Ralfinamide mesylate产品图
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Ralfinamide mesylate

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  • ¥553 - 840
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  • 2026年05月28日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 英文名:

      (S)-2-((4-((2-Fluorobenzyl)oxy)benzyl)amino)propanamide methanesulfonate

    • 供应商:

      上海安毕达生物科技有限公司

    • CAS号:

      202825-45-4

    • 规格:

      50mg/100mg

    规格:50mg产品价格:¥553.0
    规格:100mg产品价格:¥840.0
    Ralfinamide mesylate是一种 Na+ 通道阻断剂,具有镇痛作用。

    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 pain1. 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 microM2. 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 function3. Ralfinamide (25 microM) suppressed afferent hyperexcitability selectively in capsaicin-responsive, presumably nociceptive neurons, but had no measurable effects on firing in CAPS-unresponsive neurons4.

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    图标文献和实验
    该产品被引用文献
    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

    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

    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

    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

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    • Synthesis of (2S, 4S, 5S)-5-(t-Butoxycarbonylamino)-4-(t-Butyldimethylsilyloxy)-2-Isopropyl-7-Methyl Octanoic Acid

      -4 and C-5 centers ( 3 ). After formatron of the mesylate, from the recycled material the amine function is introduced through azrde displacement of the mesylate, followed by reduction ( 4 ) and protectron with the t -BOC group. Finally, the lactone

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    Ralfinamide mesylate
    ¥553 - 840