Table 7. Agonist Potencies of Synthetic Prostaglandins for FP-Receptors Expressed in Various Cell-Typesa.
| stimulation
of PI turnover and production of IPs (functional response) in different
cell types (agonist potency, EC50 [nM]) |
|||||
|---|---|---|---|---|---|
| compound | human ciliary muscle (h-CM) cells | human trabecular meshwork (h-TM) cells | human cells (HEK-293) expressing cloned human ocular FP receptor | mouse Swiss 3T3 fibroblast cells | rat A7r5 vascular smooth muscle cells |
| travoprost free acid ((S)-fluprostenol) | 1.4 ± 0.2 | 3.6 ± 1.3 | 2.4 ± 0.3 | 2.6 ± 0.2 | 2.6 ± 0.5 |
| bimatoprost free acid (17-phenyl-PGF2α) | 3.8 ± 0.9 | 28 ± 18 | 3.3 ± 0.7 | 2.8 ± 0.2 | 2.8 ± 0.6 |
| (R/S)-fluprostenol | 4.3 ± 1.3 | 11 ± 2 | 4.6 ± 0.4 | 3.7 ± 0.4 | 4.4 ± 0.2 |
| PGF2α | 104 ± 19 | 62 ± 16 | 29 ± 2 | 26 ± 3 | 31 ± 3 |
| travoprost (isopropyl ester) | 123 ± 65 | 103 ± 27 | 40.2 ± 8.3 | 81 ± 18 | 46 ± 6 |
| latanoprost free acid (PHXA85) | 124 ± 47 | 35 ± 2 | 45.7 ± 8.4 | 32 ± 4 | 35 ± 8 |
| latanoprost (isopropyl ester) | 313 ± 90 | 564 ± 168 | 173 ± 58 | 142 ± 24 | 110 ± 19 |
| unoprostone (UF-021; free acid) | 3 503 ± 1 107 | 3 306 ± 1 700 | 3 220 ± 358 | 617 ± 99 | 878 ± 473 |
| unoprostone isopropyl ester | 8 420 ± 912 | 2 310 ± 1 240 | 9 100 ± 2 870 | 560 ± 200 | 458 ± 85 |
| bimatoprost (amide) | 9 600 ± 1 100 | 3 245 ± 980 | 681 ± 165 | 12 100 ± 1 200 | 6 850 ± 1 590 |
a
Data taken from ref (158).