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Rufinamide CAS: 106308-44-5

Category: Inhibitors
Product Name: Rufinamide
Cat No: I000319
CAS No: 106308-44-5
Synonyms: 1-[(2,6-difluorophenyl)methyl]triazole-4-carboxamide
Molecular Formula: C10H8F2N4O
Molecular Weight: 238.2
SMILES: FC1=CC=CC(F)=C1CN2N=NC(C(N)=O)=C2
InChI: None
InChIKey: POGQSBRIGCQNEG-UHFFFAOYSA-N
Solubility: DMSO 48mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
Target: GABA Receptor
Storage: powder
CAS 106308-44-5,Rufinamide
  • Description

Rufinamide(E 2080; CGP 33101; RUF 331) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS). 

in vivo: Rufinamide and amitriptyline alleviated injury-induced mechanical allodynia for 4 h (maximal effect: 0.10 ± 0.03 g (mean ± SD) to 1.99 ± 0.26 g for rufinamide and 0.25 ± 0.22 g to 1.92 ± 0.85 g for amitriptyline) in mice [1]. Oral rufinamide suppressed pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and was active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg) [2]. Intraperitoneal rufinamide suppressed pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). 

Clinical trial: Exploratory Study to Evaluate the Effect of SYN-111 (Rufinamide) in Patients With Generalized Anxiety Disorder (GAD). Phase 2

  • Spec

Appearance:XXXX solid powder
Purity: > 98%

  • References


1:Dosing considerations for rufinamide in patients with Lennox-Gastaut syndrome: Phase III trial results and real-world clinical data. Kothare S, Kluger G, Sachdeo R, Williams B, Olhaye O, Perdomo C, Bibbiani F.Seizure. 2017 Apr;47:25-33. doi: 10.1016/j.seizure.2017.02.008. Epub 2017 Feb 17. Review. PMID: 28284045 Free Article
2:The anti-convulsants lacosamide, lamotrigine, and rufinamide reduce myotonia in isolated human and rat skeletal muscle. Skov M, de Paoli FV, Nielsen OB, Pedersen TH.Muscle Nerve. 2016 Oct 26. doi: 10.1002/mus.25452. [Epub ahead of print] PMID: 27783415
3:[Effectiveness and safety of rufinamide at treatment of epilepsy with complications and drug-resistant epilepsy (according to meta-analysis data)]. Mazin PV, Sheshunov IV, Kislitsyn YV, Mazina NK.Zh Nevrol Psikhiatr Im S S Korsakova. 2016;116(8):40-3. Russian. PMID: 27635610
4:Successful treatment of super-refractory tonic status epilepticus with rufinamide: First clinical report. Thompson AG, Cock HR.Seizure. 2016 Jul;39:1-4. doi: 10.1016/j.seizure.2016.04.003. Epub 2016 Apr 19. No abstract available. PMID: 27161668
5:Rufinamide in children and adults in routine clinical practice. Jaraba S, Santamarina E, Miró J, Toledo M, Molins A, Burcet J, Becerra JL, Raspall M, Pico G, Miravet E, Cano A, Fossas P, Fernández S, Falip M.Acta Neurol Scand. 2017 Jan;135(1):122-128. doi: 10.1111/ane.12572. Epub 2016 Feb 29. PMID: 26923380
6:Aggravation of atonic seizures by rufinamide: A case report. Bektaş G, Çalışkan M, Aydın A, Pembegül Yıldız E, Tatlı B, Aydınlı N, Özmen M.Brain Dev. 2016 Aug;38(7):654-7. doi: 10.1016/j.braindev.2016.02.005. Epub 2016 Feb 20. PMID: 26906013
7:Treatment of Adults with Lennox-Gastaut Syndrome: Further Analysis of Efficacy and Safety/Tolerability of Rufinamide. McMurray R, Striano P.Neurol Ther. 2016 Jun;5(1):35-43. doi: 10.1007/s40120-016-0041-9. Epub 2016 Feb 10. PMID: 26861566 Free PMC Article
8:Long-term safety and seizure outcome in Japanese patients with Lennox-Gastaut syndrome receiving adjunctive rufinamide therapy: An open-label study following a randomized clinical trial. Ohtsuka Y, Yoshinaga H, Shirasaka Y, Takayama R, Takano H, Iyoda K.Epilepsy Res. 2016 Mar;121:1-7. doi: 10.1016/j.eplepsyres.2016.01.002. Epub 2016 Jan 12. PMID: 26827266 Free Article
9:The efficacy and safety of rufinamide in drug-resistant epilepsy: A meta-analysis of double-blind, randomized, placebo controlled trials. Xu Z, Zhao H, Chen Z.Epilepsy Res. 2016 Feb;120:104-10. doi: 10.1016/j.eplepsyres.2016.01.001. Epub 2016 Jan 7. PMID: 26811934
10:Safety and pharmacokinetic profile of rufinamide in pediatric patients aged less than 4 years with Lennox-Gastaut syndrome: An interim analysis from a multicenter, randomized, active-controlled, open-label study. Arzimanoglou A, Ferreira JA, Satlin A, Mendes S, Williams B, Critchley D, Schuck E, Hussein Z, Kumar D, Dhadda S, Bibbiani F.Eur J Paediatr Neurol. 2016 May;20(3):393-402. doi: 10.1016/j.ejpn.2015.12.015. Epub 2016 Jan 11. PMID: 26805435 Free Article


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