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Tolperisone-d10 is intended for use as an internal standard for the quantification of tolperisone by GC- or LC-MS. Tolperisone is a piperidine that acts as an inhibitor of voltage-gated sodium channels with an IC50 value of 198 µM, for inhibition of peak sodium currents evoked by step depolarizations in dorsal root ganglion (DRG) neurons, in vitro.1 Tolperisone acts as an antispastic agent that attenuates monosynaptic, disynaptic, and polysynaptic reflux response to dorsal root stimulation in vivo. Formulations containing tolperisone are used as analgesics and muscle relaxants.

1.Kocsis, P., Farkas, S., Fodor, L., et al.Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channelsJ. Pharmacol. Exp. Ther.315(3)1237-1246(2005)

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