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A-803467 is a potent and selective blocker of Nav1.8 sodium channel with IC50 value of 8nM [1].

A-803467 is a sodium channel blocker with high affinity and selectivity. It blocks the human Nav1.8 channels with IC50 value of 79nM. It also blocks the recombinant rat Nav1.8 channels with IC50 value of 45nM when the holding potential is -40mV. A-803467 is highly selective against Nav1.8 since the inhibition of Nav1.8 is 300- to 1000-fold more potent than of NaV1.2, NaV1.3, NaV1.5, and NaV1.7. It is found that A-803467 effectively suppresses the evoked and spontaneous action potential firing in DRG neurons in which TTX-R currents play a remarkable role. Furthermore, the selective blockade of Nav1.8 channels results in a significant reduction in nociceptive sensitivity. A-803467 potently attenuates mechanical allodynia in models of neuropathic pain. It also potently reduces thermal hyperalgesia in the CFA model of inflammatory pain [1].

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