Table 1.
Receptor classification, intracellular signalling, ligands and selective agonists and antagonists
| P2 subtype | I.c. signalling | Ligand | Selective agonist | Selective antagonist | Non-selective antagonist |
|---|---|---|---|---|---|
| P2Y1 | ↑IP3 | ADP (ATP) | MRS2365 | MRS 2179, MRS2500 | |
| P2Y2 | ↑IP3 | UTP = ATP | MRS2498, UTPγS, INS3717 | Suramin > RB2 | |
| P2Y4 | ↑IP3 | UTP (=ATP in rodents) | UTPγS, INS3717 | – | RB2 > Suramin |
| P2Y6 | ↑IP3 | UDP | MRS2666, MRS2633, UDPβS | MRS2578 | |
| P2Y11 | ↑IP3, ↑cAMP | ATP | AR-C67085MX, NF546 | NF157 | Suramin > RB2 |
| P2Y12 | ↓cAMP | ADP | – | Clopidogrel, prasugrel, AZD6140, INS50589, AR-C9931 (cangrelor) | |
| P2Y13 | ↓cAMP | ADP | – | MRS2211 | |
| P2Y14 | IP3 | UDP-glucose, UDP-galactose | UDP-glucose, UDP-galactose | – | |
| P2X1 | Positive ion channel | ATP | α,β-mATP | NF023, NF449 | TNP-ATP, Ip5I |
| P2X2 | Positive ion channel | ATP | – | NF770 | Suramin, isoPPADS, RB2 |
| P2X3 | Positive ion channel | ATP | α,β-mATP | A317491, NF110 | Suramin |
| P2X4 | Positive ion channel | ATP | Ivermectin potentiates | – | TNP-ATP |
| P2X5 | Positive ion channel | ATP | – | – | Suramin, PPADS |
| P2X6 | Positive ion channel | ATP | – | – | – |
| P2X7 | Positive ion channel | ATP | – | KN62, KN04, MRS2427 | Coomassie brilliant blue G |
| Ectonucleotidase | Apyrase, human SolCD39 | ARC67156 |