pIC50 values for lidocaine and lidocaine dimers at rNav1.2a, hNav1.5, and rNav1.8 recombinant VGSCs determined using FLIPR membrane potential assay
Data represents mean ± S.D. of number of observations (n) indicated. Activation of Na+ channels in FMP-dye loaded rNav1.2a-CHO, hNav1.5-293-EBNA, and rNav1.8-F-11 cells was achieved using veratridine (20 μM), veratridine (20 μM) plus deltamethrin (3 μM), and veratridine (20 μM) plus deltamethrin (20 μM), respectively.
| rNav1.2a pIC50 | n | hNav1.5 pIC50 | n | rNav1.8 pIC50 | n | |
|---|---|---|---|---|---|---|
| Lidocaine | 3.7 ± 0.2 | 21 | 4.1 ± 0.1 | 26 | 4.1 ± 0.2 | 23 |
| Compound 2 | 4.7 ± 0.2 | 7 | 5.7 ± 0.1 | 4 | 5.4 ± 0.1 | 4 |
| Compound 3 | 5.4 ± 0.2 | 8 | 5.5 ± 0.2 | 4 | 6.2 ± 0.3 | 4 |
| Compound 4 | 6.0 ± 0.4 | 15 | 6.2 ± 0.2 | 11 | 6.8 ± 0.1 | 9 |
| Compound 5 | 5.0 ± 0.2 | 9 | 5.4 ± 0.3 | 6 | 5.2 ± 0.1 | 4 |
| Compound 6 | 5.0 ± 0.3 | 5 | 5.5 ± 0.1 | 4 | 5.1 ± 0.2 | 4 |
| Compound 7 | <4 | 4 | <4 | 4 | 3.5 ± 0.2 | 4 |
| Compound 8 | <4 | 4 | 4.7 ± 0.4 | 4 | 4.7 ± 0.1 | 4 |
| Compound 9 | 5.0 ± 0.2 | 4 | 4.9 ± 0.2 | 4 | 5.3 ± 0.1 | 4 |
| Tetrodotoxin | 8.7 ± 0.2 | 4 | 5.6 ± 0.2 | 22 | < 4.0 | 8 |