Rufinamide

Catalog No.S1256 Synonyms: CGP 33101

Rufinamide Chemical Structure

Molecular Weight(MW): 238.19

Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

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Biological Activity

Description Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
Targets
Sodium channel [1]
In vitro

Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Rufinamide’s mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. [1] Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM. [2]

In vivo Rufinamide given orally at 20 mg/kg every 12 h in healthy dogs should result in a plasma concentration and half-life sufficient to achieve the therapeutic level extrapolated from humans without short-term adverse effects in adult dogs. [3] Rufinamide alleviates injury-induced mechanical allodynia for 4 hours. Rufinamide reduces peak current and stabilizes the inactivated state of voltage-gated sodium channel Nav1.7, with similar effects in dorsal root ganglion neurons in the Spared Nerve Injury neuropathic pain model in mice. [4] Rufinamide suppresses pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and is active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg). Rufinamide suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). Rufinamide is partially effective in the mouse strychnine test. [5]

Protocol

Solubility (25°C)

In vitro DMSO 18 mg/mL warmed (75.56 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 238.19
Formula

C10H8F2N4O

CAS No. 106308-44-5
Storage powder
Synonyms CGP 33101

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02095899 Withdrawn Peripheral Nerve Injuries|Pain University of Zurich March 2014 Phase 2
NCT02332174 Completed Seizures Wuhan Union Hospital, China March 2014 Phase 1
NCT02175173 Active, not recruiting Lennox-Gastaut Syndrome Eisai Co., Ltd.|Eisai Inc. June 2013 --
NCT01405053 Completed Lennox-Gastaut Syndrome Eisai Inc. June 2011 Phase 3
NCT01146951 Completed Lennox-Gastaut Syndrome Eisai Limited|Eisai Inc. June 2010 Phase 3
NCT00448539 Completed Refractory Partial Onset Seizures Eisai Inc. March 2007 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Sodium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID