity at P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12 or P2Y13 receptors, exhibiting anti-inflammatory and anti-immune effects.

PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

PIT (2,2'-Pyridylisatogen tosylate) is a specific and non-competitive antagonist of the Purinergic receptor P2Y1 with an IC50 of 0.14 μM for human P2Y1. PIT does not affect nucleotide binding and can be used in studies about chronic bronchitis and asthma.