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 diphosphate≫uridine 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] |