Time Post-Dosing (Hours) | Change in IOP (% relative to baseline) by Compound (50μg [0.16%] IVT) | |||
(S)-WIN-64338 | FR-165649 | FR-173657 | LF23-1591 | |
(B2-selective) | (B2-selective) | (B2-selective) | (B1-selective) | |
4 | -4.1 ± 1.7% | -0.2 ± 1.8% | -22.9 ± 4.5% | 2.9 ± 5.1% |
5 | -7.4 ± 2.3% | 0.6 ± 1.4% | nd | 5.4 ± 4.2% |
6 | -7.7 ± 3.8% | -1.0 ± 2.0% | -7.6 ± 3.2% | 9.6 ± 4.0% |
8 | -15.9 ± 4.9%* | -4.2 ± 1.2% | -15.9 ± 4.9% | 5.4 ± 2.8% |
24 | -35.3 ± 4.0%** | -6.5 ± 2.5% | -13.2 ± 4.2% | 1.3 ± 3.0% |
30 | -45.6 ± 2.9%** | -9.4 ± 4.0% | -12.7 ± 2.8% | 4.3 ± 3.3% |
48 | -43.2 ± 4.0%** | -10.8 ± 3.4% | -9.2 ± 2.9% | -13.8 ± 5.6% |
72 | -47.4 ± 2.9%** | nd | nd | nd |
168 | -16.2 ± 2.3%* | nd | nd | nd |
Receptor Antagonist Potencies (IC50s) |
298 ± 81 nM (n=3) |
195 ± 80 nM (n=6) |
323 ± 150 nM (n=6) |
nd |