Table 3.
The properties of GW627368X in functional assays at human recombinant prostanoid receptors (n=3–9)
|
Recombinant systems |
CRTH2 |
EP1 |
EP2 |
EP3I |
EP4 |
FP |
IP |
|---|---|---|---|---|---|---|---|
| GW627368X pA2/pIC501/pKb2 | <5.41 | 6.0 (n=2) | <5.0 | <5.01 | 7.9±0.22 | <4.5 | 5.6±0.8 |
| GW627368X max effect as % standard |
— |
0 |
43±9 |
— |
−5±1.8 |
0 |
5±2 |
| Standard agonist pEC50 ipo GW627368X |
— |
7.1±0.2 |
7.4±0.3 |
— |
7.3±0.3 |
7.1±0.3 |
8.9±0.7 |
| Standard agonist max effect i.p.o. GW627368X as % control (=100) |
— |
83±21 |
95±32 |
— |
103±25 |
46±9 |
155±53 |
| % Inhibition vs standard agonist EC80 |
12 |
— |
— |
37 |
— |
— |
— |
| | |||||||
| Cell type |
CHO |
CHO |
CHO |
CHO |
HEK |
CHO |
CHO |
| Readout |
Calcium flux (FLIPR) |
CRE-Luc reporter |
cAMP |
Calcium flux (FLIPR) |
cAMP |
Calcium flux (FLIPR) |
cAMP |
| Antagonist concentration (μM) |
10 |
10 |
10 |
10 |
10 |
30 |
10 |
| Standard agonist |
PGD2 |
PGE2 |
PGE2 |
PGE2 |
PGE2 |
PGF2α |
Iloprost |
| Standard agonist pEC50 | 7.6±0.1 | 8.7±0.2 | 7.5±0.3 | 8.4±0.2 | 10.3±0.1 | 7.2±0.3 | 9.8±0.2 |
ipo: in the presence of.
Data are mean±s.d.