A GABAA receptor antagonist and partial agonist
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Labeled Version(s)
28529Flumazenil-d5
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Flumazenil

Item No. 14252

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester
CAS Number
78755-81-4
Synonyms
  • Ro 1722
  • Ro 15-1788
  • Ro 41-8157
Molecular Formula
C15H14FN3O3
Formula Weight
303.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 11 mg/mlDMSO: 16 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
244 nm
SMILES
O=C(OCC)C1=C2CN(C)C(C(C=C(F)C=C3)=C3N2C=N1)=O
InChi Code
InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3
InChi Key
OFBIFZUFASYYRE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Product Description

    Flumazenil is a GABAA receptor antagonist (IC50 = 2 nM in a radioligand binding assay using rat cortical synaptosomes).1 Flumazenil also acts as a partial agonist of GABAA receptors, decreasing the amplitude of electrically stimulated population spikes in rat hippocampal CA1 pyramidal neurons.2 It increases the number of entries into the open arms of the elevated plus maze in high-anxiety BALB/c, but not C57BL/6, mice when administered at doses ranging from 0.1 to 1,000 µg/kg.3 Flumazenil (5 and 10 mg/kg) prevents a reduction in burying behavior induced by the GABAA receptor positive allosteric modulator allopregnanolone (Item No. 16930) in ovariectomized rats when administered at doses of 5 and 10 mg/kg.4 Formulations containing flumazenil have been used to reverse sedation induced by benzodiazepines and in the treatment of benzodiazepine overdose or withdrawal.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Möhler, H., Burkard, W.P., Keller, H.H., et al. Benzodiazepine antagonist Ro 15-1788: Binding characteristics and interaction with drug-induced changes in dopamine turnover and cerebellar cGMP levels. J. Neurochem. 37(3), 714-722 (1981).

    2. Buldalkova, S., and Weiss, M. Electrophysiological evidence for agonist properties of flumazenil, a benzodiazepine receptor antagonist, in rat hippocampus slices. J. Neurol. Sci. 149(2), 121-126 (1997).

    3. Belzung, C., Le Guisquet, A.M., and Crestani, F. Flumazenil induces benzodiazepine partial agonist-like effects in BALB/c but not C57BL/6 mice. Psychopharmacol. (Berl) 148(1), 24-32 (2000).

    4. Fernández-Guasti, A., and Picazo, O. Flumazenil blocks the anxiolytic action of allopregnanolone. Eur. J. Pharmacol. 281(1), 113-115 (1995).