A positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity; potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing α1β1γ2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM

Bretazenil – 1 mg

Brand:
Cayman
CAS:
84379-13-5
Storage:
-20
UN-No:
Non-Hazardous - /

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 α1β1γ2 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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Description

A positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity; potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing α1β1γ2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM, respectively); inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM); inhibits PTZ- and MES-induced tonic convulsions in rats (ED50s = 0.07 and 0.48 mg/kg, respectively); increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice at 5-30 mg/kg

Formal name: (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

Synonyms:  Ro 16-6028

Molecular weight: 418.3

CAS: 84379-13-5

Purity: ≥98%

Formulation: A solid

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