Catalog No.S1256 Synonyms: CGP 33101
Molecular Weight(MW): 238.19
Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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|Description||Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.|
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.  Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM. 
|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.  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.  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. |
-  Cheng-Hakimian A, et al. Int J Clin Pract,?006, 60(11), 1497-1501.
-  Williams ET, et al. Drug Metab Lett,?011, 5(4), 280-289.
-  Wright HM, et al. J Vet Pharmacol Ther,?012, 35(6), 529-533.
|In vitro||DMSO||18 mg/mL warmed (75.56 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02332174||Completed||Seizures||Wuhan Union Hospital China||March 2014||Phase 1|
|NCT02095899||Withdrawn||Peripheral Nerve Injuries|Pain||University of Zurich||March 2014||Phase 2|
|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|
|NCT00334958||Completed||Epilepsy||Eisai Inc.||February 2006||Phase 3|
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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