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. 2015 Jul 24;6:155. doi: 10.3389/fphar.2015.00155

Table 1.

Comparison between half-maximum inhibitory concentrations of sumatriptan and its analogs on hNav1.7 sodium channels and of (S)-22b on wild-type and mutated hNav1.4.

Drug 0.1 Hz 10 Hz 0.1 Hz/10 Hz IC50 ratio

IC50 (μM) nH IC50 (μM) nH
hNav1.7
Sumatriptan 2399 ± 56 1.4 ± 0.1 2187 ± 106 1.4 ± 0.1 1,1
20b 127 ± 16 1.2 ± 0.2 54 ± 4 1.1 ± 0.1 2,4
(R)-31b 118 ± 5 1.4 ± 0.1 39 ± 3 1.1 ± 0.1 3,0
(S)-22b 77 ± 10 1.3 ± 0.2 21 ± 2 1.3 ± 0.1 3,7
Mexiletine 338 ± 18 1.4 ± 0.1 114 ± 12 1.0 ± 0.1 3,0
hNav1.4
(S)-22b 51 ± 2 1.4 ± 0.1 12 ± 1 1.3 ± 0.1 4,3
hNav1.4 – F1586C
(S)-22b 215 ± 5 1.4 ± 0.1 175 ± 9 1.4 ± 0.1 1,2

The values were obtained from the fit of the concentration–response curves illustrated in Figures 2 and 5. The half-maximum inhibitory concentration (IC50) and the slope factor (nH) are given as the fit value ± SE of the fit.