product name Rufinamide
Description: Rufinamide (also known as CGP 33101) is a voltage-gated sodium channel blocker. It is a board spectrum anticonvulsant that is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other seizure disorders. Rufinamide has efficacy for partial seizures. Rufinamide prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons.
References: Int J Clin Pract. 2006 Nov;60(11):1497-501; J Vet Pharmacol Ther. 2012 Dec;35(6):529-33
238.19
Formula
C10H8F2N4O
CAS No.
106308-44-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 47 mg/mL (197.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CGP 33101
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
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| References | Int J Clin Pract. 2006 Nov;60(11):1497-501; J Vet Pharmacol Ther. 2012 Dec;35(6):529-33 |
