Product overview

Name GYKI 52466 hydrochloride
Description Selective, non-competitive AMPA receptor antagonist
Alternative names GYKI-52466
Purity >98%
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Biological Data

Biological description

Selective, non-competitive AMPA receptor antagonist (IC50 values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). Inactive at NMDA receptors.

GYKI 52466 shows anti-convulsant and neuroprotective actions. It also acts as a skeletal muscle relaxant. The compounds is active in vivo and its effects have been shown to last from 60 to 90 min with plasma concentrations peaking within 15min and decreasing to <5% of peak levels within 90min of i.p. injection.

Solubility & Handling

Storage instructions room temperature (desiccate)
Solubility overview Soluble in water (10mM) or DMSO (25mM, heating)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine hydrochloride
Molecular Weight 329.79
Chemical structure GYKI 52466  [102771-26-6] Chemical Structure
Molecular Formula C17H15N3O2.HCl
CAS Number 102771-26-6
PubChem identifier 3538
SMILES CC1=NN=C(C2=CC3=C(C=C2C1)OCO3)C4=CC=C(C=C4)N
Source Synthetic
InChi InChI=1S/C17H15N3O2/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
InChiKey LFBZZHVSGAHQPP-UHFFFAOYSA-N
MDL number MFCD00153803
Appearance Yellow solid

References for GYKI 52466 hydrochloride

References are publications that support the biological activity of the product
  • Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.

    Goulton et al (doi: 10.3389) Front Cell Neurosci. : 54
  • Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.

    Goulton CS et al (2010) Front Neurosci 4 :
  • Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655.

    Szabados T et al (2001) Brain Res Bull 55(3) : 387-91.
  • GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses.

    Donevan SD et al (1993) Neuron 10(1) : 51-9.