Table 1.
Characteristics, preferred agonists, and signaling of cloned P2 receptors
| Preferred Agonists (Potency EC50) |
Useful Agonist | Useful Antagonist | Transduction Mechanism | |
|---|---|---|---|---|
| P2Y1 | ADP (10 µM) > ATP (Ap4U ~1 µM) | 2-MeS-ADP; MRS2365 | MRS2500; BPTU | Gq/G11; PLC-β↑ |
| P2Y2 | ATP (0.1 µM) = UTP (0.01 µM) | PSB-1114 | AR-C1189251XX | Gq/G11 (Gi/Go?); PLC-β↑ |
| P2Y4 | UTP (human) (~1 µM); UTP = ATP (rodent) | MRS4062 | Gq/G11 (Gi?); PLC-β↑ | |
| P2Y6 | UDP (~0.3 µM) > UTP > ADP | MRS2957; PSB-0474 | MRS2578 | Gq/G11; PLC-β↑ |
| P2Y11 | ATP (~10 µM) and ADP (and UTP (547) (human) | γ-Thio-ATP; NF546 | NF340 | Gq/G11 and GS; PLC-β↑ |
| P2Y12 | ADP (0.1 µM) > ATP | 2-MeS-ADP | PSB-0739; ticagrelor | Gi/others |
| P2Y13 | ADP (0.01 µM) > ATP | 2-MeS-ADP | MRS2211 | Gi/Go/others |
| P2Y14 | UDP (0.1 µM) UDP-glucose (0.3 µM) and UDP-galactose | MRS2690 | PPTN | Gi/Go/others |
| P2X1 | ATP (0.1–0.7 µM) | ATP; 2-MeS-ATP | NF449 | ICC (Ca2+ and Na+) |
| P2X2 | ATP (2–8 µM) | ATP | PSB-1011; NF770 | IIC (particularly Ca2+) |
| P2X3 | ATP (~1 µM) | ATP; 2-MeS-ATP | A-317491; R0-4 | ICC |
| P2X4 | ATP (1–10 µM) | ATP; γ-Thio-ATP | AF353; R0-51; AF906 | IIC (especially Ca2+) |
| P2X5 | ATP (0.5 µM) | Benzoyl-ATP* | 5-BDBD; PSB-12054 | IIC |
| P2X6 | Functions poorly as homomultimer | BX-430 | IIC | |
| P2X7 | ATP (2–4 mM) | ATP; benzoyl-ATP | A-740003; A438079; AZ11657312 | ICN; large pore |