TABLE 1

Representative examples of different types of synthetic or natural ligands (agonists, unless noted), either mononucleotide or dinucleotide (or nucleotide sugar), for each of the P2YRs

The potency (nM) was measured in functional assays at the human P2YRs.

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P2YRSynthetic Agonist (Mononucleotide), PotencyBifunctional Ligand, PotencyReferences
nM
P2Y11, MRS2365, 0.42, Up4(β-B)A, A isomer, 500Houston et al., 2008; Yelovitch et al., 2012
P2Y23, MRS2698, 8.04, INS37217, 220Houston et al., 2008; Yerxa et al., 2002
P2Y45, MRS4062, 266, INS365 (Up4U)a, 130Ko et al., 2008; Maruoka et al., 2011
P2Y67, 5-OMe-UDPαB, 88, MRS2957, 12Maruoka et al., 2010; Haas et al., 2014
P2Y119, ATP-γ-S, 24,00010, NAADP, 64,000Djerada and Millart, 2013
P2Y1211, 2MeSADPb, 512, compound 17 (R/S)c, 13Zhang et al., 2002; Yanachkov and Wright, 2010
P2Y1311, 2MeSADPb, 1913, Ap3A, 72Zhang et al., 2002
P2Y1414, MRS2905, 2.015, MRS2690, 70Das et al., 2010

  • NAADP, nicotinic acid adenine dinucleotide phosphate.

  • ↵a INS365 also activates P2Y2R (EC50 = 210 nM).

  • ↵b 2MeSADP activates P2Y1R (EC50 = 6.6 nM), P2Y12R, and P2Y13R (also used as a high affinity 3H- or 33P-radioligand) (Takasaki et al., 2001).

  • ↵c Antagonist.