Bretazenil

Bretazenil

CAT N°: 28411
Price:

From 55.00 46.75

Bretazenil is a positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity.{48491} It potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing ?1?1?2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM, respectively).{48491} Bretazenil inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM).{48492} It inhibits tonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) and maximal electroshock (MES) in rats (ED50s = 0.07 and 0.48 mg/kg, respectively). Bretazenil (5-30 mg/kg) increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.{48493}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (13aS)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, 1,1-dimethylethyl ester
  • Correlated keywords
    • GABA A anti convulsant HEK 293 ?1 ?1 ?2 ? ? 1? 2 Ro166028 166028 6028/000 166028/000 Ro166028/000
  • Product Overview:
    Bretazenil is a positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity.{48491} It potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing ?1?1?2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM, respectively).{48491} Bretazenil inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM).{48492} It inhibits tonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) and maximal electroshock (MES) in rats (ED50s = 0.07 and 0.48 mg/kg, respectively). Bretazenil (5-30 mg/kg) increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.{48493}

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