Table 5.
Characteristics of P2Y receptors [Modified and updated from Burnstock (2003), with permission]
| P2Y Receptor | Main distribution | Agonists | Antagonists | Transduction mechanisms |
|---|---|---|---|---|
| P2Y1 | Epithelial and endothelial cells, platelets, immune cells, osteoclasts, brain | MRS2365 > 2-MeSADP = Ap5(γB) >> ADPβS > ATP > 2-MeSATP = ADP | MRS2500 > MRS2279 > MRS2179, PIT, A3P5P | Gq/G11; PLC-β activation |
| P2Y2 | Immune cells, epithelial and endothelial cells, kidney tubules, osteoblasts | 2-thio-UTP > UTP, MRS2698 ≥ ATP, INS 365 > INS 37217, UTPγS > Ap4A > MRS 2768, Up4-phenyl ester | AR-C126313 > Suramin > RB2, PSB-716, MRS2576 | Gq/G11 and possibly Gi/Go; PLC-β activation |
| P2Y4 | Endothelial cells, placenta, spleen, thymus | 2′-azido-dUTP > UTPγS, UTP ≥ ATP ≥ Ap4A Up4U | ATP (human) > Reactive Blue 2 > Suramin, MRS2577, PPADS | Gq/G11 and possibly Gi; PLC-β activation |
| P2Y6 | Airway and intestinal epithelial cells, placenta, T cells, thymus, microglia (activated) | MRS2693 > UDPβS, PBS0474 > INS48823, Up3U, 3-phenacyl-UDP >> UDP > UTP >> ATP, α,β-meUDP | MRS2578 > Reactive Blue 2, PPADS, MRS2567, MRS2575 (human) | Gq/G11; PLC-β activation |
| P2Y11 | Spleen, intestine, granulocytes | ATPγS > AR-C67085MX > BzATP ≥ ATP, NF546, NAD+, NAADP+ | NF157 > Suramin > RB2, 5′-AMPS, NF340, AMP-α-5, | Gq/G11 and GS; PLC-β activation |
| P2Y12 | Platelets, glial cells | 2-MeSADP ≥ ADP > ATP, ADP-β-S | AR-C69931MX > AZD6140, INS50589 > RB2 > 2-MeSAMP AR-C66096, CT50547,PSB-0413, Carba-nucleosides, MRS2395, AR-C67085 | GαI; inhibition of adenylate cyclase |
| P2Y13 | Spleen, brain, lymph nodes, bone marrow, erythrocytes | ADP = 2-MeSADP > 2-MeSATP, ATP | AR-C69931MX > AR-C67085 > MRS2211, 2-MeSAMP | Gi/Go |
| P2Y14 | Placenta, adipose tissue, stomach, intestine, discrete brain regions, mast cells | MRS2690 > UDP > UDP glucose ≥ UDP-galactose, UDP-glucosamine | Gq/G11 |
PIT, 2,2′-pyridylisatogen tosylate, UDP, uridine diphosphate; UTP, uridine 5′-triphosphate.