Table 11. Relative Affinities of DP-Receptor Agonists for Tissues in Human Eye Sections Determined by Quantitative Autoradiographic Techniques and Using [3H]-BWA868C as the Radioliganda.
| DP-Class
prostaglandin inhibition constant (Ki, nM; mean ± SEMs) in human ocular tissues determined
by quantitative autoradiography |
||||
|---|---|---|---|---|
| compound | ciliary epithelium/processes | longitudinal ciliary muscle | circular ciliary muscle | iris |
| BW-245C (free acid) | 8.0 ± 1.8 | 7.0 ± 1.0 | 5.7 ± 0.8 | 4.4 ± 0.7 |
| SQ-27986 (free acid) | 9.0 ± 1.9 | 6.1 ± 0.8 | 6.4 ± 1.3 | 8.5; 6.6 |
| ZK-118182 (free acid) | 32.9 ± 7.4 | ±2.9 | ±2.6 | 7.3; 15.4 |
| AL-6556 (free acid of AL-6598) | ±1310 | ±160 | ±413 | nd |
| AL-6598 (isopropyl ester) | ±3000 | ±665 | ±825 | nd |
a
Note: the smaller is the Ki value, the higher is the affinity of the compound for the DP-receptors. nd = not determined. Data reproduced and updated from ref (273).