Stereo selectivity of BW202W92 over BW203W92 for inhibition of [3H]BW202W92 binding and in other sodium channel assays in rat forebrain synaptosomes Values are means ± S.E.M. Ratio indicates IC50 values for BW203W92 relative to BW202W92.
| Assay | BW202W92 IC50 | Binding Slope | n | BW203W92 IC50 | Binding Slope | n | Ratio |
|---|---|---|---|---|---|---|---|
| μM | μM | ||||||
| [3H]BW202W92 | |||||||
| 1 mM K+ + TTXa | 0.048 ± 0.006 | 0.81 ± 0.03 | 6 | 1.5 ± 0.3 | 0.91 ± 0.02 | 4 | 32 |
| 1 mM K+ | 0.73 ± 0.09 | 0.94 ± 0.17 | 5 | 4.4 ± 1.1 | 1.31 ± 0.30 | 4 | 6.0 |
| 100 mM K+ + TTXa | 0.20 ± 0.02 | 0.95 ± 0.03 | 4 | 2.4 ± 0.6 | 0.91 ± 0.01 | 3 | 12 |
| 100 mM K+ | 0.64 ± 0.13 | 0.89 ± 0.08 | 4 | 5.0 ± 1.5 | 0.99 ± 0.01 | 3 | 7.8 |
| [14C]Guanidinium ion flux | 2.0 ± 0.2 | 0.88 ± 0.03 | 9 | 15 ± 4 | 1.13 ± 0.05 | 4 | 7.5 |
| [3H]BTX-B | 4.4 ± 0.3 | 0.81 ± 0.03 | 3 | 33 ± 9 | 0.80 ± 0.06 | 2 | 7.5 |
↵ a The tetrodotoxin (TTX) concentration was 1 μM