Felbamate

Felbamate is an anti-epileptic drug used in the treatment of epilepsy. Felbamate has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptors, the relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.

Product information

CAS Number: 25451-15-4

Molecular Weight: 238.24

Formula: C11H14N2O4

Synonym:

W-554

ADD-03055

Felbatol

Felbamyl

Taloxa

W 554

W554

ADD03055

ADD 03055

Felbamate

Chemical Name: 2-phenylpropane-1,3-diyl dicarbamate

Smiles: NC(=O)OCC(COC(N)=O)C1C=CC=CC=1

InChiKey: WKGXYQFOCVYPAC-UHFFFAOYSA-N

InChi: InChI=1S/C11H14N2O4/c12-10(14)16-6-9(7-17-11(13)15)8-4-2-1-3-5-8/h1-5,9H,6-7H2,(H2,12,14)(H2,13,15)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Felbamate (W-554) is an anti-epileptic drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drugs usage to severe refractory epilepsy. Felbamate (W-554) has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptor of relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.

References:

1. Shi LL, Dong J, Ni H, Geng J, Wu T. Felbamate as an add-on therapy for refractory epilepsy. Cochrane Database Syst Rev. 2014 Jul 18;7:CD008295. doi: 10.1002/14651858.CD008295.pub3. Review. PubMed PMID: 25036694.
2. Shi LL, Dong J, Ni H, Geng J, Wu T. Felbamate as an add-on therapy for refractory epilepsy. Cochrane Database Syst Rev. 2011 Jan 19;(1):CD008295. doi: 10.1002/14651858.CD008295.pub2. Review. Update in: Cochrane Database Syst Rev. 2014;7:CD008295. PubMed PMID: 21249704.
3. Tribut O, Bentué-Ferrer D, Verdier MC; le groupe Suivi Thérapeutique Pharmacologique de la Société Française de Pharmacologie et de Thérapeutique. [Therapeutic drug monitoring of felbamate]. Therapie. 2010 Jan-Feb;65(1):35-8. doi: 10.2515/therapie/2009068. Epub 2010 Mar 8. Review. French. PubMed PMID: 20205993.
4. Pellock JM, Faught E, Leppik IE, Shinnar S, Zupanc ML. Felbamate: consensus of current clinical experience. Epilepsy Res. 2006 Oct;71(2-3):89-101. Epub 2006 Aug 4. Review. PubMed PMID: 16889941.
5. Borowicz KK, Piskorska B, Kimber-Trojnar Z, Małek R, Sobieszek G, Czuczwar SJ. Is there any future for felbamate treatment? Pol J Pharmacol. 2004 May-Jun;56(3):289-94. Review. PubMed PMID: 15215558.
6. Dieckhaus CM, Thompson CD, Roller SG, Macdonald TL. Mechanisms of idiosyncratic drug reactions: the case of felbamate. Chem Biol Interact. 2002 Nov 10;142(1-2):99-117. Review. PubMed PMID: 12399158.

Products are for research use only. Not for human use.