TABLE 1.
| |||
---|---|---|---|
P2YR |
Synthetic Agonist (Mononucleotide), Potency |
Bifunctional Ligand, Potency |
References |
nM | |||
P2Y1 | 1, MRS2365, 0.4 | 2, Up4(β-B)A, A isomer, 500 | Houston et al., 2008; Yelovitch et al., 2012 |
P2Y2 | 3, MRS2698, 8.0 | 4, INS37217, 220 | Houston et al., 2008; Yerxa et al., 2002 |
P2Y4 | 5, MRS4062, 26 | 6, INS365 (Up4U)a, 130 | Ko et al., 2008; Maruoka et al., 2011 |
P2Y6 | 7, 5-OMe-UDPαB, 8 | 8, MRS2957, 12 | Maruoka et al., 2010; Haas et al., 2014 |
P2Y11 | 9, ATP-γ-S, 24,000 | 10, NAADP, 64,000 | Djerada and Millart, 2013 |
P2Y12 | 11, 2MeSADPb, 5 | 12, compound 17 (R/S)c, 13 | Zhang et al., 2002; Yanachkov and Wright, 2010 |
P2Y13 | 11, 2MeSADPb, 19 | 13, Ap3A, 72 | Zhang et al., 2002 |
P2Y14 | 14, MRS2905, 2.0 | 15, MRS2690, 70 | Das et al., 2010 |
NAADP, nicotinic acid adenine dinucleotide phosphate.
INS365 also activates P2Y2R (EC50 = 210 nM).
2MeSADP activates P2Y1R (EC50 = 6.6 nM), P2Y12R, and P2Y13R (also used as a high affinity 3H- or 33P-radioligand) (Takasaki et al., 2001).
Antagonist.