Compound | Functional Potencies in PI Turnover Assays in Swiss 3T3 Cells | FP Receptor Binding Affinity Data, IC50 | |||
---|---|---|---|---|---|
EC50 (mean ± S.E.M.) | Emax2-a | Bovine corpus luteum2-b | Swiss 3T3 cells2-c | Human cloned FP receptors2-d | |
nM | % | nM | |||
16-Phenoxy-PGF2α | 0.61 ± 0.10 | 94.7 | 36 ± 2.3 | ||
Cloprostenol (standard) | 0.73 ± 0.04 | 100 | 35 ± 3.2 | ||
17-Phenyl-PGF2α | 2.71 ± 0.35 | 87.9 | 53 ± 6.1 | 10 | |
Fluprostenol | 3.67 ± 0.61 | 100 | 110 ± 13.2 | 20 | 3.5 |
PhXA85 | 27.3 ± 5.63 | 79.6 | 92 ± 26 | ||
PGF2α | 28.5 ± 5.26 | 90.6 | 140 ± 9.1 | 25–90 | 2.8 |
11-β-PGF2α | 47.6 ± 6.8 | 100 | 208 ± 16 | ||
15-Cyclohexyl-PGF2α | 124 ± 2.5 | 95 | 1,390 ± 3.5 | ||
17-Phenyl-PGE2 | 126 ± 26.2 | 80.3 | 1,600 ± 624 | ||
PGD2 | 155 ± 29.9 | 49.2 | 2,900 ± 870 | 300–580 | 7 |
Enprostil | 174 ± 45.9 | 87.3 | 1,160 ± 259 | ||
13,14-Dihydro-15-keto-20-ethyl-PGF2α | 726 ± 147 | 48.3 | 6,700 ± 804 | ||
U46619 | 1,060 ± 310 | 63.4 | 10,000 ± 160 | 146 | |
Sulprostone | 1,990 ± 451 | 86.8 | 2,800 ± 392 | 3,900–10,000 | |
PGE2 | 2,570 ± 566 | 59.2 | 3,900 ± 819 | 4,000–6,000 | 85 |
15-Keto-PGF2α | 1,560 ± 295 | 74.8 | ND2-e | ||
Misoprostol | >100,000 | ND 2-e | |||
SC-46275 | >100,000 | ND 2-e | |||
Iloprost | Inactive | 235,000 ± 224,000 | 1,200 | ||
BW 245C | Inactive | >100,000 | >100,000 | ||
8-Isoprostane | Inactive | 100,000 ± 77,900 | |||
Butaprost | Inactive | ND 2-e | |||
Anandamide | Inactive | ND 2-e | |||
11-Deoxy-16,16-dimethyl-PGE2 | Inactive | ND 2-e |
PI turnover data are mean ± S.E.M. from three to seven experiments, except for cloprostenol (n = 45).
↵2-a E max, efficacy, maximum response as a percentage of the cloprostenol response (S.E.M. < 10%).
↵2-b This study, using [3H]PGF2α as the radioligand, (n = 3 or 4 experiments).
↵2-c Estimates from Woodward and Lawrence (1994) and Woodwardet al. (1995), using [3H]17-phenyl-PGF2αas the radioligand.
↵2-d From Abramovitz et al. (1994), using [3H]PGF2α as the radioligand.
↵2-e ND, not determined.