Catalog No.S1256 Synonyms: CGP 33101

For research use only.

Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

Rufinamide Chemical Structure

CAS No. 106308-44-5

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Biological Activity

Description Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 238.19


CAS No. 106308-44-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01151540 Completed Drug: Rufinamide Lennox-Gastaut Syndrome Eisai Co. Ltd.|Eisai Inc. November 2010 Phase 3
NCT01991041 Completed -- Lennox-Gastaut Syndrome Eisai Limited|Eisai Inc. June 2008 --

(data from, updated on 2022-01-17)

Tech Support

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Handling Instructions

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