Ralfinamide mesylate is an blocker of Na+ channel with function of suppressing pain.
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Ralfinamide mesylate is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain. Ralfinamide (30 mg/kg, 60 mg/kg; p.o.; twice daily; 42 days) treated with Ralfinamide (80 mg/kg; p.o.; twice daily; 7 days) preoperatively suppresses neuropathic pain[1]. Ralfinamide inhibition was voltage-dependent showing highest potency towards inactivated channels. IC50 values for tonic block of half-maximal inactivated tetrodotoxin-resistant and tetrodotoxin-sensitive currents were 10 microM and 22 microM[2]. Oral ralfinamide dose-dependently alleviated spared nerve injury-induced allodynia in rats and mice. Ralfinamide increased mechanical withdrawal thresholds in oxaliplatin-induced and paclitaxel-induced neuropathic pain. Ralfinamide did not affect physiological pain, locomotion, or cardiovascular function[3]. Ralfinamide (25 microM) suppressed afferent hyperexcitability selectively in capsaicin-responsive, presumably nociceptive neurons, but had no measurable effects on firing in CAPS-unresponsive neurons[4].
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