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GYKI 52466 hydrochloride

(HB0311)
Data

Product overview

  • Name
    GYKI 52466 hydrochloride
  • Short description
    Selective, non-competitive AMPA receptor antagonist
  • 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.

  • Alternative names
    GYKI-52466
  • Biological action
    Antagonist
  • Purity
    >98%
  • Citations

Properties

  • 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]
  • 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

Storing and Using Your Product

  • Storage instructions
    -20°C
  • Solubility overview
    Soluble in water (10mM with warming), and in DMSO (50 mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for GYKI 52466 hydrochloride

  • 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.
    PubMedID: 7678966
  • Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.

    Goulton CS et al (2010) Front Neurosci 4 :
    PubMedID: 20953290
  • 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.
    PubMedID: 11489346
  • Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.

    Goulton et al (doi: 10.3389) Front Cell Neurosci. : 54
    PubMedID: 20953290
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