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A 887826 is a potent and voltage-dependent Nav1.8 sodium channel blocker. It blocked recombinant human Nav1.8 channels with an IC50 value of 11nM [1].

Voltage-gated sodium channels are important in the generation and propagation of action potential. At least 9 genes encode functional sodium channels, namely Nav1.1-Nav1.9. Nav1.8 is a TTX-resistant (TTX-R) sodium channel. Nav1.8 is highly localized on primary sensory afferent neurons. Nav1.8 is involved in the processing of nociceptive information.

-100 mV without prepulse did make a resting state for rat DRG neurons. Prepulse to -40 mV did make an inactivated state for channels. In rat DRG neurons in these two states, treatment with A 887826 at 1 µM significantly blocked TTXR Na+ currents. A 887826 blocked TTX-R Na+ currents with an IC50 value of 7.9 ± 0.2 nM (n= 5~9) when channels were in an inactivated state (-40 mV). A 887826 showed an IC50 value of 63.6 ± 0.2 nM (n=5~9) to less depolarized (at -60, -80 or -100 mV) TTX-R Na+ currents. That meant A 887826 state-dependently blocked TTX-R Na+ currents [1].

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