An allosteric AMPA receptor antagonist
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GYKI 53655

Item No. 39842

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(4-aminophenyl)-8,9-dihydro-N,8-dimethyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide, monohydrochloride
CAS Number
143692-48-2
Synonyms
  • LY300168
Molecular Formula
C19H20N4O3 • HCl
Formula Weight
388.9
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C(N1N=C(C2=C(CC1C)C=C3OCOC3=C2)C4=CC=C(N)C=C4)NC.Cl
InChi Code
InChI=1S/C19H20N4O3.ClH/c1-11-7-13-8-16-17(26-10-25-16)9-15(13)18(22-23(11)19(24)21-2)12-3-5-14(20)6-4-12;/h3-6,8-9,11H,7,10,20H2,1-2H3,(H,21,24);1H
InChi Key
ASLCSBBDVWPSQT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

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    10 mg

    $242

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    25 mg

    $548

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    Product Description

    GYKI 53655 is an allosteric AMPA receptor antagonist.1 It inhibits AMPA- and kainite-induced inward currents in whole-cell patch-clamp assays using primary rat hippocampal neurons (IC50s = 1.1 and 1.5 µM, respectively). GYKI 53655 decreases tonic and clonic audiogenic seizure severity in mice (ED50s = 1.3 and 2 mg/kg, respectively) and reduces mortality in a mouse model of global cerebral ischemia induced by magnesium dichloride (ED50 = 8.2 mg/kg).2 It inhibits seizures induced by maximal electroshock (MES) in mice (ED50 = 4.6 mg/kg) but induces motor impairment at a half-maximal toxic dose (TD50) value of 8.7 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Donevan, S.D., Yamaguchi, S.-I., and Rogawski, M.A. Non-N-methyl-D-aspartate receptor antagonism by 3-N-substituted 2,3-benzodiazepines: Relationship to anticonvulsant activity. J. Pharmacol. Exp. Ther. 271(1), 25-29 (1994).

    2. Szabados, T., Gigler, G., Gacsályi, I., et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res. Bull. 55(3), 387-391 (2001).