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. 2017 Oct 21;174(Suppl Suppl 1):S17–S129. doi: 10.1111/bph.13878
Nomenclature P2Y 1 receptor P2Y 2 receptor P2Y 4 receptor P2Y 6 receptor
HGNC, UniProt P2RY1, P47900 P2RY2, P41231 P2RY4, P51582 P2RY6, Q15077
Potency order of endogenous ligands ADP>ATP uridine triphosphate>ATP [1112] uridine triphosphate>ATP (at rat recombinant receptors, UTP = ATP) uridine diphosphateuridine triphosphate>ADP
Endogenous agonists uridine triphosphate [989, 1112]
Agonists ADP βS [1921], 2MeSADP [1729, 2054]
Sub/family‐selective agonists diquafosol [1554], denufosol [1113, 1554, 2181], UTP γS [1112] diquafosol [240], denufosol [2181], UTP γS [1113]
Selective agonists MRS2365 [329], 2‐Cl‐ADP( α‐BH3) [76] MRS2698 [874], 2‐thioUTP [498], PSB1114 (EC50 value determined using an IP3 functional assay) [498, 499, 873] MRS4062 [1276], MRS2927 [1276], (N)methanocarba‐UTP [989] Rp‐5‐OMe‐UDP αB [644, 702], MRS2957 [1275], MRS2693 [146]
Antagonists suramin (pK i 5.3) [2054], PPADS (pK i 5.2) [2054] ATP (pK d 6.2) [970]
Sub/family‐selective antagonists reactive blue‐2 (pIC50 6) [892], suramin (pIC50 4.3) [892, 1729] PPADS (pEC50 2–5) [881], reactive blue‐2 (pIC50 4.7) [171] – Rat reactive blue‐2 (pK B 6) [2045], PPADS (pK B 4) [2045], suramin (pK B 4) [2045]
Selective antagonists MRS2500 (pK i 8.8–9.1) [286, 988], MRS2279 (pK i 7.9) [2054], MRS2179 (pK i 7–7.1) [203, 2054] AR‐C118925XX (pIC50∼6) [968], AR‐C126313 (pEC50 6) [874], PSB‐416 (pIC50 4.7) [792] ATP (pK d 6.2) [970] MRS2578 (pIC50 7.4) [1257], MRS2567 (pIC50 6.9) [1257]
Allosteric modulators 2,2'‐pyridylisatogen tosylate (Negative) (pIC50 7.8) [601]
Selective allosteric modulators BMS compound 16 (Negative) (pK i 6.9) [2206]
Labelled ligands [3 H]MRS2279 (Antagonist) (pK d 8.1) [2054], [3 H]2MeSADP (Agonist) [1921], [35 S]ADP βS (Agonist) MRS4162 (Selective Antagonist) (pEC50 7.6) [897]