Table 4.
Summary of 4-fluoropropofol binding at various sites in NaChBac
RegionResidueSTDmaxksatσ × 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†† 
RegionResidueSTDmaxksatσ × 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.

a

Measured by using 100 µM 4-fluoropropofol without the local anesthetic etidocaine.

b

Measured by using 100 µM 4-fluoropropofol in competition with 50 µM etidocaine.

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