Nomenclature |
P2Y1 receptor |
P2Y2 receptor |
P2Y4 receptor |
P2Y6 receptor |
HGNC, UniProt |
P2RY1, P47900
|
P2RY2, P41231
|
P2RY4, P51582
|
P2RY6, Q15077
|
Principal transduction |
Gq/11
|
Gq/11
|
Gq/11
|
Gq/11
|
Rank order of potency |
ADP>ATP |
UTP=ATP |
UTP>ATP (at rat recombinant receptors, UTP = ATP) |
UDP>>UTP>ATP |
Endogenous agonists (pKi) |
– |
– |
– |
UDP (pEC50 6.5) 1423
|
Selective agonists (pKi) |
MRS2365 (pEC50 9.4) 1421, ADPβS (pEC50 7.3) 1459, 2MeSADP (pIC50 5.4 – 7.0) 1458,1461
|
2-thioUTP (pEC50 7.3) 1426, PSB1114 (pEC50 6.9) 1427, Ap4A (pEC50 6.1) 1419,1457, UTPγS (pEC50 5.8) 1443, MRS2768 (pEC50 5.7) 1441
|
UTPγS 1444, MRS4062 (pEC50 7.6) 1448
|
MRS2957 (pEC50 7.9) 1447, 5-iodoUDP (pEC50 7.82) 1416, 3-phenacyl-UDP (pEC50 7.2) 1426
|
Selective antagonists (pKi) |
MRS2500 (8.8 – 9.1) 1420,1438, MRS2279 (7.9) 1461, MRS2179 (7.0 – 7.1) 1418,1461, 2,2'-pyridylisatogen tosylate (6.8) 1429
|
AR-C118925XX (pIC50 ∼6.0) 1436
|
ATP (pKd 6.2) 1437
|
MRS2578 (pIC50 7.4) 1445
|
Radioligands (Kd) |
[35S]ADPβS (Agonist), [3H]2MeSADP (Agonist), [3H]MRS2279 (Antagonist) (8x10-9 M) 1461
|
– |
– |
– |