An inhibitor of NMDA receptors and a modulator of GABAA receptors; has broad-spectrum inhibitory activity against excitatory amino acid receptors; binds to NMDA channels with dissociation constants of approximately 200

Felbamate – 5 mg

Brand:
Cayman
CAS:
25451-15-4
Storage:
-20
UN-No:
Non-Hazardous - /

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 α1β2γ2S, α1β3γ2S, α2β2γ2S, and α2β3γ2S subunit-containing GABAA receptors expressed in X. laevis oocytes, with negative modulation of GABAA receptors containing the subunits α1β1, α1β3γ2L, α4β1γ2S, α4β3γ2S, and α6β1γ2S.{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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An inhibitor of NMDA receptors and a modulator of GABAA receptors; has broad-spectrum inhibitory activity against excitatory amino acid receptors; binds to NMDA channels with dissociation constants of approximately 200, 110, and 55 µM in the resting, activated, and desensitized states, respectively; inhibits NMDA currents in a use-dependent manner; a positive modulator of α1β2γ2S, α1β3γ2S, α2β2γ2S, and α2β3γ2S subunit-containing GABAA receptors expressed in X. laevis oocytes; a negative modulator of α1β1, α1β3γ2L, α4β1γ2S, α4β3γ2S, and α6β1γ2S subunit-containing GABAA receptors expressed in X. laevis oocytes; inhibits seizures induced by maximal electroshock, pentylenetetrazole, and picrotoxin in mice (ED50s = 16.3, 5.51, and 5.23 mg/kg, respectively)

Formal name: 2-phenyl-1,3-propanediol 1,3-dicarbamate

Synonyms:  ADD 03055

Molecular weight: 238.2

CAS: 25451-15-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Seizure Disorders

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