产品说明书

	同义名 :	FCE-26742A mesylate
	CAS号 :	202825-45-4
	货号 :	A423772
	分子式 :	C18H23FN2O5S
	纯度 :	98+%
	分子量 :	398.449
	MDL号 :	MFCD19690932
	存储条件：	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

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].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.51mL 0.50mL 0.25mL	12.55mL 2.51mL 1.25mL	25.10mL 5.02mL 2.51mL

参考文献

[1]Zhang SH, Blech-Hermoni Y, Faravelli L, Seltzer Z. Ralfinamide administered orally before hindpaw neurectomy or postoperatively provided long-lasting suppression of spontaneous neuropathic pain-related behavior in the rat. Pain. 2008 Oct 15;139(2):293-305 [2]Stummann TC, Salvati P, Fariello RG, Faravelli L. The anti-nociceptive agent ralfinamide inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive Na+ currents in dorsal root ganglion neurons. Eur J Pharmacol. 2005 Mar 14;510(3):197-208 [3]Liang X, Yu G, Su R. Effects of ralfinamide in models of nerve injury and chemotherapy-induced neuropathic pain. Eur J Pharmacol. 2018 Mar 15;823:27-34 [4]Yamane H, de Groat WC, Sculptoreanu A. Effects of ralfinamide, a Na+ channel blocker, on firing properties of nociceptive dorsal root ganglion neurons of adult rats. Exp Neurol. 2007 Nov;208(1):63-72