Felbamate

Felbamate is an inhibitor of NMDA receptors and a modulator of GABAA receptors that also has broad-spectrum inhibitory activity against excitatory amino acid receptors. It binds to NMDA channels with dissociation constants of approximately 200, 110, and 55 µM in the resting, activated, and desensitized states, respectively, and inhibits NMDA currents in a use-dependent manner. Felbamate is a positive modulator of alpha1beta2gamma2S, alpha1beta3gamma2S, alpha2beta2gamma2S, and alpha2beta3gamma2S subunit-containing GABAA receptors expressed in X. laevis oocytes, with negative modulation of GABAA receptors containing the subunits alpha1beta1, alpha1beta3gamma2L, alpha4beta1gamma2S, alpha4beta3gamma2S, and alpha6beta1gamma2S. It inhibits seizures induced by maximal electroshock, pentylenetetrazole (Cay-18682), and picrotoxin (Cay-20771) in mice (ED50s = 16.3, 5.51, and 5.23 mg/kg, respectively). Formulations containing felbamate have been used in the treatment of severe refractory seizures.Formal Name: 2-phenyl-1,3-propanediol 1,3-dicarbamate. CAS Number: 25451-15-4. Synonyms: ADD 03055. Molecular Formula: C11H14N2O4. Formula Weight: 238.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 30 mg/ml, Ethanol: 1 mg/ml. SMILES: NC(OCC(COC(N)=O)C1=CC=CC=C1)=O. InChi Code: 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). InChi Key: WKGXYQFOCVYPAC-UHFFFAOYSA-N.