Felbamate

Felbamate

CAT N°: 18000
Price:

From 66.00 56.10

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.{45398,45399,45400} 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.{45398} Felbamate is a positive modulator of ?1?2?2S, ?1?3?2S, ?2?2?2S, and ?2?3?2S subunit-containing GABAA receptors expressed in X. laevis oocytes, with negative modulation of GABAA receptors containing the subunits ?1?1, ?1?3?2L, ?4?1?2S, ?4?3?2S, and ?6?1?2S.{45399} It inhibits seizures induced by maximal electroshock, pentylenetetrazole (Item No. 18682), and picrotoxin (Item No. 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.{45401}

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