Table 1.
Comparison of nucleotide sensitivity of various P2Y receptors
Subtype | P2Y1 | P2Y2 | P2Y4 | P2Y6 | P2Y11 | P2Y12 | P2Y(pot) | P2Y(inh) |
G-protein | Gq/11 | G q/11 | G q/11 | Gq/11 | Gs,G q/11 | Gi/o | Gs | G q/11 |
Coupling | PLC β/IP3↑ | PLC β/IP3↑ | PLC β/IP3↑ | PLCβ/IP3↑ | PLCb/IP3↑ | AC/cAMP↓ | AC/cAMP↑ | PLC β/IP3↑ |
AC/cAMP↑ | (DAG/PKC) | |||||||
Antagonists | ||||||||
PPADS(10 μm) | + | − | − | +* | na | − | + | + |
suramin(100 μm) | + | + | − | + | + | + | + | + |
Agonist | 2MeSATP | UTP≥ATP | UTP=ATP | UDP>UTP | ATPγS>ATP | 2MeSATP | ATPγS> | 2MeSATP> |
sensitivity | ≫ATP γS | >ATP γS | ≫2MeSATP | >2MeSATP | >ADP | ATP≥ | ATPγS>ATP | |
>ATP>ADP | ≫ATPγS | ADP | >ADP | |||||
(MeSATP:NE) |
The agonist sensitivity in the second column is determined based on EC50 values of Jacobson et al. (2000). Other information is based on Boarder & Hourani (1998), King et al. (1998), Kunapuli & Daniel (1998) and Hollopeter et al. (2001). The data in the third column are from the present work. +, effective; + *, effective at 100 μm; −, ineffective. PLCβ, phospholipase Cβ; IP3, inositol 1,4,5-trisphosphate; DAG, diacylglycerol; AC, adenylate cyclase; NE, not effective. Affixes ‘(pot)’ and ‘(inh)’ indicate the potentiation and inhibition of ImVDCC, respectively, na, not available.