Table 2.
Binding affinity constants of agonists and antagonists at Gi protein-coupled purinergic P2YGi-like receptors (which consist of the P2Y12, P2Y13 and P2Y14 subtypes)
| P2Y12 | P2Y13 | P2Y14 | P2Y1# | |
|---|---|---|---|---|
| Agonists | ||||
| ADPβS | 7.5a | 7.5b | – | 5.6c,ϕ |
| UDP-G | – | – | 8d | – |
| Antagonists | ||||
| PSB 0739 | 7.6e | > 6f | > 6f | > 6f |
| MRS 2211 | > 5g | 6.3g | – | > 5g |
| MRS 2500 | > 4h | > 4i,Ψ | – | 9.1j |
Data collected from: a [40]; b [41]; c [42]; d [43]; e [44]; f [45]; g [46]; h [47]; i [48]; j [49]
All data are presented as pKi/pEC50 values at human receptors. It is important to note that the P2Y2, P2Y4 and P2Y6 receptor subtypes (which are also included in the family of P2Y receptors) are activated by UTP- or UDP-glucose, but not by ADPβS
#Note that several compounds also display some degree of affinity for the P2Y1 receptor subtype (a Gq-coupled receptor whose activation results in platelet aggregation) and that MRS 2179 is a selective P2Y1 receptor antagonist with similar structure and chemical properties as MRS 2500
ϕBehaves as a partial agonist
ΨBased on the compound MRS 2179