An allosteric AMPA receptor antagonist
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GYKI 52466 (hydrochloride)

Item No. 34418

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(8-methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine, monohydrochloride
CAS Number
192065-56-8
Molecular Formula
C17H15N3O2 • HCl
Formula Weight
329.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: 1 mg/ml
SMILES
CC1=NN=C(C2=CC=C(N)C=C2)C3=C(C=C4OCOC4=C3)C1.Cl
InChi Code
InChI=1S/C17H15N3O2.ClH/c1-10-6-12-7-15-16(22-9-21-15)8-14(12)17(20-19-10)11-2-4-13(18)5-3-11;/h2-5,7-8H,6,9,18H2,1H3;1H
InChi Key
RUBSCPARMVJNKX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $146

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    25 mg

    $345

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    50 mg

    $614

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    Product Description

    GYKI 52466 is an allosteric AMPA receptor antagonist.1 It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP; Item No. 18511) when administered at doses of 25 and 50 mg/kg.1 GYKI 52466 (30 mg/kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Weiczner, R., Krisztin-Péva, B., and Mihály, A. Blockade of AMPA-receptors attenuates 4-aminopyridine seizures, decreases the activation of inhibitory neurons but is ineffective against seizure-related astrocytic swelling. Epilepsy Res. 78(1), 22-32 (2008).

    2. Donevan, S.D., and Rogawski, M.A. GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron 10(1), 51-59 (1993).

    3. Block, F., Schmitt, W., and Schwarz, M. Pretreatment but not posttreatment with GYKI 52466 reduces functional deficits and neuronal damage after global ischemia in rats. J. Neurol. Sci. 139(2), 167-172 (1996).