BUY A-803467

A-803467. A Potent and Selective Inhibitor of the TTX-Resistant Na_v1.8 Channel.

The TTX-resistant, Na_v1.8 channel is expressed almost exclusively in the PNS and has been shown to mediate most of the well documented TTX-resistant currents of DRG neurons' action potentials. Hyperexcitability, manifested by increased action potential firing and coded information transfer to the CNS�of nociceptive DRG neurons, probably lie on the basis of several pathological pain states. Both genetic and pharmacological evidence suggest that Na_v1.8 channel might serve as a target in pain control.
A-803467 is a potent and selective blocker of the TTX-resistant Na_v1.8 channels. A-803467 is a state dependent inhibitor of the channel, with IC₅₀ = 8 nM at depolarized membrane potential (-40 mV) and 80 nM at -100 mV. As an efficient inhibitor of TTX-resistant currents in DRG neurons, A-803467 was also effective as an analgesic in several rodent models of different pathological pain states.

A-803467, was used as a pharmacological tool to demonstrate the expression of Na_v1.8 in the heart conduction system and its contribution to QRS interval in the mouse heart.
Ion Channel Modulators; Voltage - Gated Na⁺ Channel Blockers.