| Assay Method Information | |
| | Inhibitory Activity on Nav1.8 Ion Channel of Compounds |
| Description: | Reagents were purchased from Sigma (St. Louis, MO) except NaOH and KOH for acid-base titration. The final concentrations of the test compounds were all prepared on the day of the test and then dissolved in an extracellular fluid. The extracellular fluid (mM) was NaCl, 137; KCl, 4; CaCl2), 1.8; MgCl2, 1; HEPES, 10; glucose 10; and pH 7.4 (NaOH titration). All test and control compound solutions contained 1 μM TTX. The intracellular fluid (mM) was: aspartic acid, 140; magnesium chloride, 2; ethylene glycol tetraacetic acid (EGTA), 11; and N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid (HEPES), 10. The pH was adjusted to 7.4 with cesium hydroxide. The test compounds were dissolved in dimethylsulfoxide (DMSO) at a concentration of 9 mM. On the day of the test, the compounds were then dissolved in the extracellular fluid and prepared into the required concentration. |
| Affinity data for this assay | |
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