Table 4. Summary of 4-fluoropropofol binding at various sites in NaChBac.
| Region | Residue | STDmax | ksat | σ × 100 |
|---|---|---|---|---|
| % | s–1 | s−1 | ||
| Intrasubunit extracellular interface | S208 | 3.0 ± 1.0* | 0.7 ± 0.5 | 2.1 ± 1.7 |
| Voltage sensing domain | N36 | 11.4 ± 0.5*** | 2.0 ± 0.3** | 22.3 ± 3.7** |
| V40 | 9.1 ± 0.5*** | 2.8 ± 0.6** | 25.5 ± 5.5** | |
| S4–S5 linker | S129 | 8.4 ± 0.3*** | 1.9 ± 0.3** | 15.8 ± 2.7** |
| L150 | 9.5 ± 0.6*** | 1.6 ± 0.3** | 15.5 ± 3.1** | |
| Selectivity filter | T189 | 9.0 ± 0.5*** | 2.2 ± 0.4** | 19.7 ± 3.8** |
| Activation gate | F227 | 17.4 ± 0.9*** | 2.5 ± 0.4** | 42.6 ± 7.6** |
| I223 | 9.7 ± 0.5*** | 1.4 ± 0.2** | 13.3 ± 2.3** | |
| I223a | 10.0 ± 0.4† | 1.7 ± 0.2† | 17.4 ± 1.5†† | |
| I223b | 8.0 ± 0.5† | 1.1 ± 0.2† | 8.4 ± 1.2†† |
Values are given as mean ± SEM. Difference from zero was evaluated individually for each parameter by the Student’s t test: *, P < 0.05; **, P < 0.01; ***, P < 0.001. Difference between parameters obtained in the absence and presence of etidocaine was evaluated by the Student’s t test: †, P < 0.05; ††, P < 0.01.
Measured by using 100 µM 4-fluoropropofol without the local anesthetic etidocaine.
Measured by using 100 µM 4-fluoropropofol in competition with 50 µM etidocaine.