P2X and P2Y receptor agonists and antagonists
All of the ligands are commercially available, except for PPTN, 4-[(piperidin-4-yl)-phenyl]-7-[4-(trifluoromethyl)-phenyl]-2-naphthoic acid (Barrett et al., 2013).
| Ion Channel/Principal Transduction | Agonists | Selective Agonists | Selective Antagonists | |
|---|---|---|---|---|
| P2X1 | Ion channel | ATP | α,β-meATP, l-β,γ-meATP | NF023, NF449 |
| Ro 0437626 | ||||
| P2X2 | Ion channel | ATP | — | — |
| P2X3 | Ion channel | ATP | A317491 | Ro51, RO3 |
| P2X4 | Ion channel | ATP | — | — |
| P2X5 | Ion channel | ATP | — | — |
| P2X6 | Ion channel | ATP | — | — |
| P2X7 | Ion channel | ATP | — | A839977, A740003 |
| A438079, AZ 11645373 | ||||
| P2Y1 | Gq/11 | ADP > ATP | 2-MeSADP, ADPβS, MRS2365 | MRS2179 |
| MRS2500 | ||||
| P2Y2 | Gq/11 | UTP = ATP | UTPγS, PSB1114 | |
| P2Y4 | Gq/11 | UTP > ATP | UTPγS, MRS4062 | |
| P2Y6 | Gq/11 | UDP > > UTP > ATP | UDP, PSB 0474 (≡ 3- phenacylUDP) | MRS2578 |
| MRS2957 | ||||
| P2Y11 | Gs, Gq/11 | ATP > UTP | NF546, NAD+ NAADP+ | NF157 |
| NF340 | ||||
| P2Y12 | Gi/o | ADP > > ATP | ADP, 2-MeSADP | AR-C 66096 |
| P2Y13 | Gi/o | ADP > > ATP | — | MRS2211 |
| P2Y14 | Gi/o | UDP-glucose | MRS2690 | PPTN |
| UDP-galactose |